STIMULATION OF PROSTAGLANDIN BIOSYNTHESIS BY DRUGS: EFFECTS in vitro OF SOME DRUGS AFFECTING GUT FUNCTION
STIMULATION OF PROSTAGLANDIN BIOSYNTHESIS BY DRUGS: EFFECTS in vitro OF SOME DRUGS AFFECTING GUT FUNCTION
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药物刺激前列腺素生物合成：一些影响肠道功能的药物的体外作用
DOI：
10.1111/j.1476-5381.1976.tb10396.x
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发表时间：
1976
影响因子：
7.3
通讯作者：
Shaukat Saeed
中科院分区：
文献类型：
--
作者：
H. Collier;W. Mcdonald;Shaukat Saeed
1 在不添加辅因子的情况下，低浓度的几种催吐药、泻药或刺激性药物会刺激从公牛精囊中提取的前列腺素合成酶（BSV 前列腺素合成酶）将花生四烯酸转化为前列腺素 E2 和 F2α。它们的效果取决于浓度和时间。 2 通过在培养介质中添加还原型谷胱甘肽，阿扑吗啡、芦荟、酪胺或姜油酮对 BSV 前列腺素合成酶的刺激作用增加数倍，而前列腺素合成酶的酚类辅因子对苯二酚则造成轻微抑制。 3 根据这一发现以及观察到许多兴奋剂药物具有酚基团，而其非活性相关药物则缺乏这样的基团，表明这些兴奋剂药物代替对苯二酚充当前列腺素合成酶的辅助因子。 4 芦荟、酪胺、乙醇和喹嗪也会使离体大鼠胃底的静息张力产生剂量相关的增加。这种增加发生在与有效刺激 BSV 前列腺素合成酶的浓度相当的浓度下，并被乙酰水杨酸盐消除。 5 这些发现支持这样的观点，即某些药物通过刺激前列腺素合成酶来发挥其部分药理作用。
1 Low concentrations of several emetic, purgative or irritant drugs in the absence of added co‐factors stimulated conversion of arachidonic acid to prostaglandin E2 and F2α by prostaglandin synthetase extracted from bull seminal vesicles (BSV prostaglandin synthetase). Their effect was dependent on concentration and time. 2 Stimulation of BSV prostaglandin synthetase by apomorphine, aloes, tyramine or zingerone was increased several‐fold by addition of reduced glutathione to the incubation medium, whereas hydroquinone, a phenolic co‐factor of prostaglandin synthetase caused slight depression. 3 From this finding and from the observation that many of the stimulant drugs possess a phenolic group, whereas their inactive relatives lack such a group, it is suggested that these stimulant drugs act as co‐factors for prostaglandin synthetase in place of hydroquinone. 4 Aloes, tyramine, ethanol and quipazine also produced a dose‐related increase in resting tone of the isolated fundus of the rat stomach. This increase occurred at concentrations comparable to those effective in stimulating BSV prostaglandin synthetase, and was abolished by acetylsalicylate. 5 These findings support the view that certain drugs exert some of their pharmacological effects by stimulating prostaglandin synthetase.