RES-1214-1 and -2, Novel Non-peptidic Endothelin Type A Receptor Antagonists Produced by Pestalotiopsis sp.

TATSUHIRO OGAWA; KATSUHIKO ANDO; YUMIKO AOTANI; KATSUMI SHINODA; TAKEO TANAKA; Em TSUKUDA; MAYUMI YOSHIDA; YUZURU MATSUDA

doi:10.7164/antibiotics.48.1401

RES-1214-1 and -2, Novel Non-peptidic Endothelin Type A Receptor Antagonists Produced by Pestalotiopsis sp.

TATSUHIRO OGAWA, KATSUHIKO ANDO, YUMIKO AOTANI, KATSUMI SHINODA, TAKEO TANAKA, Em TSUKUDA, MAYUMI YOSHIDA, YUZURU MATSUDA

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JOURNAL FREE ACCESS

1995 Volume 48 Issue 12 Pages 1401-1406

DOI https://doi.org/10.7164/antibiotics.48.1401

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Abstract

RES-1214-1 and -2, novel and non-peptidic endothelin antagonists, were isolated from the culture broth of a fungus, Pestalotiopsis sp. RE-1214. RES-1214-1 and -2 selectively inhibited the ET-1 binding to endothelin type A receptor (ET_A receptor) with IC₅₀ values of 1.5μM and 20μM, respectively. RES-1214-1 and -2 inhibited the increase in intracellular Ca²⁺ concentration elicited by 1 nM ET-1 in A10 cells. Taxonomy of producing strains, fermentation, isolation, structural determination, and biochemical properties of RES-1214-1 and -2 are described.

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