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.
Chin J Nat Med
; 15(6): 467-473, 2017 Jun.
Article
en En
| MEDLINE
| ID: mdl-28629538
ABSTRACT
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 µmol·L-1in 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-1in vivo. This investigation provided valuable information for the potential use of B. chinense as anti-obesity agent.
Palabras clave
Texto completo:
1
Banco de datos:
MEDLINE
Asunto principal:
Ácido Oleanólico
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Saponinas
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Fármacos Antiobesidad
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Bupleurum
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Agonistas del Receptor de Serotonina 5-HT2
Límite:
Animals
Idioma:
En
Revista:
Chin J Nat Med
Año:
2017
Tipo del documento:
Article
País de afiliación:
China