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Chebulagic acid, a COX-LOX dual inhibitor isolated from the fruits of Terminalia chebula Retz., induces apoptosis in COLO-205 cell line

teipruel 添加于 2009-10-13 09:36 | 2009 次阅读 | 0 个评论
  •  作 者

    Reddy DB, Reddy TCM, Jyotsna G, Sharan S, Priya N, Lakshmipathi V, Reddanna P
  •  摘 要

    ETHNOPHARMACOLOGICAL RELEVANCE: Terminalia chebula has an esteemed origin in Indian mythology; its fruits are used to treat many diseases such as digestive, diabetes, colic pain, chronic cough, sore throat, asthma, etc. AIM OF THE STUDY: The water or ethanolic extracts of the fruits were reported to have anti-oxidant, anti-inflammatory, anti-cancer and radio-protector properties. The present study is to isolate and identify the compounds that inhibit COX and 5-LOX, the key enzymes involved in inflammation and carcinogenesis. MATERIALS AND METHODS: The ethanolic extract of the fruits was fractionated by RP-HPLC and fractions were tested for enzyme inhibition activity against COX and 5-LOX. One of the fractionated compounds showed potent dual inhibition against COX and 5-LOX. It was identified as chebulagic acid by LC-MS, NMR and IR analyses. The chebulagic acid was also tested for anti-proliferative activity. RESULTS: Chebulagic acid showed potent COX-LOX dual inhibition activity with IC(50) values of 15+/-0.288, 0.92+/-0.011 and 2.1+/-0.057 microM for COX-1, COX-2 and 5-LOX respectively. It also showed anti-proliferative activity against HCT-15, COLO-205, MDA-MB-231, DU-145 and K562 cell lines. Further mechanistic studies on COLO-205 cells revealed induction of apoptosis by chebulagic acid. CONCLUSIONS: Chebulagic acid, a COX-2 and 5-LOX dual inhibitor isolated from the fruits of Terminalia chebula, induces apoptosis in COLO-205 cells.
  •  详细资料

    • 文献种类:期刊
    • 期刊名称: Journal of Ethnopharmacology
    • 期刊缩写: J Ethnopharmacol
    • 期卷页: 2009  124 3 506-512
    • 地址: Department of Animal Sciences, School of Life Sciences, University of Hyderabad, Hyderabad 500046, India
    • ISBN: 1872-7573
    • 备注:PMID:19481594
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