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. doi: 10.1021/np400850g.
Henrik Harms  1 ,  Viktor Rempel ,  Stefan Kehraus ,  Marcel Kaiser ,  Peter Hufendiek ,  Christa E Müller ,  Gabriele M König
Affiliations
  • 1. Institute for Pharmaceutical Biology, University of Bonn , Nussallee 6, D-53115 Bonn, Germany.
PMID: 24471526 DOI: 10.1021/np400850g
Abstract

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.