Hupehenols A–E, Selective 11β-Hydroxysteroid Dehydrogenase Type 1 (11β-HSD1) Inhibitors from Viburnum hupehense
- 15 January 2015
- journal article
- research article
- Published by American Chemical Society (ACS) in Journal of Natural Products
- Vol. 78 (2) , 330-334
Abstract
Five selective 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) competitive inhibitors, hupehenols A–E (1–5), were isolated from Viburnum hupehense. The structure elucidation indicated that compounds 1–5 are new 20,21,22,23,24,25,26,27-octanordammarane triterpenoids. Their structures were established on the basis of NMR spectroscopic and mass spectrometric analysis. Hupehenols A–E (1–5) showed inhibition against human 11β-HSD1, with hupehenols B (2) and E (5) having IC50 values of 15.3 and 34.0 nM, respectively. Moreover, hupehenols C (3) and D (4) are highly selective inhibitors of human 11β-HSD1 when compared to murine 11β-HSD1.Keywords
Funding Information
- National Natural Science Foundation of China (81102347)
- Ministry of Science and Technology of the People's Republic of China (2011CB915503)
This publication has 36 references indexed in Scilit:
- Lithocarpic Acids A–N, 3,4-seco-Cycloartane Derivatives from the Cupules ofLithocarpus polystachyusJournal of Natural Products, 2014
- Ingol-Type Diterpenes from Euphorbia antiquorum with Mouse 11β-Hydroxysteroid Dehydrogenase Type 1 Inhibition ActivityJournal of Natural Products, 2014
- Dammarane-type triterpenoids as 11β-HSD1 inhibitors from Homonoia ripariaOrganic & Biomolecular Chemistry, 2014
- 11beta-Hydroxysteroid dehydrogenase type 1 inhibitors: novel agents for the treatment of metabolic syndrome and obesity-related disorders?Metabolism, 2013
- 11 β ‐Hydroxysteroid dehydrogenase type 1: relevance of its modulation in the pathophysiology of obesity, the metabolic syndrome and type 2 diabetes mellitusDiabetes, Obesity and Metabolism, 2012
- 11β-Hydroxysteroid dehydrogenase type 1 in obesity and the metabolic syndromeMolecular and Cellular Endocrinology, 2004
- A Transgenic Model of Visceral Obesity and the Metabolic SyndromeScience, 2001
- Type 1 11β-Hydroxysteroid Dehydrogenase Mediates Glucocorticoid Activation and Insulin Release in Pancreatic IsletsJournal of Biological Chemistry, 2000
- Hypertension in mice lacking 11β-hydroxysteroid dehydrogenase type 2Journal of Clinical Investigation, 1999
- 11β-Hydroxysteroid Dehydrogenase1997