CINATRINS, A NOVEL FAMILY OF PHOSPHOLIPASE-A2 INHIBITORS .2. BIOLOGICAL-ACTIVITIES

被引：44

作者：

TANAKA, K ^{[1
]}

ITAZAKI, H ^{[1
]}

YOSHIDA, T ^{[1
]}

机构：

[1] SHIONOGI & CO LTD,SHIONOGI RES LAB,FUKUSHIMA KU,OSAKA 553,JAPAN

来源：

JOURNAL OF ANTIBIOTICS | 1992年 / 45卷 / 01期

关键词：

D O I：

10.7164/antibiotics.45.50

中图分类号：

Q81 [生物工程学（生物技术）]; Q93 [微生物学];

学科分类号：

071005 ; 0836 ; 090102 ; 100705 ;

摘要：

Cinatrins A, B and C3 inhibited phospholipase A2 purified from rat platelets in a dose-dependent manner. Cinatrin C3, the most potent component (IC50 70-mu-M), was noncompetitive with a Ki value of 36-mu-M. Cinatrins B and C3 also inhibited both porcine pancreas and Naja naja venom phospholipase A2. Inhibition of rat platelet phospholipase A2 by cinatrin C3 was independent of Ca2+ and substrate concentration. Comparison with duramycin, another phospholipase A2 inhibitor, displayed inhibition dependent on substrate concentration when phosphatidylethanolamine was the substrate. These results indicate that the inhibition of phospholipase A2 by cinatrin C3 may result from direct interaction with the enzyme.

引用

页码：50 / 55

页数：6

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