Indoloditerpenes from a marine-derived fungal strain of Dichotomomyces cejpii with antagonistic activity at GPR18 and cannabinoid receptors.

J Nat Prod 2014 Mar 28;77(3):673-7. Epub 2014 Jan 28.

Institute for Pharmaceutical Biology, University of Bonn , Nussallee 6, D-53115 Bonn, Germany.

A marine-derived strain of Dichotomomyces cejpii produces the new compounds emindole SB beta-mannoside (1) and 27-O-methylasporyzin C (2), as well as the known indoloditerpenes JBIR-03 (3) and emindole SB (4). Indole derivative 1 was found to be a CB2 antagonist, while 2 was identified as the first selective GPR18 antagonist with an indole structure. Compound 4 was found to be a nonselective CB1/CB2 antagonist. The new natural indole derivatives may serve as lead structures for the development of GPR18- and CB receptor-blocking drugs.

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Source
http://pubs.acs.org/doi/10.1021/np400850g
Publisher Site
http://dx.doi.org/10.1021/np400850gDOI Listing
March 2014
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