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古古甾酮——一种强效生物活性植物甾醇:合成、结构修饰及其增强的生物活性。

Guggulsterone - a potent bioactive phytosteroid: synthesis, structural modification, and its improved bioactivities.

作者信息

Adarsh Krishna T P, Ajeesh Krishna T P, Edachery Baldev, Antony Ceasar S

机构信息

R & D Division, Sreedhareeyam Farmherbs India Pvt. Ltd Kerala 686 662 India

Division of Plant Molecular Biology and Biotechnology, Department of Bioscience, Rajagiri College of Social Sciences Kochi Kerala 683 104 India.

出版信息

RSC Med Chem. 2023 Nov 2;15(1):55-69. doi: 10.1039/d3md00432e. eCollection 2024 Jan 25.

Abstract

Guggulsterone is a phytosteroid derived from the oleo-gum resin of the critically endangered plant . This molecule has attracted increasing attention due to its excellent biochemistry potential and the compound has consequently been evaluated in clinical trials. With a low concentration in natural resources but wide medicinal and therapeutic value, chemists have developed several synthetic routes for guggulsterone starting from various steroid precursors. Moreover, numerous studies have attempted to modify its structure to improve the biological properties. Nowadays, green and sustainable chemistry has also attracted more attention for advanced chemical processes and reactions in steroid chemistry. The present review aimed to summarize the literature and provide an update about the improvements in the chemical synthesis and structural modification of guggulsterone from the view of green chemistry. Moreover, this review encompasses the improved activities of structurally modified guggulsterone derivatives. We expect that the information provided here will be useful to researchers working in this field and on this molecule.

摘要

古古甾酮是一种从极度濒危植物的油胶树脂中提取的植物甾醇。由于其出色的生物化学潜力,这种分子已引起越来越多的关注,该化合物因此已在临床试验中进行了评估。由于其在自然资源中的含量较低,但具有广泛的药用和治疗价值,化学家们已从各种甾体前体出发开发了几种古古甾酮的合成路线。此外,众多研究试图对其结构进行修饰以改善其生物学特性。如今,绿色可持续化学在甾体化学的先进化学过程和反应中也引起了更多关注。本综述旨在总结文献,并从绿色化学的角度提供古古甾酮化学合成和结构修饰改进的最新情况。此外,本综述还涵盖了结构修饰的古古甾酮衍生物活性的提高。我们希望这里提供的信息对从事该领域和该分子研究的人员有用。

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