Hupehenols A-E, Selective 11β-Hydroxysteroid Dehydrogenase Type 1 (11β-HSD1) Inhibitors from Viburnum hupehense

被引：20
|
作者：
Chen, Xuan-Qin [1 ]
Shao, Li-Dong [1 ]
Pal, Mahesh [2 ]
Shen, Yu [3 ]
Cheng, Xiao [1 ]
Xu, Gang [1 ]
Peng, Li-Yan [1 ]
Wang, Kou [1 ]
Pan, Zheng-Hong [1 ]
Li, Ming-Ming [1 ]
Leng, Ying [3 ]
He, Juan [1 ]
Zhao, Qin-Shi [1 ]
机构：
[1] Chinese Acad Sci, Kunming Inst Bot, State Key Lab Phytochem & Plant Resources West Ch, Kunming 650204, Yunnan, Peoples R China
[2] CSIR Natl Bot Res Inst, Phytochem Div, Lucknow 226001, Uttar Pradesh, India
[3] Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China
来源：
JOURNAL OF NATURAL PRODUCTS | 2015年 / 78卷 / 02期
基金：
中国国家自然科学基金;
关键词：
NOR-DAMMARANE TRITERPENOIDS; METABOLIC SYNDROME; OBESITY; DISCOVERY; DITERPENOIDS; GLYCOSIDES; POTENT;
D O I：
10.1021/np500896n
中图分类号：
Q94 [植物学];
学科分类号：
071001 ;
摘要：
Five selective 11 beta-hydroxysteroid dehydrogenase type 1 (11 beta-HSD1) competitive inhibitors, hupehenols AE (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 AE (1-5) showed inhibition against human 11 beta-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 11 beta-HSD1 when compared to murine 11 beta-HSD1.T
引用
收藏
页码：330 / 334
页数：5
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