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刺盘孢内酯A-J,极地真菌sp. D-1的倍半萜多样性扩展

Eutypellaolides A-J, Sesquiterpene diversity expansion of the polar fungus sp. D-1.

作者信息

Ning Zhe, Hu Bo, Sun Yuan-Yuan, Ding Jin-Feng, Han Xiang-Ying, Lu Xiao-Ling, Yin Zi-Fei, He Ying, Jiao Bing-Hua, Yu Hao-Bing, Liu Xiao-Yu

机构信息

Department of Marine Biomedicine and Polar Medicine, Naval Medical Center of PLA, Naval Medical University, Shanghai, China.

Department of Biochemistry and Molecular Biology, College of Basic Medical Sciences, Naval Medical University, Shanghai, China.

出版信息

Front Microbiol. 2024 Jan 25;15:1349151. doi: 10.3389/fmicb.2024.1349151. eCollection 2024.

Abstract

Eight new 12,8-eudesmanolide sesquiterpenes, eutypellaolides A-H (-), and two new eudesmane-type sesquiterpenes, eutypellaolides I-J (-), along with four known 12,8-eudesmanolide compounds -, were isolated from the culture extract of the polar fungus sp. D-1 by one strain many compounds (OSMAC) approach. The structures of these compounds were determined through comprehensive spectroscopic data and experimental and calculated ECD analysis. Antibacterial, immunosuppressive, and PTP1B inhibition activities of these compounds were evaluated. Compounds and exhibited strong inhibitory activities against and , with each showing an MIC value of 2 μg/mL. Compound displayed weak immunosuppressive activity against ConA-induced T-cell proliferation with an inhibitory rate of 61.7% at a concentration of 19.8 μM. Compounds , , and exhibited weak PTP1B inhibition activities with IC values of 44.8, 43.2, and 49.5 μM, respectively.

摘要

通过“一个菌株,多种化合物”(OSMAC)方法,从极地真菌D-1菌株的培养提取物中分离出8个新的12,8-桉叶烷内酯倍半萜类化合物,即eutypellaolides A-H(-),以及2个新的桉叶烷型倍半萜类化合物,即eutypellaolides I-J(-),同时还分离出4个已知的12,8-桉叶烷内酯类化合物。通过综合光谱数据以及实验和计算的电子圆二色谱(ECD)分析确定了这些化合物的结构。评估了这些化合物的抗菌、免疫抑制和蛋白酪氨酸磷酸酶1B(PTP1B)抑制活性。化合物 和 对 和 表现出较强的抑制活性,其最低抑菌浓度(MIC)值均为2μg/mL。化合物 对刀豆蛋白A(ConA)诱导的T细胞增殖表现出较弱的免疫抑制活性,在浓度为19.8μM时抑制率为61.7%。化合物 、 和 表现出较弱的PTP1B抑制活性,其半数抑制浓度(IC)值分别为44.8、43.2和49.5μM。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2065/10850561/76fcddfd62bf/fmicb-15-1349151-g001.jpg

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