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(+)-氰定醇-3作为前列腺素合成酶抑制剂。大鼠肾髓质和肝脏的体外及体内研究

(+)-Cyanidanol-3 as inhibitor of prostaglandin synthetase. Studies on renal medulla and liver of the rat in vitro and in vivo.

作者信息

Baumann J, von Bruchhausen F

出版信息

Naunyn Schmiedebergs Arch Pharmacol. 1979 Jan;306(1):85-7. doi: 10.1007/BF00515598.

Abstract

(+)-Cyanidanol-3 inhibits the prostaglandin synthetase of the renal medulla and of the liver of rats in vitro and after treatment of the animals with 200 mg/kg. A half-maximal inhibition of the enzyme was obtained with 5 . 10(-5) M cyanidanol. If the microsomal inhibitor CFT1201 is first applied, the inhibitory effect in vivo of 50% is increased to 80%. It is supposed that cyanidanol is converted to metabolites which, according to our earlier studies, activate the enzyme system. An enzyme activity of the rat liver was measured which - with a turnover of 18-20% - was significantly higher than the values obtained by other authors.

摘要

(+)-氰定醇-3在体外以及用200mg/kg剂量处理动物后,可抑制大鼠肾髓质和肝脏中的前列腺素合成酶。用5×10⁻⁵M氰定醇可使该酶活性受到半数最大抑制。若先应用微粒体抑制剂CFT1201,其体内抑制作用可从50%增至80%。据推测,氰定醇会转化为代谢产物,根据我们早期的研究,这些代谢产物会激活酶系统。所测定的大鼠肝脏酶活性(周转率为18 - 20%)显著高于其他作者所获得的值。

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