Omega-3, 6,9 fatty acids are phytochemincals in the class of Lipids, found abundantly in dark-green leafy vegetables, grains, legumes, nuts, etc.
Health Benefits
1. Vascular smooth muscle tone
In the investigation of the comparative effects of omega-3, omega-6 and omega-9 fatty acids
on vascular smooth muscle tone, showed that Docosahexaenoic acid (1-255
microM) and eicosapentaenoic acid (31-255 microM) inhibited
phenylephrine-induced contractions, (8-63%) and (20-65%), respectively,
which were not altered by indomethacin, NDGA, or by removal of the
endothelium. Linoleic acid (18:2n6) and arachidonic acid (20:4n6) also
induced significant relaxation. Therefore, fatty acid-induced relaxation of the rat aorta is specific to polyunsaturated fatty acids, 20:5n3, 22:6n3, 18:2n6 and 20:4n6, according to "Effects of omega-3, omega-6 and omega-9 fatty acids on vascular smooth muscle tone" by Engler MB.(1)
2. Breast cancer
In the review of the literature concerning the role of fatty acids and eicosanoid synthesis inhibitors in breast carcinoma, indicated that The omega-6 polyunsaturated fatty acids
(PUFAs), primarily linoleic acid, promote breast cancer tumorigenesis
and tumor cell proliferation directly and indirectly via increased
synthesis of cyclooxygenase- and lipoxygenase-catalyzed products. The omega-3
PUFAs, primarily docosahexaenoic acid (DHA) and eicosapentaenoic acid
(EPA), suppress breast carcinoma tumorigenesis and tumor cell
proliferation, although the effect of DHA may be partly ascribed to
increased amounts of EPA derived from DHA. Both cyclooxygenase and
lipoxygenase inhibitors suppress tumorigenesis and/or tumor
proliferation, with the latter being more active. Thus, arachidonic
acid-derived eicosanoids play an important role in breast cancer, and
the balance of the various eicosanoids may be a critical determinant of
cell proliferation, according to "The role of fatty acids and eicosanoid synthesis inhibitors in breast carcinoma" by Noguchi M, Rose DP, Earashi M, Miyazaki I.(2)
3. Regulatory effects
In the examination of the effects of individual n-6 (linoleic acid) and
n-3 (alpha-linolenic, eicosapentaenoic, and docosahexaenoic acid) PUFAs
on plasma lipid levels and on the major transport processes that
determine plasma LDL concentrations, found that Rats were fed a
semisynthetic cholesterol-free diet supplemented with 4% (by wt)
linoleic, alpha-linolenic, eicosapentaenoic, or docosahexaenoic acid
for 2 weeks. Dietary eicosapentaenoic and docosahexaenoic acids
lowered plasma triglyceride concentrations by 62% and 52%,
respectively, and lowered plasma cholesterol concentrations by 54% and
43%, respectively. In contrast, dietary linoleic and alpha-linolenic acids
had relatively little effect on plasma triglyceride or cholesterol
concentrations. Dietary eicosapentaenoic and docosahexaenoic acids
increased hepatic LDL receptor activity by 72% and 58%, respectively,
and reduced the rate of LDL cholesterol entry into plasma by 36% and
30%, respectively, according to "Regulatory effects of individual n-6 and n-3 polyunsaturated fatty acids on LDL transport in the rat" by Spady DK.(3)
4. Systolic blood pressure, triglycerides and LDL cholesterol
In the ccomparison of the cardiovascular risk-reduction potential of three major polyunsaturated fatty acids
in a double-blind study. showed that for the diet supplemented with EPA
plus DHA compared with the linoleic acid diet systolic blood pressure
fell 5.1 mm Hg (p = 0.01); plasma triglyceride and VLDL cholesterol
fell by 39% (p = 0.001) and 49% (p = 0.01), respectively; and LDL
cholesterol rose by 9% (p = 0.01). There were no significant changes
with the diet supplemented with alpha-linolenic acid. The net effect on
cardiovascular risk therefore is complex and the systolic blood
pressure reduction was substantial, according to "n-3 fatty acids of marine origin lower systolic blood pressure and triglycerides but raise LDL cholesterol compared with n-3 and n-6 fatty acids from plants" by Kestin M, Clifton P, Belling GB, Nestel PJ.(4)
5. Cardiovascular effects
In the comparison of the effects of alpha-linolenic acid (ALA, C18:3n-3)
to those of eicosapentaenoic acid (EPA, C20:5n-3) plus docosahexaenoic
acid (DHA, C22:6n-3) on cardiovascular risk markers in healthy elderly
subjects, found that Both n-3 fatty
acid diets did not change concentrations of total-cholesterol,
LDL-cholesterol, HDL-cholesterol, triacylglycerol and apoA-1 when
compared with the oleic acid-rich diet. However, after the EPA/DHA-rich
diet, LDL-cholesterol increased by 0.39 mmol/l (P = 0.0323, 95% CI
(0.030, 0.780 mmol/l)) when compared with the ALA-rich diet. Intake of
EPA/DHA also increased apoB concentrations by 14 mg/dl (P = 0.0031, 95%
CI (4, 23 mg/dl)) and 12 mg/dl (P = 0.005, 95% CI (3, 21 mg/dl)) versus
the oleic acid and ALA-rich diet, respectively. Except for an
EPA/DHA-induced increase in tissue factor pathway inhibitor (TFPI) of
14.6% (P = 0.0184 versus ALA diet, 95% CI (1.5, 18.3%)), changes in
markers of hemostasis and endothelial integrity did not reach
statistical significance following consumption of the two n-3 fatty acid diets, according to "Effects of alpha-linolenic acid versus those of EPA/DHA on cardiovascular risk markers in healthy elderly subjects" by Goyens PL, Mensink RP.(5)
6. Cognitive effects
In the assessment of the cognitive effects of fish oil supplementation
at college age, hypothesizing benefits on affect, executive control,
inhibition, and verbal learning and memory. College-aged participants,
indicated that the benefits of n-3 PUFA on RAVLT performance derived
more from depreciated placebo performance than improved performance due
to fish oil. The placebo gain on TMT performance likely derived from a
learning effect. Together, these results present limited cognitive
benefits of n-3 PUFA at college age; however, the treatment may have
been subtherapeutic, with a larger sample needed to generalize these
results, according to "Omega-3 polyunsaturated fatty acids and cognition in a college-aged population" by Karr JE, Grindstaff TR, Alexander JE.(6)
7. Depression-related cognition
In the investigation of the effects of n-3 PUFA on depression-relevant
cognitive functioning in healthy individuals, found that The n-3 PUFA
group made fewer risk-averse decisions than the placebo group. This
difference appeared only in non-normative trials of the decision-making
test, and was not accompanied by increased impulsiveness. N-3 PUFAs
improved scores on the control/perfectionism scale of the cognitive
reactivity measure. No effects were found on the other cognitive tasks
and no consistent effects on mood were observed. The present findings
indicate that n-3 PUFA supplementation may have a selective effect on
risky decision making in healthy volunteers, which is unrelated to
impulsiveness, according to "Omega-3 fatty acids (fish-oil) and depression-related cognition in healthy volunteers" by Antypa N, Van der Does AJ, Smelt AH, Rogers RD.(7)
8. Mental illness
In the review of the double blind placebo controlled clinical trials published prior to April 2007 to determine whether omega-3
PUFA are likely to be efficacious in these psychiatric disorders, found
that for schizophrenia and borderline personality disorder we found
little evidence of a robust clinically relevant effect. In the case of
attention deficit hyperactivity disorder and related disorders, most
trials showed at most small benefits over placebo. A limited
meta-analysis of these trials suggested that benefits of omega-3 PUFA supplementation may be greater in a classroom setting than at home. Some evidence indicates that omega-3
PUFA may reduce symptoms of anxiety although the data is preliminary
and inconclusive. The most convincing evidence for beneficial effects of
omega-3 PUFA is to be found in mood
disorders. A meta-analysis of trials involving patients with major
depressive disorder and bipolar disorder provided evidence that omega-3
PUFA supplementation reduces symptoms of depression. Furthermore,
meta-regression analysis suggests that supplementation with
eicosapentaenoic acid may be more beneficial in mood disorders than with
docosahexaenoic acid, although several confounding factors prevented a
definitive conclusion being made regarding which species of omega-3 PUFA is most beneficial, according to "Omega-3 fatty acids as treatments for mental illness: which disorder and which fatty acid?" by Ross BM, Seguin J, Sieswerda LE.(8)
9. Antioxidant, antimicrobial activities
In the investigation of the hexane extract from different parts in
several Hypericum species, found that The antioxidant activity of all
hexane extracts was evaluated by the 2,2-diphenyl-1-picrylhydrazyl
(DPPH) radical scavenging method. The results indicate that hexane
extracts from different parts of H. scabrum possess considerable
antioxidant activity. The highest radical scavenging activity was
detected in seed, which had an IC50 = 165 microg/mL. The antimicrobial
activity of the extracts of those samples were determined against seven
Gram-positive and Gram-negative bacteria (Bacillus subtilis,
Enterococcus faecalis, Staphylococcus aureus, S. epidermidis,
Escherichia coli, Pseudomonas aeruginosa, and Klebsiella pneumoniae),
as well as three fungi (Candida albicans, Saccharomyces cerevisiae, and
Aspergillus niger), according to "Antioxidant, antimicrobial activities and fatty acid components of flower, leaf, stem and seed of Hypericum scabrum" by Shafaghat A.(9)
10. Post-partum depression PPD
In the investigation of the effect of unbalanced dietary intake of omega-6/omega-3
ratio >9:1 in the prevalence for PPD, comprising a prospective
cohort with four waves of follow-up during pregnancy and one following
delivery. PPD was evaluated according to the Edinburgh Post-partum
Depression Scale (PPD ≥ 11) in 106 puerperae between 2005 and 2007, in
Rio de Janeiro, Brazil. Independent variables included
socio-demographic, obstetric, pre-pregnancy body mass index (BMI) and
dietary intake data, which were obtained by means of a food frequency
questionnaire in the first trimester of pregnancy, verified that an
association between omega-6/omega-3
ratio above 9:1, the levels recommended by the Institute of Medicine,
and the prevalence of PPD. These results add to the evidence regarding
the importance of omega-6 and omega-3 fatty acids in the regulation of mental health mechanisms, according to "High dietary ratio of omega-6 to omega-3 polyunsaturated acids during pregnancy and prevalence of post-partum depression" by da Rocha CM, Kac G.(10)
11. Relieving inflammation
In the evaluation of the effects of lymphatic drainage and omega-3 polyunsaturated fatty
acid (omega-3PUFA) on high mobility group box 1 (HMGB1), inflammatory
cytokines and endotoxin in rats with intestinal ischemia-reperfusion
(I/R) injury, found that Lymphatic drainage may reduce the levels of
endotoxin, inflammatory cytokines and HMGB1 so as to alleviate the
intestinal I/R injury. The intervention of omega-3PUFA has some
protective effect through relieving inflammation, according to "[Effects of lymphatic drainage and omega-3 polyunsaturated fatty acids on intestinal ischemia-reperfusion injury in rats].[Article in Chinese]" by Zhou KG, He GZ, Zhang R, Chen XF.(11)
12. Suppression of inflammatory
In the determination of whether salmon (rich in n-3 LCPUFAs) consumption
twice a week during pregnancy affected offspring umbilical vein EC CAM
expression, showed that increased dietary salmon intake in pregnancy
dampens offspring EC activation, which implicates a role for n-3
LCPUFAs in the suppression of inflammatory processes in humans. This
trial was registered at clinicaltrials.gov as NCT00801502, according to
"Salmon consumption by pregnant women reduces ex vivo umbilical cord endothelial cell activation"
by van den Elsen LW, Noakes PS, van der Maarel MA, Kremmyda LS,
Vlachava M, Diaper ND, Miles EA, Eussen SR, Garssen J, Willemsen LE,
Wilson SJ, Godfrey KM, Calder PC.(12)
13. Neonatal immune responses
In thye assessment of whether an increased intake of oily fish in
pregnancy modifies neonatal immune responses and early markers of atopy,
showed that Oily fish intervention in pregnancy modifies neonatal
immune responses but may not affect markers of infant atopy assessed at
6 mo of age, according to "Increased intake of oily fish in pregnancy:
effects on neonatal immune responses and on clinical outcomes in infants
at 6 mo" by Noakes PS, Vlachava M, Kremmyda LS, Diaper ND, Miles EA,
Erlewyn-Lajeunesse M, Williams AP, Godfrey KM, Calder PC.(13)
14. Allergic disease
In the study of the effects of maternal n-3 (PUFA)-rich fish oil
supplementation on cord blood (CB) IgE and cytokine levels in neonates
at risk of developing allergic disease, found that increasing neonatal
n-3 PUFA levels with maternal dietary supplementation can achieve
subtle modification of neonatal cytokine levels. Further assessment of
immune function and clinical follow-up of these infants will help
determine if there are any significant effects on postnatal immune
development and expression of allergic disease, according to " Maternal fish oil supplementation in pregnancy reduces interleukin-13 levels in cord blood of infants at high risk of atopy' by Dunstan JA, Mori TA, Barden A, Beilin LJ, Taylor AL, Holt PG, Prescott SL.(14)
15. Mucosal immune function
In the evaluation of if changes in breast milk omega-3 polyunsaturated fatty
acid (n-3 PUFA) composition as a result of maternal dietary fish oil
supplementation during pregnancy can modify levels of these
immunological parameters in breast milk, found that Supplementation with
fish oil during pregnancy significantly alters early post-partum breast
milk fatty acid composition. omega-3 PUFA levels were positively associated with IgA and sCD14 levels, suggesting a relationship between fatty acid status and mucosal immune function, according to "The effect of supplementation with fish oil during pregnancy on breast milk immunoglobulin A, soluble CD14, cytokine levels and fatty acid composition" by Dunstan JA, Roper J, Mitoulas L, Hartmann PE, Simmer K, Prescott SL.(15)
16. Ventricular arrhythmias and myocardial infarction
In the investigation of the effectiveness of prescription medication containing 90% omega-3 polyunsaturated fatty acids
for 6 months on ventricular arrhythmias in patients with myocardial
infarction less than a year ago, found that Administration of highly
concentration preparation of omega-3
PUFAs for 3 months reduced number of PVCs per day, frequencies of
grades 2, 3, 4A, 4B, and high grade PVCs (grades 3 - 5) as a whole.
