Health benefits
1. Anti cancer
In the investigation of luteolin, a natural bioflavonoid and its chemopreventive properties found that luteolin-induced apoptosis involves reactive oxygen species generation, DNA damage, activation of ATR→Chk2→p53 signaling pathway, inhibition of NF-kB signaling pathway, activation of p38 pathway and depletion of anti-apoptotic proteins. Importantly, use of luteolin in these analyses also identified specific molecular characteristics of NCI-ADR/RES and MCF-7/Mito(R) cells that highlight their different tissue origins. according to "Luteolin induces apoptosis in multidrug resistant cancer cells without affecting the drug transporter function: involvement of cell line-specific apoptotic mechanisms." by
Rao PS, Satelli A, Moridani M, Jenkins M, Subrahmanyeswara Rao U.(1)
2. Prostate cancer
In the evaluation of Luteolin, a polyphenolic flavone and its anti-tumor activity for many cancers
found that The enhancement of prostate-derived Ets factor (PDEF) expression, which induced B-cell translocation gene 2 (BTG2), N-myc downstream regulated gene 1 (NDRG1), and Maspin gene expression, could account for the function of luteolin for anti-proliferation and anti-invasion in LNCaP cells, according to "Upregulation of prostate-derived Ets factor by luteolin causes inhibition of cell prolifertation and cell invasion in prostate carcinoma cells" by Tsui KH, Chung LC, Feng TH, Chang PL, Juang HH.(2)
3. Cancer prevention
In the demonstration of Luteolin, a plant flavonoid and its effecu in inhibition of tumor growth, found that luteolin treatment causes the release of reactive oxygen species (ROS) and that these intracellular ROS in turn mediate AMPK-NF-κB signaling in HepG2 hepatocarcinoma cells. In conclusion, we propose that AMPK is a novel regulator of NF-κB in luteolin-induced cancer cell death. Furthermore, our results suggest that AMPK is an attractive target for cancer prevention by flavonoids, according to "Anti-tumor effect of luteolin is accompanied by AMP-activated protein kinase and nuclear factor-κB modulation in HepG2 hepatocarcinoma cells" by Hwang JT, Park OJ, Lee YK, Sung MJ, Hur HJ, Kim MS, Ha JH, Kwon DY.(3)
4. Hyperresponsiveness and inflammation
In the assessment of assess of the preventive effects of omega-3 polyunsaturated fatty acids (omega3 PUFA) and luteolin supplementation on allergen-induced inflammation found that omega3-luteolin supplementation may have some beneficial effects on airway responsiveness (AR) through a BALF lipoxin A(4) (LXA(4)),-dependent pathway in cats with experimentally-induced asthma, according to "Prophylactic effects of omega-3 polyunsaturated fatty acids and luteolin on airway hyperresponsiveness and inflammation in cats with experimentally-induced asthma" by Leemans J, Cambier C, Chandler T, Billen F, Clercx C, Kirschvink N, Gustin P.(4)
5. Multiple sclerosis (MS)
In the efforts of an effective treatment for Multiple sclerosis (MS) found that luteolin and structurally similar flavonoids can inhibit experimental allergic allergic encephalomyelitis (EAE), an animal model of MS in rodents. An appropriate luteolin formulation that permits sufficient absorption and reduces its metabolism could be a useful adjuvant to IFN-beta for MS therapy, according to "Luteolin as a therapeutic option for multiple sclerosis" by Theoharides TC.(5)
6. Hypermonoaminergic neuropsychological disorders
In the observation of monoamine transporters in regulating normal and abnormal synaptic activity and theirs effect on various neuropsychological disorders found that luteolin and apigenin function as monoamine transporter activators, which would improve several hypermonoaminergic neuropsychological disorders, especially cocaine dependence, through up-regulating monoamine transporter activity, according to "Functional activation of monoamine transporters by luteolin and apigenin isolated from the fruit of Perilla frutescens (L.) Britt" by Zhao G, Qin GW, Wang J, Chu WJ, Guo LH.(6)
7. Nausea, vomiting, and gastric hypersecretion
In the determination of the mode of action of luteolin on phisphodiesterase (PDE) 1–5, and the possible adverse effects in nausea, vomiting, and gastric hypersecretion,
found that luteolin non-selectively and competitively inhibited PDE1–5, only PDE4 inhibition contributed to a reversing effect. In conclusion, because of the low therapeutic (PDE4H/PDE4L) ratio of luteolin, the gastrointestinal adverse effects such as nausea, vomiting and gastric hypersecretion should be carefully monitored, whenever luteolin is used for treating allergies, asthma or chronic obstructive pulmonary disease, according to "Luteolin, a non-selective competitive inhibitor of phosphodiesterases 1–5, displaced [3H]-rolipram from high-affinity rolipram binding sites and reversed xylazine/ketamine-induced anesthesia" by Ming-Chih Yu, Jun-Hao Chen, Chi-Yin Lai, Cheng-Ying Han, Wun-Chang Ko.(7)
