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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.

PMID:354677
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC2149379/
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。

相似文献

1
Metronidazole (flagyl) and misonidazole (Ro-07-0582): reduction by facultative anaerobes and cytotoxic action on hypoxic bacteria and mammalian cells in vivo.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
Br J Cancer Suppl. 1978 Jun;3:132-5.
2
[Toxic and radiosensitizing effect of reduced nitroimidazoles on E. coli B/r cells].[还原型硝基咪唑对大肠杆菌B/r细胞的毒性及放射增敏作用]
Radiobiologiia. 1983 Jul-Aug;23(4):505-9.
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Metronidazole (Flagyl), misonidazole (Ro 07-0582), iron, zinc and sulphur compounds in cancer therapy.甲硝唑(灭滴灵)、米索硝唑(Ro 07 - 0582)、铁、锌及硫化合物在癌症治疗中的应用
Br J Cancer Suppl. 1978 Jun;3:16-9.
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["In vitro" susceptibility of some aerobic and anaerobic bacteria to three 5-nitro-imidazole derivatives: metronidazole, ornidazole and tinidazole (author's transl)].某些需氧菌和厌氧菌对三种5-硝基咪唑衍生物:甲硝唑、奥硝唑和替硝唑的“体外”敏感性(作者译)
Ann Microbiol (Paris). 1980 Jan-Feb;131(1):45-59.
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Cytotoxicity of metronidazole (Flagyl) and misonidazole (Ro-07-0582): enhancement by lactate.甲硝唑(灭滴灵)和米索硝唑(Ro-07-0582)的细胞毒性:乳酸的增强作用
Br J Cancer. 1981 Mar;43(3):350-4. doi: 10.1038/bjc.1981.55.
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Electron affinic sensitization. V. Radiosensitization of hypoxic bacteria and mammalian cells in vitro by some nitroimidazoles and nitropyrazoles.亲电子致敏作用。V. 某些硝基咪唑和硝基吡唑对缺氧细菌和哺乳动物细胞的体外放射致敏作用
Radiat Res. 1974 Oct;60(1):108-18.
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Activation of radiosensitizers by hypoxic cells.缺氧细胞对放射增敏剂的激活作用。
Br J Cancer Suppl. 1978 Jun;3:124-8.
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Action of clinically utilized 5-nitroimidazoles on microorganisms.临床应用的5-硝基咪唑类对微生物的作用。
Scand J Infect Dis Suppl. 1981;26:31-41.
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The mechanism of binding of the radiosensitizers metronidazole and misonidazole (Ro-07-0582) to bovine and human serum albumin--a proton NMR study.放射增敏剂甲硝唑和米索硝唑(Ro-07-0582)与牛血清白蛋白和人血清白蛋白结合机制的质子核磁共振研究
Radiat Res. 1981 Jan;85(1):1-12.
10
In vitro susceptibility of anaerobic bacteria to nitroimidazoles.厌氧菌对硝基咪唑类药物的体外敏感性
Scand J Infect Dis Suppl. 1981;26:42-5.

引用本文的文献

1
Cytotoxicity of metronidazole (Flagyl) and misonidazole (Ro-07-0582): enhancement by lactate.甲硝唑(灭滴灵)和米索硝唑(Ro-07-0582)的细胞毒性:乳酸的增强作用
Br J Cancer. 1981 Mar;43(3):350-4. doi: 10.1038/bjc.1981.55.

本文引用的文献

1
Effects of l-(2-nitro-l-imidazolyl)-3-methoxy-2-propanol and 2-methyl-5-nitroimidazole-l-ethanol against anaerobic and aerobic bacteria and protozoa.1-(2-硝基-1-咪唑基)-3-甲氧基-2-丙醇和2-甲基-5-硝基咪唑-1-乙醇对厌氧及需氧细菌和原生动物的作用
Appl Microbiol. 1969 Nov;18(5):728-30. doi: 10.1128/am.18.5.728-730.1969.
2
Medium for the propagation and assay of lactic and other phages.用于乳酸噬菌体及其他噬菌体增殖和检测的培养基。
Lab Pract. 1974 Jan;23(1):3-4.
3
Metronidazole (Flagyl): characterization as a cytotoxic drug specific for hypoxic tumour cells.甲硝唑(灭滴灵):作为一种对缺氧肿瘤细胞具有特异性的细胞毒性药物的特性
Br J Cancer. 1976 May;33(5):485-90. doi: 10.1038/bjc.1976.78.
4
Metronidazole (Flagyl): degradation by the intestinal flora.
Xenobiotica. 1976 Aug;6(8):457-64. doi: 10.3109/00498257609151658.