(±)-Lucidumone, a COX-2 InhibitoryCaged Fungal Meroterpenoid from Ganoderma lucidum
(±)-Lucidumone, a COX-2 InhibitoryCaged Fungal Meroterpenoid from Ganoderma lucidum
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( /â)-Lucidumone，一种来自灵芝的 COX-2 抑制性笼养真菌类萜
DOI：
10.1021/acs.orglett.9b02840
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发表时间：
2019-11-01
期刊：
影响因子：
5.2
通讯作者：
Cheng, Yong-Xian
中科院分区：
文献类型：
--
作者：
Yan, Yong-Ming;Zhang, Hao-Xing;Cheng, Yong-Xian
（+/-）-Lucidumone（1）是从灵芝（Ganoderma lucidum）中分离得到的一种对映异构体，具有6/5/6/6/5稠合多环结构。用单晶X射线晶体学方法确定了（-）-I的绝对构型。提出了一个合理的生物合成途径1。化学生物学方法发现，（-）-1通过直接与Tyr 385的氨基酸残基结合而选择性抑制考克斯-2，代表考克斯-2抑制剂的新结构支架。
(+/-)-Lucidumone (1), an enantiomeric meroterpenoid possessing an unprecedented skeleton comprising a fused 6/5/6/6/5 polycyclic system, was isolated from Ganoderma lucidum and structurally identified. The absolute configuration of (-)-I was assigned by single-crystal X-ray crystallography. A plausible biosynthetic pathway for 1 is proposed. A chemical biology approach reveals that (-)-1 selectively inhibits COX-2 by directly binding with an amino acid residue of Tyr385, representing a new structure scaffold of COX-2 inhibitors.