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 / 中国天然药物
Chinese Journal of Natural Medicines (English Ed.)
;
(6): 467-473, 2017.
Article
in English
| WPRIM
| ID: wpr-812092
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.
Full text:
Available
Index:
WPRIM (Western Pacific)
Main subject:
Oleanolic Acid
/
Pharmacology
/
Saponins
/
Structure-Activity Relationship
/
Biological Assay
/
Chemistry
/
Rats, Sprague-Dawley
/
Anti-Obesity Agents
/
Bupleurum
/
Serotonin 5-HT2 Receptor Agonists
Limits:
Animals
Language:
English
Journal:
Chinese Journal of Natural Medicines (English Ed.)
Year:
2017
Type:
Article
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