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

	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-Li 1,2; Geng Chang-An 1; Huang Xiao-Yan 1; Ma Yun-Bao 1; Zheng Xiao-Hong 1,2; Yang Tong-Hua 1,2; Chen Xing-Long 1,2; Yin Xiu-Juan 1,2; Zhang Xue-Mei1 ; Chen Ji-Jun1
	2017-06-01
发表期刊	CHINESE JOURNAL OF NATURAL MEDICINES
ISSN	2095-6975
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
学科领域	Integrative & Complementary Medicine ; Pharmacology & Pharmacy
收录类别	SCI
语种	英语
WOS记录号	WOS:000406660400009
引用统计
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
推荐引用方式 GB/T 7714	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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