A novel non‐peptide endothelin antagonist isolated from bayberry, <i>Myrica cerifera</i>

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.