These effects persisted after 6 months of treatment, according to
"[Possibilities of a preparation omega-3 polyunsaturated fatty acids in the treatment of patients with ventricular arrhythmias and myocardial infarction].[Article in Russian]" by Gogolashvili NG, Litvinenko MV, Pochikaeva TN, Vavitova ES, Polikarpov LS, Novgorodtseva NIa.(16)
17. Health effects
In the investigation of the health effects of Perilla frutescens seeds, a good source of polyunsaturated fatty acids
(PUFAs), showed that in comparing to other plant oils, perilla seed oil
consistently contains the one of the highest proportion of omega-3 (ALA) fatty acids,
at 54-64%. The omega-6 (linoleic acid) component is usually around 14%
and omega-9 (Oleic acid) is also present in perilla oil. These
polyunsaturated fatty acids are most beneficial to human health and in prevention of different diseases like cardiovascular disorders, cancer, inflammatory, rheumatoid arthritis etc., according to "Health effects of omega-3,6,9 fatty acids: Perilla frutescens is a good example of plant oils" by Asif M.(17)
18. Obesity
in the determination of whether obesity modifies the association between plasma phospholipid polyunsaturated fatty acids
(PUFAs) and markers of inflammation and endothelial activation in
Multi-Ethnic Study of Atherosclerosis (MESA) participants, found that
the modifying effect of obesity on the association of plasma PUFAs with
IL-6 and sICAM-1 suggests differences in fatty acid metabolism and may also have implications in dietary fatty
acid intake for obese individuals, particularly for linoleic and EPAs.
Further study is warranted to confirm and explain the strong
associations of dihomo-γ-linolenic acid (DGLA) with inflammatory and
endothelial activation markers, according to "Obesity modifies the association between plasma phospholipid polyunsaturated fatty acids and markers of inflammation: the Multi-Ethnic Study of Atherosclerosis" by Steffen BT, Steffen LM, Tracy R, Siscovick D, Hanson NQ, Nettleton J, Tsai MY.(18)
19. Crohn's disease (CD)
In the investigation of the effects of a nutritionally balanced
inflammatory bowel disease nutrition formula (IBDNF) on nutrition
status in CD patients, indicate that twenty patients completed the final
visit. After 4 months, there was a significant decrease in plasma
phospholipid levels of arachidonic acid with increases in
eicosapentaenoic acid (EPA) and docosahexaenoic acid. Ten patients had a
final EPA concentration of >2%. There was improvement in fat-free
and fat mass in patients with final EPA >2% (P = .014 and P = .05).
Vitamin D (25-OH) levels improved in all patients (18.5-25.9 ng/mL, P
< .001). Those with EPA >2% had significantly lower CDAI (116 ±
94.5 vs 261.8 ± 86.5; P = .005) and higher IBDQ (179.1 ± 26.6 vs 114.6 ±
35.9, P < .001) compared to those with EPA <2%, according to "The
effects of an oral supplement enriched with fish oil, prebiotics, and
antioxidants on nutrition status in Crohn's disease patients" by Wiese DM, Lashner BA, Lerner E, DeMichele SJ, Seidner DL.(19)
20. Etc.
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Use The Revolutionary Findings To Achieve
Optimal Health And Loose Weight
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Sources
(1) http://www.ncbi.nlm.nih.gov/pubmed/1396998
(2) http://www.ncbi.nlm.nih.gov/pubmed/7777237
(3) http://www.ncbi.nlm.nih.gov/pubmed/8105015
(4) http://www.ncbi.nlm.nih.gov/pubmed/1971991
(5) http://www.ncbi.nlm.nih.gov/pubmed/16482073
(6) http://www.ncbi.nlm.nih.gov/pubmed/22250656
(7) http://www.ncbi.nlm.nih.gov/pubmed/18583436
(8) http://www.ncbi.nlm.nih.gov/pubmed/17877810
(9) http://www.ncbi.nlm.nih.gov/pubmed/22224301
(10) http://www.ncbi.nlm.nih.gov/pubmed/22136220
(11) http://www.ncbi.nlm.nih.gov/pubmed/22093738
(12) http://www.ncbi.nlm.nih.gov/pubmed/22011457
(13) http://www.ncbi.nlm.nih.gov/pubmed/22218160
(14) http://www.ncbi.nlm.nih.gov/pubmed/12680858
(15) http://www.ncbi.nlm.nih.gov/pubmed/15298564
(16) http://www.ncbi.nlm.nih.gov/pubmed/21942955
(17) http://www.ncbi.nlm.nih.gov/pubmed/21909287
(18) http://www.ncbi.nlm.nih.gov/pubmed/21829163
(19) http://www.ncbi.nlm.nih.gov/pubmed/21775642
Saturday, 2 November 2013
Phytochemicals in Foods - 10 Health Benefits of Gamma-linolenic Acid
Gamma-linolenic acid is a
phytochemincalsin the group of Omega-3, 6,9 fatty acids, belonging the
class of Lipids, found abundantly in evening primrose, borage,
blackcurrant, etc.
Health Benefits
1. Neuropathic symptoms
in the evaluation of the effects of alpha-lipoic acid (ALA) and gamma-linolenic acid (GLA) and the beneficial effect of physical exercise on positive sensory symptoms and neuropathic pain in patients with compressive radiculopathy syndrome from disc-nerve root conflict, found that oral treatment with alpha-lipoic acid (ALA) and gamma-linolenic acid (GLA) for six weeks in synergy with rehabilitation therapy improved neuropathic symptoms and deficits in patients with radicular neuropathy, according to "The use of alpha-lipoic acid (ALA), gamma linolenic acid (GLA) and rehabilitation in the treatment of back pain: effect on health-related quality of life" by Ranieri M, Sciuscio M, Cortese AM, Santamato A, Di Teo L, Ianieri G, Bellomo RG, Stasi M, Megna M.(1)
2. Anti inflammatory effects
In the evaluation of wheather The PUFAs of omega-3 and omega-6 series play a significant role in health and disease by generating potent modulatory molecules for inflammatory responses,
found that GLA and its metabolites also affect expression of various genes where by regulating the levels of gene products including matrix proteins. These gene products play a significant role in immune functions and also in cell death (apoptosis). The present review will emphasize the role of GLA in modulating inflammatory response, and hence its potential applications as an anti-inflammatory nutrient or adjuvant, according to "Gamma linolenic acid: an antiinflammatory omega-6 fatty acid" by Kapoor R, Huang YS.(2)
3. Brain tumor
In the investigation of the effects of oral consumption of gamma linolenic acid (GLA) and docosahexaenoic acid (DHA) on brain tumor fatty acid composition, showed that dietary supplementation of DHA containing oil could be an effective way to increase levels of long chain n-3 fatty acids in brain tumors and this increase may be mediated partly by up-regulation of FABP7 expression, according to "The influence of feeding linoleic, gamma-linolenic and docosahexaenoic acid rich oils on rat brain tumor fatty acids composition and fatty acid binding protein 7 mRNA expression" by Nasrollahzadeh J, Siassi F, Doosti M, Eshraghian MR, Shokri F, Modarressi MH, Mohammadi-Asl J, Abdi K, Nikmanesh A, Karimian SM.(3)
4. Proliferation diseases
In the determination of a controversial dietary approaches focused on the diverse function of dihomo-dietary gamma-linolenic acid (DGLA) in anti-inflammation and anti-proliferation diseases, especially for cancers, found that hese compounds possess both anti-inflammatory and anti-proliferative properties. PGE1 could also induce growth inhibition and differentiation of cancer cells. Although the mechanism of DGLA has not yet been elucidated, it is significant to anticipate the antitumor potential benefits from DGLA, according to "Multiple roles of dihomo-gamma-linolenic acid against proliferation diseases" by Wang X, Lin H, Gu Y.(4)
5. Human health and nutrition
In the deiermination of weather a controversial dietary approaches has been the possible prophylactic role of dietary gamma-linolenic acid (GLA) in treating various chronic disease states, showed that these compounds possess both anti-inflammatory and antiproliferative properties. Although an optimal feeding regimen to maximize the potential benefits of dietary GLA has not yet been determined, it is the purpose of this review to summarize the most recent research that has focused on objectively and reproducibly determining the mechanism(s) by which GLA may ameliorate health problems, according to "Importance of dietary gamma-linolenic acid in human health and nutrition" by Fan YY, Chapkin RS.(5)
6. Skin protection
in the elucidation of the effect of GLA-rich oil on skin function, found that the mechanism of improvement of skin barrier has been associated with possible generation of anti-inflammatory metabolites from GLA. The clinical physician also confirmed that none of the subjects showed any noteworthy side effects. GLA-enriched food appears to be safe and to improve skin barrier function in subjects with dry skin conditions and mild atopic dermatitis, according to 'Dietary supplementation of gamma-linolenic acid improves skin parameters in subjects with dry skin and mild atopic dermatitis" by Kawamura A, Ooyama K, Kojima K, Kachi H, Abe T, Amano K, Aoyama T.(6)
7. Drug-sensitive and resistant tumor cells
In the investigation of weather dihomo-gamma-linolenic acid (DGLA) and AA, EPA and DHA have cytotoxic action on both vincristine-sensitive (KB-3-1) and resistant (KB-Ch(R)-8-5) cancer cells in vitro, indicated that GLA, DGLA, AA, EPA and DHA enhanced the uptake and decreased efflux in both drug-sensitive and drug-resistant cells and augmented the susceptibility of tumor cells especially, of drug-resistant cells to the cytotoxic action of vincristine. These results suggest that certain polyunsaturated fatty acids have tumoricidal action and are capable of enhancing the cytotoxic action of anti-cancer drugs specifically, on drug-resistant cells by enhancing drug uptake and reducing its efflux. Thus, polyunsaturated fatty acids either by themselves or in combination with chemotherapeutic drugs have the potential as anti-cancer molecules, according to "Effect of polyunsaturated fatty acids on drug-sensitive and resistant tumor cells in vitro" by Das UN, Madhavi N.(7)
8. Acute lung injury or acute respiratory distress syndrome (ARDS)
In the assessment of the effect of an enteral diet enriched with eicosapentaenoic acid (EPA), gamma-linolenic acid (GLA), and anti-oxidants on the incidence of organ dysfunction and nosocomial infections in septic patients with acute lung injury or acute respiratory distress syndrome (ARDS) compared with a standard enteral diet, found that A diet enriched with EPA, GLA, and anti-oxidants does not improve gas exchange or decrease the incidence of novel organ failures in critically ill septic patients with acute lung injury or ARDS. Patients treated with the EPA-GLA diet stayed in the ICU for less time, but we did not find any differences in infectious complications, according to "Effect of an enteral diet enriched with eicosapentaenoic acid, gamma-linolenic acid and anti-oxidants on the outcome of mechanically ventilated, critically ill, septic patients" by Grau-Carmona T, Morán-García V, García-de-Lorenzo A, Heras-de-la-Calle G, Quesada-Bellver B, López-Martínez J, González-Fernández C, Montejo-González JC, Blesa-Malpica A, Albert-Bonamusa I, Bonet-Saris A, Herrero-Meseguer JI, Mesejo A, Acosta J.(8)
9. Antineoplastic effects
In the investigation of the effect and the mechanism of gamma linolenic acid (GLA) treatment on human hepatocellular (HCC) cell lines, showed that GLA treatment has induced cell growth inhibition, ROS generation including lipid peroxidation, and HO-1 production for antioxidant protection against oxidative stress caused by GLA in Huh7 cells. GLA treatment should be considered as a therapeutic modality in patients with advanced HCC, according to "Antineoplastic effects of gamma linolenic Acid on hepatocellular carcinoma cell lines' by Itoh S, Taketomi A, Harimoto N, Tsujita E, Rikimaru T, Shirabe K, Shimada M, Maehara Y.(9)
10. Chronic myelogenous leukemia
In the testing the apoptotic effect of GLA on human chronic myelogenous leukemia K562 cells,
showed that the apoptosis could be inhibited by a pancaspase inhibitor (z-VAD-fmk), suggesting the involvement of caspases. Further, release of cytochrome c, activation of caspase-3 and cleavage of PARP were found in GLA-induced apoptosis.GLA treatment could also elevate lipid peroxidation in K562 cells, and antioxidant alpha-tocopherol could reverse the cytotoxicity of GLA. The saturated fatty acid SA, which did not exhibit significant increase in lipid peroxidation, also did not induce cytotoxicity. Intracellular GSH was also determined, and there was no marked change of GSH levels in cells after incubation with GLA compared with the control. These results demonstrate that GLA could induce apoptosis in K562 cells. Apoptosis is mediated by release of cytochrome c, activation of caspase-3. Lipid peroxidation may play a role in GLA cytotoxicity, according to "Gamma-linolenic acid induces apoptosis and lipid peroxidation in human chronic myelogenous leukemia K562 cells" by Ge H, Kong X, Shi L, Hou L, Liu Z, Li P.(10)
