The antineoplastic potential of a stable monomeric Au(II) complex with hematoporphyrin IX (Hp), namely [Au(II)Hp(-2H).(H(2)O)(2)], was investigated in a panel of tumor cell lines. The complex exhibits strong cytotoxicity, whereby the leukaemia- and lymphoma-derived cell lines are more sensitive, with IC(50) values comparable to those of the reference anticancer drug cisplatin. In contrast, the solid tumor models are more sensitive to the platinum drug. A comparative assessment of both agents against the human kidney cell line 293T has shown that [Au(II)Hp(-2H).(H(2)O)(2)] is less cytotoxic. The gold complex induces oligonucleosomal DNA fragmentation in tumour cells following 24-hour treatment and hence its cytotoxic effect is at least partly mediated by induction of apoptotic cell death. A prominent intracellular gold accumulation was detected after treating tumor cells with [Au(II)Hp(-2H).(H(2)O)(2)] which shows that its putative pharmacological targets are readily accessible after a short incubation period.

中文翻译：

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具有血卟啉 IX 的稳定单体金 (II) 复合物的体外评估：对肿瘤和肾细胞的细胞毒性、细胞积累和诱导细胞凋亡。

在一组肿瘤中研究了稳定的单体 Au(II) 复合物与血卟啉 IX (Hp) 的抗肿瘤潜力，即 [Au(II)Hp(-2H).(H(2)O)(2)]细胞系。该复合物表现出强烈的细胞毒性，由此白血病和淋巴瘤衍生的细胞系更加敏感，其 IC(50) 值与参考抗癌药物顺铂的 IC(50) 值相当。相比之下，实体瘤模型对铂类药物更敏感。对人类肾细胞系 293T 两种药物的比较评估表明 [Au(II)Hp(-2H).(H(2)O)(2)] 的细胞毒性较小。金复合物在治疗 24 小时后诱导肿瘤细胞中的寡核小体 DNA 片段化，因此其细胞毒作用至少部分是通过诱导凋亡细胞死亡来介导的。