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In vitro toxicological evaluation of a dinuclear platinum(II) complex with acetate ligands.

机译:具有乙酸盐配体的双核铂(II)配合物的体外毒理学评估。

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In the present study the toxicological potential of a tumor-inhibiting dinuclear platinum(II) complex (bis(acetato)diammine-bis-mu-acetato diplatinum(II) dihydrate (BAP)) was evaluated, utilizing in vitro models of nephrotoxicity, myelosuppression and neurotoxicity. Regarding the discrepancies between the hallmark toxicity of the clinically utilized platinum drugs, we used three distinct referent compounds as follows cisplatin for the assessment of in vitro nephrotoxicity, carboplatin in case of cultured bone marrow cells and oxaliplatin for the determination of the in vitro neurotoxicty, respectively. The results obtained indicate that the investigated dinuclear complex is endowed by a lower potential to induce detrimental effects upon these typically susceptible platinum toxicity cellular populations as compared to the corresponding referent drugs. These findings, together with the previously encountered profound cytotoxic efficiency of this dinuclear platinum(II) complex against human tumor cell lines, recall for a further detailed evaluation of BAP as potential antineoplastic agent.
机译:在本研究中,利用肾毒性,骨髓抑制的体外模型评估了抑制肿瘤的双核铂(II)配合物(双(乙酰氨基)diammine-双-mu-乙酰基双铂(II)二水合物(BAP))的毒理学潜力。和神经毒性。关于临床使用的铂类药物的标志性毒性之间的差异,我们使用了三种不同的参考化合物,如下所述:顺铂用于评估体外肾毒性;卡铂用于培养的骨髓细胞;奥沙利铂用于测定体外神经毒性,分别。获得的结果表明,与相应的参照药物相比,所研究的双核复合物具有较低的诱导这些典型易感的铂毒性细胞群的有害作用的潜力。这些发现,连同该双核铂(II)配合物对人类肿瘤细胞系先前所遇到的深远的细胞毒性作用,使人想起对BAP作为潜在抗肿瘤药的进一步详细评估。

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