11. Etc.
Chinese Secrets To Fatty Liver And Obesity Reversal
Use The Revolutionary Findings To Achieve
Optimal Health And Loose Weight
Super foods Library, Eat Yourself Healthy With The Best of the Best Nature Has to Offer
Back to Popular Herbs http://kylejnorton.blogspot.ca/p/popular-herbs.html
Back to Kyle J. Norton Home page http://kylejnorton.blogspot.ca
Sources
(1) http://www.ncbi.nlm.nih.gov/pubmed/19887043
(2) http://www.ncbi.nlm.nih.gov/pubmed/17168669
(3) http://www.ncbi.nlm.nih.gov/pubmed/19014610
(4) http://www.ncbi.nlm.nih.gov/pubmed/22333072
(5) http://www.ncbi.nlm.nih.gov/pubmed/9732298
(6) http://www.ncbi.nlm.nih.gov/pubmed/22123240
(7) http://www.ncbi.nlm.nih.gov/pubmed/21917129
(8) http://www.ncbi.nlm.nih.gov/pubmed/21474219
(9) http://www.ncbi.nlm.nih.gov/pubmed/20664735
(10) http://www.ncbi.nlm.nih.gov/pubmed/19356705
Health Benefits
1. Neuropathic symptoms
in the evaluation of the effects of alpha-lipoic acid (ALA) and gamma-linolenic acid (GLA) and the beneficial effect of physical exercise on positive sensory symptoms and neuropathic pain in patients with compressive radiculopathy syndrome from disc-nerve root conflict, found that oral treatment with alpha-lipoic acid (ALA) and gamma-linolenic acid (GLA) for six weeks in synergy with rehabilitation therapy improved neuropathic symptoms and deficits in patients with radicular neuropathy, according to "The use of alpha-lipoic acid (ALA), gamma linolenic acid (GLA) and rehabilitation in the treatment of back pain: effect on health-related quality of life" by Ranieri M, Sciuscio M, Cortese AM, Santamato A, Di Teo L, Ianieri G, Bellomo RG, Stasi M, Megna M.(1)
2. Anti inflammatory effects
In the evaluation of wheather The PUFAs of omega-3 and omega-6 series play a significant role in health and disease by generating potent modulatory molecules for inflammatory responses,
found that GLA and its metabolites also affect expression of various genes where by regulating the levels of gene products including matrix proteins. These gene products play a significant role in immune functions and also in cell death (apoptosis). The present review will emphasize the role of GLA in modulating inflammatory response, and hence its potential applications as an anti-inflammatory nutrient or adjuvant, according to "Gamma linolenic acid: an antiinflammatory omega-6 fatty acid" by Kapoor R, Huang YS.(2)
3. Brain tumor
In the investigation of the effects of oral consumption of gamma linolenic acid (GLA) and docosahexaenoic acid (DHA) on brain tumor fatty acid composition, showed that dietary supplementation of DHA containing oil could be an effective way to increase levels of long chain n-3 fatty acids in brain tumors and this increase may be mediated partly by up-regulation of FABP7 expression, according to "The influence of feeding linoleic, gamma-linolenic and docosahexaenoic acid rich oils on rat brain tumor fatty acids composition and fatty acid binding protein 7 mRNA expression" by Nasrollahzadeh J, Siassi F, Doosti M, Eshraghian MR, Shokri F, Modarressi MH, Mohammadi-Asl J, Abdi K, Nikmanesh A, Karimian SM.(3)
4. Proliferation diseases
In the determination of a controversial dietary approaches focused on the diverse function of dihomo-dietary gamma-linolenic acid (DGLA) in anti-inflammation and anti-proliferation diseases, especially for cancers, found that hese compounds possess both anti-inflammatory and anti-proliferative properties. PGE1 could also induce growth inhibition and differentiation of cancer cells. Although the mechanism of DGLA has not yet been elucidated, it is significant to anticipate the antitumor potential benefits from DGLA, according to "Multiple roles of dihomo-gamma-linolenic acid against proliferation diseases" by Wang X, Lin H, Gu Y.(4)
5. Human health and nutrition
In the deiermination of weather a controversial dietary approaches has been the possible prophylactic role of dietary gamma-linolenic acid (GLA) in treating various chronic disease states, showed that these compounds possess both anti-inflammatory and antiproliferative properties. Although an optimal feeding regimen to maximize the potential benefits of dietary GLA has not yet been determined, it is the purpose of this review to summarize the most recent research that has focused on objectively and reproducibly determining the mechanism(s) by which GLA may ameliorate health problems, according to "Importance of dietary gamma-linolenic acid in human health and nutrition" by Fan YY, Chapkin RS.(5)
6. Skin protection
in the elucidation of the effect of GLA-rich oil on skin function, found that the mechanism of improvement of skin barrier has been associated with possible generation of anti-inflammatory metabolites from GLA. The clinical physician also confirmed that none of the subjects showed any noteworthy side effects. GLA-enriched food appears to be safe and to improve skin barrier function in subjects with dry skin conditions and mild atopic dermatitis, according to 'Dietary supplementation of gamma-linolenic acid improves skin parameters in subjects with dry skin and mild atopic dermatitis" by Kawamura A, Ooyama K, Kojima K, Kachi H, Abe T, Amano K, Aoyama T.(6)
7. Drug-sensitive and resistant tumor cells
In the investigation of weather dihomo-gamma-linolenic acid (DGLA) and AA, EPA and DHA have cytotoxic action on both vincristine-sensitive (KB-3-1) and resistant (KB-Ch(R)-8-5) cancer cells in vitro, indicated that GLA, DGLA, AA, EPA and DHA enhanced the uptake and decreased efflux in both drug-sensitive and drug-resistant cells and augmented the susceptibility of tumor cells especially, of drug-resistant cells to the cytotoxic action of vincristine. These results suggest that certain polyunsaturated fatty acids have tumoricidal action and are capable of enhancing the cytotoxic action of anti-cancer drugs specifically, on drug-resistant cells by enhancing drug uptake and reducing its efflux. Thus, polyunsaturated fatty acids either by themselves or in combination with chemotherapeutic drugs have the potential as anti-cancer molecules, according to "Effect of polyunsaturated fatty acids on drug-sensitive and resistant tumor cells in vitro" by Das UN, Madhavi N.(7)
8. Acute lung injury or acute respiratory distress syndrome (ARDS)
In the assessment of the effect of an enteral diet enriched with eicosapentaenoic acid (EPA), gamma-linolenic acid (GLA), and anti-oxidants on the incidence of organ dysfunction and nosocomial infections in septic patients with acute lung injury or acute respiratory distress syndrome (ARDS) compared with a standard enteral diet, found that A diet enriched with EPA, GLA, and anti-oxidants does not improve gas exchange or decrease the incidence of novel organ failures in critically ill septic patients with acute lung injury or ARDS. Patients treated with the EPA-GLA diet stayed in the ICU for less time, but we did not find any differences in infectious complications, according to "Effect of an enteral diet enriched with eicosapentaenoic acid, gamma-linolenic acid and anti-oxidants on the outcome of mechanically ventilated, critically ill, septic patients" by Grau-Carmona T, Morán-García V, García-de-Lorenzo A, Heras-de-la-Calle G, Quesada-Bellver B, López-Martínez J, González-Fernández C, Montejo-González JC, Blesa-Malpica A, Albert-Bonamusa I, Bonet-Saris A, Herrero-Meseguer JI, Mesejo A, Acosta J.(8)
9. Antineoplastic effects
In the investigation of the effect and the mechanism of gamma linolenic acid (GLA) treatment on human hepatocellular (HCC) cell lines, showed that GLA treatment has induced cell growth inhibition, ROS generation including lipid peroxidation, and HO-1 production for antioxidant protection against oxidative stress caused by GLA in Huh7 cells. GLA treatment should be considered as a therapeutic modality in patients with advanced HCC, according to "Antineoplastic effects of gamma linolenic Acid on hepatocellular carcinoma cell lines' by Itoh S, Taketomi A, Harimoto N, Tsujita E, Rikimaru T, Shirabe K, Shimada M, Maehara Y.(9)
10. Chronic myelogenous leukemia
In the testing the apoptotic effect of GLA on human chronic myelogenous leukemia K562 cells,
showed that the apoptosis could be inhibited by a pancaspase inhibitor (z-VAD-fmk), suggesting the involvement of caspases. Further, release of cytochrome c, activation of caspase-3 and cleavage of PARP were found in GLA-induced apoptosis.GLA treatment could also elevate lipid peroxidation in K562 cells, and antioxidant alpha-tocopherol could reverse the cytotoxicity of GLA. The saturated fatty acid SA, which did not exhibit significant increase in lipid peroxidation, also did not induce cytotoxicity. Intracellular GSH was also determined, and there was no marked change of GSH levels in cells after incubation with GLA compared with the control. These results demonstrate that GLA could induce apoptosis in K562 cells. Apoptosis is mediated by release of cytochrome c, activation of caspase-3. Lipid peroxidation may play a role in GLA cytotoxicity, according to "Gamma-linolenic acid induces apoptosis and lipid peroxidation in human chronic myelogenous leukemia K562 cells" by Ge H, Kong X, Shi L, Hou L, Liu Z, Li P.(10)
11. Etc.
Chinese Secrets To Fatty Liver And Obesity Reversal
Use The Revolutionary Findings To Achieve
Optimal Health And Loose Weight
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Back to Popular Herbs http://kylejnorton.blogspot.ca/p/popular-herbs.html
Back to Kyle J. Norton Home page http://kylejnorton.blogspot.ca
Sources
(1) http://www.ncbi.nlm.nih.gov/pubmed/19887043
(2) http://www.ncbi.nlm.nih.gov/pubmed/17168669
(3) http://www.ncbi.nlm.nih.gov/pubmed/19014610
(4) http://www.ncbi.nlm.nih.gov/pubmed/22333072
(5) http://www.ncbi.nlm.nih.gov/pubmed/9732298
(6) http://www.ncbi.nlm.nih.gov/pubmed/22123240
(7) http://www.ncbi.nlm.nih.gov/pubmed/21917129
(8) http://www.ncbi.nlm.nih.gov/pubmed/21474219
(9) http://www.ncbi.nlm.nih.gov/pubmed/20664735
(10) http://www.ncbi.nlm.nih.gov/pubmed/19356705
Phytochemicals in Foods - 12 Health Benefits of Oleanolic acid
Oleanolic acid is a phytochemincal in the subclass of
Triterpenoid, belonging to the group of Terpenes found abundantly in
honey mesquite, garlic, java apple, clove, etc.
Health Benefits
1. Anti infammatory effects
In the investigation by monitoring the effect of OA on lipopolysaccharide (LPS)-mediated release of HMGB1 and the HMGB1-mediated modulation of inflammatory responses in human umbilical vein endothelial cells (HUVECs), showed that OA potently inhibited the release of HMGB1 by HUVECs as well as down-regulated HMGB1-dependent adhesion and migration of the monocytic cell line THP-1 to activated HUVECs. OA also down-regulated the cell surface expression of the receptor of HMGB1, thereby inhibiting HMGB1-dependent pro-inflammatory responses by inhibiting activation of nuclear factor-κB (NF-κB) and production of tumor necrosis factor-α (TNF-α) by HMGB1, according to "Anti-inflammatory activities of oleanolic acid on HMGB1 activated HUVECs" by Yang EJ, Lee W, Ku SK, Song KS, Bae JS.(1)
2. Anti tumors effects
In the examination of the anti tumor effect of a new oleanolic triterpene, 3β,6β,19α-trihydroxy-12-oleanen-28-oic acid (1) obtained from the chloroform-soluble portion of the 90% alcohol-water extract of the stem bark of Uncaria macrophylla, found that as the cytotoxicities of the compound was evaluated against two cancer cell lines of MCF-7 and HepG2 by the MTT method, and the compound exhibited weak activities with the IC(50) values of 78.2 µg/mL and 73.9 µg/mL, according to "A New Triterpene From Uncaria macrophylla and Its Antitumor Activity" by Sun G, Zhang X, Xu X, Yang J, Zhong M, Yuan J.(2)
3. Non-small cell lung cancer
In the evaluation of wheather oleanolic acid (OA), a pentacyclic triterpene present in several plants, is able to circumvent the mechanisms of drug resistance present in non-small cell lung cancer (NSCLC) cell lines and to induce their death, indicated that the data provide a significant insight into the antitumoral and antimetastatic activity of OA in NSCLC and suggest that including OA in the NSCLC regimens may help to decrease the number of relapses and reduce the development of metastases, according to "Oleanolic acid initiates apoptosis in non-small cell lung cancer cell lines and reduces metastasis of a B16F10 melanoma model in vivo" by Lúcio KA, Rocha Gda G, Monção-Ribeiro LC, Fernandes J, Takiya CM, Gattass CR.(3)
4. Ovarian cancer
In the observation of the anticancer activity of methyl-2-cyano-3, 12-dioxooleana-1, 9(11)-dien-28-oate (CDDO-Me) derived from CDDO, a synthetic analog of oleanolic acid, and its mechanism of action in killing of human ovarian cancer cells, found that CDDO-Me strongly inhibited the growth of ovarian cancer cells by inducing apoptosis characterized by increased annexin V binding, cleavage of poly (ADP-ribose) polymerase (PARP-1) and procaspases-3, -8 and -9. In addition, CDDO-Me induced mitochondrial depolarization, according to "Synthetic oleanane triterpenoid, CDDO-Me, induces apoptosis in ovarian cancer cells by inhibiting prosurvival AKT/NF-κB/mTOR signaling" by Gao X, Liu Y, Deeb D, Arbab AS, Guo AM, Dulchavsky SA, Gautam SC.(4)
5. Prostate Cancer
In the deternimation of the efficacy of 2-Cyano-3,12-dioxooleana-1,9(11)-dien-28-oic acid (CDDO), a synthetic analog of oleanolic acid, and its C28 methyl ester derivative (CDDO-Me in preventing the development and progression of prostate cancer in the transgenic adenocarinoma of the mouse prostate (TRAMP) model, showed that treatment with CDDO-Me inhibited the expression of prosurvival p-Akt and NF-κB in the prostate and knocking-down Akt in TRAMPC-1 tumor cells sensitized them to CDDO-Me. These findings indicated that Akt is a target for apoptoxicity in TRAMPC-1 cells in vitro and potentially a target of CDDO-Me for inhibition of prostate cancer in vivo, according to 'Prevention of Prostate Cancer with Oleanane Synthetic Triterpenoid CDDO-Me in the TRAMP Mouse Model of Prostate Cancer" by Gao X, Deeb D, Liu Y, Arbab AS, Divine GW, Dulchavsky SA, Gautam SC.(5)
6. Multi-drug resistance cancers
In the study of the proliferation-inhibiting and apoptosis-inducing effects of ursolic acid (UA) and oleanolic acid (OA) on multi-drug resistance (MDR) cancer cells in vitro, indicated that Both UA and OA have antitumor effects on cancer cells with MDR, and the optimal effect is shown by UA on colonic cancer cells. Also, UA shows cell apoptosis-inducing effect on SW480, possibly by way of down-regulating the expressions of apoptosis antagonistic proteins, Bcl-2, Bcl-xL, and surviving, according to "Proliferation-inhibiting and apoptosis-inducing effects of ursolic acid and oleanolic acid on multi-drug resistance cancer cells in vitro" by Shan JZ, Xuan YY, Ruan SQ, Sun M.(6)
7. Pancreatic Cancer
In the evaluation of the antitumor activity and the mechanism of action of methyl-2-cyano-3,12-dioxooleana-1,9(11)-dien-28-oate (CDDO-Me), a oleanane-derived synthetic triterpenoid for human pancreatic cancer cell lines, found that CDDO-Me inhibited the growth of both K-ras mutated (MiaPaca2, Panc1 and Capan2) and wild-type K-ras (BxPC3) pancreatic cancer cells at very low concentrations. The growth inhibitory activity of CDDO-Me was attributed to the induction of apoptosis characterized by increased annexin-V-FITC binding and cleavage of PARP-1 and procaspases-3, -8 and-9. In addition, CDDO-Me induced the loss of mitochondrial membrane potential and release of cytochrome C. The antitumor activity of CDDO-Me was associated with the inhibition of prosurvival p-Akt, NF-κB and mammalian target of rapamycin (mTOR) signaling proteins and the downstream targets of Akt and mTOR, such as p-Foxo3a (Akt) and p-S6K1, p-eIF-4E and p-4E-BP1 (mTOR), according to "CDDO-Me: A Novel Synthetic Triterpenoid for the Treatment of Pancreatic Cancer" by Deeb D, Gao X, Arbab AS, Barton K, Dulchavsky SA, Gautam SC.(6)
7. Colorectal cancer
In the study of the role of free radicals in the growth inhibitory and apoptosis-inducing activity of CDDO-Me in colorectal cancer cells lines, found that CDDO-Me potently inhibited the growth of colorectal cancer cells and pretreatment of cancer cells with small-molecule antioxidant N-acetylcysteine (NAC) completely blocked the growth inhibitory activity of CDDO-Me. CDDO-Me caused the generation of reactive oxygen species, which was inhibited by NAC and mitochondrial chain 1 complex inhibitors DPI and rotenone. CDDO-Me induced apoptosis as demonstrated by the cleavage of PARP-1, activation of procaspases -3, -8, and -9 and mitochondrial depolarization and NAC blocked the activation of these apoptosis related processes, according to "Role of reactive oxygen species (ROS) in CDDO-Me-mediated growth inhibition and apoptosis in colorectal cancer cells" by Gao X, Deeb D, Liu P, Liu Y, Arbab-Ali S, Dulchavsky SA, Gautam SC.(7)
8. Neuroinflammatory disorders
In the demonstration of the dual capacity of triterpenoids to simultaneously repress production of IL-17 and other pro-inflammatory mediators while exerting neuroprotective effects directly through Nrf2-dependent induction of anti-oxidant genes, founm that CDDO-trifluoroethyl-amide (CDDO-TFEA), completely suppressed disease in a murine model of MS, experimental autoimmune encephalomyelitis (EAE), by inhibiting Th1 and Th17 mRNA and cytokine production. Encephalitogenic T cells recovered from treated mice were hypo-responsive to myelin antigen and failed to adoptively transfer the disease. Microarray analyses showed significant suppression of pro-inflammatory transcripts with concomitant induction of anti-inflammatory genes including Ptgds and Hsd11b1, according to "Triterpenoid modulation of IL-17 and Nrf-2 expression ameliorates neuroinflammation and promotes remyelination in autoimmune encephalomyelitis" by Pareek TK, Belkadi A, Kesavapany S, Zaremba A, Loh SL, Bai L, Cohen ML, Meyer C, Liby KT, Miller RH, Sporn MB, Letterio JJ.(8)
9. Antibiotic resistance
In the investigation of antibiotic resistance effects of oleanolic acid (OA) and ursolic acid (UA), among bacterial pathogens (Pseudomonas aeruginosa, Listeria monocytogenes, Staphylococcus aureus and Staphylococcus epidermidis), found that Using FICI value estimation and the time-kill method it was demonstrated that in some combinations, the tested compounds acted in synergy to lower the susceptibility of S. aureus, S. epidermidis and L. monocytogenes to ampicillin and oxacillin, but no synergy was observed for P. aeruginosa, according to "Modulation of antibiotic resistance in bacterial pathogens by oleanolic acid and ursolic acid" by Kurek A, Nadkowska P, Pliszka S, Wolska KI.(9)
10. Skin fibroblast cells
In the observation of how ursolic and oleanolic acids can be used for the purpose of quality control of natural products used in dermatocosmetology as well as of various other therapeutic preparations, showed that Of the two isomeric compounds, UA showed a higher cytotoxic activity against HSF cells than did OA. Our investigations showed that OA, in view of its non-toxic nature, may be used as a supplementary factor for dermal preparations, according to "The effect of ursolic and oleanolic acids on human skin fibroblast cells" by Wójciak-Kosior M, Paduch R, Matysik-Woźniak A, Niedziela P, Donica H.(10)
11. Diabetic nephropathy
In the investigation of the effect of a herbomineral formulation (HMF) on early diabetic nephropathy, indicated that our experimental findings clearly demonstrate that HMF has an ability to prevent the progression of early diabetic nephropathy. Such protective effect of HMF might be due to the presence of flavonoids (catechin, quercetin, rutin) and triterpene saponins (oleanolic acid and gymnemic acid) which are known to possess potent antioxidant properties, according to "Protective effect of herbomineral formulation (Dolabi) on early diabetic nephropathy in streptozotocin-induced diabetic rats' by Baig MA, Gawali VB, Patil RR, Naik SR.(11)
12. Antihypertensive, antiatherosclerotic, insulin resistanceand antioxidant activity
In the study of triterpenoids isolated of the African wild olive leaves (AO) used in the experiments was found to contain 0.27% 1:1 mixture of oleanolic acid and ursolic acid, named oleuafricein and of Greek olive leaves (GO) found to contain 0.71% oleanolic acid, and the Cape Town cultivar (CT) contained 2.47% oleanolic acid. No ursolic acid was found in either GO or CT.
