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Chaetolactam A,一种来源于内生真菌 sp. g1 的吖啶酮衍生物。

Chaetolactam A, an Azaphilone Derivative from the Endophytic Fungus sp. g1.

机构信息

State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Sciences, and Yunnan Key Laboratory of Natural Medicinal Chemistry, Kunming 650201, Yunnan, People's Republic of China.

University of Chinese Academy of Sciences, Beijing 100049, People's Republic of China.

出版信息

J Org Chem. 2021 Jan 1;86(1):475-483. doi: 10.1021/acs.joc.0c02214. Epub 2020 Dec 2.

Abstract

Chaetolactam A (), an unprecedented azaphilone derivative bearing a unique 9-oxa-7-azabicyclo[4.2.1]octan-8-onering system, together with two new compounds, 11--chaetomugilide B () and chaetomugilide D () was isolated from an endophytic fungus, sp. g1. Notably, extensive NMR data analyses, NMR calculations with DP4 and DP4+ analyses, ECD calculations, and the RDC method were employed to establish the structure of . Furthermore, exhibited potent apoptosis induction activity by mediating caspase-3 activation and PARP degradation at 3 μM in HL-60.

摘要

从一株内生真菌 sp. g1 中分离得到了 Chaetolactam A(),这是一种具有独特的 9-氧杂-7-氮杂双环[4.2.1]辛烷-8-酮环系统的前所未有的氮杂菲酮衍生物,此外还分离得到了两个新化合物,11--chaetomugilide B()和 chaetomugilide D()。值得注意的是,通过广泛的 NMR 数据分析、NMR 计算与 DP4 和 DP4+分析、ECD 计算和 RDC 方法,确定了的结构。此外,在 3 μM 浓度下,通过介导 caspase-3 激活和 PARP 降解,表现出强烈的诱导细胞凋亡活性。

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