Protostane Triterpenoids from the Rhizome of Alisma orientale Exhibit Inhibitory Effects on Human Carboxylesterase 2

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• 作者：Zhen-Peng Mai ; Kun Zhou ; Guang-Bo Ge ; Chao Wang ; Xiao-Kui Huo ; Pei-Pei Dong ; Sa Deng ; Bao-Jing Zhang ; Hou-Li Zhang ; Shan-Shan Huang ; Xiao-Chi Ma
• 刊名：Journal of Natural Products
• 出版年：2015
• 出版时间：October 23, 2015
• 年：2015
• 卷：78
• 期：10
• 页码：2372-2380
• 全文大小：437K
• ISSN：1520-6025

文摘

Twelve new and 10 known protostane triterpenoids were isolated from the rhizome of Alisma orientale. Their structures were elucidated based on physical data analyses, including UV, HRESIMS, NMR experiments (¹H, ¹³C NMR, ¹H鈥?sup>1H COSY, HSQC, HMBC, and NOESY), and induced electronic circular dichroism. New compounds 1鈥?b>12 were classified as protostanes (1鈥?b>10), 29-norprotostane (11), and 24-norprotostane (12) by structure analyses. Furthermore, the inhibitory effects on human carboxylesterases (hCE-1, hCE-2) of compounds 1鈥?b>22 were evaluated. Compounds 2, 6, 9, and 11 showed moderate inhibitory activities and were selective toward hCE-2 enzymes, with IC₅₀ values of 8.68, 4.72, 4.58, and 2.02 渭M, respectively. The inhibition kinetics of compound 11 toward hCE-2 were established, and the K_i value was determined as 1.76 渭M using a mixed inhibition model. The interaction of bioactive compound 11 with hCE-2 was shown using molecular docking.