title: Synthesis and hypoglycemic activity of 9-O-(lipophilic group substituted) berberine derivatives.
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.
authors: Department of Pharmaceutical Engineering, School of Chemistry and Chemical Engineering, Central South University, Changsha 410083, China.
authors: Shanshan
authors: S
authors: Zhang
authors: Department of Pharmaceutical Engineering, School of Chemistry and Chemical Engineering, Central South University, Changsha 410083, China.
authors: Xiaohong
authors: X
authors: Wang
authors: Department of Medicinal Chemistry, School of Pharmacy, Hunan University of Chinese Medicine, Changsha 410208, China.
authors: Weicheng
authors: W
authors: Yin
authors: Department of Pharmaceutics, School of Pharmaceutical Sciences, Central South University, Changsha 410013, China.
authors: Zhenbao
authors: Z
authors: Liu
authors: Department of Medicinal Chemistry, School of Pharmacy, Hunan University of Chinese Medicine, Changsha 410208, China.
authors: Mi
authors: M
authors: Zhou
authors: Department of Pharmaceutical Engineering, School of Chemistry and Chemical Engineering, Central South University, Changsha 410083, China.
authors: Daipeng
authors: D
authors: Xiao
authors: Department of Pharmaceutical Engineering, School of Chemistry and Chemical Engineering, Central South University, Changsha 410083, China. Electronic address: liuyfcsu@163.com.
authors: Yanfei
authors: Y
authors: Liu
authors: Department of Medicinal Chemistry, School of Pharmacy, Hunan University of Chinese Medicine, Changsha 410208, China. Electronic address: pdmcsu@126.com.
authors: Dongming
authors: D
authors: Peng
mesh_terms: D001599:Berberine / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D003924:Diabetes Mellitus, Type 2 / Q000188:drug therapy; D056945:Hep G2 Cells; D006801:Humans; D007004:Hypoglycemic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use; D013057:Spectrum Analysis / Q000379:methods
chemical_list: D007004:Hypoglycemic Agents; D001599:Berberine
keywords: Berberine derivatives; Cytotoxicity; Hypoglycemic activity; Structure–activity analysis; Synthesis