Polydiscamides B-D from a marine sponge Ircinia sp. as potent human sensory neuron-specific G protein coupled receptor agonists

J Nat Prod. 2008 Jan;71(1):8-11. doi: 10.1021/np070094r. Epub 2007 Dec 29.

Abstract

Polydiscamides B, C, and D (1-3) were isolated from a sponge Ircinia sp. The structures of 1 to 3 were elucidated by the comparison of their NMR and HRESIMS spectroscopic data with that of a structurally related compound, polydiscamide A. All compounds showed potent agonist activity against human sensory neuron-specific G protein couple receptor (SNSR), a receptor involved in the modulation of pain, and they are the first examples of nonendogenous human SNSR agonists.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Australia
  • Humans
  • Molecular Structure
  • Neurons, Afferent / drug effects*
  • Pain Measurement / drug effects
  • Peptides, Cyclic / chemistry
  • Peptides, Cyclic / isolation & purification*
  • Peptides, Cyclic / pharmacology*
  • Porifera / chemistry*
  • Receptors, G-Protein-Coupled / agonists*

Substances

  • Peptides, Cyclic
  • Receptors, G-Protein-Coupled
  • polydiscamide B
  • polydiscamide C
  • polydiscamide D