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汉斯福雷斯特菌素A - M,来自与海绵相关真菌的具有抗菌活性的聚酯。

Hansforesters A-M, polyesters from the sponge-associated fungus with antibacterial activities.

作者信息

Wu Zehong, Liu Dong, Huang Jian, Proksch Peter, Zhu Kui, Lin Wenhan

机构信息

State Key Laboratory of Natural and Biomimetic Drugs, Peking University Beijing 100191 P. R. China

Institute für Pharmazeutische Biologie und Biotechnologie, Heinrich-Heine-Universität Düsseldorf Düsseldorf 40225 Germany.

出版信息

RSC Adv. 2018 Nov 28;8(69):39756-39768. doi: 10.1039/c8ra08606k. eCollection 2018 Nov 23.

Abstract

Bioassay-guided fractionation and chromatographic separation of a sponge-derived fungus , resulted in the isolation of thirteen new polyesters namely hansforesters A-M (1-13), along with five known analogues involving ascotrichalactone A, ascotrichester B, 15G256π, 6-hydroxymellein, and (-)orthosporin. The structures of the new compounds were determined through extensive spectroscopic analysis, in addition to the chemical conversion for the configurational assignment. The polyesters incorporating the motifs of orsellinic acid, 2,4-dihydroxy-6-acetonylbenzoic acid, and orcinotriol were found from nature for the first time. Hansforester A (1) and ascotrichalactone A exhibited potent inhibition against a panel of bacterial strains, including the agricultural pathogenic bacteria, , , , and , with the MIC values of 15.6 μM, and the human infected bacterium with the MIC values of 3.9 μM. These findings suggested that hansforester A and ascotrichalactone A are the potential leads to be developed as the antibacterial agents for the treatment of agriculture bacterial pathogens.

摘要

对一种海绵来源真菌进行生物测定引导的分级分离和色谱分离,得到了13种新的聚酯类化合物,即汉斯福酯A - M(1 - 13),以及5种已知类似物,包括曲霉内酯A、曲霉酯B、15G256π、6 - 羟基麦角硫因和(-)邻孢菌素。除了通过化学转化进行构型归属外,还通过广泛的光谱分析确定了新化合物的结构。首次从自然界中发现了含有苔色酸、2,4 - 二羟基 - 6 - 乙酰基苯甲酸和苔色三醇基序的聚酯。汉斯福酯A(1)和曲霉内酯A对一组细菌菌株表现出强效抑制作用,包括农业病原菌、、、和,其最小抑菌浓度(MIC)值为15.6 μM,对人类感染细菌的MIC值为3.9 μM。这些发现表明,汉斯福酯A和曲霉内酯A是有潜力开发为治疗农业细菌病原体的抗菌剂的先导化合物。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/33ae/9091286/264b27173af8/c8ra08606k-f1.jpg

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