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.
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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
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