8. Antiarthritic effect
In the research of lonicerin and its effect anti fungal arthritis found that the lonicerin treatment reduced the edema at all dose levels, and, furthermore, there was app. 54% edema reduction in animals given the 2 mg-dose at the peak (day 10) of septic arthritis (p < 0.05). Since the peak, the edema was reduced in similar rates. This antiarthritic activity appeared to be mediated by lonicerin's ability to suppress T cell proliferation, nitric oxide production from macrophages, and shift of cellular immunity from Th1- toward Th2-type responses, all of which are beneficial to treat arthritis, according to "Antiarthritic effect of lonicerin on Candida albicans arthritis in mice" by Lee JH, Han Y.(8)
9. Inflammatory diseases and immune disorders
In the examination of the PRRs recognize pathogen-associated molecular patterns (PAMPs) or danger-associated molecular patterns (DAMPs) in regulating the innate and adaptive immune responses found that TBK1 kinase can be a target for certain flavonoids such as EGCG, luteolin, quercetin, chrysin, and eriodictyol to regulate TRIF-dependent TLR pathways. This review focuses on the features of PRR signaling pathways and the therapeutic targets of intrinsic and extrinsic regulators in order to provide beneficial strategies for controlling the activity of PRRs and the related inflammatory diseases and immune disorders, according to "Intrinsic and extrinsic regulation of innate immune receptors" by Jeong E, Lee JY.(9)
10. Mercury-induced toxicity
In the investigation of luteolin and thiosalicylate and theirs effect on human mast cells found that Pretreatment for 10 min with the flavonoid luteolin (0.1 mM) before HgCl2 or thimerosal compeletly blocked their effect. Luteolin and methyl thiosalicylate may be useful in preventing mercury-induced toxicity, according to "Luteolin and thiosalicylate inhibit HgCl(2) and thimerosal-induced VEGF release from human mast cells" by Asadi S, Zhang B, Weng Z, Angelidou A, Kempuraj D, Alysandratos KD, Theoharides TC.(10)
11. Antioxidants
In the observation of luteolin, kaempferol and apigenin and its binding to calf thymus (ct)-DNA
found that in the cell culture medium. Luteolin, followed by apigenin and kaempferol, was shown to be the most effective in protecting DNA from oxidative damage induced by hydrogen peroxide, according to "Spectrophotometric analysis of flavonoid-DNA interactions and DNA damaging/protecting and cytotoxic potential of flavonoids in human peripheral blood lymphocytes" by Rusak G, Piantanida I, Masić L, Kapuralin K, Durgo K, Kopjar N.(11)
12. Osteoporosis
In the evaluation of Flavonoids, found abundantly in plants and their effect in preventing bone loss in ovariectomized (OVX) animal models found that Serum biochemical markers assays revealed that luteolin prevents OVX-induced increases in bone turnover. These data strongly suggest that luteolin has the potential for prevention of bone loss in postmenopausal osteoporosis by reducing both osteoclast differentiation and function, according to "The effects of luteolin on osteoclast differentiation, function in vitro and ovariectomy-induced bone loss" by Kim TH, Jung JW, Ha BG, Hong JM, Park EK, Kim HJ, Kim SY.(12)
13. Anti-allergic effects
In the analyzing the structure-activity relationships of 45 flavones, flavonols and their related compounds, luteolin, ayanin, apigenin and fisetin and theirs anti-allergic effects, found that flavonoids inhibit histamine release, synthesis of IL-4 and IL-13 and CD40 ligand expression by basophils. were the strongest inhibitors of IL-4 production with an IC(50) value of 2-5 microM and determined a fundamental structure for the inhibitory activity. The inhibitory activity of flavonoids on IL-4 and CD40 ligand expression was possibly mediated through their inhibitory action on activation of nuclear factors of activated T cells and AP-1., according to "Flavonoids and related compounds as anti-allergic substances" by Kawai M, Hirano T, Higa S, Arimitsu J, Maruta M, Kuwahara Y, Ohkawara T, Hagihara K, Yamadori T, Shima Y, Ogata A, Kawase I, Tanaka T.(13)
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Sources
(1) http://www.ncbi.nlm.nih.gov/pubmed/21792893
(2) http://www.ncbi.nlm.nih.gov/pubmed/21780100
(3) http://www.ncbi.nlm.nih.gov/pubmed/21468539
(4) http://www.ncbi.nlm.nih.gov/pubmed/19231257
(5) http://www.ncbi.nlm.nih.gov/pubmed/19825165
(6) http://www.ncbi.nlm.nih.gov/pubmed/19815045
(7) http://www.sciencedirect.com/science/article/pii/S0014299909009224
(8) http://www.ncbi.nlm.nih.gov/pubmed/21656372
(9) http://www.ncbi.nlm.nih.gov/pubmed/21488180
(10) http://www.ncbi.nlm.nih.gov/pubmed/21244751
(11) http://www.ncbi.nlm.nih.gov/pubmed/20637747
(12) http://www.ncbi.nlm.nih.gov/pubmed/20233653
(13) http://www.ncbi.nlm.nih.gov/pubmed/17384531
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