title: Sterenin A, B, C and D, novel 11beta-hydroxysteroid dehydrogenase type 1 inhibitors from Stereum sp. SANK 21205.
abstract: The novel 11beta-hydroxysteroid dehydrogenase type 1 (11beta-HSD1) inhibitors known as sterenin A, B, C and D were found in a solid-state culture of the producing basidiomycetes identified as Stereum sp. SANK 21205. Purification of the 50% aq Me(2)CO extract of the culture was performed by EtOAc extraction, reversed phase open-column chromatography and successive ODS HPLC preparation. These compounds, whose structures were determined by several spectroscopic methods, were found to be novel isoindolinone alkaloids which exhibited potent selective inhibitory activities against 11beta-HSD1.
authors.affiliation: Exploratory Research Laboratories II, Daiichi Sankyo Co., Ltd, Edogawa-ku, Tokyo, Japan.
authors.forename: Mariko
authors.initials: M
authors.lastname: Ito-Kobayashi
authors.forename: Azusa
authors.initials: A
authors.lastname: Aoyagi
authors.forename: Isshin
authors.initials: I
authors.lastname: Tanaka
authors.forename: Yasunori
authors.initials: Y
authors.lastname: Muramatsu
authors.forename: Megumi
authors.initials: M
authors.lastname: Umetani
authors.forename: Toshio
authors.initials: T
authors.lastname: Takatsu
mesh_terms: D043205:11-beta-Hydroxysteroid Dehydrogenase Type 1 / Q000037:antagonists & inhibitors* / Q000096:biosynthesis; D043209:11-beta-Hydroxysteroid Dehydrogenase Type 2 / Q000037:antagonists & inhibitors / Q000096:biosynthesis; D000818:Animals; D001487:Basidiomycota / Q000737:chemistry*; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D004305:Dose-Response Relationship, Drug; D004791:Enzyme Inhibitors / Q000494:pharmacology*; D005285:Fermentation; D006801:Humans; D007211:Indoles / Q000737:chemistry / Q000494:pharmacology*; D007700:Kinetics; D009682:Magnetic Resonance Spectroscopy; D051379:Mice; D008862:Microsomes, Liver / Q000187:drug effects / Q000201:enzymology; D020133:Reverse Transcriptase Polymerase Chain Reaction; D016339:Spectrometry, Mass, Fast Atom Bombardment; D013172:Spores, Fungal / Q000201:enzymology
chemical_list: D004791:Enzyme Inhibitors; D007211:Indoles; C532322:sterenin A; C532321:sterenin B; C532320:sterenin C; C532323:sterenin D; D043205:11-beta-Hydroxysteroid Dehydrogenase Type 1; D043209:11-beta-Hydroxysteroid Dehydrogenase Type 2