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.
10.1016/S1875-5364(17)30070-5
- Author:
Chang-Li SUN
1
,
2
;
Chang-An GENG
3
;
Xiao-Yan HUANG
3
;
Yun-Bao MA
3
;
Xiao-Hong ZHENG
1
,
2
;
Tong-Hua YANG
1
,
2
;
Xing-Long CHEN
1
,
2
;
Xiu-Juan YIN
1
,
2
;
Xue-Mei ZHANG
3
;
Ji-Jun CHEN
4
Author Information
1. State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Sciences, Kunming 650201, China
2. University of Chinese Academy of Sciences, Beijing 100049, China.
3. State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Sciences, Kunming 650201, China.
4. State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Sciences, Kunming 650201, China. Electronic address: chenjj@mail.kib.ac.cn.
- Publication Type:Journal Article
- Keywords:
5-hydroxytryptamine 2C (5-HT(2C)) receptor;
Anti-obesity;
Bupleurum chinense;
Saikosaponins
- MeSH:
Animals;
Anti-Obesity Agents;
chemistry;
isolation & purification;
pharmacology;
Biological Assay;
Bupleurum;
chemistry;
Male;
Oleanolic Acid;
analogs & derivatives;
chemistry;
isolation & purification;
pharmacology;
Rats;
Rats, Sprague-Dawley;
Saponins;
chemistry;
isolation & purification;
pharmacology;
Serotonin 5-HT2 Receptor Agonists;
chemistry;
isolation & purification;
pharmacology;
Structure-Activity Relationship
- From:
Chinese Journal of Natural Medicines (English Ed.)
2017;15(6):467-473
- CountryChina
- Language:English
-
Abstract:
5-Hydroxytryptamine 2C (5-HT) 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-HT receptor, and the subsequent bioassay-guided isolation led to identification of several saikosaponins as the active constituents with 5-HT 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-HT receptor agonistic activity. Saikosaponin a (3), the main saponin in B. chinense, showed obviously agonistic activity on 5-HT receptor with an EC value of 21.08 ± 0.33 μmol·Lin 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·kgin vivo. This investigation provided valuable information for the potential use of B. chinense as anti-obesity agent.
