Ganoderma cochlear Metabolites as Probes to Identify a COX‑2 Active Site and as in Vitro and in Vivo Anti-Inflammatory Agents

(±)-Dispirocochlearoids A–C (1–3), meroterpenoids with a 6/6/5/6/6/6 ring system, were isolated from Ganoderma cochlear. 1–3 are selective COX-2 inhibitors with an IC50 value of (−)-2 at 386 nM. Site-directed mutagenesis identified His351 as a COX-2 active site. In vivo anti-inflammatory activities...

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Bibliographic Details
Published in:Organic letters 2020-04, Vol.22 (7), p.2574-2578
Main Authors: Qin, Fu-Ying, Zhang, Hao-Xing, Di, Qian-Qian, Wang, Yan, Yan, Yong-Ming, Chen, Wei-Lin, Cheng, Yong-Xian
Format: Article
Language:English
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Summary:(±)-Dispirocochlearoids A–C (1–3), meroterpenoids with a 6/6/5/6/6/6 ring system, were isolated from Ganoderma cochlear. 1–3 are selective COX-2 inhibitors with an IC50 value of (−)-2 at 386 nM. Site-directed mutagenesis identified His351 as a COX-2 active site. In vivo anti-inflammatory activities of (−)-2 were performed against acute lung injury in mice.
ISSN:1523-7060
1523-7052
DOI:10.1021/acs.orglett.0c00452