Sesquiterpenes from Cultures of the Basidiomycete Clitocybe conglobata and Their 11β-Hydroxysteroid Dehydrogenase Inhibitory Activity

抄録

A new drimane sesquiterpenoid, 3-keto-drimenol (1), were isolated from cultures of the basidiomycete Clitocybe conglobata together with 3β-hydroxy-11-acetyldrimene (2), 3β-hydroxydrimenol (3), 11,12-dihydroxydrimene (4), 3β-hydroxy-11,12-O-isopropyldrimene (5), and 3β,11,12-trihydroxydrimene (6). Their structures were established from MS and NMR experiments. Compounds 1, 3, and 6 showed inhibitory activities against two isozymes of 11β-hydroxysteroid dehydrogenases with IC₅₀ 1.7—8.0 μg/ml (human 11β-HSD1), 10.7—24.1 μg/ml (mouse 11β-HSD1); 177.0—220.0 μg/ml (human 11β-HSD2), 250.5—500.2 μg/ml (mouse 11β-HSD2), respectively, which catalyze the interconversion of active cortisol and inactive cortisone.