title: Synthesis and biological activity of novel tiliroside derivants.
abstract: A series of new tiliroside derivatives were synthesized and characterized by analytical (1)H NMR, (13)C NMR and mass spectrometry. All of the compounds were evaluated for anti-diabetic properties in vitro using HepG2 cells. Compounds 3c, 3d, and 3i-l caused significant enhancements in glucose consumption by insulin-resistant HepG2 cells compared with control cells and cells that were exposed to metformin (an anti-diabetic drug). Moreover, compound 3l significantly activated adenosine 5'-monophosphate-activated protein kinase activity and reduced acetyl-CoA carboxylase activity. Thus, the tiliroside derivative 3l offers potential to be developed as a new approach for treating type II diabetes.
authors.affiliation: Tianjin Medical University, Tianjin Key Laboratory on Technologies Enabling Development Clinical Therapeutics and Diagnostics, School of Pharmaceutical Sciences, Research Center of Basic Medical Sciences, China.
authors.forename: Nan
authors.initials: N
authors.lastname: Qin
authors.forename: Chun-Bao
authors.initials: CB
authors.lastname: Li
authors.forename: Mei-Na
authors.initials: MN
authors.lastname: Jin
authors.forename: Li-Huan
authors.initials: LH
authors.lastname: Shi
authors.forename: Hong-Quan
authors.initials: HQ
authors.lastname: Duan
authors.forename: Wen-Yan
authors.initials: WY
authors.lastname: Niu
mesh_terms: D055372:AMP-Activated Protein Kinases / Q000378:metabolism; D000103:Acetyl-CoA Carboxylase / Q000378:metabolism; D003924:Diabetes Mellitus, Type 2 / Q000188:drug therapy; D004789:Enzyme Activation / Q000187:drug effects; D005419:Flavonoids / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D005947:Glucose / Q000378:metabolism*; D056945:Hep G2 Cells; D006801:Humans; D007004:Hypoglycemic Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D010936:Plant Extracts / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D031987:Potentilla / Q000737:chemistry*
chemical_list: D005419:Flavonoids; D007004:Hypoglycemic Agents; D010936:Plant Extracts; C052083:tiliroside; D055372:AMP-Activated Protein Kinases; D000103:Acetyl-CoA Carboxylase; D005947:Glucose