Inflammation

, Volume 21, Issue 3, pp 347–356

Flavonoids as Phospholipase A2 Inhibitors: Importance of Their Structure for Selective Inhibition of Group II Phospholipase A2

  • Mats Lindahl
  • Christer Tagesson
Article

Abstract

The inhibitory effect of the plant flavonoid, rutin, on group I phospholipase A2 (PLA2-I) from porcine pancreas and Naja naja, and on group II phospholipase A2 (PLA2-II) from Vipera russelli and Crotalus atrox was investigated. Rutin efficiently inhibited PLA2-II from both Vipera russelli and Crotalus atrox but was only a weak inhibitor of PLA2-I from porcine pancreas and Naja naja. The lack of strong inhibition of pancreatic PLA2-I was not due to contaminating proteins in the enzyme preparation, since the same weak inhibition was obtained against pancreatic PLA2 purified to homogeneity as judged by two-dimensional gel electrophoresis. Rutin also efficiently inhibited human PLA2-II from synovial fluid but was only a weak inhibitor of human PLA2-I from pancreatic juice, suggesting that rutin is a selective PLA2-II inhibitor. A number of structurally similar flavonoids were tested for their ability to inhibit PLA2-II from Crotalus atrox and, for comparison, PLA2-I from porcine pancreas. The results obtained indicate that the hydroxyl group in 5-position as well as the double bond and the double-bonded oxygen in the oxane ring are all important for the overall ability of flavonoids to inhibit PLA2 activity, and that the hydroxyl groups in 3′- and 4′-position are required for selective inhibition of PLA2-II.

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Copyright information

© Plenum Publishing Corporation 1997

Authors and Affiliations

  • Mats Lindahl
    • 1
  • Christer Tagesson
    • 1
  1. 1.Department of Occupational and Environmental Medicine, Faculty of Health SciencesUniversity of LinköpingSweden

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