Planta Med 2012; 78 - PD165
DOI: 10.1055/s-0032-1320523

Synthesis and biological evaluation of chalcone derivatives as a novel class of anti-diabetic agents

CT Hsieh 1, TJ Hsieh 2, YC Wu 3, FR Chang 1
  • 1Graduate Institute of Natural Products, College of Pharmacy, Kaohsiung Medical University, Kaohsiung 807, Taiwan
  • 2Department of Medical Genetics, College of Medicine, Kaohsiung Medical University, Kaohsiung 807, Taiwan
  • 3Graduate Institute of Integrated Medicine, College of Chinese Medicine, China Medical University, Taichung 404, Taiwan

Diabetes and metabolic syndrome are growing health issues and life threatening events worldwide. Therefore, developing new substances for the treatment of diabetes and metabolic syndrome will be an urgent issue. Chalcone is a kind of well-known flavonoids with several bioactivities; however, its anti-diabetic effect has not been investigated yet. The Chalcone derivatives were synthesized by Claisen-Schmidt Condensation from acetophenones with aldehydes. For quick anti-diabetic effect screening, we established an in vitro model by measuring the 24-hour glucose consumption in the culture medium of 3T3-L1 adipocytes. Two halogen derivatives, AN7–13 and CHA79, showed the most potential anti-diabetic activity among the serial chalcone derivatives. From the high-fat diet fed mice model, AN7–13 and CHA-79 showed the effect to prevent the increase in body weight and improve the glucose intolerance. In addition, AN7–13 and CHA-79 showed no hepatic and renal toxicity. After completing this study, we should be able to obtain an optimized chalcone derivate for developing a new class of medication for type 2 diabetes treatment.