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活性天然产物中五环三萜类优势骨架的构建、结构修饰及生物活性评价

Construction, structural modification, and bioactivity evaluation of pentacyclic triterpenoid privileged scaffolds in active natural products.

作者信息

Zeng Ling Rong, Pan Bo Wen, Cai Juan, Liu Li Juan, Dong Zhang Chao, Zhou Ying, Feng Ting Ting, Shi Yang

机构信息

College of Pharmacy, Guizhou University of Traditional Chinese Medicine Guiyang 550025 China

出版信息

RSC Adv. 2024 Dec 13;14(53):39436-39461. doi: 10.1039/d4ra07602h. eCollection 2024 Dec 10.

DOI:10.1039/d4ra07602h
PMID:39679419
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC11640457/
Abstract

Pentacyclic triterpenoids, as important representatives of natural products, have garnered widespread attention due to their diverse biological activities, including anti-inflammatory, antiviral, and antitumor effects. Oleanolic acid (OA), betulinic acid (BA), ursolic acid (UA), triptolide, and glycyrrhetinic acid (GA) are typical examples of pentacyclic triterpenoids. Despite their significant biological activities, their poor water solubility and low bioavailability have limited further development and application. In recent years, researchers have developed a series of derivatives with enhanced biological activities and improved drug properties through structural modifications of these compounds, particularly achieving notable progress in the field of antitumor therapy. This review summarizes recent advances in the structural modification of pentacyclic triterpenoids and explores their promising applications in the development of antitumor, antiviral, and other therapeutic agents.

摘要

五环三萜类化合物作为天然产物的重要代表，因其具有抗炎、抗病毒和抗肿瘤等多种生物活性而受到广泛关注。齐墩果酸（OA）、桦木酸（BA）、熊果酸（UA）、雷公藤甲素和甘草次酸（GA）是五环三萜类化合物的典型例子。尽管它们具有显著的生物活性，但其水溶性差和生物利用度低限制了其进一步的开发和应用。近年来，研究人员通过对这些化合物进行结构修饰，开发出了一系列具有增强生物活性和改善药物性质的衍生物，尤其在抗肿瘤治疗领域取得了显著进展。本文综述了五环三萜类化合物结构修饰的最新进展，并探讨了它们在抗肿瘤、抗病毒和其他治疗药物开发中的应用前景。

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Bioorg Chem. 2020 Apr;97:103694. doi: 10.1016/j.bioorg.2020.103694. Epub 2020 Feb 22.
9
Synthesis, biological evaluation and SAR studies of ursolic acid 3β-ester derivatives as novel CETP inhibitors.熊果酸 3β-酯衍生物作为新型 CETP 抑制剂的合成、生物评价及构效关系研究。
Bioorg Med Chem Lett. 2020 Jan 15;30(2):126824. doi: 10.1016/j.bmcl.2019.126824. Epub 2019 Nov 17.
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Synthesis and Anticancer Activity of CDDO and CDDO-Me, Two Derivatives of Natural Triterpenoids.天然三萜类化合物 CDDO 和 CDDO-Me 的合成及抗癌活性。
Molecules. 2019 Nov 13;24(22):4097. doi: 10.3390/molecules24224097.