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An in vitro study comparing the cytotoxicity of three platinum complexes with regard to the effect of thiol depletion.

机译:一项体外研究比较了三种铂配合物在巯基耗竭方面的细胞毒性。

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摘要

The cytotoxicity of three platinum complexes, cis-diamminedichloroplatinum(II) (cis-platin), cis-dichloro-trans-dihydroxy-cis-bis (isopropylamine) platinum(IV), (CHIP) and diammine (1, 1-cyclobutane-dicarboxylato) platinum(II) (carboplatin) on Chinese Hamster ovary (CHO) and mouse sarcoma RIF-1 cells cultured in vitro has been compared. The tumour cell line was much more sensitive to the cytotoxic action of the three agents compared to the CHO cell line. CHIP and carboplatin gave similar dose-response curves, both being much less toxic than cis-platin. The effect of thiol modification on platinum toxicity was also investigated. Substantial reduction in the intracellular non-protein sulphydryl content markedly enhanced the cytotoxicity of CHIP but had much less effect on carboplatin and cis-platin. Thiol depletion by diethylmaleate had a negligible effect on cis-platin toxicity.
机译:三种铂配合物的细胞毒性:顺二氨二氯铂(II)(顺铂),顺二氯-反式-二羟基-顺-双(异丙胺)铂(IV),(CHIP)和二氨(1,1-环丁烷-比较了中国仓鼠卵巢(CHO)和体外培养的小鼠肉瘤RIF-1细胞上的二羧基二甲基铂(II)(卡铂)。与CHO细胞系相比,肿瘤细胞系对这三种药物的细胞毒性作用更为敏感。 CHIP和卡铂给出相似的剂量反应曲线,两者的毒性均低于顺铂。还研究了硫醇修饰对铂毒性的影响。细胞内非蛋白硫代含量的显着降低显着增强了CHIP的细胞毒性,但对卡铂和顺铂的影响却小得多。马来酸二乙酯对硫醇的消耗对顺铂毒性的影响可忽略不计。

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