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首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >A new rhodium(I) NHC complex inhibits TrxR: In vitro cytotoxicity and in vivo hepatocellular carcinoma suppression
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A new rhodium(I) NHC complex inhibits TrxR: In vitro cytotoxicity and in vivo hepatocellular carcinoma suppression

机译：新的铑（I）NHC复合物抑制TRXR：体外细胞毒性和体内肝细胞癌抑制

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摘要

Thioredoxin reductase (TrxR) is often overexpressed in different types of cancer cells including hepatocellular carcinoma (HCC) cells and regarded as a target with great promise for anticancer drug research and development. Here, we have synthesized and characterized nine new designed rhodium(I) N-heterocyclic carbene (NHC) complexes. All of them were effective towards cancer cells, especially complex le was more active than cisplatin and manifested strong antiproliferative activity against HCC cells. In vivo anticancer studies showed that le significantly repressed tumor growth in an HCC nude mouse model and ameliorated liver lesions in a chronic HCC model caused by CCl4. Notably, a mechanistic study revealed that le can strongly inhibit TrxR system both in vitro and in vivo. Furthermore, le promoted intracellular ROS accumulation, damaged mitochondrial membrane potential, promoted cancer cell apoptosis and blocked the cells in the Cl phase. (C) 2019 Elsevier Masson SAS. All rights reserved.
机译：硫昔林还原酶（TRXR）通常在不同类型的癌细胞中过表达，包括肝细胞癌（HCC）细胞，并视为具有抗癌药物研究和发展的巨大希望的目标。在这里，我们已经合成并表征了九种新设计的铑（I）N-杂环基石（NHC）配合物。所有这些都对癌细胞有效，尤其是复合Le比顺铂更活跃，并表现出对HCC细胞的强烈抗增殖活性。体内抗癌研究表明，在CCL4引起的慢性HCC模型中，LE在HCC裸鼠模型中的肿瘤生长显着压抑肿瘤生长和改善肝脏病变。值得注意的是，机械研究表明，LE可以在体外和体内强烈抑制TRXR系统。此外，Le促进细胞内ROS积累，受损的线粒体膜电位，促进癌细胞凋亡并阻断CL相中的细胞。 （c）2019年Elsevier Masson SAS。版权所有。

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