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真菌混合萜类化合物的化学和生物学(2009-2019 年)。

The chemistry and biology of fungal meroterpenoids (2009-2019).

机构信息

School of Marine Sciences, Sun Yat-sen University, Guangzhou 510006, China.

出版信息

Org Biomol Chem. 2021 Mar 4;19(8):1644-1704. doi: 10.1039/d0ob02162h.

Abstract

Fungal meroterpenoids are secondary metabolites from mixed terpene-biosynthetic origins. Their intriguing chemical structural diversification and complexity, potential bioactivities, and pharmacological significance make them attractive targets in natural product chemistry, organic synthesis, and biosynthesis. This review provides a systematic overview of the isolation, chemical structural features, biological activities, and fungal biodiversity of 1585 novel meroterpenoids from 79 genera terrestrial and marine-derived fungi including macrofungi, Basidiomycetes, in 441 research papers in 2009-2019. Based on the nonterpenoid starting moiety in their biosynthesis pathway, meroterpenoids were classified into four categories (polyketide-terpenoid, indole-, shikimate-, and miscellaneous-) with polyketide-terpenoids (mainly tetraketide-) and shikimate-terpenoids as the primary source. Basidiomycota produced 37.5% of meroterpenoids, mostly shikimate-terpenoids. The genera of Ganoderma, Penicillium, Aspergillus, and Stachybotrys are the four dominant producers. Moreover, about 56% of meroterpenoids display various pronounced bioactivities, including cytotoxicity, enzyme inhibition, antibacterial, anti-inflammatory, antiviral, antifungal activities. It's exciting that several meroterpenoids including antroquinonol and 4-acetyl antroquinonol B were developed into phase II clinically used drugs. We assume that the chemical diversity and therapeutic potential of these fungal meroterpenoids will provide biologists and medicinal chemists with a large promising sustainable treasure-trove for drug discovery.

摘要

真菌生源二萜类化合物是萜类生物合成起源的混合次生代谢产物。它们引人入胜的化学结构多样化和复杂性、潜在的生物活性和药理学意义,使它们成为天然产物化学、有机合成和生物合成的有吸引力的目标。本综述提供了 2009 年至 2019 年期间,从 79 属陆生和海洋来源真菌(包括大型真菌、担子菌)中分离得到的 1585 种新型生源二萜类化合物的分离、化学结构特征、生物活性和真菌生物多样性的系统概述,这些真菌相关论文有 441 篇。根据其生物合成途径中的非萜烯起始部分,生源二萜类化合物被分为四类(聚酮-萜类、吲哚类、莽草酸-萜类和杂类),其中聚酮-萜类(主要是四酮)和莽草酸-萜类是主要来源。担子菌门产生了 37.5%的生源二萜类化合物,主要是莽草酸-萜类化合物。灵芝属、青霉属、曲霉属和木霉属是四个主要的生源二萜类化合物产生菌。此外,约 56%的生源二萜类化合物表现出各种显著的生物活性,包括细胞毒性、酶抑制、抗菌、抗炎、抗病毒、抗真菌活性。令人兴奋的是,包括antroquinonol 和 4-acetylantroquinonol B 在内的几种生源二萜类化合物已被开发为 II 期临床应用药物。我们假设这些真菌生源二萜类化合物的化学多样性和治疗潜力将为生物学家和药物化学家提供一个巨大的、有前途的可持续药物发现宝库。

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