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生物合成假说指导的内生真菌拟茎点属中聚酮合酶-非核糖体肽合酶杂合代谢产物的发现和全合成。

Biosynthetic Hypothesis-Guided Discovery and Total Syntheses of PKS-NRPS Hybrid Metabolites from Endophytic Fungus Periconia Species.

机构信息

School of Pharmaceutical Sciences, MOE Key Laboratory of Bioorganic Phosphorus Chemistry & Chemical Biology , Tsinghua University , Beijing 100084 , China.

College of Chemistry, Chemical Engineering and Environmental Engineering , Liaoning Shihua University , Fushun 113001 , China.

出版信息

Org Lett. 2019 Mar 15;21(6):1794-1798. doi: 10.1021/acs.orglett.9b00371. Epub 2019 Feb 25.

Abstract

Guided by our biosynthetic hypothesis, pericoannosins C-F, four new PKS-NRPS hybrid metabolites, were discovered from the endophytic fungus Periconia sp. F-31. Their structures and absolute configurations were elucidated by extensive spectroscopic data and electronic circular dichroism analyses. Preliminary biological evaluation revealed that pericoannosins C-D exhibited anti-HIV activities with IC values of 15.5 and 13.5 μM. Furthermore, the bioinspired syntheses of pericoannosins C-E have also been completed with high efficiency.

摘要

受我们生物合成假说的指导,我们从内生真菌 Periconia sp. F-31 中发现了四种新的 PKS-NRPS 杂合代谢产物——佩里考诺辛 C-F。通过广泛的光谱数据分析和电子圆二色性分析,阐明了它们的结构和绝对构型。初步的生物评估表明,佩里考诺辛 C-D 具有抗 HIV 活性,IC 值分别为 15.5 和 13.5 μM。此外,还高效地完成了佩里考诺辛 C-E 的生物启发合成。

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