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体外刺激UDP-葡萄糖醛酸基转移酶活性的亚硝胺和硝胺的构效关系。

Structure-activity relationships of nitrosamines and nitramines which stimulate UDP-glucuronosyltransferase activities in vitro.

作者信息

Matsui M, Nagai F, Suzuki E, Okada M

出版信息

Biochem Pharmacol. 1984 Aug 15;33(16):2647-51. doi: 10.1016/0006-2952(84)90639-7.

Abstract

Examination of twelve nitrosamines and seven nitramines revealed that nitramines modify UDP-glucuronosyltransferase activity in a manner similar to that of nitrosamines. Only N,N-diethyl-substituted nitrosamine and nitramine significantly stimulated transferase activity toward 2-aminophenol and 4-nitrophenol but not toward phenolphthalein and androsterone. Elongation of the alkyl chains or introduction of carboxy, hydroxy, or oxo groups into the alkyl chains did not result in stimulatory ability, and some of these compounds inhibited the transferase activity.

摘要

对12种亚硝胺和7种硝胺的检测表明,硝胺对UDP-葡萄糖醛酸基转移酶活性的影响方式与亚硝胺类似。只有N,N-二乙基取代的亚硝胺和硝胺能显著刺激该转移酶对2-氨基酚和4-硝基苯酚的活性,但对酚酞和雄甾酮则无此作用。烷基链的延长或在烷基链中引入羧基、羟基或氧代基团并不会产生刺激活性,并且其中一些化合物还会抑制转移酶活性。

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