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.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Arrestins / drug effects
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Ascomycota / chemistry*
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Australia
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Diterpenes / chemistry
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Diterpenes / isolation & purification*
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Diterpenes / pharmacology*
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Humans
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Indoles / chemistry
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Indoles / isolation & purification*
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Indoles / pharmacology*
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Mannosides / chemistry
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Mannosides / isolation & purification*
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Mannosides / pharmacology*
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Marine Biology
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Molecular Structure
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Nuclear Magnetic Resonance, Biomolecular
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Receptor, Cannabinoid, CB2 / antagonists & inhibitors*
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Receptors, G-Protein-Coupled / antagonists & inhibitors*
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beta-Arrestins
Substances
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27-O-methylasporyzin C
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Arrestins
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Diterpenes
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GPR18 protein, human
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Indoles
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JBIR-03
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Mannosides
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Receptor, Cannabinoid, CB2
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Receptors, G-Protein-Coupled
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beta-Arrestins
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emindole SB beta-mannoside