Evaluation of in vitro cytotoxicity and hepatotoxicity of platinum(II) and palladium(II) oxalato complexes with adenine derivatives as carrier ligands.
Evaluation of in vitro cytotoxicity and hepatotoxicity of platinum(II) and palladium(II) oxalato complexes with adenine derivatives as carrier ligands.
复制标题
以腺嘌呤衍生物为载体配体的铂(II)和钯(II)草酸配合物的体外细胞毒性和肝毒性评价。
DOI：
10.1016/j.jinorgbio.2010.07.002
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发表时间：
2010
影响因子：
3.9
通讯作者：
Z. Trávníček
中科院分区：
文献类型：
--
作者：
R. Vrzal;P. Štarha;Z. Dvořák;Z. Trávníček
涉及基于N6-苄基-9-异丙基腺嘌呤的N-供体载体配体（Ln）的[Pt（ox）（Ln）2]（1-7）和[Pd（ox）（Ln）2]（8-14）氨合（ox）配合物对卵巢癌（A2780）、顺铂抗性卵巢癌本实验研究了A2780 cis、恶性黑色素瘤（G-361）、肺癌（A549）、宫颈上皮样癌（HeLa）、乳腺癌（MCF 7）和骨肉瘤（HOS）等人癌细胞系的生长情况。与用作阳性对照的顺铂相比，一些测试的复合物甚至具有数倍的细胞毒性。铂（II）配合物3（IC 50 =3.2±1.0μM和3.2±0.6μM）和5（IC 50 =4.0±1.0μM和4.1±1.4μM）对A2780和A2780 cis的细胞毒性作用有所改善，而顺铂的IC 50分别为11.5±1.6μM和30.3±6.1μM。评价了钯（II）络合物对MCF 7（12的IC 50 =8.2±3.8μM）和A2780（14的IC 50 =5.4±1.2μM）的显著体外细胞毒性，其再次超过顺铂，顺铂对MCF 7细胞的IC 50等于19.6±4.3μM。还筛选了所选复合物在人肝细胞原代培养物中的体外细胞毒性作用，发现它们无肝毒性。
In vitro antitumour activity of the [Pt(ox)(Ln)2] (1–7) and [Pd(ox)(Ln)2] (8–14) oxalato (ox) complexes involving N6-benzyl-9-isopropyladenine-based N-donor carrier ligands (Ln) against ovarian carcinoma (A2780), cisplatin resistant ovarian carcinoma (A2780cis), malignant melanoma (G-361), lung carcinoma (A549), cervix epitheloid carcinoma (HeLa), breast adenocarcinoma (MCF7) and osteosarcoma (HOS) human cancer cell lines was studied. Some of the tested complexes were even several times more cytotoxic as compared with cisplatin employed as a positive control. The improved cytotoxic effect was demonstrated for the platinum(II) complexes 3 (IC50=3.2±1.0μM and 3.2±0.6μM) and 5 (IC50=4.0±1.0μM and 4.1±1.4μM) against A2780 and A2780cis, as compared with 11.5±1.6μM, and 30.3±6.1μM determined for cisplatin, respectively. The significant in vitro cytotoxicity against MCF7 (IC50=8.2±3.8μM for 12) and A2780 (IC50=5.4±1.2μM for 14) was evaluated for the palladium(II) oxalato complexes, which again exceeded cisplatin, whose IC50equalled 19.6±4.3μM against the MCF7 cells. Selected complexes were also screened for their in vitro cytotoxic effect in primary cultures of human hepatocytes and they were found to be non-hepatotoxic.