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首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Discovery of polyoxometalate-based HDAC inhibitors with profound anticancer activity in vitro and in vivo.
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Discovery of polyoxometalate-based HDAC inhibitors with profound anticancer activity in vitro and in vivo.

机译：发现基于多金属氧酸盐的HDAC抑制剂在体内外均具有强​​大的抗癌活性。

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摘要

We obtained 5 positive novel histone deacetylase inhibitors (HDACIs) from a polyoxometalate (POM) library by using a cell-based screening system targeting the p21 gene promoter. Among them, PAC-320, a new tri-organic-tin-substitute germanotungstate, displayed remarkable extracellular inhibitory activity. Meanwhile, the crystal structure of PAC-320 was characterized by X-ray crystallography. PAC-320 could stably exist under physiological conditions as revealed by UV spectrum, CV and TG. PAC-320 possessed a strong inhibitory effect to intracellular HDAC activity. More significantly, PAC-320 inhibited the growth of a variety of cancer cells, and exhibited remarkable anticancer effect in a hepatocarcinoma H22 cell mice model. This study revealed, for the first time, that the HDAC inhibitory activity is a mechanism by which POMs exert their anticancer effect.
机译：我们通过使用针对p21基因启动子的基于细胞的筛选系统，从多金属氧酸盐（POM）库中获得了5种阳性新型组蛋白脱乙酰基酶抑制剂（HDACIs）。其中，PAC-320是一种新型的三有机锡替代锗钨酸盐，具有出色的细胞外抑制活性。同时，通过X射线晶体学对PAC-320的晶体结构进行了表征。紫外光谱，CV和TG表明，PAC-320可以在生理条件下稳定存在。 PAC-320对细胞内HDAC活性具有很强的抑制作用。更重要的是，PAC-320可抑制多种癌细胞的生长，并在肝癌H22细胞小鼠模型中表现出显着的抗癌作用。这项研究首次揭示了HDAC抑制活性是POM发挥其抗癌作用的机制。

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