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抗肿瘤先导化合物埃里安宁的最新研究进展:作用机制与结构修饰。

Recent advances of antitumor leading compound Erianin: Mechanisms of action and structural modification.

机构信息

Basic Medical Research Center, Academy of Medical Science, Zhengzhou University, Zhengzhou, Henan, 450001, China.

Basic Medical Research Center, Academy of Medical Science, Zhengzhou University, Zhengzhou, Henan, 450001, China.

出版信息

Eur J Med Chem. 2023 Dec 5;261:115844. doi: 10.1016/j.ejmech.2023.115844. Epub 2023 Sep 29.

Abstract

Erianin, a bioactive compound extracted from Dendrobium, a traditional Chinese medicine, exhibits remarkable anti-cancer properties through diverse molecular mechanisms and has attracted the attention of medicinal chemists. However, the low solubility in water, rapid metabolism and elimination from the body lead to poor bioavailability of Erianin, and greatly hinder its clinical application. The development of new Erianin derivatives is continuously proceed to improve its anticancer effects. In recent years, although important progress in the development of Erianin and the publication of some reviews in this aspect, the mechanism against various cancers, pharmacokinetic study, structural modification as well as structure-activity relationships have not been thoroughly considered. This review is aimed at providing complete picture regarding the above aspects by reviewing studies from 2000 to 2023.06. This review also supplies some important viewpoints on the design and future directions for the development of Erianin derivatives as possible clinically effective anticancer agents.

摘要

冬凌草甲素是从中国传统中药石斛中提取的一种具有生物活性的化合物,通过多种分子机制表现出显著的抗癌特性,引起了药物化学家的关注。然而,冬凌草甲素在水中的溶解度低、代谢和消除速度快,导致其生物利用度差,极大地阻碍了其临床应用。因此,不断开发新的冬凌草甲素衍生物以提高其抗癌效果。近年来,虽然在冬凌草甲素的开发方面取得了重要进展,并发表了一些相关综述,但对其针对各种癌症的作用机制、药代动力学研究、结构修饰以及构效关系等方面还没有进行全面的考虑。本综述通过对 2000 年至 2023.06 年的研究进行回顾,旨在提供关于上述方面的完整信息。本综述还就设计和未来发展方向提供了一些重要观点,以期开发出具有临床应用潜力的有效抗癌药物。

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