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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.

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          Author and article information

          Journal
          CJNM
          Chinese Journal of Natural Medicines
          Elsevier
          1875-5364
          20 June 2017
          : 15
          : 6
          : 467-473
          Affiliations
          1State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Sciences, Kunming 650201, China
          2University of Chinese Academy of Sciences, Beijing 100049, China
          Author notes
          *Corresponding author: CHEN Ji-Jun, Tel: 86-871-65223265, Fax: 86-871-65227197; E-mail: chenjj@ 123456mail.kib.ac.cn

          These authors have no conflict of interest to declare.

          Article
          S1875-5364(17)30070-5
          10.1016/S1875-5364(17)30070-5
          Copyright © 2017 China Pharmaceutical University. Published by Elsevier B.V. All rights reserved.
          Funding
          Funded by: National Science Foundation of China
          Award ID: 81573322
          This work was supported by the National Science Foundation of China (No. 81573322), the Hundred-Talent Program of CAS, the CAS “Light of West China” Program, and the Youth Innovation Promotion Association of CAS.

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