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铑(I)、铱(I)和钌(II)配合物与顺二氯二氨铂(II)相比对荷Lewis肺癌小鼠的抗肿瘤作用

Antitumor effects of rhodium(I), iridium(I) and ruthenium(II) complexes in comparison with cis-dichlorodiammino platinum(II) in mice bearing Lewis lung carcinoma.

作者信息

Sava G, Giraldi T, Mestroni G, Zassinovich G

出版信息

Chem Biol Interact. 1983 Jul 1;45(1):1-6. doi: 10.1016/0009-2797(83)90037-6.

Abstract

The effects of square planar rhodium, [RhacacCOD]o and iridium, [IracacCOD]o complexes and of octahedral ruthenium, [cis-RuCl2 (DMSO)4]o complex have been examined in comparison with cis-dichlorodiammino platinum(II) (cis-PDD). The toxicity in BDF1 mice varies widely and decreasing LD50-values, ranging from 0.94 mg/kg to 1000 mg/kg, have been obtained for cis-PDD, [RhacacCOD]o, [IracacCOD]o and [cis-RuCl2(DMSO)4]o, respectively. All the tested complexes similarly inhibit the growth of subcutaneous Lewis lung carcinoma and the development of spontaneous as well as of artificial metastases, with the exception of [IracacCOD]o which is inactive on metastases. The antitumor activity of [RhacacCOD]o and [cis-RuCl2(DMSO)4]o appears interesting, since it is of the same magnitude as that of cis-PDD, considering also that they were found to be only marginally nephrotoxic.

摘要

已将平面正方形铑配合物[RhacacCOD]o、铱配合物[IracacCOD]o以及八面体钌配合物[cis-RuCl2 (DMSO)4]o的效果与顺二氯二氨合铂(II)(顺铂)进行了比较研究。BDF1小鼠中的毒性差异很大,顺铂、[RhacacCOD]o、[IracacCOD]o和[cis-RuCl2(DMSO)4]o的半数致死剂量(LD50)值分别为0.94 mg/kg至1000 mg/kg,呈递减趋势。除了对转移灶无活性的[IracacCOD]o外,所有测试的配合物均同样抑制皮下Lewis肺癌的生长以及自发转移和人工转移的发生。[RhacacCOD]o和[cis-RuCl2(DMSO)4]o的抗肿瘤活性似乎很有意思,因为其活性与顺铂相当,同时还发现它们仅具有轻微的肾毒性。

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