2. Academic Validation
  3. Synthesis and hypoglycemic activity of 9-O-(lipophilic group substituted) berberine derivatives

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.
Shanshan Zhang 1,  Xiaohong Wang 1,  Weicheng Yin 2,  Zhenbao Liu 3,  Mi Zhou 2,  Daipeng Xiao 1,  Yanfei Liu 4,  Dongming Peng 5
Affiliations

Affiliations

  • 1 Department of Pharmaceutical Engineering, School of Chemistry and Chemical Engineering, Central South University, Changsha 410083, China.
  • 2 Department of Medicinal Chemistry, School of Pharmacy, Hunan University of Chinese Medicine, Changsha 410208, China.
  • 3 Department of Pharmaceutics, School of Pharmaceutical Sciences, Central South University, Changsha 410013, China.
  • 4 Department of Pharmaceutical Engineering, School of Chemistry and Chemical Engineering, Central South University, Changsha 410083, China. Electronic address: liuyfcsu@163.com.
  • 5 Department of Medicinal Chemistry, School of Pharmacy, Hunan University of Chinese Medicine, Changsha 410208, China. Electronic address: pdmcsu@126.com.
PMID: 27561717 DOI: 10.1016/j.bmcl.2016.08.027
Abstract

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.

Figures