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Ganoderma cochlear Metabolites as Probes to Identify a COX-2 Active Site and as in Vitro and in Vivo
Fu-Ying Qin1, Hao-Xing Zhang1, Qian-Qian Di1
1School of Pharmaceutical Sciences, School of Medicine, College of Life Sciences and Oceanography, Shenzhen University, Shenzhen 518060, P. R. China.
Abstract:
(±)-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.
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