found that Aal three isolates, in a dose 60 mg/kg b.w. for 6 weeks treatment, prevented the development of severe hypertension and atherosclerosis and improved the insulin resistance of the experimental animals. GO, OA and CT isolates could provide an effective and cheap treatment of this particular, most common type of salt-sensitive hypertension in the African population, according to "Antihypertensive, antiatherosclerotic and antioxidant activity of triterpenoids isolated from Olea europaea, subspecies africana leaves" by Somova LI, Shode FO, Ramnanan P, Nadar A.(12)
Chinese Secrets To Fatty Liver And Obesity Reversal
Use The Revolutionary Findings To Achieve
Optimal Health And Loose Weight
Super foods Library, Eat Yourself Healthy With The Best of the Best Nature Has to Offer
Back to Popular Herbs http://kylejnorton.blogspot.ca/p/popular-herbs.html
Back to Kyle J. Norton Home page http://kylejnorton.blogspot.ca
Sources
(1) http://www.ncbi.nlm.nih.gov/pubmed/22386814
(2) http://www.ncbi.nlm.nih.gov/pubmed/22334066
(3) http://www.ncbi.nlm.nih.gov/pubmed/22174843
(4) http://www.ncbi.nlm.nih.gov/pubmed/22110186
(5) http://www.ncbi.nlm.nih.gov/pubmed/21961053
(6) http://www.ncbi.nlm.nih.gov/pubmed/21799944
(7) http://www.ncbi.nlm.nih.gov/pubmed/21699019
(8) http://www.ncbi.nlm.nih.gov/pubmed/22355716
(9) http://www.ncbi.nlm.nih.gov/pubmed/22341643
(10) http://www.ncbi.nlm.nih.gov/pubmed/22252762
(11) http://www.ncbi.nlm.nih.gov/pubmed/22116744
(12) http://www.ncbi.nlm.nih.gov/pubmed/12648829
Health Benefits
1. Anti infammatory effects
In the investigation by monitoring the effect of OA on lipopolysaccharide (LPS)-mediated release of HMGB1 and the HMGB1-mediated modulation of inflammatory responses in human umbilical vein endothelial cells (HUVECs), showed that OA potently inhibited the release of HMGB1 by HUVECs as well as down-regulated HMGB1-dependent adhesion and migration of the monocytic cell line THP-1 to activated HUVECs. OA also down-regulated the cell surface expression of the receptor of HMGB1, thereby inhibiting HMGB1-dependent pro-inflammatory responses by inhibiting activation of nuclear factor-κB (NF-κB) and production of tumor necrosis factor-α (TNF-α) by HMGB1, according to "Anti-inflammatory activities of oleanolic acid on HMGB1 activated HUVECs" by Yang EJ, Lee W, Ku SK, Song KS, Bae JS.(1)
2. Anti tumors effects
In the examination of the anti tumor effect of a new oleanolic triterpene, 3β,6β,19α-trihydroxy-12-oleanen-28-oic acid (1) obtained from the chloroform-soluble portion of the 90% alcohol-water extract of the stem bark of Uncaria macrophylla, found that as the cytotoxicities of the compound was evaluated against two cancer cell lines of MCF-7 and HepG2 by the MTT method, and the compound exhibited weak activities with the IC(50) values of 78.2 µg/mL and 73.9 µg/mL, according to "A New Triterpene From Uncaria macrophylla and Its Antitumor Activity" by Sun G, Zhang X, Xu X, Yang J, Zhong M, Yuan J.(2)
3. Non-small cell lung cancer
In the evaluation of wheather oleanolic acid (OA), a pentacyclic triterpene present in several plants, is able to circumvent the mechanisms of drug resistance present in non-small cell lung cancer (NSCLC) cell lines and to induce their death, indicated that the data provide a significant insight into the antitumoral and antimetastatic activity of OA in NSCLC and suggest that including OA in the NSCLC regimens may help to decrease the number of relapses and reduce the development of metastases, according to "Oleanolic acid initiates apoptosis in non-small cell lung cancer cell lines and reduces metastasis of a B16F10 melanoma model in vivo" by Lúcio KA, Rocha Gda G, Monção-Ribeiro LC, Fernandes J, Takiya CM, Gattass CR.(3)
4. Ovarian cancer
In the observation of the anticancer activity of methyl-2-cyano-3, 12-dioxooleana-1, 9(11)-dien-28-oate (CDDO-Me) derived from CDDO, a synthetic analog of oleanolic acid, and its mechanism of action in killing of human ovarian cancer cells, found that CDDO-Me strongly inhibited the growth of ovarian cancer cells by inducing apoptosis characterized by increased annexin V binding, cleavage of poly (ADP-ribose) polymerase (PARP-1) and procaspases-3, -8 and -9. In addition, CDDO-Me induced mitochondrial depolarization, according to "Synthetic oleanane triterpenoid, CDDO-Me, induces apoptosis in ovarian cancer cells by inhibiting prosurvival AKT/NF-κB/mTOR signaling" by Gao X, Liu Y, Deeb D, Arbab AS, Guo AM, Dulchavsky SA, Gautam SC.(4)
5. Prostate Cancer
In the deternimation of the efficacy of 2-Cyano-3,12-dioxooleana-1,9(11)-dien-28-oic acid (CDDO), a synthetic analog of oleanolic acid, and its C28 methyl ester derivative (CDDO-Me in preventing the development and progression of prostate cancer in the transgenic adenocarinoma of the mouse prostate (TRAMP) model, showed that treatment with CDDO-Me inhibited the expression of prosurvival p-Akt and NF-κB in the prostate and knocking-down Akt in TRAMPC-1 tumor cells sensitized them to CDDO-Me. These findings indicated that Akt is a target for apoptoxicity in TRAMPC-1 cells in vitro and potentially a target of CDDO-Me for inhibition of prostate cancer in vivo, according to 'Prevention of Prostate Cancer with Oleanane Synthetic Triterpenoid CDDO-Me in the TRAMP Mouse Model of Prostate Cancer" by Gao X, Deeb D, Liu Y, Arbab AS, Divine GW, Dulchavsky SA, Gautam SC.(5)
6. Multi-drug resistance cancers
In the study of the proliferation-inhibiting and apoptosis-inducing effects of ursolic acid (UA) and oleanolic acid (OA) on multi-drug resistance (MDR) cancer cells in vitro, indicated that Both UA and OA have antitumor effects on cancer cells with MDR, and the optimal effect is shown by UA on colonic cancer cells. Also, UA shows cell apoptosis-inducing effect on SW480, possibly by way of down-regulating the expressions of apoptosis antagonistic proteins, Bcl-2, Bcl-xL, and surviving, according to "Proliferation-inhibiting and apoptosis-inducing effects of ursolic acid and oleanolic acid on multi-drug resistance cancer cells in vitro" by Shan JZ, Xuan YY, Ruan SQ, Sun M.(6)
7. Pancreatic Cancer
In the evaluation of the antitumor activity and the mechanism of action of methyl-2-cyano-3,12-dioxooleana-1,9(11)-dien-28-oate (CDDO-Me), a oleanane-derived synthetic triterpenoid for human pancreatic cancer cell lines, found that CDDO-Me inhibited the growth of both K-ras mutated (MiaPaca2, Panc1 and Capan2) and wild-type K-ras (BxPC3) pancreatic cancer cells at very low concentrations. The growth inhibitory activity of CDDO-Me was attributed to the induction of apoptosis characterized by increased annexin-V-FITC binding and cleavage of PARP-1 and procaspases-3, -8 and-9. In addition, CDDO-Me induced the loss of mitochondrial membrane potential and release of cytochrome C. The antitumor activity of CDDO-Me was associated with the inhibition of prosurvival p-Akt, NF-κB and mammalian target of rapamycin (mTOR) signaling proteins and the downstream targets of Akt and mTOR, such as p-Foxo3a (Akt) and p-S6K1, p-eIF-4E and p-4E-BP1 (mTOR), according to "CDDO-Me: A Novel Synthetic Triterpenoid for the Treatment of Pancreatic Cancer" by Deeb D, Gao X, Arbab AS, Barton K, Dulchavsky SA, Gautam SC.(6)
7. Colorectal cancer
In the study of the role of free radicals in the growth inhibitory and apoptosis-inducing activity of CDDO-Me in colorectal cancer cells lines, found that CDDO-Me potently inhibited the growth of colorectal cancer cells and pretreatment of cancer cells with small-molecule antioxidant N-acetylcysteine (NAC) completely blocked the growth inhibitory activity of CDDO-Me. CDDO-Me caused the generation of reactive oxygen species, which was inhibited by NAC and mitochondrial chain 1 complex inhibitors DPI and rotenone. CDDO-Me induced apoptosis as demonstrated by the cleavage of PARP-1, activation of procaspases -3, -8, and -9 and mitochondrial depolarization and NAC blocked the activation of these apoptosis related processes, according to "Role of reactive oxygen species (ROS) in CDDO-Me-mediated growth inhibition and apoptosis in colorectal cancer cells" by Gao X, Deeb D, Liu P, Liu Y, Arbab-Ali S, Dulchavsky SA, Gautam SC.(7)
8. Neuroinflammatory disorders
In the demonstration of the dual capacity of triterpenoids to simultaneously repress production of IL-17 and other pro-inflammatory mediators while exerting neuroprotective effects directly through Nrf2-dependent induction of anti-oxidant genes, founm that CDDO-trifluoroethyl-amide (CDDO-TFEA), completely suppressed disease in a murine model of MS, experimental autoimmune encephalomyelitis (EAE), by inhibiting Th1 and Th17 mRNA and cytokine production. Encephalitogenic T cells recovered from treated mice were hypo-responsive to myelin antigen and failed to adoptively transfer the disease. Microarray analyses showed significant suppression of pro-inflammatory transcripts with concomitant induction of anti-inflammatory genes including Ptgds and Hsd11b1, according to "Triterpenoid modulation of IL-17 and Nrf-2 expression ameliorates neuroinflammation and promotes remyelination in autoimmune encephalomyelitis" by Pareek TK, Belkadi A, Kesavapany S, Zaremba A, Loh SL, Bai L, Cohen ML, Meyer C, Liby KT, Miller RH, Sporn MB, Letterio JJ.(8)
9. Antibiotic resistance
In the investigation of antibiotic resistance effects of oleanolic acid (OA) and ursolic acid (UA), among bacterial pathogens (Pseudomonas aeruginosa, Listeria monocytogenes, Staphylococcus aureus and Staphylococcus epidermidis), found that Using FICI value estimation and the time-kill method it was demonstrated that in some combinations, the tested compounds acted in synergy to lower the susceptibility of S. aureus, S. epidermidis and L. monocytogenes to ampicillin and oxacillin, but no synergy was observed for P. aeruginosa, according to "Modulation of antibiotic resistance in bacterial pathogens by oleanolic acid and ursolic acid" by Kurek A, Nadkowska P, Pliszka S, Wolska KI.(9)
10. Skin fibroblast cells
In the observation of how ursolic and oleanolic acids can be used for the purpose of quality control of natural products used in dermatocosmetology as well as of various other therapeutic preparations, showed that Of the two isomeric compounds, UA showed a higher cytotoxic activity against HSF cells than did OA. Our investigations showed that OA, in view of its non-toxic nature, may be used as a supplementary factor for dermal preparations, according to "The effect of ursolic and oleanolic acids on human skin fibroblast cells" by Wójciak-Kosior M, Paduch R, Matysik-Woźniak A, Niedziela P, Donica H.(10)
11. Diabetic nephropathy
In the investigation of the effect of a herbomineral formulation (HMF) on early diabetic nephropathy, indicated that our experimental findings clearly demonstrate that HMF has an ability to prevent the progression of early diabetic nephropathy. Such protective effect of HMF might be due to the presence of flavonoids (catechin, quercetin, rutin) and triterpene saponins (oleanolic acid and gymnemic acid) which are known to possess potent antioxidant properties, according to "Protective effect of herbomineral formulation (Dolabi) on early diabetic nephropathy in streptozotocin-induced diabetic rats' by Baig MA, Gawali VB, Patil RR, Naik SR.(11)
12. Antihypertensive, antiatherosclerotic, insulin resistanceand antioxidant activity
In the study of triterpenoids isolated of the African wild olive leaves (AO) used in the experiments was found to contain 0.27% 1:1 mixture of oleanolic acid and ursolic acid, named oleuafricein and of Greek olive leaves (GO) found to contain 0.71% oleanolic acid, and the Cape Town cultivar (CT) contained 2.47% oleanolic acid. No ursolic acid was found in either GO or CT.
