Synthesis and hypoglycemic activity of 9-O-(lipophilic group substituted) berberine derivatives

Bioorg Med Chem Lett. 2016 Oct 1;26(19):4799-4803. doi: 10.1016/j.bmcl.2016.08.027. Epub 2016 Aug 11.


A series of 9-O-(lipophilic group substituted) berberine derivatives were synthesized and evaluated for their cytotoxicity and hypoglycemic activity against HepG2 cells. All the results indicated that most of the synthesized compounds exhibited lower cytotoxicity and a certain degree of hypoglycemic activity. Especially the compounds 5g and 5h displayed dramatically increased hypoglycemic activity compared with berberine, and the cytotoxicity maintained or even lower than berberine, indicating that they are potential candidates for new anti-type 2 diabetes mellitus drugs.

Keywords: Berberine derivatives; Cytotoxicity; Hypoglycemic activity; Structure–activity analysis; Synthesis.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Berberine / chemical synthesis*
  • Berberine / chemistry
  • Berberine / pharmacology*
  • Diabetes Mellitus, Type 2 / drug therapy
  • Hep G2 Cells
  • Humans
  • Hypoglycemic Agents / chemical synthesis*
  • Hypoglycemic Agents / chemistry
  • Hypoglycemic Agents / pharmacology*
  • Hypoglycemic Agents / therapeutic use
  • Spectrum Analysis / methods


  • Hypoglycemic Agents
  • Berberine