Cytotoxicity and DNA binding properties of a chloro glycylhistidinate gold(III) complex (GHAu)
Cytotoxicity and DNA binding properties of a chloro glycylhistidinate gold(III) complex (GHAu)
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DOI：
10.1016/s0009-2797(99)00160-x
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发表时间：
2000-02-15
影响因子：
5.1
通讯作者：
Orioli, P
中科院分区：
文献类型：
--
作者：
Carotti, S;Marcon, G;Orioli, P
氯甘氨酰组氨酸金（III）配合物（GHAu）显示出对已建立的A2780卵巢癌人细胞系（对顺铂敏感或耐药）具有相当的细胞毒性。值得注意的是，GHAu的细胞毒性远大于相应的锌（II）、钯（II）、铂（II）和钴（II）络合物，这意味着细胞毒性基本上归因于金（III）中心的存在。圆二色性（CD）光谱，原子吸收测量和DNA熔解曲线表明，GHAu在体外能够结合DNA，几种抗肿瘤金属配合物的假定目标，并修改其构象，即使观察到的变化一般很小。这些研究结果的细胞毒性金（III）配合物的作用机制的影响进行了讨论。(C)2000由Elsevier Science爱尔兰有限公司出版。保留所有权利。
The chloro glycylhistidinate gold(III) complex (GHAu) is shown to be fairly cytotoxic towards the established A2780 ovarian carcinoma human cell line either sensitive or resistant to cisplatin. Remarkably, GHAu is far more cytotoxic than the corresponding zinc(II), palladium(II), platinum(II) and cobalt(II) complexes implying that cytotoxicity is essentially to be ascribed to the presence of a gold(III) center. Circular dichroism (CD) spectra, atomic absorption measurements and DNA melting profiles suggest that GHAu in vitro is able to bind DNA, the presumed target for several antitumor metal complexes, and to modify its conformation, even if the observed changes are generally small. Implications of these findings for the mechanism of action of cytotoxic gold(III) complexes are discussed. (C) 2000 Published by Elsevier Science Ireland Ltd. All rights reserved.