| Chebulagic acid, a COX-LOX dual inhibitor isolated from the fruits of Terminalia chebula Retz., induces apoptosis in COLO-205 cell line. | |
MedLine Citation:
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PMID: 19481594 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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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. |
Authors:
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D Bharat Reddy; T C M Reddy; G Jyotsna; Satish Sharan; Nalini Priya; V Lakshmipathi; Pallu Reddanna |
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Publication Detail:
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Type: Journal Article; Research Support, Non-U.S. Gov't Date: 2009-05-28 |
Journal Detail:
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Title: Journal of ethnopharmacology Volume: 124 ISSN: 1872-7573 ISO Abbreviation: J Ethnopharmacol Publication Date: 2009 Jul |
Date Detail:
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Created Date: 2009-07-27 Completed Date: 2009-10-14 Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 7903310 Medline TA: J Ethnopharmacol Country: Ireland |
Other Details:
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Languages: eng Pagination: 506-12 Citation Subset: IM |
Affiliation:
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Department of Animal Sciences, School of Life Sciences, University of Hyderabad, Hyderabad 500046, India. |
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| MeSH Terms | |
Descriptor/Qualifier:
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Antioxidants
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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* Humans Indicators and Reagents Lipoxygenase Inhibitors / pharmacology* Magnetic Resonance Spectroscopy Mass Spectrometry Picrates / chemistry Spectrophotometry, Infrared Terminalia / chemistry* |
| Chemical | |
Reg. No./Substance:
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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 1.13.11.34/Arachidonate 5-Lipoxygenase |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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