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In vitro pharmacological study of monomeric platinum(III) hematoporphyrin IX complexes.

机译:单体铂(III)血卟啉IX配合物的体外药理研究。

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摘要

Three stable mononuclear hematoporphyrin IX ((7,12-bis(1-hydroxyethyl)-3,8,13,17-tetramethyl-21H-23H-porphyn-2,18-dipropionic acid), Hp) complexes of Pt(III), namely cis-[ Pt(III)(NH(3))(2)(Hp(-3H))(H(2)O)(2)].H(2)O 1, [Pt(III)(Hp(-3H))(H(2)O)(2)].H(2)O 2 and [Pt(III)((O,O)Hp(-2H))Cl(H(2)O)(3)] 3 with distorted octahedral structure and (d(z)2)(1) ground state have been tested in vitro for antineoplastic activity in a panel of tumor cell lines. The novel platinum(III) complexes showed cytotoxic activity in a concentration-dependent manner with IC(50) values comparable to those of referent cytotoxic agent cisplatin together with lower cytotoxicity against renal cells. Further detailed evaluation of the active analogue 2 and the less active complex 3 showed that their potency greatly correlates with the ability to induce apoptosis and to bind DNA. Despite the structural dissimilarities between complex 2 and cisplatin, their DNA-adducts were equally effectively recognized and repaired by the nucleotide excision repair system. Complex 2 showed quite superior ability to accumulate in K-562 cells relative to cisplatin.
机译:Pt(III)的三种稳定的单核血卟啉IX((7,12-双(1-羟乙基)-3,8,13,17-四甲基-21H-23H-卟啉-2,18-二丙酸),Hp)配合物,即cis- [Pt(III)(NH(3))(2)(Hp(-3H))(H(2)O)(2)]。H(2)O 1,[Pt(III)( Hp(-3H))(H(2)O)(2)]。H(2)O 2和[Pt(III)((O,O)Hp(-2H))Cl(H(2)O) (3)]具有八面体结构变形和(d(z)2)(1)基态的3已在体外测试了一组肿瘤细胞系中的抗肿瘤活性。新型铂(III)配合物以浓度依赖性方式显示出细胞毒活性,其IC(50)值可与参照的细胞毒剂顺铂相媲美,而且对肾细胞的毒性更低。对活性类似物2和活性较低的复合物3的进一步详细评估表明,它们的效能与诱导凋亡和结合DNA的能力密切相关。尽管复合物2和顺铂之间在结构上存在差异,但它们的DNA加合物仍被核苷酸切除修复系统有效地识别和修复。相对于顺铂,复合物2显示出在K-562细胞中积累的相当优异的能力。

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