found that Aal three isolates, in a dose 60 mg/kg b.w. for 6 weeks treatment, prevented the development of severe hypertension and atherosclerosis and improved the insulin resistance of the experimental animals. GO, OA and CT isolates could provide an effective and cheap treatment of this particular, most common type of salt-sensitive hypertension in the African population, according to "Antihypertensive, antiatherosclerotic and antioxidant activity of triterpenoids isolated from Olea europaea, subspecies africana leaves" by Somova LI, Shode FO, Ramnanan P, Nadar A.(12)
Chinese Secrets To Fatty Liver And Obesity Reversal
Use The Revolutionary Findings To Achieve
Optimal Health And Loose Weight
Super foods Library, Eat Yourself Healthy With The Best of the Best Nature Has to Offer
Back to Popular Herbs http://kylejnorton.blogspot.ca/p/popular-herbs.html
Back to Kyle J. Norton Home page http://kylejnorton.blogspot.ca
Sources
(1) http://www.ncbi.nlm.nih.gov/pubmed/22386814
(2) http://www.ncbi.nlm.nih.gov/pubmed/22334066
(3) http://www.ncbi.nlm.nih.gov/pubmed/22174843
(4) http://www.ncbi.nlm.nih.gov/pubmed/22110186
(5) http://www.ncbi.nlm.nih.gov/pubmed/21961053
(6) http://www.ncbi.nlm.nih.gov/pubmed/21799944
(7) http://www.ncbi.nlm.nih.gov/pubmed/21699019
(8) http://www.ncbi.nlm.nih.gov/pubmed/22355716
(9) http://www.ncbi.nlm.nih.gov/pubmed/22341643
(10) http://www.ncbi.nlm.nih.gov/pubmed/22252762
(11) http://www.ncbi.nlm.nih.gov/pubmed/22116744
(12) http://www.ncbi.nlm.nih.gov/pubmed/12648829
Phytochemicals in Foods - 13 Health Benefits of Ursolic acid
Ursolic acid is a phytochemincal in the subclass of
Triterpenoid, belonging to the group of Terpenes found abundantly in
apples, basil, bilberries, cranberries, peppermint, lavender, oregano,
hawthorn, prunes., etc.
Health Benefits
1. Multi-drug resistance cancers
In the study of the proliferation-inhibiting and apoptosis-inducing effects of ursolic acid (UA) and oleanolic acid (OA) on multi-drug resistance (MDR) cancer cells in vitro, indicated that Both UA and OA have antitumor effects on cancer cells with MDR, and the optimal effect is shown by UA on colonic cancer cells. Also, UA shows cell apoptosis-inducing effect on SW480, possibly by way of down-regulating the expressions of apoptosis antagonistic proteins, Bcl-2, Bcl-xL, and surviving, according to "Proliferation-inhibiting and apoptosis-inducing effects of ursolic acid and oleanolic acid on multi-drug resistance cancer cells in vitro" by Shan JZ, Xuan YY, Ruan SQ, Sun M.(1)
2. Skin fibroblast cells
In the observation of how ursolic and oleanolic acids can be used for the purpose of quality control of natural products used in dermatocosmetology as well as of various other therapeutic preparations, showed that Of the two isomeric compounds, UA showed a higher cytotoxic activity against HSF cells than did OA. Our investigations showed that OA, in view of its non-toxic nature, may be used as a supplementary factor for dermal preparations, according to "The effect of ursolic and oleanolic acids on human skin fibroblast cells" by Wójciak-Kosior M, Paduch R, Matysik-Woźniak A, Niedziela P, Donica H.(2)
3. Antibiotic resistance
In the investigation of antibiotic resistance effects of oleanolic acid (OA) and ursolic acid (UA), among bacterial pathogens (Pseudomonas aeruginosa, Listeria monocytogenes, Staphylococcus aureus and Staphylococcus epidermidis), found that Using FICI value estimation and the time-kill method it was demonstrated that in some combinations, the tested compounds acted in synergy to lower the susceptibility of S. aureus, S. epidermidis and L. monocytogenes to ampicillin and oxacillin, but no synergy was observed for P. aeruginosa, according to "Modulation of antibiotic resistance in bacterial pathogens by oleanolic acid and ursolic acid" by Kurek A, Nadkowska P, Pliszka S, Wolska KI.(3)
4. Cytotoxic activites
In the evaluation of the anti-proliferative capability of the derivatives of C-3 and C-28 positions of ursolic acid (UA). against HepG2, AGS, HT-29 and PC-3 cells by the MTT assay, showed the cytotoxic capacity of the compounds was: Group I
5. Hepatocellular carcinoma
In the study of the inhibitory effect and mechanisms of UA on the human hepatoma cell line SMMC-7721, indicated that the proliferation of SMMC-7721 cells was significantly inhibited in a dose- and time-dependent manner after UA treatment. UA induced cell cycle arrest and apoptosis. The DNA microarray analysis indicated that 64 genes were found to be markedly up- or down-expressed, including GDF15, SOD2, ATF3, and fos, according to "Ursolic acid induces human hepatoma cell line SMMC-7721 apoptosis via p53-dependent pathway" by Yu YX, Gu ZL, Yin JL, Chou WH, Kwok CY, Qin ZH, Liang ZQ.(5)
6. Bladder cancer
In the investigation of Ursolic acid (UA) anti-tumor properties against bladder cancer, found that the ceramide level was increased after UA treatment in T24 cells, and UA-induced AMPK activation and T24 cell apoptosis were inhibited by ceramide synthase inhibitor fumonisin B1, and was enhanced by exogenously adding cell permeable short-chain ceramide (C6), suggesting that ceramide might serve as an upstream signal for AMPK activation. Further, activation of AMPK by UA promoted c-Jun N-terminal kinase (JNK) activation, but inhibited mTOR complex 1 (mTORC1) signaling to cause survivin down-regulation, according to " Ursolic acid-induced AMP-activated protein kinase (AMPK) activation contributes to growth inhibition and apoptosis in human bladder cancer T24 cells" by Zheng QY, Yao C, Jin F, Zhang Y, Zhang GH.(6)
7. Anti cancers
In the investigation of QSAR models for predicting the activities of ursolic acid analogs against human lung (A-549) and CNS (SF-295) cancer cell lines, indicated that The QSAR study indicated that the LUMO energy, ring count, and solvent-accessible surface area were strongly correlated with anticancer activity. Similarly, the QSAR model for cytotoxic activity against the human CNS cancer cell line (SF-295) also showed a high correlation (r (2) = 0.99 and rCV(2) = 0.96), and indicated that dipole vector and solvent-accessible surface area were strongly correlated with activity. Ursolic acid analogs that were predicted to be active against these cancer cell lines by the QSAR models were semisynthesized and characterized on the basis of their (1)H and (13)C NMR spectroscopic data, and were then tested in vitro against the human lung (A-549) and CNS (SF-295) cancer cell lines. The experimental results obtained agreed well with the predicted values, according to "Pharmacophore, QSAR, and ADME based semisynthesis and in vitro evaluation of ursolic acid analogs for anticancer activity" by Kalani K, Yadav DK, Khan F, Srivastava SK, Suri N.(7)
8. Hippocrates, "Let food be thy medicine and medicine be thy food"
In the determination of the traditional medicine and diet on mankind through the ages for prevention and treatment of most chronic diseases, found that suggests that chronic inflammation mediates most chronic diseases, including cancer. More than other transcription factors, nuclear factor-kappaB (NF-κB) and STAT3 have emerged as major regulators of inflammation, cellular transformation, and tumor cell survival, proliferation, invasion, angiogenesis, and metastasis. Thus, agents ( avicins, betulinic acid, boswellic acid, celastrol, diosgenin, madecassic acid, maslinic acid, momordin, saikosaponins, platycodon, pristimerin, ursolic acid, and withanolide) that can inhibit NF-κB and STAT3 activation pathways have the potential to both prevent and treat cancer, according to "Targeting inflammatory pathways by triterpenoids for prevention and treatment of cancer" by Yadav VR, Prasad S, Sung B, Kannappan R, Aggarwal BB.(8)
9. Photoprotection
Inn the evaluation of photoprotective effects of against UVAR of triterpenoids, indicated that natural material-derived triterpenoids such as oleanolic acid can abrogate UVA-induced gene expression by raft stabilization. This effect depends on the structure of the molecule, because its isomer ursolic acid also integrates within the rafts without inhibiting ceramide formation and upregulation of gene expression, according to "Photoprotection against UVAR: effective triterpenoids require a lipid raft stabilizing chemical structure" by Bayer M, Proksch P, Felsner I, Brenden H, Kohne Z, Walli R, Duong TN, Götz C, Krutmann J, Grether-Beck S.(9)
10. Cardiotonic and antidysrhythmic effects
In the study of the cardiotonic and antidysrhythmic effects of four triterpenoid derivatives, namely oleanolic acid (OA), ursolic acid (UA), and uvaol (UV), isolated from the leaves of African wild olive (Olea europaea, subsp. africana) as well as methyl maslinate (MM) isolated from the leaves of Olea europaea (Cape cultivar), found that OA and UV isolated from wild African olive leaves, or crude extract containing all components, can provide a cheap and accessible source of additive to conventional treatment of hypertension, complicated by stenocardia and cardiac failure, according to "Cardiotonic and antidysrhythmic effects of oleanolic and ursolic acids, methyl maslinate and uvaol" by Somova LI, Shode FO, Mipando M.(10)
