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Application of 18β-glycyrrhetinic acid in the structural modification of natural products: a review

  • Wan-Xin Li,
  • Ye-Fang Lu,
  • Fei Wang,
  • Bing Ai,
  • Sheng-Bo Jin,
  • Siqi Li,
  • Guang-Hua Xu,
  • Cheng-Hua Jin

摘要

18β-Glycyrrhetinic acid (GA) is an oleane-type pentacyclic triterpene saponin obtained from glycyrrhizic acid by removing 2 glucuronic acid groups. GA and its analogues are active substances of glycyrrhiza aicd, with similar structure and important pharmacological effects such as anti-inflammatory, anti-diabetes, anti-tumor and anti-fibrosis. Although GA combined compounds are in the clinical trial stages, its application potential is severely restricted by its low bioavailability, water solubility and membrane permeability. In this article, synthetic methods and structure–activity relationships (SARs) of GA derivatives from 2018 to present are reviewed based on pharmacological activity. It is hoped that this review can provide reference for the future development of potential GA preclinical candidate compounds, and furnish ideas for the development of pentacyclic triterpenoid lead compounds.