A novel non-peptide endothelin antagonist isolated from bayberry, Myrica cerifera.
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.
Fujimoto
M
M
Shionogi Research Laboratories, Shionogi & Co., Osaka, Japan.
Mihara
S
S
Nakajima
S
S
Ueda
M
M
Nakamura
M
M
Sakurai
K
K
D016475:3T3 Cells; D000595:Amino Acid Sequence; D000818:Animals; D002109:Caffeic Acids / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D016232:Endothelins; D008297:Male; D051379:Mice; D008969:Molecular Sequence Data; D015394:Molecular Structure; D010944:Plants / Q000737:chemistry*; D051381:Rats; D011919:Rats, Inbred Strains; D011956:Receptors, Cell Surface / Q000037:antagonists & inhibitors*; D017466:Receptors, Endothelin
D002109:Caffeic Acids; D016232:Endothelins; D011956:Receptors, Cell Surface; D017466:Receptors, Endothelin; C075745:myriceron caffeoyl ester