RESUMEN
Cochinmicins I, II, III are novel peptolides produced in submerged-fermentation cultures of Microbispora sp. ATCC 55140. These closely related compounds are separated by HPLC and are novel competitive endothelin antagonists. Cochinmicins II and III are stereoisomeric to each other. Cochinmicin I is the deschloro analog of cochinmicin III.
Asunto(s)
Endotelinas/antagonistas & inhibidores , Micromonosporaceae/metabolismo , Péptidos Cíclicos/biosíntesis , Animales , Antibacterianos/farmacología , Aorta/metabolismo , Bacterias/efectos de los fármacos , Unión Competitiva , Fenómenos Químicos , Química Física , Cromatografía Líquida de Alta Presión , Fermentación , Hongos/efectos de los fármacos , Hipocampo/metabolismo , Pruebas de Sensibilidad Microbiana , Micromonosporaceae/crecimiento & desarrollo , Estructura Molecular , Péptidos Cíclicos/aislamiento & purificación , Péptidos Cíclicos/farmacología , Ratas , EstereoisomerismoRESUMEN
Cytosporin A, B and C, three antagonists of [125I]-angiotensin II binding to rat adrenal glands were discovered in fermentations of an endophytic Cytospora sp. during routine screening using semi-automated procedures. The most potent of these displayed an IC50 of 1.5-3 microM and was specific for angiotensin II AT2.
Asunto(s)
Angiotensina II/antagonistas & inhibidores , Benzopiranos/farmacología , Hongos Mitospóricos/química , Glándulas Suprarrenales/metabolismo , Angiotensina II/metabolismo , Animales , Benzopiranos/química , Fermentación , Espectrometría de Masas , RatasRESUMEN
A novel oleic acid ester of the carotane sesquiterpene 14-hydroxy CAF-603 was isolated from Trichoderma virens grown in a solid brown rice-based medium, a solid millet-based medium, or a mannitol-based liquid medium. Its structure was determined on the basis of ms and nmr analysis. It retains distinct biological activity on the high conductance calcium-activated potassium channel, unlike its analogues 14-hydroxy CAF-603, CAF-603 3-oleate, or CAF-603 3-linoleate.