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来自内生菌sp. JC-J7的潜在降血脂聚酮化合物，存在于……中

Potential antihyperlipidemic polyketones from endophytic sp. JC-J7 in .

作者信息

Hu Ming, Yang Xue-Qiong, Wan Chuen-Ping, Wang Bang-Yan, Yin Hai-Yue, Shi Li-Jiao, Wu Ya-Mei, Yang Ya-Bin, Zhou Hao, Ding Zhong-Tao

机构信息

Functional Molecules Analysis and Biotransformation Key Laboratory of Universities in Yunnan Province, School of Chemical Science and Technology, Yunnan University Kunming People's Republic of China

Affiliated Hospital of Yunnan University of Traditional Chinese Medicine Kunming 650021 PR China.

出版信息

RSC Adv. 2018 Dec 14;8(73):41810-41817. doi: 10.1039/c8ra08822e. eCollection 2018 Dec 12.

DOI:10.1039/c8ra08822e
PMID:35558782
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC9091869/
Abstract

Eleven new polyketones named diaporthsins A-K (1-11) were isolated from the fermentation of sp. JC-J7. The chemical structures of compounds (1-11) were elucidated by spectroscopic methods including HRESIMS, 2DNMR, NMR and chemical methods. Compound 11 features an unusual acyclic polyketone-phenolic polyketone hybrid structure that integrates the characteristics of different fungal metabolites (cytosporone and multiplolide). Compound 3 was the only C-polyketone obtained in this research. These new polyketones showed inhibitory activity on triglycerides (TG) in steatosis hepatocyte L-02 cells. Among them, compound 5 and (4)-6,7,9-trihydroxydec-4-enoic acid displayed inhibitory activities on TG in steatotic L-02 cells with inhibition ratios of 26% and 21% at concentration of 5 μg mL; also, inhibition ratios of 8--acetylmultiplolide A and phomopsisporone A at concentration of 5 μg mL were calculated to be about 24% and 16%, respectively, which were equivalent to the antihyperlipidemic activity of lovastatin. The preliminary structure-activity relationship indicated that acetyl at C-8 can increase the antihyperlipidemic activity of multiplolide A and the glycol ester and hydroxyl at C-6 can also increase the corresponding activity of diaporthsin B.

摘要

从链格孢属菌株JC-J7的发酵产物中分离出11种新的聚酮化合物，命名为diaporthsins A-K（1-11）。通过高分辨电喷雾电离质谱（HRESIMS）、二维核磁共振（2DNMR）、核磁共振（NMR）等光谱方法以及化学方法阐明了化合物（1-11）的化学结构。化合物11具有不寻常的无环聚酮-酚类聚酮杂化结构，融合了不同真菌代谢产物（细胞孢子素和多聚内酯）的特征。化合物3是本研究中获得的唯一一种碳聚酮。这些新的聚酮化合物对脂肪变性的肝细胞L-02细胞中的甘油三酯（TG）具有抑制活性。其中，化合物5和（4）-6,7,9-三羟基癸-4-烯酸对脂肪变性的L-02细胞中的TG具有抑制活性，在浓度为5 μg/mL时抑制率分别为26%和21%；此外，8-乙酰基多聚内酯A和拟茎点霉孢素A在浓度为5 μg/mL时的抑制率经计算分别约为24%和16%，与洛伐他汀的抗高血脂活性相当。初步的构效关系表明，C-8位的乙酰基可增强多聚内酯A的抗高血脂活性，C-6位的二醇酯和羟基也可增强diaporthsin B的相应活性。

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