2. Academic Validation
  3. Synthesis of nature product kinsenoside analogues with anti-inflammatory activity

Synthesis of nature product kinsenoside analogues with anti-inflammatory activity

  • Bioorg Med Chem. 2021 Jan 1;29:115854. doi: 10.1016/j.bmc.2020.115854.
Wei Song 1,  Yong Sun 1,  Lintao Xu 1,  Yajing Sun 2,  Tianlu Li 3,  Peng Peng 4,  Hongxiang Lou 5
Affiliations

Affiliations

  • 1 Key Laboratory of Chemical Biology of Ministry of Education, School of Pharmaceutical Sciences, Shandong University, Jinan 250012, PR China.
  • 2 National Glycoengineering Research Center, Shandong University, Jinan 250012, PR China.
  • 3 Key Laboratory of Chemical Biology of Ministry of Education, School of Pharmaceutical Sciences, Shandong University, Jinan 250012, PR China; National Glycoengineering Research Center, Shandong University, Jinan 250012, PR China.
  • 4 National Glycoengineering Research Center, Shandong University, Jinan 250012, PR China. Electronic address: pengpeng@sdu.edu.cn.
  • 5 Key Laboratory of Chemical Biology of Ministry of Education, School of Pharmaceutical Sciences, Shandong University, Jinan 250012, PR China. Electronic address: louhongxiang@sdu.edu.cn.
PMID: 33223464 DOI: 10.1016/j.bmc.2020.115854
Abstract

Kinsenoside is the major bioactive component from herbal medicine with a broad range of pharmacological functions. Goodyeroside A, an epimer of kinsenoside, remains less explored. In this report we chemically synthesized kinsenoside, goodyeroside A and their analogues with glycan variation, chirality inversion at chiral center(s), and bioisosteric replacement of lactone with lactam. Among these compounds, goodyeroside A and its mannosyl counterpart demonstrated superior anti-inflammatory efficacy. Furthermore, goodyeroside A was found to suppresses inflammatory through inhibiting NF-κB signal pathway, effectively. Structure-activity relationship is also explored for further development of more promising kinsenoside analogues as drug candidates.

Keywords

Anti-inflammatory; Goodyeroside A; Kinsenoside; Nitric Oxide Release; Structure-activity Relationship.

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