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 En
| WPRIM
| ID: wpr-812092
Responsible library:
WPRO
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.
Key words
Full text:
1
Database:
WPRIM
Main subject:
Oleanolic Acid
/
Pharmacology
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Saponins
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Structure-Activity Relationship
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Biological Assay
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Chemistry
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Rats, Sprague-Dawley
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Anti-Obesity Agents
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Bupleurum
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Serotonin 5-HT2 Receptor Agonists
Limits:
Animals
Language:
En
Journal:
Chinese Journal of Natural Medicines (English Ed.)
Year:
2017
Document type:
Article