New Derivatives of Natural Acyclic Guanidine Alkaloids with TRPV Receptor-Regulating Properties

Nat Prod Commun. 2015 Jul;10(7):1171-3.

Abstract

The guanidine alkaloids, dihydropulchranin A (2), prepared from pulchranin A from the sponge Monanchora pulchra, and hexadecylguanidine (3), a synthetic analog of pulchranins, were studied for their TRPV channel-regulating activities. Compound 2 was active as an inhibitor of rTRPV1 and hTRPV3 receptors with EC50 values of 24.3 and 59.1 μM, respectively. Hexadecylguanidine (3) was not active against these receptors.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Alkaloids / chemical synthesis*
  • Animals
  • CHO Cells
  • Cricetulus
  • Guanidine / analogs & derivatives*
  • Guanidine / chemical synthesis
  • Guanidines / chemical synthesis*
  • Humans
  • Porifera / chemistry*
  • Rats
  • TRPV Cation Channels / antagonists & inhibitors*

Substances

  • Alkaloids
  • Guanidines
  • TRPV Cation Channels
  • dihydropulchranin A
  • Guanidine