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硝呋替莫在大鼠肝脏及其他组织中的硝基还原酶活性研究。

Studies on nifurtimox nitroreductase activity in liver and other rat tissues.

作者信息

Masana M, de Toranzo E G, Castro J A

出版信息

Arch Int Pharmacodyn Ther. 1984 Jul;270(1):4-10.

PMID:6497502
Abstract

Rat liver microsomes exhibit nifurtimox (NFX) nitroreductase activity, which is mostly NADPH-dependent and is completely abolished by heating and under an atmosphere of air. Pure carbon monoxide inhibits for 28% microsomal NFX nitroreductase activity while FAD 1 mM significantly enhances it. Smaller activities than in liver were found in brain, small intestine, testes, lung and heart. Rat liver cytosol also showed NFX nitroreductase activity using either hypoxanthine or N-methylnicotinamide as substrates. These activities were inhibited by allopurinol or menadione respectively. Results suggest that cytochrome P-450, NADPH cytochrome c reductase, xanthinoxidase and aldehyde oxidase are able to reduce NFX nitrogroups in rat liver and other tissues.

摘要

大鼠肝脏微粒体具有硝呋替莫(NFX)硝基还原酶活性,该活性大多依赖于NADPH,并且通过加热和在空气氛围下会完全丧失。纯一氧化碳抑制微粒体NFX硝基还原酶活性达28%,而1 mM的黄素腺嘌呤二核苷酸(FAD)则显著增强该活性。在脑、小肠、睾丸、肺和心脏中发现的活性低于肝脏中的活性。大鼠肝脏胞质溶胶以次黄嘌呤或N-甲基烟酰胺作为底物时也表现出NFX硝基还原酶活性。这些活性分别被别嘌呤醇或甲萘醌抑制。结果表明,细胞色素P-450、NADPH细胞色素c还原酶、黄嘌呤氧化酶和醛氧化酶能够还原大鼠肝脏及其他组织中的NFX硝基。

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Studies on nifurtimox nitroreductase activity in liver and other rat tissues.硝呋替莫在大鼠肝脏及其他组织中的硝基还原酶活性研究。
Arch Int Pharmacodyn Ther. 1984 Jul;270(1):4-10.
2
Benznidazole and nifurtimox nitroreductase activity in liver microsomes from male rats preinduced with phenobarbital or 3-methylcholanthrene.苯巴比妥或3-甲基胆蒽预诱导的雄性大鼠肝微粒体中苯并硝唑和硝呋替莫的硝基还原酶活性。
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Rat liver nuclear nifurtimox nitroreductase activity.大鼠肝脏细胞核中硝呋替莫的硝基还原酶活性。
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Species and sex differences in the liver microsomal nitroreductive biotransformation of nifurtimox and benznidazole.硝呋替莫和苯硝唑在肝脏微粒体中的硝基还原生物转化的物种和性别差异。
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Mechanism of azoreduction of dimethylaminoazobenzene by rat liver NADPH-cytochrome P-450 reductase and partially purified cytochrome P-450. Oxygen and carbon monoxide sensitivity and stimulation by FAD and FMN.大鼠肝脏NADPH-细胞色素P-450还原酶和部分纯化的细胞色素P-450对二甲基氨基偶氮苯的偶氮还原机制。对氧气和一氧化碳的敏感性以及FAD和FMN的刺激作用。
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Ultrastructural effects of Nifurtimox on rat adrenal cortex related to reductive biotransformation.硝呋替莫对大鼠肾上腺皮质与还原生物转化相关的超微结构影响
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Reductive metabolism and activation of benznidazole.苄硝唑的还原代谢与活化
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