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A Customizable Approach for the Enzymatic Production and Purification of Diterpenoid Natural Products
Published on: October 4, 2019
Dammarane-type triterpenoids as 11β-HSD1 inhibitors from Homonoia riparia
Jin-Hai Yu1, Yu Shen, Hong-Bing Liu
1State 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.
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.
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