11. Etc.
Chinese Secrets To Fatty Liver And Obesity Reversal
Use The Revolutionary Findings To Achieve
Optimal Health And Loose Weight
Super foods Library, Eat Yourself Healthy With The Best of the Best Nature Has to Offer
Back to Popular Herbs http://kylejnorton.blogspot.ca/p/popular-herbs.html
Back to Kyle J. Norton Home page http://kylejnorton.blogspot.ca
Sources
(1) http://www.ncbi.nlm.nih.gov/pubmed/21799944
(2) http://www.ncbi.nlm.nih.gov/pubmed/22252762
(3)
(4) http://www.ncbi.nlm.nih.gov/pubmed/22370266
(5) http://www.ncbi.nlm.nih.gov/pubmed/20819578
(6) http://www.ncbi.nlm.nih.gov/pubmed/22387548
(7) http://www.ncbi.nlm.nih.gov/pubmed/22271093
(8) http://www.ncbi.nlm.nih.gov/pubmed/22069560
(9) http://www.ncbi.nlm.nih.gov/pubmed/21824200
(10) http://www.ncbi.nlm.nih.gov/pubmed/15070161
(11) http://www.ncbi.nlm.nih.gov/pubmed/12648829
Health Benefits
1. Multi-drug resistance cancers
In the study of the proliferation-inhibiting and apoptosis-inducing effects of ursolic acid (UA) and oleanolic acid (OA) on multi-drug resistance (MDR) cancer cells in vitro, indicated that Both UA and OA have antitumor effects on cancer cells with MDR, and the optimal effect is shown by UA on colonic cancer cells. Also, UA shows cell apoptosis-inducing effect on SW480, possibly by way of down-regulating the expressions of apoptosis antagonistic proteins, Bcl-2, Bcl-xL, and surviving, according to "Proliferation-inhibiting and apoptosis-inducing effects of ursolic acid and oleanolic acid on multi-drug resistance cancer cells in vitro" by Shan JZ, Xuan YY, Ruan SQ, Sun M.(1)
2. Skin fibroblast cells
In the observation of how ursolic and oleanolic acids can be used for the purpose of quality control of natural products used in dermatocosmetology as well as of various other therapeutic preparations, showed that Of the two isomeric compounds, UA showed a higher cytotoxic activity against HSF cells than did OA. Our investigations showed that OA, in view of its non-toxic nature, may be used as a supplementary factor for dermal preparations, according to "The effect of ursolic and oleanolic acids on human skin fibroblast cells" by Wójciak-Kosior M, Paduch R, Matysik-Woźniak A, Niedziela P, Donica H.(2)
3. Antibiotic resistance
In the investigation of antibiotic resistance effects of oleanolic acid (OA) and ursolic acid (UA), among bacterial pathogens (Pseudomonas aeruginosa, Listeria monocytogenes, Staphylococcus aureus and Staphylococcus epidermidis), found that Using FICI value estimation and the time-kill method it was demonstrated that in some combinations, the tested compounds acted in synergy to lower the susceptibility of S. aureus, S. epidermidis and L. monocytogenes to ampicillin and oxacillin, but no synergy was observed for P. aeruginosa, according to "Modulation of antibiotic resistance in bacterial pathogens by oleanolic acid and ursolic acid" by Kurek A, Nadkowska P, Pliszka S, Wolska KI.(3)
4. Cytotoxic activites
In the evaluation of the anti-proliferative capability of the derivatives of C-3 and C-28 positions of ursolic acid (UA). against HepG2, AGS, HT-29 and PC-3 cells by the MTT assay, showed the cytotoxic capacity of the compounds was: Group I
5. Hepatocellular carcinoma
In the study of the inhibitory effect and mechanisms of UA on the human hepatoma cell line SMMC-7721, indicated that the proliferation of SMMC-7721 cells was significantly inhibited in a dose- and time-dependent manner after UA treatment. UA induced cell cycle arrest and apoptosis. The DNA microarray analysis indicated that 64 genes were found to be markedly up- or down-expressed, including GDF15, SOD2, ATF3, and fos, according to "Ursolic acid induces human hepatoma cell line SMMC-7721 apoptosis via p53-dependent pathway" by Yu YX, Gu ZL, Yin JL, Chou WH, Kwok CY, Qin ZH, Liang ZQ.(5)
6. Bladder cancer
In the investigation of Ursolic acid (UA) anti-tumor properties against bladder cancer, found that the ceramide level was increased after UA treatment in T24 cells, and UA-induced AMPK activation and T24 cell apoptosis were inhibited by ceramide synthase inhibitor fumonisin B1, and was enhanced by exogenously adding cell permeable short-chain ceramide (C6), suggesting that ceramide might serve as an upstream signal for AMPK activation. Further, activation of AMPK by UA promoted c-Jun N-terminal kinase (JNK) activation, but inhibited mTOR complex 1 (mTORC1) signaling to cause survivin down-regulation, according to " Ursolic acid-induced AMP-activated protein kinase (AMPK) activation contributes to growth inhibition and apoptosis in human bladder cancer T24 cells" by Zheng QY, Yao C, Jin F, Zhang Y, Zhang GH.(6)
7. Anti cancers
In the investigation of QSAR models for predicting the activities of ursolic acid analogs against human lung (A-549) and CNS (SF-295) cancer cell lines, indicated that The QSAR study indicated that the LUMO energy, ring count, and solvent-accessible surface area were strongly correlated with anticancer activity. Similarly, the QSAR model for cytotoxic activity against the human CNS cancer cell line (SF-295) also showed a high correlation (r (2) = 0.99 and rCV(2) = 0.96), and indicated that dipole vector and solvent-accessible surface area were strongly correlated with activity. Ursolic acid analogs that were predicted to be active against these cancer cell lines by the QSAR models were semisynthesized and characterized on the basis of their (1)H and (13)C NMR spectroscopic data, and were then tested in vitro against the human lung (A-549) and CNS (SF-295) cancer cell lines. The experimental results obtained agreed well with the predicted values, according to "Pharmacophore, QSAR, and ADME based semisynthesis and in vitro evaluation of ursolic acid analogs for anticancer activity" by Kalani K, Yadav DK, Khan F, Srivastava SK, Suri N.(7)
8. Hippocrates, "Let food be thy medicine and medicine be thy food"
In the determination of the traditional medicine and diet on mankind through the ages for prevention and treatment of most chronic diseases, found that suggests that chronic inflammation mediates most chronic diseases, including cancer. More than other transcription factors, nuclear factor-kappaB (NF-κB) and STAT3 have emerged as major regulators of inflammation, cellular transformation, and tumor cell survival, proliferation, invasion, angiogenesis, and metastasis. Thus, agents ( avicins, betulinic acid, boswellic acid, celastrol, diosgenin, madecassic acid, maslinic acid, momordin, saikosaponins, platycodon, pristimerin, ursolic acid, and withanolide) that can inhibit NF-κB and STAT3 activation pathways have the potential to both prevent and treat cancer, according to "Targeting inflammatory pathways by triterpenoids for prevention and treatment of cancer" by Yadav VR, Prasad S, Sung B, Kannappan R, Aggarwal BB.(8)
9. Photoprotection
Inn the evaluation of photoprotective effects of against UVAR of triterpenoids, indicated that natural material-derived triterpenoids such as oleanolic acid can abrogate UVA-induced gene expression by raft stabilization. This effect depends on the structure of the molecule, because its isomer ursolic acid also integrates within the rafts without inhibiting ceramide formation and upregulation of gene expression, according to "Photoprotection against UVAR: effective triterpenoids require a lipid raft stabilizing chemical structure" by Bayer M, Proksch P, Felsner I, Brenden H, Kohne Z, Walli R, Duong TN, Götz C, Krutmann J, Grether-Beck S.(9)
10. Cardiotonic and antidysrhythmic effects
In the study of the cardiotonic and antidysrhythmic effects of four triterpenoid derivatives, namely oleanolic acid (OA), ursolic acid (UA), and uvaol (UV), isolated from the leaves of African wild olive (Olea europaea, subsp. africana) as well as methyl maslinate (MM) isolated from the leaves of Olea europaea (Cape cultivar), found that OA and UV isolated from wild African olive leaves, or crude extract containing all components, can provide a cheap and accessible source of additive to conventional treatment of hypertension, complicated by stenocardia and cardiac failure, according to "Cardiotonic and antidysrhythmic effects of oleanolic and ursolic acids, methyl maslinate and uvaol" by Somova LI, Shode FO, Mipando M.(10)
11. Etc.
Chinese Secrets To Fatty Liver And Obesity Reversal
Use The Revolutionary Findings To Achieve
Optimal Health And Loose Weight
Super foods Library, Eat Yourself Healthy With The Best of the Best Nature Has to Offer
Back to Popular Herbs http://kylejnorton.blogspot.ca/p/popular-herbs.html
Back to Kyle J. Norton Home page http://kylejnorton.blogspot.ca
Sources
(1) http://www.ncbi.nlm.nih.gov/pubmed/21799944
(2) http://www.ncbi.nlm.nih.gov/pubmed/22252762
(3)
(4) http://www.ncbi.nlm.nih.gov/pubmed/22370266
(5) http://www.ncbi.nlm.nih.gov/pubmed/20819578
(6) http://www.ncbi.nlm.nih.gov/pubmed/22387548
(7) http://www.ncbi.nlm.nih.gov/pubmed/22271093
(8) http://www.ncbi.nlm.nih.gov/pubmed/22069560
(9) http://www.ncbi.nlm.nih.gov/pubmed/21824200
(10) http://www.ncbi.nlm.nih.gov/pubmed/15070161
(11) http://www.ncbi.nlm.nih.gov/pubmed/12648829
Phytochemicals in Foods - 6 Health Benefits of Moronic acid
Moronic acid is a phytochemincal in the subclass of Triterpenoid, belonging to the group of Terpenes found in extracted from Rhus javanica, Mistletoe, etc.
Health Benefits
1. HIV maturation inhibitor
In the study of triterpene derivatives as potent anti-HIV agents, different C-3 conformationally restricted betulinic acid (BA, 1) derivatives were designed and synthesized in order to explore the conformational space of the C-3 pharmacophore. 3-O-Monomethylsuccinyl-betulinic acid (MSB) analogues were also designed to better understand the contribution of the C-3' dimethyl group of bevirimat (2), the first-in-class HIV maturation inhibitor, which is currently in phase IIb clinical trials. In addition, another triterpene skeleton, moronic acid (MA, 3), was also employed to study the influence of the backbone and the C-3 modification toward the anti-HIV activity of this compound class, may lead to led to the design and synthesis of compound 12 (EC(50): 0.0006 microM), which displayed slightly better activity than 2 as a HIV-1 maturation inhibitor, according to " Anti-AIDS agents 81. Design, synthesis, and structure-activity relationship study of betulinic acid and moronic acid derivatives as potent HIV maturation inhibitors" by Qian K, Kuo RY, Chen CH, Huang L, Morris-Natschke SL, Lee KH.(1)
2. Anti- Epstein-Barr virus
In the investigation of moronic acid, found in galls of Rhus chinensis and Brazilian propolis, at 10microM inhibits the expression of Rta, Zta, and an EBV early protein, EA-D, after lytic induction with sodium butyrate, found that moronic acids inhibits the capacity of Rta to activate a promoter that contains an Rta-response element, indicating that moronic acid interferes with the function of Rta. On the other hand, moronic acid does not appear to influence with the transactivation function of Zta. Therefore, the lack of expression of Zta and EA-D after moronic acid treatment is attributable to the inhibition of the transactivation functions of Rta. Because the expression of Zta, EA-D and many EBV lytic genes depends on Rta, the treatment of P3HR1 cells with moronic acid substantially reduces the numbers of EBV particles produced by the cells after lytic induction, according to "Inhibition of the Epstein-Barr virus lytic cycle by moronic acid" by Chang FR, Hsieh YC, Chang YF, Lee KH, Wu YC, Chang LK.(2)
3. Anti fungal effects
In the determination of The effect of compound isolated from ethanol extract from Xyris pteygoblephara aerial parts against five microorganism strains, by the microdilution and agar diffusion methods, indicated that assay of 1 (100 microg/disc) by the agar diffusion method against clinical isolates of the dermatophytes Epidermophyton floccosum (inhibition zone, mm+/-s.d.: 4.5+/-0.8), Trichophyton mentagrophytes (4.8+/-0.4) and Trichophyton rubrum (10.2+/-0.8) revealed similar inhibition zones to the positive control amphotericin B (32 microg/disc; 5.0+/-0.2; 5.0+/-0.6 and 8.8+/-1.2, respectively), according to "Dihydroisocoumarin from Xyris pterygoblephara active against dermatophyte fungi" by Guimarães KG, de Souza Filho JD, Dos Mares-Guia TR, Braga FC.(3)
4. Cytotoxic activity
In the isolation of the cytotoxic compound moronic acid (1) and the new tetracyclic triterpene 3,4-seco-olean-18-ene-3,28-dioic acid (2), from the aerial parts of the medicinal plant Phoradendron reichenbachianum (mistletoe, Loranthaceae) through a bioassay-guided fractionation, indicated that the structures were elucidated on the basis of chemical and spectroscopic evidence, according to "Cytotoxic activity of moronic acid and identification of the new triterpene 3,4-seco-olean-18-ene-3,28-dioic acid from Phoradendron reichenbachianum`by Rios MY, Salina D, Villarreal ML.(4)
5. Antimicrobial activity
In the isolation of the active factor C30H46O3 of the Root bark extract of the East African medicinal plant Ozoroa mucronata showed antimicrobial activity against Gram-positive bacteria, according to "Moronic acid, a simple triterpenoid keto acid with antimicrobial activity isolated from Ozoroa mucronata" by Hostettmann-Kaldas M, Nakanishi K.(5)
6. Anti-herpes simplex virus
In the study of purification two major anti-HSV compounds, moronic acid and betulonic acid, from the herbal extract by extraction with ethyl acetate at pH 10 followed by chromatographic separations and examined their anti-HSV activity in vitro and in vivo, found that Moronic acid suppressed virus yields in the brain more efficiently than those in the skin. This was consistent with the prolongation of mean survival times. Thus, moronic acid was purified as a major anti-HSV compound from the herbal extract of Rhus javanica. Mode of the anti-HSV activity was different from that of ACV, according to "Anti-herpes simplex virus activity of moronic acid purified from Rhus javanica in vitro and in vivo" by Kurokawa M, Basnet P, Ohsugi M, Hozumi T, Kadota S, Namba T, Kawana T, Shiraki K.(6)
7. Etc.
Chinese Secrets To Fatty Liver And Obesity Reversal
Use The Revolutionary Findings To Achieve
Optimal Health And Loose Weight
Super foods Library, Eat Yourself Healthy With The Best of the Best Nature Has to Offer
Back to Popular Herbs http://kylejnorton.blogspot.ca/p/popular-herbs.html
Back to Kyle J. Norton Home page http://kylejnorton.blogspot.ca
Sources
(1) http://www.ncbi.nlm.nih.gov/pubmed/20329730
(2) http://www.ncbi.nlm.nih.gov/pubmed/19969023
(3) http://www.ncbi.nlm.nih.gov/pubmed/17870137
(4) http://www.ncbi.nlm.nih.gov/pubmed/11488459
(5) https://www.thieme-connect.com/ejournals/abstract/plantamedica/doi/10.1055/s-0028-1097349
(6) http://www.ncbi.nlm.nih.gov/pubmed/10086989
Health Benefits
1. HIV maturation inhibitor
In the study of triterpene derivatives as potent anti-HIV agents, different C-3 conformationally restricted betulinic acid (BA, 1) derivatives were designed and synthesized in order to explore the conformational space of the C-3 pharmacophore. 3-O-Monomethylsuccinyl-betulinic acid (MSB) analogues were also designed to better understand the contribution of the C-3' dimethyl group of bevirimat (2), the first-in-class HIV maturation inhibitor, which is currently in phase IIb clinical trials. In addition, another triterpene skeleton, moronic acid (MA, 3), was also employed to study the influence of the backbone and the C-3 modification toward the anti-HIV activity of this compound class, may lead to led to the design and synthesis of compound 12 (EC(50): 0.0006 microM), which displayed slightly better activity than 2 as a HIV-1 maturation inhibitor, according to " Anti-AIDS agents 81. Design, synthesis, and structure-activity relationship study of betulinic acid and moronic acid derivatives as potent HIV maturation inhibitors" by Qian K, Kuo RY, Chen CH, Huang L, Morris-Natschke SL, Lee KH.(1)
2. Anti- Epstein-Barr virus
In the investigation of moronic acid, found in galls of Rhus chinensis and Brazilian propolis, at 10microM inhibits the expression of Rta, Zta, and an EBV early protein, EA-D, after lytic induction with sodium butyrate, found that moronic acids inhibits the capacity of Rta to activate a promoter that contains an Rta-response element, indicating that moronic acid interferes with the function of Rta. On the other hand, moronic acid does not appear to influence with the transactivation function of Zta. Therefore, the lack of expression of Zta and EA-D after moronic acid treatment is attributable to the inhibition of the transactivation functions of Rta. Because the expression of Zta, EA-D and many EBV lytic genes depends on Rta, the treatment of P3HR1 cells with moronic acid substantially reduces the numbers of EBV particles produced by the cells after lytic induction, according to "Inhibition of the Epstein-Barr virus lytic cycle by moronic acid" by Chang FR, Hsieh YC, Chang YF, Lee KH, Wu YC, Chang LK.(2)
3. Anti fungal effects
In the determination of The effect of compound isolated from ethanol extract from Xyris pteygoblephara aerial parts against five microorganism strains, by the microdilution and agar diffusion methods, indicated that assay of 1 (100 microg/disc) by the agar diffusion method against clinical isolates of the dermatophytes Epidermophyton floccosum (inhibition zone, mm+/-s.d.: 4.5+/-0.8), Trichophyton mentagrophytes (4.8+/-0.4) and Trichophyton rubrum (10.2+/-0.8) revealed similar inhibition zones to the positive control amphotericin B (32 microg/disc; 5.0+/-0.2; 5.0+/-0.6 and 8.8+/-1.2, respectively), according to "Dihydroisocoumarin from Xyris pterygoblephara active against dermatophyte fungi" by Guimarães KG, de Souza Filho JD, Dos Mares-Guia TR, Braga FC.(3)
4. Cytotoxic activity
In the isolation of the cytotoxic compound moronic acid (1) and the new tetracyclic triterpene 3,4-seco-olean-18-ene-3,28-dioic acid (2), from the aerial parts of the medicinal plant Phoradendron reichenbachianum (mistletoe, Loranthaceae) through a bioassay-guided fractionation, indicated that the structures were elucidated on the basis of chemical and spectroscopic evidence, according to "Cytotoxic activity of moronic acid and identification of the new triterpene 3,4-seco-olean-18-ene-3,28-dioic acid from Phoradendron reichenbachianum`by Rios MY, Salina D, Villarreal ML.(4)
5. Antimicrobial activity
In the isolation of the active factor C30H46O3 of the Root bark extract of the East African medicinal plant Ozoroa mucronata showed antimicrobial activity against Gram-positive bacteria, according to "Moronic acid, a simple triterpenoid keto acid with antimicrobial activity isolated from Ozoroa mucronata" by Hostettmann-Kaldas M, Nakanishi K.(5)
6. Anti-herpes simplex virus
In the study of purification two major anti-HSV compounds, moronic acid and betulonic acid, from the herbal extract by extraction with ethyl acetate at pH 10 followed by chromatographic separations and examined their anti-HSV activity in vitro and in vivo, found that Moronic acid suppressed virus yields in the brain more efficiently than those in the skin. This was consistent with the prolongation of mean survival times. Thus, moronic acid was purified as a major anti-HSV compound from the herbal extract of Rhus javanica. Mode of the anti-HSV activity was different from that of ACV, according to "Anti-herpes simplex virus activity of moronic acid purified from Rhus javanica in vitro and in vivo" by Kurokawa M, Basnet P, Ohsugi M, Hozumi T, Kadota S, Namba T, Kawana T, Shiraki K.(6)
