Marcon Giordana, Messori Luigi, Orioli Pierluigi
Department of Chemistry, University of Florence, Via Gino Capponi 7, 50121, Italy.
Expert Rev Anticancer Ther. 2002 Jun;2(3):337-46. doi: 10.1586/14737140.2.3.337.
In recent years, owing to the contributions of a few research groups, some new gold(III) compounds--either simple coordination complexes or organogold compounds--have been prepared that are sufficiently stable under physiological conditions and are promising candidates for pharmacological testing as cytotoxic and antitumor agents. In vitro pharmacological studies point out that some of these novel gold(III) complexes are highly cytotoxic toward cultured human tumor cell lines and are able to overcome resistance to platinum. Significant differences in the spectrum of action were observed compared with cisplatin. Studies are in progress to elucidate the mechanism of action of these compounds. The cellular effects of two representative gold(III) complexes are described. Preliminary results on binding to DNA in vitro are presented, pointing out that the interactions are generally weak. The implications of these results for the development of gold(III) complexes as a new family of cytotoxic and antitumor agents are discussed.
近年来,由于一些研究小组的贡献,已经制备出了一些新的金(III)化合物——无论是简单的配位络合物还是有机金化合物——它们在生理条件下具有足够的稳定性,并且作为细胞毒性和抗肿瘤药物进行药理测试很有前景。体外药理研究指出,其中一些新型金(III)络合物对培养的人肿瘤细胞系具有高度细胞毒性,并且能够克服对铂的耐药性。与顺铂相比,观察到作用谱存在显著差异。目前正在进行研究以阐明这些化合物的作用机制。描述了两种代表性金(III)络合物的细胞效应。给出了体外与DNA结合的初步结果,指出相互作用通常较弱。讨论了这些结果对开发金(III)络合物作为新型细胞毒性和抗肿瘤药物家族的意义。