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
文献类型：期刊论文
| 作者 | 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
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| 刊名 | CHINESE JOURNAL OF NATURAL MEDICINES
 |
| 出版日期 | 2017-06-01 |
| 卷号 | 15期号:6页码:467-473 |
| ISSN号 | 2095-6975 |
| 关键词 | Bupleurum Chinense 5-hydroxytryptamine 2c (5-ht2c) Receptor Anti-obesity Saikosaponins |
| 英文摘要 | 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. |
| 学科主题 | Integrative & Complementary Medicine ; Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000406660400009 |
| 源URL | [http://ir.kib.ac.cn/handle/151853/54951]  |
| 专题 | 昆明植物研究所_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. |
入库方式： OAI收割
来源：昆明植物研究所
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