RES-1149-1 and -2, novel non-peptidic endothelin type B receptor antagonists produced by Aspergillus sp. I. Taxonomy of producing strain, fermentation, isolation, and physico-chemical and biological properties.

Abstract

RES-1149-1 and -2, novel and non-peptidic endothelin antagonists, were isolated from the cultured broth of a fungus, Aspergillus sp. RE-1149. RES-1149-1 and -2 selectively inhibited the ET-1 binding to endothelin type B receptor (ETB receptor) with IC50 values of 1.5 microM and 20 microM, respectively. Taxonomy of producing strains, fermentation, isolation, and physico-chemical properties of RES-1149-1 and -2 are described.