Bioassay-guided isolation of saikosaponins with agonistic activity on 5-hydroxytryptamine 2C receptor from Bupleurum chinense and their potential use for the treatment of obesity
Sun Chang-Li1,2; Geng Chang-An1; Huang Xiao-Yan1; Ma Yun-Bao1; Zheng Xiao-Hong1,2; Yang Tong-Hua1,2; Chen Xing-Long1,2; Yin Xiu-Juan1,2; Zhang Xue-Mei1; Chen Ji-Jun1
2017-06-01
发表期刊CHINESE JOURNAL OF NATURAL MEDICINES
ISSN2095-6975
卷号15期号:6页码:467-473
摘要5-Hydroxytryptamine 2C (5-HT2C) receptor is one of the major targets of anti-obesity agents, due to its role in regulation of appetite. In the present study, the 70% EtOH extract of the roots of Bupleurum chinense was revealed to have agonistic activity on 5-HT2C receptor, and the subsequent bioassay-guided isolation led to identification of several saikosaponins as the active constituents with 5-HT2C receptor agonistic activity in vitro and anti-obesity activity in vivo. The new compound, 22-oxosaikosaponin d (1), was determined by extensive spectroscopic analyses (HR-ESI-MS, IR, and 1D and 2D NMR). The primary structure-activity relationship study suggested that the intramolecular ether bond between C-13 and C-28 and the number of sugars at C-3 position were closely related to the 5-HT2C receptor agonistic activity. Saikosaponin a (3), the main saponin in B. chinense, showed obviously agonistic activity on 5-HT2C receptor with an EC50 value of 21.08 +/- 0.33 mu mol.L-1 in vitro and could reduce food intake by 39.1% and 69.2%, and weight gain by 13.6% and 16.4%, respectively, at 3.0 and 6.0 mg.kg(-1) in vivo. This investigation provided valuable information for the potential use of B. chinense as anti-obesity agent.
关键词Bupleurum Chinense 5-hydroxytryptamine 2c (5-ht2c) Receptor Anti-obesity Saikosaponins
收录类别SCI
语种英语
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文献类型期刊论文
条目标识符http://ir.kib.ac.cn/handle/151853/54951
专题植物化学与西部植物资源持续利用国家重点实验室
作者单位1.Chinese Acad Sci, Kunming Inst Bot, State Key Lab Phytochem & Plant Resources West Ch, Kunming 650201, Yunnan, Peoples R China
2.Univ Chinese Acad Sci, Beijing 100049, Peoples R China
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Sun Chang-Li,Geng Chang-An,Huang Xiao-Yan,et al. Bioassay-guided isolation of saikosaponins with agonistic activity on 5-hydroxytryptamine 2C receptor from Bupleurum chinense and their potential use for the treatment of obesity[J]. CHINESE JOURNAL OF NATURAL MEDICINES,2017,15(6):467-473.
APA Sun Chang-Li.,Geng Chang-An.,Huang Xiao-Yan.,Ma Yun-Bao.,Zheng Xiao-Hong.,...&Chen Ji-Jun.(2017).Bioassay-guided isolation of saikosaponins with agonistic activity on 5-hydroxytryptamine 2C receptor from Bupleurum chinense and their potential use for the treatment of obesity.CHINESE JOURNAL OF NATURAL MEDICINES,15(6),467-473.
MLA Sun Chang-Li,et al."Bioassay-guided isolation of saikosaponins with agonistic activity on 5-hydroxytryptamine 2C receptor from Bupleurum chinense and their potential use for the treatment of obesity".CHINESE JOURNAL OF NATURAL MEDICINES 15.6(2017):467-473.
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