Document Detail

Chebulagic acid, a COX-LOX dual inhibitor isolated from the fruits of Terminalia chebula Retz., induces apoptosis in COLO-205 cell line.
MedLine Citation:
PMID:  19481594     Owner:  NLM     Status:  MEDLINE    
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.
D Bharat Reddy; T C M Reddy; G Jyotsna; Satish Sharan; Nalini Priya; V Lakshmipathi; Pallu Reddanna
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't     Date:  2009-05-28
Journal Detail:
Title:  Journal of ethnopharmacology     Volume:  124     ISSN:  1872-7573     ISO Abbreviation:  J Ethnopharmacol     Publication Date:  2009 Jul 
Date Detail:
Created Date:  2009-07-27     Completed Date:  2009-10-14     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  7903310     Medline TA:  J Ethnopharmacol     Country:  Ireland    
Other Details:
Languages:  eng     Pagination:  506-12     Citation Subset:  IM    
Department of Animal Sciences, School of Life Sciences, University of Hyderabad, Hyderabad 500046, India.
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MeSH Terms
Antioxidants / pharmacology
Apoptosis / drug effects*
Arachidonate 5-Lipoxygenase / antagonists & inhibitors,  isolation & purification
Benzopyrans / pharmacology*
Biphenyl Compounds / chemistry
Blotting, Western
Cell Line, Tumor
Cell Proliferation / drug effects
Chromatography, High Pressure Liquid
Cyclooxygenase 2 Inhibitors / pharmacology
Cyclooxygenase Inhibitors / pharmacology*
DNA Fragmentation / drug effects
Flow Cytometry
Free Radical Scavengers / chemistry
Free Radicals / chemistry
Fruit / chemistry
Glucosides / pharmacology*
Indicators and Reagents
Lipoxygenase Inhibitors / pharmacology*
Magnetic Resonance Spectroscopy
Mass Spectrometry
Picrates / chemistry
Spectrophotometry, Infrared
Terminalia / chemistry*
Reg. No./Substance:
0/Antioxidants; 0/Benzopyrans; 0/Biphenyl Compounds; 0/Cyclooxygenase 2 Inhibitors; 0/Cyclooxygenase Inhibitors; 0/Free Radical Scavengers; 0/Free Radicals; 0/Glucosides; 0/Indicators and Reagents; 0/Lipoxygenase Inhibitors; 0/Picrates; 1898-66-4/2,2-diphenyl-1-picrylhydrazyl; 23094-71-5/chebulagic acid; EC 5-Lipoxygenase

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine

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