7. Etc.
Chinese Secrets To Fatty Liver And Obesity Reversal
Use The Revolutionary Findings To Achieve
Optimal Health And Loose Weight
Super foods Library, Eat Yourself Healthy With The Best of the Best Nature Has to Offer
Back to Popular Herbs http://kylejnorton.blogspot.ca/p/popular-herbs.html
Back to Kyle J. Norton Home page http://kylejnorton.blogspot.ca
Sources
(1) http://www.ncbi.nlm.nih.gov/pubmed/20329730
(2) http://www.ncbi.nlm.nih.gov/pubmed/19969023
(3) http://www.ncbi.nlm.nih.gov/pubmed/17870137
(4) http://www.ncbi.nlm.nih.gov/pubmed/11488459
(5) https://www.thieme-connect.com/ejournals/abstract/plantamedica/doi/10.1055/s-0028-1097349
(6) http://www.ncbi.nlm.nih.gov/pubmed/10086989
Phytochemicals in Foods - 11 Health Benefits of Betulinic acid
Betulinic acid is a phytochemincal in the subclass
of Triterpenoid, belonging to the group of Terpenes found abundantly in
Ber tree, white birch, rosemary etc.
Health Benefits
1. Colorectal cancer
In
the investigation of the enhancement of Betulinic acid (BA)
cytotoxicity by α-mangostin, and the cytoprotection effect of
α-mangostin and BA on cisplatin-induced cytotoxicity on HCT 116 human
colorectal carcinoma cells, found that α-Mangostin and BA were more
cytotoxic to the colon cancer cells than to the normal colonic cells,
and both compounds showed a cytoprotective effect against
cisplatin-induced cytotoxicity. On the other hand, α-mangostin enhanced
the cytotoxic and apoptotic effects of BA. Combination therapy hits
multiple targets, which may improve the overall response to the
treatment, and may reduce the likelihood of developing drug resistance
by the tumor cells, according to 'α-Mangostin Enhances Betulinic Acid Cytotoxicity and Inhibits Cisplatin Cytotoxicity on HCT 116 Colorectal Carcinoma Cells" by Aisha AF, Abu-Salah KM, Ismail Z, Majid AM.(1)
2. Anti cancers
In
the identifitification of the agent as potently effective against a
wide variety of cancer cells, also those derived from therapy-resistant
and refractory tumors, found that In-vivo preclinically applied BetA
showed some remarkable anticancer effects and a complete absence of
systemic toxicity in rodents. BetA also cooperated with other therapies
to induce tumor cell death and several potent derivatives have been
discovered. Its antitumor activity has been related to its direct
effects on mitochondria where it induces Bax/Bak-independent
cytochrome-c release, according to 'Betulinic acid, a natural compound with potent anticancer effects" by Mullauer FB, Kessler JH, Medema JP.(2)
3. Anti inflammatory effects
In
the investigation of the effect of betulinic acid (BA) on acute lung
damage induced by bacterial endotoxin (lipopolysaccharide, LPS) in male
Sprague-Dawley rats, found that Treatment with BA was found to
significantly attenuate all these alterations. The present results
suggest that BA is endowed with antiinflammatory and antioxidant
properties that protect the lung against the deleterious actions of LPS,
according to 'Effect of betulinic acid on neutrophil
recruitment and inflammatory mediator expression in
lipopolysaccharide-induced lung inflammation in rats" by Nader MA, Baraka HN.(3)
4. Ovarian Cancer
In elucidation of the effect of BH3-only proteins on cisplatin-resistant ovarian cancer cells,
indicate
that Puma plays a critical role in the apoptosis of chemo-resistant
ovarian cancer cells treated with betulinic acid (BetA). The reduction
of Puma expression inhibits Bax activation and apoptosis, according to "JNK and Akt-mediated Puma Expression in the Apoptosis of Cisplatin-resistant Ovarian Cancer Cells" by Zhao Z, Wang J, Tang J, Liu X, Zhong Q, Wang F, Hu W, Yuan Z, Nie C, Wei Y.(4)
5. Anti-fibrotic effect
In
the to investigation of the anti-fibrotic effect and the potential
mechanisms of action of betulinic acid (BA) against hepatic fibrosis in
vivo and in vitro, showed that BA effectively decreased the HSC-T6 cell
viability induced by TNF-α and showed low toxicity in normal human chang
liver cells. Moreover, BA significantly attenuated the expression of
α-SMA and tissue inhibitor of metalloproteinase-1 (TIMP-1) and increased
the levels of matrix metalloprotease (MMP)-13. BA also inhibited the
expression of Toll-like receptor 4 (TLR4), myeloid differentiation
factor 88 (MyD88) and the activation of nuclear factor-κB (NF-κB) in a
time-dependent manner, according to 'The anti-fibrotic effect of betulinic acid is mediated through the inhibition of NF-κB nuclear protein translocation" by Wan Y, Wu YL, Lian LH, Xie WX, Li X, Ouyang BQ, Bai T, Li Q, Yang N, Nan JX.(5)
6. Antifungal metabolites
In
the investigation of the Antifungal effects of two new natural
compounds, 4-hydroxy-5,6-dimethoxynaphthalene-2-carbaldehyde (1) and
12,13-didehydro-20,29-dihydrobetulin (2) together with nine known
compounds, including 7-methyljuglone (3), diospyrin (4), isodiospyrin
(5), shinanolone (6), lupeol (7), betulin (8), betulinic acid (9),
betulinaldehyde (10), and ursolic acid (11) from the acetone extract of
the roots of Diospyros virginiana, found that All the isolated compounds
were evaluated for their antifungal activities against Colletotrichum
fragariae, C. gloeosporioides, C. acutatum, Botrytis cinerea, Fusarium
oxysporum, Phomopsis obscurans, and P. viticola using in vitro
micro-dilution broth assay, according to 'Antifungal metabolites from the roots of Diospyros virginiana by overpressure layer chromatography" by Wang X, Habib E, León F, Radwan MM, Tabanca N, Gao J, Wedge DE, Cutler SJ.(6)
7. Antileukemic activity
In
an easy and efficient route to partial synthesis of bioactive
28-hydroxy-3-oxolup-20(29)-en-30-al (1), starting from betulinic acid
(2), found that Compound 1 and the precursors (2, 3, 5, and 7) showed
antiproliferative activities against human K562 leukemia, murine WEHI3
leukemia, and murine MEL erythroid progenitor, according to 'Synthesis
of bioactive 28-hydroxy-3-oxolup-20(29)-en-30-al with antileukemic
activity by Ghosh P, Mandal A, Ghosh J, Pal C, Nanda AK.(7)
8. HIV maturation inhibitor
In the study of triterpene derivatives as potent anti-HIV agents, different C-3 conformationally restricted betulinic acid (BA, 1) derivatives were designed and synthesized in order to explore the conformational space of the C-3 pharmacophore. 3-O-Monomethylsuccinyl-betulinic acid (MSB) analogues were also designed to better understand the contribution of the C-3' dimethyl group of bevirimat (2), the first-in-class HIV maturation inhibitor, which is currently in phase IIb clinical trials. In addition, another triterpene skeleton, moronic acid (MA, 3), was also employed to study the influence of the backbone and the C-3 modification toward the anti-HIV activity of this compound class, may lead to led to the design and synthesis of compound 12 (EC(50): 0.0006 microM), which displayed slightly better activity than 2 as a HIV-1 maturation inhibitor, according to " Anti-AIDS agents 81. Design, synthesis, and structure-activity relationship study of betulinic acid and moronic acid derivatives as potent HIV maturation inhibitors" by Qian K, Kuo RY, Chen CH, Huang L, Morris-Natschke SL, Lee KH.(8)
9. Cytokine production and proliferation of CD4(+) T cells and CD19(+) B cells
In the examination of the effects of the triterpene acid mixture on the cytokine production and proliferation of CD4(+) T cells and CD19(+) B cells induced by a self-antigen, human thyroglobulin and by lipopolysaccharide in cultures of normal mononuclear cells, found that the mixture also inhibited CD4(+) T-cell and CD19(+) B-cell proliferation (IC(50) value 22 and 12 µg/mL, respectively). Together, these data demonstrate that oleanolic, ursolic and betulinic acid are active immunomodulatory constituents of the standardized rose hip powder, according to "Triterpene Acids from Rose Hip Powder Inhibit Self-antigen- and LPS-induced Cytokine Production and CD4(+) T-cell Proliferation in Human Mononuclear Cell Cultures" by Saaby L, Nielsen CH.(9)
10. Antiobesity effects
In the investigation of the antilipase function of betulinic acid, the ability of betulinic acid to inhibit pancreatic lipase activity in vitro and and prevention of the elevation of plasma triacylglycerol levels tested after oral administration of a lipid emulsion in rats, suggested that betulinic acid may exert antiobesity effects by directly inhibiting pancreatic lipase, which would prevent the absorption of lipid from the small intestine. In addition, it was found that betulinic acid may further accelerate fat mobilization by enhancing the levels of lipolysis in adipose tissues, according to "Betulinic Acid has an Inhibitory Effect on Pancreatic Lipase and Induces Adipocyte Lipolysis" by Kim J, Lee YS, Kim CS, Kim JS.(10)
11. Antimicrobial activity
In the investigation of the extract from of the isolation from leaves of Clusia burlemarxii, (3-O-α-L- rhamnopyranosylquercetin, 3-O-α-L-rhamnopyranosylkaempferol, 4-hydroxy-5,5-dimethyldihydrofuran-2-one, 2Z-δ-tocotrienoloic acid and friedelin) and from trunk (betulinic acid, protocatechuic acid, lyoniresinol, and a new biphenyl 2,2-dimethyl-3,5-dihydroxy-7-(4-hydroxyphenyl)chromane), found that the extracts and compounds showed significant activity against tested Gram-positive bacteria, none activity against tested Gram-negative bacteria and fungi, according to "A new biphenyl and antimicrobial activity of extracts and compounds from Clusia burlemarxii" by Ribeiro PR, Ferraz CG, Guedes ML, Martins D, Cruz FG.(11)
12. Etc.
8. HIV maturation inhibitor
In the study of triterpene derivatives as potent anti-HIV agents, different C-3 conformationally restricted betulinic acid (BA, 1) derivatives were designed and synthesized in order to explore the conformational space of the C-3 pharmacophore. 3-O-Monomethylsuccinyl-betulinic acid (MSB) analogues were also designed to better understand the contribution of the C-3' dimethyl group of bevirimat (2), the first-in-class HIV maturation inhibitor, which is currently in phase IIb clinical trials. In addition, another triterpene skeleton, moronic acid (MA, 3), was also employed to study the influence of the backbone and the C-3 modification toward the anti-HIV activity of this compound class, may lead to led to the design and synthesis of compound 12 (EC(50): 0.0006 microM), which displayed slightly better activity than 2 as a HIV-1 maturation inhibitor, according to " Anti-AIDS agents 81. Design, synthesis, and structure-activity relationship study of betulinic acid and moronic acid derivatives as potent HIV maturation inhibitors" by Qian K, Kuo RY, Chen CH, Huang L, Morris-Natschke SL, Lee KH.(8)
9. Cytokine production and proliferation of CD4(+) T cells and CD19(+) B cells
In the examination of the effects of the triterpene acid mixture on the cytokine production and proliferation of CD4(+) T cells and CD19(+) B cells induced by a self-antigen, human thyroglobulin and by lipopolysaccharide in cultures of normal mononuclear cells, found that the mixture also inhibited CD4(+) T-cell and CD19(+) B-cell proliferation (IC(50) value 22 and 12 µg/mL, respectively). Together, these data demonstrate that oleanolic, ursolic and betulinic acid are active immunomodulatory constituents of the standardized rose hip powder, according to "Triterpene Acids from Rose Hip Powder Inhibit Self-antigen- and LPS-induced Cytokine Production and CD4(+) T-cell Proliferation in Human Mononuclear Cell Cultures" by Saaby L, Nielsen CH.(9)
10. Antiobesity effects
In the investigation of the antilipase function of betulinic acid, the ability of betulinic acid to inhibit pancreatic lipase activity in vitro and and prevention of the elevation of plasma triacylglycerol levels tested after oral administration of a lipid emulsion in rats, suggested that betulinic acid may exert antiobesity effects by directly inhibiting pancreatic lipase, which would prevent the absorption of lipid from the small intestine. In addition, it was found that betulinic acid may further accelerate fat mobilization by enhancing the levels of lipolysis in adipose tissues, according to "Betulinic Acid has an Inhibitory Effect on Pancreatic Lipase and Induces Adipocyte Lipolysis" by Kim J, Lee YS, Kim CS, Kim JS.(10)
11. Antimicrobial activity
In the investigation of the extract from of the isolation from leaves of Clusia burlemarxii, (3-O-α-L- rhamnopyranosylquercetin, 3-O-α-L-rhamnopyranosylkaempferol, 4-hydroxy-5,5-dimethyldihydrofuran-2-one, 2Z-δ-tocotrienoloic acid and friedelin) and from trunk (betulinic acid, protocatechuic acid, lyoniresinol, and a new biphenyl 2,2-dimethyl-3,5-dihydroxy-7-(4-hydroxyphenyl)chromane), found that the extracts and compounds showed significant activity against tested Gram-positive bacteria, none activity against tested Gram-negative bacteria and fungi, according to "A new biphenyl and antimicrobial activity of extracts and compounds from Clusia burlemarxii" by Ribeiro PR, Ferraz CG, Guedes ML, Martins D, Cruz FG.(11)
12. Etc.
Chinese Secrets To Fatty Liver And Obesity Reversal
Use The Revolutionary Findings To Achieve
Optimal Health And Loose Weight
Super foods Library, Eat Yourself Healthy With The Best of the Best Nature Has to Offer
Back to Popular Herbs http://kylejnorton.blogspot.ca/p/popular-herbs.html
Back to Kyle J. Norton Home page http://kylejnorton.blogspot.ca
Sources
(1) http://www.ncbi.nlm.nih.gov/pubmed/22402764(2) http://www.ncbi.nlm.nih.gov/pubmed/20075711
(3) http://www.ncbi.nlm.nih.gov/pubmed/22402186
(4) http://www.ncbi.nlm.nih.gov/pubmed/22394200
(5) http://www.ncbi.nlm.nih.gov/pubmed/22285267
(6) http://www.ncbi.nlm.nih.gov/pubmed/22162171
(7) http://www.ncbi.nlm.nih.gov/pubmed/22166062
(8) http://www.ncbi.nlm.nih.gov/pubmed/20329730
(9) http://www.ncbi.nlm.nih.gov/pubmed/22170858
(10) http://www.ncbi.nlm.nih.gov/pubmed/22114077
(11) http://www.ncbi.nlm.nih.gov/pubmed/21893172
Phytochemicals in Foods - 8 Health Benefits of Betalains
Betalains are Phytochemicals in the class of red and yellow
indole-derived pigments found in cacti, carnations, amaranths, ice
plants of which belongs to the group of flower plant Caryophyllales.
