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酚类化合物和生物类黄酮对大鼠肾前列腺素合成酶影响的构效关系研究

A structure-activity study on the influence of phenolic compounds and bioflavonoids on rat renal prostaglandin synthetase.

作者信息

Baumann J, von Bruchhausen F, Wurm G

出版信息

Naunyn Schmiedebergs Arch Pharmacol. 1979 May;307(1):73-8. doi: 10.1007/BF00506554.

Abstract

The stimulating or inhibiting influences of 33 phenolic compounds on the prostaglandin synthetase of rat renal medulla were tested. Dihydroxyphenylcarbonic acids clearly proved to be activators of the prostaglandin synthetase. Dimethoxyphenylcarbonic acids were ineffective. Aminoethylphenols as well as p-substituted monohydroxybenzenes with a carbonic acid side chain were clear stimulators in contrast to their alkyl derivatives which are pronounced inhibitors. Among the tested bioflavonoids (+)-cyanidanol-3 and morin were inhibitors of the prostaglandin synthesis. Flavonoids with polar substitution in 3,5,7-position such as rutin on the other hand showed activating properties.

摘要

测试了33种酚类化合物对大鼠肾髓质前列腺素合成酶的刺激或抑制作用。二羟基苯基碳酸明显被证明是前列腺素合成酶的激活剂。二甲氧基苯基碳酸无效。氨基乙基酚以及带有碳酸侧链的对取代单羟基苯是明显的刺激剂,而它们的烷基衍生物则是显著的抑制剂。在所测试的生物类黄酮中,(+)-氰定醇-3和桑色素是前列腺素合成的抑制剂。另一方面,在3、5、7位具有极性取代的黄酮类化合物,如芦丁,则表现出激活特性。

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