Group IIA secretory PLA(2) inhibition by ursolic acid: A potent anti-inflammatory molecule

Nataraju, A. and Raghavendra Gowda, C. D. and Rajesh, R. and Vishwanath, B. S. (2007) Group IIA secretory PLA(2) inhibition by ursolic acid: A potent anti-inflammatory molecule. CURRENT TOPICS IN MEDICINAL CHEMISTRY, 7 (8). pp. 801-809.

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Ursolic acid (3 beta-hydroxy-urs-12-en-28-oic acid) isolated from many medicinal plants has diverse pharmacologically important properties, including strong anti-inflammatory activity. However its interaction with proinflammatory PLA(2) is not known. Ursolic acid inhibited secretory PLA(2) (sPLA(2)) enzymes purified from Vipera russelli, Naja naja venom and human pleural fluid and synovial fluid. IC50 values determined for these enzymes ranged from 12 to 18 mu M. Group II secretory PLA(2) from both venoms & human inflammatory source were found to be sensitive to inhibition in comparison with group I cobra venom sPLA(2). Variation in Ca2+ concentration from 2.5-15 mM did not alter the level of inhibition. Similarly sPLA(2) inhibition by ursolic acid is independent of substrate concentration. Ursolic acid interacts with purified venom sPLA(2) enzymes and enhances relative fluorescence intensity in a dose dependent manner. In the presence of ursolic acid apparent shift in the far UV-CD spectra of sPLA(2) was observed, indicating a direct interaction with the enzyme and formation of enzyme-ursolic acid complex. This complex results in irreversible inhibition of sPLA(2) as evident by dialysis study. Inhibition of sPLA(2) induced mouse paw edema and indirect hemolytic activity confirmed its sPLA(2) inhibitory activity in vivo and in situ respectively. These studies revealed that the strong anti-inflammatory activity of ursolic acid is by inhibiting sPLA(2) enzymes.

Item Type: Article
Subjects: Agriculture Biological Sciences > Biochemistry
University of Mysore > PG Campuses > Manasagangotri, Mysore > Agriculture Biological Sciences > Biochemistry
Divisions: PG Campuses > Manasagangotri, Mysore > Biochemistry
Depositing User: Users 7 not found.
Date Deposited: 16 Apr 2013 07:10
Last Modified: 14 Dec 2015 05:45

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