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Inhibition of 11b-HSD1 by Tetracyclic Triterpenoids from Euphorbia kansui
Laboratory of Chemical Genomics, School of Chemical Biology and Biotechnology, Peking University Shenzhen Graduate School, Shenzhen 518055, Guangdong, China
Key Laboratory of Bioorganic Chemistry and Molecular Engineering, Ministry of Education and Beijing National Laboratory for Molecular Science, College of Chemistry, Peking University, Beijing 100871, China
State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Sciences, Kunming 650204, Yunnan, China
Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China
* Author to whom correspondence should be addressed.
Received: 6 August 2012; in revised form: 13 September 2012 / Accepted: 18 September 2012 / Published: 9 October 2012
Abstract: The roots of Euphorbia kansui are considered an important traditional folk medicine. In this study the ethanol extracts of E. kansui were investigated. A new tetracyclic triterpenoid, euphane-3b,20-dihydroxy-24-ene, in addition to five known triterpenoids with euphane skeletons were isolated. Their structures were elucidated on the basis of physical and spectral techniques (1D-, 2D-NMR and MS, respectively). Furthermore, these compounds 1–6 exhibited strong inhibitory activity against human 11b-hydroxysteroid dehydrogenase type 1 (11b-HSD1), with IC50 values of 34.86 nM, 1.115 mM, 16.08 nM, 2.815 nM, 26.47 nM, 15.99 nM, and 41.86 nM, respectively. The docking results show that the ring part of compounds can insert into the hydrophobic core of h11b-HSD1 and the alkane chain orientates toward the outside. The results presented herein provide a scientific explanation for the usage of the E. kansui in clinical treatment of diabetes.
Keywords: tetracyclic triterpenoids; Euphorbia kansui; inhibition of 11b-HSD1; docking
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Guo, J.; Zhou, L.-Y.; He, H.-P.; Leng, Y.; Yang, Z.; Hao, X.-J. Inhibition of 11b-HSD1 by Tetracyclic Triterpenoids from Euphorbia kansui. Molecules 2012, 17, 11826-11838.
Guo J, Zhou L-Y, He H-P, Leng Y, Yang Z, Hao X-J. Inhibition of 11b-HSD1 by Tetracyclic Triterpenoids from Euphorbia kansui. Molecules. 2012; 17(10):11826-11838.
Guo, Jie; Zhou, Li-Yan; He, Hong-Ping; Leng, Ying; Yang, Zhen; Hao, Xiao-Jiang. 2012. "Inhibition of 11b-HSD1 by Tetracyclic Triterpenoids from Euphorbia kansui." Molecules 17, no. 10: 11826-11838.