Health Benefits
1. Antioxidant
In the analyzing the stability of betalains in juices prepared from Moroccan yellow cactus pears (Opuntia ficus indica (L.) Mill.) as a function of temperature and pH, found that the presence of natural pigments reduces the corrosion rate of the tested metal, especially on addition of the red pigments (97%). The inhibition efficiency increases as the pigment concentration of extracts increases. It was also found that the pigments tested act as mixed inhibitors. The inhibitive action of the extracts is discussed in term of adsorption and that such adsorption follows a Langmuir adsorption isotherm, according to "Betalain: a particular class of antioxidant pigment" by El Gharras H.(1)
2. Cytotoxic effect
In the comparison of the cytotoxic effect of the red beetroot extract with anticancer drug, doxorubicin (adriamycin) in the androgen-independent human prostate cancer cells (PC-3) and in the well-established estrogen receptor-positive human breast cancer cells (MCF-7), found that
Both doxorubicin and the beetroot extract exhibited a dose-dependent cytotoxic effect in the two cancer cell lines tested. Although the cytotoxicity of the beetroot extract was significantly lower when compared to doxorubicin, it continued to decrease the growth rate of the PC-3 cells (3.7% in 3 days vs. 12.5% in 7 days) when tested at the concentration of 29 µg/ml, according to "Cytotoxic effect of the red beetroot (Beta vulgaris L.) extract compared to doxorubicin (Adriamycin) in the human prostate (PC-3) and breast (MCF-7) cancer cell lines" by Kapadia GJ, Azuine MA, Rao GS, Arai T, Iida A, Tokuda H.(2)
3. Antiradical activity
In the exploration of different structural features of the betalains, revealing the clues for the switch from yellow to violet color, and the loss of fluorescence, showed that A relevant series of 15 betalain-related compounds (both natural and novel semisynthetic ones) is obtained and characterized by chromatography, UV-vis spectrophotometry, fluorescence, and electrospray ionization mass spectroscopy. Antiradical properties of individual pure compounds in a broad pH range are studied under the ABTS(*+) radical assay. Relevance of specific bonds is studied, and differences between betaxanthins and betacyanins are used to explore in depth the structure-antiradical activity relationships in betalains, according to "Structural implications on color, fluorescence, and antiradical activity in betalains" by
Chinese Secrets To Fatty Liver And Obesity Reversal
Use The Revolutionary Findings To Achieve
Optimal Health And Loose Weight
Super foods Library, Eat Yourself Healthy With The Best of the Best Nature Has to Offer
Back to Popular Herbs http://kylejnorton.blogspot.ca/p/popular-herbs.html
Back to Kyle J. Norton Home page http://kylejnorton.blogspot.ca
Sources
(1) http://www.ncbi.nlm.nih.gov/pubmed/22164774
(2) http://www.ncbi.nlm.nih.gov/pubmed/21434853
(3) http://www.ncbi.nlm.nih.gov/pubmed/20467875
(4) http://www.ncbi.nlm.nih.gov/pubmed/19840838
(5) http://www.ncbi.nlm.nih.gov/pubmed/19468836
(6) http://www.ncbi.nlm.nih.gov/pubmed/19446548
(7) http://www.ncbi.nlm.nih.gov/pubmed/17482444
(8) http://www.ncbi.nlm.nih.gov/pubmed/17364963
Health Benefits
1. Antioxidant
In the analyzing the stability of betalains in juices prepared from Moroccan yellow cactus pears (Opuntia ficus indica (L.) Mill.) as a function of temperature and pH, found that the presence of natural pigments reduces the corrosion rate of the tested metal, especially on addition of the red pigments (97%). The inhibition efficiency increases as the pigment concentration of extracts increases. It was also found that the pigments tested act as mixed inhibitors. The inhibitive action of the extracts is discussed in term of adsorption and that such adsorption follows a Langmuir adsorption isotherm, according to "Betalain: a particular class of antioxidant pigment" by El Gharras H.(1)
2. Cytotoxic effect
In the comparison of the cytotoxic effect of the red beetroot extract with anticancer drug, doxorubicin (adriamycin) in the androgen-independent human prostate cancer cells (PC-3) and in the well-established estrogen receptor-positive human breast cancer cells (MCF-7), found that
Both doxorubicin and the beetroot extract exhibited a dose-dependent cytotoxic effect in the two cancer cell lines tested. Although the cytotoxicity of the beetroot extract was significantly lower when compared to doxorubicin, it continued to decrease the growth rate of the PC-3 cells (3.7% in 3 days vs. 12.5% in 7 days) when tested at the concentration of 29 µg/ml, according to "Cytotoxic effect of the red beetroot (Beta vulgaris L.) extract compared to doxorubicin (Adriamycin) in the human prostate (PC-3) and breast (MCF-7) cancer cell lines" by Kapadia GJ, Azuine MA, Rao GS, Arai T, Iida A, Tokuda H.(2)
3. Antiradical activity
In the exploration of different structural features of the betalains, revealing the clues for the switch from yellow to violet color, and the loss of fluorescence, showed that A relevant series of 15 betalain-related compounds (both natural and novel semisynthetic ones) is obtained and characterized by chromatography, UV-vis spectrophotometry, fluorescence, and electrospray ionization mass spectroscopy. Antiradical properties of individual pure compounds in a broad pH range are studied under the ABTS(*+) radical assay. Relevance of specific bonds is studied, and differences between betaxanthins and betacyanins are used to explore in depth the structure-antiradical activity relationships in betalains, according to "Structural implications on color, fluorescence, and antiradical activity in betalains" by
Gandía-Herrero F, Escribano J, García-Carmona F.(3)
4. Breast cancer
In the investigation of the effect of a wide range of dietary phytochemicals on the activity and expression of DNMTs in human breast cancer MCF7 cell line and their effect on DNA and histone H3 methylation, found that all phytochemicals inhibited the DNA methyltransferase activity with betanin being the weakest while rosmarinic and ellagic acids were the most potent modulators (up to 88% inhibition), according to "The effect of dietary polyphenols on the epigenetic regulation of gene expression in MCF7 breast cancer cells" by Paluszczak J, Krajka-Kuźniak V, Baer-Dubowska W.(4)
5. Cytotoxicity
In the determination of Juices of nine prickly pears (Opuntia spp.) characterized in terms of color, acidity, sugar content, phenolics, flavonoids, betalains and antioxidant activity and tested in vitro against four cancer cell lines, found that among the cancer lines tested, viability of prostate and colon cells were the most affected. Moradillo contained the highest flavonoids and diminished both prostate and colon cancer cell viability without affecting mammary or hepatic cancer cells. Rastrero reduced the growth of the four cancer cell lines without affecting normal fibroblast viability, according to "Phenolic composition, antioxidant capacity and in vitro cancer cell cytotoxicity of nine prickly pear (Opuntia spp.) juices" by Chavez-Santoscoy RA, Gutierrez-Uribe JA, Serna-Saldívar SO.(5)
6. Radioprotective activity
In the investigation of the radioprotective activity of betalains from red beets in mice irradiated by a (60)Co gamma (gamma) ray (6.0 Gy, at a dose of 1.5 Gy min(-1)), found that the administration of betalains from red beets is radioprotective in mice irradiated by (60)Co in vivo. The underlying mechanism remains unclear but appears to be mediated by the antioxidant activity of the betalains from red beets and modulation of the immune system, according to "Radioprotective activity of betalains from red beets in mice exposed to gamma irradiation" by Lu X, Wang Y, Zhang Z.(6)
7. Chronic myeloid leukemia Cell
In the evaluation of the antiproliferative effects of betanin, a principle betacyanin pigment, isolated from the fruits of Opuntia ficus-indica on human chronic myeloid leukemia cell line (K562) showed that dose and time dependent decrease in the proliferation of K562 cells treated with betanin with an IC(50) of 40 microM. Further studies involving scanning and transmission electron microscopy revealed the apoptotic characteristics such as chromatin condensation, cell shrinkage and membrane blebbing. Agarose electrophoresis of genomic DNA of cells treated with betanin showed fragmentation pattern typical for apoptotic cells, according to "Betanin a betacyanin pigment purified from fruits of Opuntia ficus-indica induces apoptosis in human chronic myeloid leukemia Cell line-K562" by Sreekanth D, Arunasree MK, Roy KR, Chandramohan Reddy T, Reddy GV, Reddanna P.(7)
8. Low-density lipoproteins
In the study of the activity of myeloperoxidase (MPO) in the presence of nitrite, now considered a key step in the pathophysiology of low-density lipoprotein (LDL) oxidation, showed that betanin, a phytochemical of the betalain class, inhibits the production of lipid hydroperoxides in human LDL submitted to a MPO/nitrite-induced oxidation. Kinetic measurements including time-course of particle oxidation and betanin consumption, either in the presence or in the absence of nitrite, suggest that the antioxidant effect is possibly the result of various actions. Betanin scavenges the initiator radical nitrogen dioxide and can also act as a lipoperoxyl radical-scavenger, according to "Betanin inhibits the myeloperoxidase/nitrite-induced oxidation of human low-density lipoproteins" by Allegra M, Tesoriere L, Livrea MA.(8)
9. Etc.
4. Breast cancer
In the investigation of the effect of a wide range of dietary phytochemicals on the activity and expression of DNMTs in human breast cancer MCF7 cell line and their effect on DNA and histone H3 methylation, found that all phytochemicals inhibited the DNA methyltransferase activity with betanin being the weakest while rosmarinic and ellagic acids were the most potent modulators (up to 88% inhibition), according to "The effect of dietary polyphenols on the epigenetic regulation of gene expression in MCF7 breast cancer cells" by Paluszczak J, Krajka-Kuźniak V, Baer-Dubowska W.(4)
5. Cytotoxicity
In the determination of Juices of nine prickly pears (Opuntia spp.) characterized in terms of color, acidity, sugar content, phenolics, flavonoids, betalains and antioxidant activity and tested in vitro against four cancer cell lines, found that among the cancer lines tested, viability of prostate and colon cells were the most affected. Moradillo contained the highest flavonoids and diminished both prostate and colon cancer cell viability without affecting mammary or hepatic cancer cells. Rastrero reduced the growth of the four cancer cell lines without affecting normal fibroblast viability, according to "Phenolic composition, antioxidant capacity and in vitro cancer cell cytotoxicity of nine prickly pear (Opuntia spp.) juices" by Chavez-Santoscoy RA, Gutierrez-Uribe JA, Serna-Saldívar SO.(5)
6. Radioprotective activity
In the investigation of the radioprotective activity of betalains from red beets in mice irradiated by a (60)Co gamma (gamma) ray (6.0 Gy, at a dose of 1.5 Gy min(-1)), found that the administration of betalains from red beets is radioprotective in mice irradiated by (60)Co in vivo. The underlying mechanism remains unclear but appears to be mediated by the antioxidant activity of the betalains from red beets and modulation of the immune system, according to "Radioprotective activity of betalains from red beets in mice exposed to gamma irradiation" by Lu X, Wang Y, Zhang Z.(6)
7. Chronic myeloid leukemia Cell
In the evaluation of the antiproliferative effects of betanin, a principle betacyanin pigment, isolated from the fruits of Opuntia ficus-indica on human chronic myeloid leukemia cell line (K562) showed that dose and time dependent decrease in the proliferation of K562 cells treated with betanin with an IC(50) of 40 microM. Further studies involving scanning and transmission electron microscopy revealed the apoptotic characteristics such as chromatin condensation, cell shrinkage and membrane blebbing. Agarose electrophoresis of genomic DNA of cells treated with betanin showed fragmentation pattern typical for apoptotic cells, according to "Betanin a betacyanin pigment purified from fruits of Opuntia ficus-indica induces apoptosis in human chronic myeloid leukemia Cell line-K562" by Sreekanth D, Arunasree MK, Roy KR, Chandramohan Reddy T, Reddy GV, Reddanna P.(7)
8. Low-density lipoproteins
In the study of the activity of myeloperoxidase (MPO) in the presence of nitrite, now considered a key step in the pathophysiology of low-density lipoprotein (LDL) oxidation, showed that betanin, a phytochemical of the betalain class, inhibits the production of lipid hydroperoxides in human LDL submitted to a MPO/nitrite-induced oxidation. Kinetic measurements including time-course of particle oxidation and betanin consumption, either in the presence or in the absence of nitrite, suggest that the antioxidant effect is possibly the result of various actions. Betanin scavenges the initiator radical nitrogen dioxide and can also act as a lipoperoxyl radical-scavenger, according to "Betanin inhibits the myeloperoxidase/nitrite-induced oxidation of human low-density lipoproteins" by Allegra M, Tesoriere L, Livrea MA.(8)
9. Etc.
Chinese Secrets To Fatty Liver And Obesity Reversal
Use The Revolutionary Findings To Achieve
Optimal Health And Loose Weight
Super foods Library, Eat Yourself Healthy With The Best of the Best Nature Has to Offer
Back to Popular Herbs http://kylejnorton.blogspot.ca/p/popular-herbs.html
Back to Kyle J. Norton Home page http://kylejnorton.blogspot.ca
Sources
(1) http://www.ncbi.nlm.nih.gov/pubmed/22164774
(2) http://www.ncbi.nlm.nih.gov/pubmed/21434853
(3) http://www.ncbi.nlm.nih.gov/pubmed/20467875
(4) http://www.ncbi.nlm.nih.gov/pubmed/19840838
(5) http://www.ncbi.nlm.nih.gov/pubmed/19468836
(6) http://www.ncbi.nlm.nih.gov/pubmed/19446548
(7) http://www.ncbi.nlm.nih.gov/pubmed/17482444
(8) http://www.ncbi.nlm.nih.gov/pubmed/17364963
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