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Lithocarpins E—G, Potent Anti‐Tumor Tenellone‐Macrolides from the Deep‐Sea Fungus Phomopsis lithocarpus FS508
Author(s) -
Xu Jianlin,
Chen Yuchan,
Liu Zhaoming,
Li Saini,
Wang Yong,
Ren Yuhong,
Liu Hongxin,
Zhang Weimin
Publication year - 2021
Publication title -
chinese journal of chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.28
H-Index - 41
eISSN - 1614-7065
pISSN - 1001-604X
DOI - 10.1002/cjoc.202000621
Subject(s) - chemistry , in vitro , fungus , circular dichroism , stereochemistry , apoptosis , inhibitory postsynaptic potential , diketopiperazines , biochemistry , botany , biology , neuroscience
Main observation and conclusion Lithocarpins E—G, featuring a rare naturally‐occurring highly oxygenated tenellone‐macrolide skeleton, were isolated from the culture extract of a marine‐derived fungus Phomopsis lithocarpus FS508. Their structures were fully elucidated by NMR and MS spectroscopic analyses and electronic circular dichroism calculations. Compounds 1 — 3 were evaluated for their in vitro cytotoxicities against HepG2, MCF‐7, SF‐268, as well as A549 cell lines, among which, compound 1 exhibited inhibitory activity against HepG2 cells with an IC 50 value of 6.3 μmol/L. The further mechanistic investigation demonstrated that lithocarpin E could cause the apoptosis of HepG2 cells through activation of p‐ERK, Bax, and caspase‐3 gene expressions.