抗炎药物的作用方式和生化特性-II。

On the mode of action and biochemical properties of anti-inflammatory drugs-II.

作者信息

Saeed S A, Cuthbert J

出版信息

Prostaglandins. 1977 Mar;13(3):565-75. doi: 10.1016/0090-6980(77)90033-8.

Abstract

The inhibition of prostaglandin (PG) synthetase by nonsteroidal anti-inflammatory drugs (NSAID) is not well understood. Co-factors (glutathione and hydroquinone) are needed for maximum enzymatic activity in vitro, and we suggest that NSAID might inhibit PG synthetase partly by interfering with co-factor induced stimulation of the enzyme. This hypothesis was tested by: A) Examining the effect of glutathione, noradrenaline and hydroquinone on bull seminal vesicle (BSV) PG synthetase in vitro. The stimulatory effects were concentration-dependent. B) Three structurally distinct NSAID, indomethacin, aspirin and paracetamol, inhibited the stimulation by each co-factor in a concentration-related manner. Drug effectiveness also depended on the concentration of co-factor.

摘要

非甾体抗炎药（NSAID）对前列腺素（PG）合成酶的抑制作用尚未完全明确。体外实验中，辅酶（谷胱甘肽和对苯二酚）对于最大酶活性是必需的，我们认为NSAID可能部分通过干扰辅酶诱导的酶刺激来抑制PG合成酶。该假设通过以下方式进行验证：A）检测谷胱甘肽、去甲肾上腺素和对苯二酚对体外公牛精囊（BSV）PG合成酶的影响。刺激作用呈浓度依赖性。B）三种结构不同的NSAID，即吲哚美辛、阿司匹林和对乙酰氨基酚，以浓度相关的方式抑制每种辅酶的刺激作用。药物效果也取决于辅酶的浓度。