title: Effects of novel chalcone derivatives on α-glucosidase, dipeptidyl peptidase-4, and adipocyte differentiation in vitro.
abstract: Chana series are new chalcone derivatives. To evaluate the possibility of Chana series as therapeutic agents of type 2 diabetes, the inhibitory effects of Chana series on the activities of α-glucosidase and DPP-4 were investigated using in vitro enzyme assays, and their effects on adipocyte differentiation were investigated in C3H10T1/2 cells. Chana 1 and Chana 7 among the Chana series showed significant inhibition of α-glucosidase activity. In DPP-4 enzyme assay, Chana 1 exhibited the highest inhibitory activity while Chana 7 did not. In MTT assay, Chana 1 did not show significant cytotoxicity up to a concentration of 250 μM, whereas cytotoxicity was observed with Chana 7 at a concentration of 300 μM. In addition, Chana 1 induced adipocyte differentiation. Therefore, Chana 1 showed inhibitory effects on α-glucosidase and DPP-4 as well as a stimulatory effect on adipocyte differentiation, suggesting that Chana 1 may be a potential beneficial agent for the treatment of type 2 diabetes.
authors.affiliation: Department of Applied Life Science, The Graduate School, Yonsei University, Seoul, 120-749 Korea.
authors.forename: Eun Jung
authors.initials: EJ
authors.lastname: Bak
authors.forename: Hong Gyu
authors.initials: HG
authors.lastname: Park
authors.forename: Choonghwan
authors.initials: C
authors.lastname: Lee
authors.forename: Tong-Il
authors.initials: TI
authors.lastname: Lee
authors.forename: Gye-Hyeong
authors.initials: GH
authors.lastname: Woo
authors.forename: Younghwa
authors.initials: Y
authors.lastname: Na
authors.forename: Yun-Jung
authors.initials: YJ
authors.lastname: Yoo
authors.forename: Jeong-Heon
authors.initials: JH
authors.lastname: Cha
mesh_terms: D017667:Adipocytes / Q000166:cytology / Q000187:drug effects* / Q000502:physiology*; D000818:Animals; D002454:Cell Differentiation / Q000187:drug effects*; D002460:Cell Line; D002599:Chalcone / Q000031:analogs & derivatives* / Q000378:metabolism / Q000494:pharmacology* / Q000627:therapeutic use; D003924:Diabetes Mellitus, Type 2 / Q000188:drug therapy; D018819:Dipeptidyl Peptidase 4 / Q000378:metabolism*; D054873:Dipeptidyl-Peptidase IV Inhibitors / Q000378:metabolism / Q000494:pharmacology / Q000627:therapeutic use; D004791:Enzyme Inhibitors / Q000378:metabolism / Q000494:pharmacology* / Q000627:therapeutic use; D065089:Glycoside Hydrolase Inhibitors; D006801:Humans; D051379:Mice; D039902:Multipotent Stem Cells / Q000166:cytology / Q000502:physiology
chemical_list: D054873:Dipeptidyl-Peptidase IV Inhibitors; D004791:Enzyme Inhibitors; D065089:Glycoside Hydrolase Inhibitors; D002599:Chalcone; D018819:Dipeptidyl Peptidase 4