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厚朴酚和和厚朴酚的结构修饰及其衍生物的生物活性研究进展。

Research Progress on the Structural Modification of Magnolol and Honokiol and the Biological Activities of Their Derivatives.

机构信息

Department of pharmacy, the Affiliated Yixing Hospital of Jiangsu University, Wuxi, Yixing, 214200, China.

New Drug Research and Development Center, Guangdong Pharmaceutical University, Guangzhou, 510006, China.

出版信息

Chem Biodivers. 2023 Aug;20(8):e202300754. doi: 10.1002/cbdv.202300754. Epub 2023 Jul 19.

Abstract

Magnolol and Honokiol are the primary active components that have been identified and extracted from Magnolia officinalis, and several investigations have demonstrated that they have significant pharmacological effects. Despite their therapeutic benefits for a wide range of illnesses, research on and the implementation of these compounds have been hindered by their poor water solubility and low bioavailability. Researchers are continually using chemical methods to alter their structures to make them more effective in treating and preventing diseases. Researchers are also continuously developing derivative drugs with high efficacy and few adverse effects. This article summarizes and analyzes derivatives with significant biological activities reported in recent research obtained by structural modification. The modification sites have mainly focused on the phenolic hydroxy groups, benzene rings, and diene bonds. Changes to the allyl bisphenol structure will result in unexpected benefits, including high activity, low toxicity, and good bioavailability. Furthermore, alongside earlier experimental research in our laboratory, the structure-activity relationships of magnolol and honokiol were preliminarily summarized, providing experimental evidence for improving their development and utilization.

摘要

厚朴酚和和厚朴酚是从厚朴中鉴定和提取的主要活性成分,多项研究表明它们具有显著的药理作用。尽管它们对多种疾病具有治疗益处,但由于其水溶性差和生物利用度低,对这些化合物的研究和应用受到了阻碍。研究人员一直在使用化学方法改变它们的结构,使其在治疗和预防疾病方面更有效。研究人员还在不断开发具有高效、低副作用的衍生药物。本文通过结构修饰综述和分析了近年来研究中报道的具有显著生物活性的衍生物。修饰部位主要集中在酚羟基、苯环和二烯键上。对烯丙基双酚结构的改变将带来意想不到的好处,包括高活性、低毒性和良好的生物利用度。此外,结合我们实验室之前的实验研究,初步总结了厚朴酚和和厚朴酚的构效关系,为其开发利用提供了实验依据。

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