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N-乙烯基马来酰亚胺对细胞抑制剂抑制活性的影响

[Effect of N-ethylenemaleimide on the inhibitory activity of cytostatics].

作者信息

Bibikova M V, Ivanitskaia L P, Makukho L V

出版信息

Antibiotiki. 1977 Jan;22(1):74-7.

PMID:843076
Abstract

The cytostatic effect of endoxan, Tiotef, bleomycin and other drugs was increased by addition of a thioloprovic compound of N-ethylenmaleimide (N-EM) to the cultures of cancer cells in doses not affecting the synthesis of nucleic acids in these cultures. The sensibilizing effect of N-EM against the antitumor drugs was due to blocking of SH-enzymes responsible of synthesis or reparation of DNA. Thus, a simultaneous effect of N-EM on the thiol cycle and synthesis of nucleic acids was synergistic for a number of antitumor drugs. It provided an increased effect of the cytostatics in doses having no activity under conditions of routine in vitro tests.

摘要

在癌细胞培养物中添加N - 乙基马来酰亚胺(N - EM)这种硫醇类化合物,在不影响这些培养物中核酸合成的剂量下,可增强癌得星、替奥拓芬、博来霉素及其他药物的细胞生长抑制作用。N - EM对抗肿瘤药物的增敏作用是由于其阻断了负责DNA合成或修复的巯基酶。因此,N - EM对硫醇循环和核酸合成的同时作用,对多种抗肿瘤药物具有协同作用。在常规体外试验条件下无活性的剂量下,它提高了细胞生长抑制剂的作用效果。

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