A novel non-peptide endothelin antagonist isolated from bayberry, Myrica cerifera

FEBS Lett. 1992 Jun 22;305(1):41-4. doi: 10.1016/0014-5793(92)80651-v.

Abstract

A potent non-peptide ET receptor antagonist, myriceron caffeoyl ester (50-235), was isolated from the bayberry, Myrica cerifera. This compound selectively antagonized specific binding of [125I]ET-1, but not of [125I]ET-3, to rat cardiac membranes, ET-1-induced increase in the intracellular free calcium concentration in Swiss 3T3 fibroblasts, and ET-1-induced contraction of rat aortic strips. Thus, 50-235 is the first non-peptide ET(A) receptor antagonist. This compound can be useful for studying the physiological role of endothelin and exploring its role in various diseases.

MeSH terms

  • 3T3 Cells
  • Amino Acid Sequence
  • Animals
  • Caffeic Acids / chemistry
  • Caffeic Acids / isolation & purification
  • Caffeic Acids / pharmacology*
  • Endothelins*
  • Male
  • Mice
  • Molecular Sequence Data
  • Molecular Structure
  • Plants / chemistry*
  • Rats
  • Rats, Inbred Strains
  • Receptors, Cell Surface / antagonists & inhibitors*
  • Receptors, Endothelin

Substances

  • Caffeic Acids
  • Endothelins
  • Receptors, Cell Surface
  • Receptors, Endothelin
  • myriceron caffeoyl ester