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

FEBS Letters

Mihara, Shin-ichi¹  Fujimoto, Masafumi¹  Sakurai, Ken-suke¹  Nakajima, Shigeyuki¹  Nakamura, Miharu¹  Ueda, Motohiko¹ 

[1] Shionogi Research Laboratories, Shionogi & Co., 5-12-4 Sagisu Fukushima-ku, Osaka 553, Japan

关键词: Endothelin antagonist;    Myriceron caffeoyl ester;    Receptor binding;    Cytosolic free calcium;    Vasoconstriction;   

DOI  :  10.1016/0014-5793(92)80651-V

学科分类：生物化学/生物物理

来源: John Wiley & Sons Ltd.

【 摘 要 】

A potent non-peptide ET receptor antagonist, myrireron 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.

【 授权许可】

Unknown