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小鼠血浆中N-亚硝基化合物的酶促失活

Enzymatic inactivation of N-nitroso compounds in murine blood plasma.

作者信息

Brundrett R B, Aukerman S L

出版信息

Cancer Res. 1985 Mar;45(3):1000-4.

PMID:3971357
Abstract

Murine blood plasma rapidly inactivates nitrosamides and nitrosocarbamates but not nitrosoureas. The mechanism of this inactivation in murine blood plasma has been investigated. The vast majority of activity (greater than 97%) was inhibited by serine hydroxylase inhibitors. Also, 92% of the activity was inhibited by bis(p-nitrophenyl)phosphate, a selective inhibitor of carboxylesterases. Decomposition products formed after blood plasma action on N-ethyl-N-nitrosoacetamide or N-methyl-N-nitrosoethylcarbamate were separated and identified by gas chromatography. The products formed were consistent with a hydrolytic cleavage of the amidic bond. These observations are consistent with the idea that the major active factor(s) in plasma is a carboxylesterase(s).

摘要

小鼠血浆能迅速使亚硝酰胺和亚硝基氨基甲酸酯失活,但不能使亚硝基脲失活。已对小鼠血浆中这种失活机制进行了研究。绝大多数活性(超过97%)被丝氨酸羟化酶抑制剂抑制。此外,92%的活性被双(对硝基苯基)磷酸酯(一种羧酸酯酶的选择性抑制剂)抑制。通过气相色谱法分离并鉴定了血浆作用于N-乙基-N-亚硝基乙酰胺或N-甲基-N-亚硝基乙基氨基甲酸酯后形成的分解产物。形成的产物与酰胺键的水解裂解一致。这些观察结果与血浆中的主要活性因子是一种羧酸酯酶的观点一致。

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