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甲硝唑(灭滴灵)和米索硝唑(Ro-07-0582):兼性厌氧菌的还原作用以及对体内缺氧细菌和哺乳动物细胞的细胞毒性作用

Metronidazole (flagyl) and misonidazole (Ro-07-0582): reduction by facultative anaerobes and cytotoxic action on hypoxic bacteria and mammalian cells in vivo.

作者信息

Basag S H, Dunlop J R, Searle A J, Willson R L

出版信息

Br J Cancer Suppl. 1978 Jun;3:132-5.

Abstract

The toxic actions of the "nitro" radiosensitizers, metronidazole and misonidazole on the bacteria E. coli B/r and Serratia marcescens have been investigated under anareobic and aerobic conditions. The rates of reduction of the drugs by suspensions of these bacteria as well as by suspensions microorganisms from the rat caecum have been measured. Both drugs were reduced or were toxic only under anaerobic conditions. In all instances misonidazole was reduced more rapidly than metronidazole but metronidazole was more toxic. It is suggested that these phenomena may model those occurring with hypoxic mammalian cells in vivo and that care should be taken before automatically extrapolating in vitro data to the in vivo situation.

摘要

对“硝基”放射增敏剂甲硝唑和米索硝唑在厌氧和好氧条件下对大肠杆菌B/r和粘质沙雷氏菌的毒性作用进行了研究。已测定了这些细菌的悬浮液以及大鼠盲肠微生物悬浮液对药物的还原速率。两种药物仅在厌氧条件下才会被还原或具有毒性。在所有情况下,米索硝唑的还原速度都比甲硝唑快,但甲硝唑的毒性更大。有人提出,这些现象可能模拟了体内缺氧哺乳动物细胞所发生的情况,因此在将体外数据自动外推至体内情况之前应谨慎。

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