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Design, Synthesis and Evaluation of Pentacyclic Triterpenoids Similar to Glycyrrhetinic Acid Via Combination of Chemical and Microbial Modification as Glycogen Phosphorylases Inhibitor

  • Zhu, Yuyao (Nanjing Research Institute for Comprehensive Utilization of Wild Plants) ;
  • Zhang, Jian (Key Laboratory of Modern Chinese Medicines, China Pharmaceutical University) ;
  • Huang, Xiaode (Nanjing Research Institute for Comprehensive Utilization of Wild Plants) ;
  • Chen, Bin (Nanjing Research Institute for Comprehensive Utilization of Wild Plants) ;
  • Qian, Hua (Nanjing Research Institute for Comprehensive Utilization of Wild Plants) ;
  • Zhao, Botao (Nanjing Research Institute for Comprehensive Utilization of Wild Plants)
  • Received : 2018.05.12
  • Accepted : 2018.07.04
  • Published : 2018.11.28

Abstract

A series of pentacyclic triterpenoids similar to glycyrrhetinic acid were designed and synthesized via the combination of chemical modification and microbial catalysis. All products were screened for the glycogen phosphorylases inhibitory activities in vitro. Within this series of derivatives, compound 5 displayed good inhibitory activities with $IC_{50}$ value of $27.7{\mu}M$, which is better than that of the other derivatives and glycyrrhetinic acid. Structure-activity relationship (SAR) analysis of these inhibitors was also discussed.

Acknowledgement

Supported by : National Nature Science Foundation of China (NSFC), National Nature Science Foundation of Jiangsu Province

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