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      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

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          Abstract

          5-Hydroxytryptamine 2C (5-HT 2C ) 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 2C receptor, and the subsequent bioassay-guided isolation led to identification of several saikosaponins as the active constituents with 5-HT 2C 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 2C receptor agonistic activity. Saikosaponin a ( 3 ), the main saponin in B. chinense , showed obviously agonistic activity on 5-HT 2C receptor with an EC 50 value of 21.08 ± 0.33 μmol·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.

          Author and article information

          Journal
          Chinese Journal of Natural Medicines
          Chinese Journal of Natural Medicines
          Elsevier BV
          18755364
          June 2017
          June 2017
          : 15
          : 6
          : 467-473
          Article
          10.1016/S1875-5364(17)30070-5
          ca6058c9-0d0d-4f41-a586-56c1724c4bb9
          © 2017

          http://www.elsevier.com/tdm/userlicense/1.0/

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