2-STEP INACTIVATION OF BEE VENOM PHOSPHOLIPASE-A2 BY SCALARADIAL

被引：64

作者：

DECARVALHO, MS

JACOBS, RS

机构：

[1] UNIV CALIF SANTA BARBARA,DEPT BIOL SCI,SANTA BARBARA,CA 93106

[2] UNIV CALIF SANTA BARBARA,INST MARINE SCI,SANTA BARBARA,CA 93106

来源：

BIOCHEMICAL PHARMACOLOGY | 1991年 / 42卷 / 08期

基金：

美国海洋和大气管理局;

关键词：

D O I：

10.1016/0006-2952(91)90432-5

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

Scalaradial (SLD), a marine natural product isolated from the sponge (Cacospongia sp., possesses anti-inflammatory properties in vivo and in vitro (Pharmacologist 32: 168, 1990). In this study we characterize its effects against bee venom phospholipase A2 (PLA2; EC 3.1.1.4). SLD is a potent inactivator of bee venom PLA2 with an IC50 value of 0.07-mu-M. Inactivation of bee venom PLA2 occurred in a time-dependent, irreversible manner. The rate of inactivation followed first-order reaction kinetics and was dependent on the concentration of SLD. Kinetic analysis suggested a two-step mechanism of inactivation: an initial apparent noncovalent binding (K(i) = 4.5 x 10(-5) M) followed by covalent modification. The rate of inactivation was reduced markedly in the presence of excess phosphatidylcholine, suggesting that modification of the enzyme occurs at or near the substrate binding site.

引用

页码：1621 / 1626

页数：6

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