Johnson N P, Hoeschele J D, Rahn R O, O'Neill J P, Hsie A W
Cancer Res. 1980 May;40(5):1463-8.
The cytotoxicity and mutagenicity at the six platinum(II)chloroammines have been investigated in Chinese hamster ovary cells. For these compounds, the observed slopes of the mutation-induction curves (mutants/10(6) cells/microM) were: cis-Pt(NH3)2Cl2 (31.5), K[Pt(NH3)Cl3] (2.78), [Pt(NH3)3Cl]Cl (0.11), K2[PtCl4] (0.12), trans-Pt(NH3)2Cl2 (0.013), and [Pt(NH3)4]Cl2 (0.0). The relative cytotoxicity of these compounds follows the same order and is of similar magnitude. The observed relative mutagenicities of these compounds paralleled their reported potencies in the Ames assay and their relative antitumor activities. Results indicate that Chinese hamster ovary cells are useful in quantifying low mutagenic activity of chemicals such as platinum compounds. Studies with 195mPt-labeled cis- and trans-Pt(NH3)2Cl2 showed that during treatment both compounds enter the cell and bind to the DNA with comparable efficiency. Hence, the relative mutagenicities of cis- and trans-Pt(NH3)2Cl2 are not a consequence of different initial levels of DNA binding.
已在中国仓鼠卵巢细胞中研究了六种氯氨铂（II）的细胞毒性和致突变性。对于这些化合物，观察到的突变诱导曲线斜率（突变体/10⁶细胞/微摩尔）分别为：顺铂（顺式-Pt(NH₃)₂Cl₂）（31.5）、K[Pt(NH₃)Cl₃]（2.78）、[Pt(NH₃)₃Cl]Cl（0.11）、K₂[PtCl₄]（0.12）、反铂（反式-Pt(NH₃)₂Cl₂）（0.013）和[Pt(NH₃)₄]Cl₂（0.0）。这些化合物的相对细胞毒性遵循相同顺序且幅度相似。观察到的这些化合物的相对致突变性与其在艾姆斯试验中报道的效力及其相对抗肿瘤活性平行。结果表明，中国仓鼠卵巢细胞可用于量化铂化合物等化学物质的低致突变活性。用¹⁹⁵mPt标记的顺铂和反铂（顺式和反式-Pt(NH₃)₂Cl₂）进行的研究表明，在处理过程中，这两种化合物均以相当的效率进入细胞并与DNA结合。因此，顺铂和反铂（顺式和反式-Pt(NH₃)₂Cl₂）的相对致突变性并非不同初始DNA结合水平的结果。
