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

Org Lett

School of Pharmaceutical Sciences, School of Medicine, College of Life Sciences and Oceanography, Shenzhen University, Shenzhen 518060, P. R. China.

Published: April 2020

(±)-Dispirocochlearoids A-C (-), meroterpenoids with a 6/6/5/6/6/6 ring system, were isolated from . - are selective COX-2 inhibitors with an IC value of (-)- at 386 nM. Site-directed mutagenesis identified His351 as a COX-2 active site. In vivo anti-inflammatory activities of (-)- were performed against acute lung injury in mice.

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http://dx.doi.org/10.1021/acs.orglett.0c00452DOI Listing

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