首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Novel effects of glycyrrhetinic acid on the central nervous system tumorigenic progenitor cells: induction of actin disruption and tumor cell-selective toxicity.
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Novel effects of glycyrrhetinic acid on the central nervous system tumorigenic progenitor cells: induction of actin disruption and tumor cell-selective toxicity.

机译:甘草次酸对中枢神经系统致瘤祖细胞的新作用:肌动蛋白破坏和肿瘤细胞选择性毒性的诱导。

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摘要

Licorice extracts are used worldwide in foods and medicines, and glycyrrhetinic acid (GA) is a licorice component that has been reported to induce various important biological activities. In the present study, we show that GA induces actin disruption and has tumor cell-selective toxic properties, and that its selectivity is superior to those of all the clinically available antitumor agents tested. The cytotoxic activity of GA and the tested antitumor agents showed better correlation with the partition coefficient (log P) values rather than the polar surface area (PSA) values. For selective toxicity against tumor cells, GA was most effective at 10 microM that was the same concentration as the previously reported maximum plasma GA level reached in humans ingesting licorice. These results suggest that GA could be utilized as a promising chemopreventive and therapeutic antitumor agent. The underlying mechanisms involved in the selective toxicity to tumor cells by GA are also preliminarily discussed.
机译:甘草提取物在全球范围内用于食品和药品,甘草次酸(GA)是甘草的一种成分,据报道可诱导多种重要的生物活性。在本研究中,我们表明GA诱导肌动蛋白破坏,并具有肿瘤细胞选择性毒性特性,并且其选择性优于测试的所有临床可用抗肿瘤剂。 GA和测试的抗肿瘤药的细胞毒活性显示出与分配系数(log P)值而非极性表面积(PSA)值更好的相关性。对于针对肿瘤细胞的选择性毒性,GA在10 microM时最有效,该浓度与先前报道的摄入甘草的人的最大血浆GA水平相同。这些结果表明,GA可以用作有前途的化学预防和治疗性抗肿瘤剂。还初步讨论了由GA对肿瘤细胞的选择性毒性所涉及的潜在机制。

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