title: Dammarane-type triterpenoids as 11β-HSD1 inhibitors from Homonoia riparia.
abstract: An exploration for 11β-HSD1 inhibitors from Homonoia riparia returned eight new dammarane-type triterpenoids, horipenoids A–H (1–8), and a known oleanane-type triterpenoid (9). Their structures were elucidated on the basis of comprehensive analysis of spectroscopic data, and the absolute configuration of horipenoid E (5) was established by single crystal X-ray crystallography. Compounds 1–4 represent a rare class of octanortriterpenoids. Horipenoids C (3) and E (5) showed potent inhibition against mouse 11β-HSD1 with IC50 values of 0.810 ± 0.058 and 0.898 ± 0.215 μM, respectively.
authors.affiliation: State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 555 Zu Chong Zhi Road, Shanghai, 201203, P. R. China. h.zhang@simm.ac.cn jmyue@simm.ac.cn.
authors.forename: Jin-Hai
authors.initials: JH
authors.lastname: Yu
authors.forename: Yu
authors.initials: Y
authors.lastname: Shen
authors.forename: Hong-Bing
authors.initials: HB
authors.lastname: Liu
authors.forename: Ying
authors.initials: Y
authors.lastname: Leng
authors.forename: Hua
authors.initials: H
authors.lastname: Zhang
authors.forename: Jian-Min
authors.initials: JM
authors.lastname: Yue
mesh_terms: D043205:11-beta-Hydroxysteroid Dehydrogenase Type 1 / Q000037:antagonists & inhibitors* / Q000378:metabolism; D000818:Animals; D066241:Carbon-13 Magnetic Resonance Spectroscopy; D018360:Crystallography, X-Ray; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D019665:Euphorbiaceae / Q000737:chemistry*; D051379:Mice; D008968:Molecular Conformation; D066244:Proton Magnetic Resonance Spectroscopy; D014315:Triterpenes / Q000737:chemistry / Q000494:pharmacology*; D000097669:Dammaranes
chemical_list: D043205:11-beta-Hydroxysteroid Dehydrogenase Type 1; D004791:Enzyme Inhibitors; D014315:Triterpenes; D000097669:Dammaranes