title: Synthesis of diosgenin-ibuprofen derivatives and their activities against insulin-dependent diabetes mellitus.
abstract: The synthesis and anti-diabetes activities of diosgenin-ibuprofen derivatives were investigated. Ibuprofen (IBU) was chemically coupled with diosgenin either directly or through amino acid esters linkers. The effects of these compounds on lipopolysaccharide (LPS)-induced nitric oxide (NO) generation were assessed. The results showed spirost-5-en-3β-yl (2-(4-isobutyl-phenyl)-propionate) (4) was of better activity to suppress the production of NO in the supernatant of LPS-stimulated RAW264.7 cells. In vivo investigation on nonobese diabetic (NOD) mice indicated that compound 4 decreased the incidence of insulin-dependent diabetes mellitus (IDDM; type 1 diabetes) of NOD mice which suggested a potential activity of compound 4 against type 1 diabetes.
authors: Laboratory of Ethnopharmacology, Institution for Nanobiomedical Technology and Membrane Biology, Regenerative Medicinal Research Center, West China Hospital, West China Medical School, Sichuan University, No. 1, Keyuansilu, Gaopeng, Dadao, Chengdu 610041, P.R. China.
authors: Guang
authors: G
authors: Xin
authors: Yanyan
authors: Y
authors: Wang
authors: Xiurong
authors: X
authors: Guo
authors: Baozhan
authors: B
authors: Huang
authors: Dan
authors: D
authors: Du
authors: Shiliang
authors: S
authors: He
authors: Rui
authors: R
authors: Zhang
authors: Zhihua
authors: Z
authors: Xing
authors: Hang
authors: H
authors: Zhao
authors: Qianming
authors: Q
authors: Chen
authors: Wen
authors: W
authors: Huang
authors: Yang
authors: Y
authors: He
mesh_terms: D000818:Animals; D002460:Cell Line; D003921:Diabetes Mellitus, Experimental / Q000188:drug therapy*; D003922:Diabetes Mellitus, Type 1 / Q000188:drug therapy*; D004144:Diosgenin / Q000737:chemistry* / Q000627:therapeutic use*; D007004:Hypoglycemic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000627:therapeutic use; D007052:Ibuprofen / Q000737:chemistry* / Q000627:therapeutic use*; D008070:Lipopolysaccharides / Q000037:antagonists & inhibitors / Q000494:pharmacology; D051379:Mice; D016688:Mice, Inbred NOD; D015394:Molecular Structure
chemical_list: D007004:Hypoglycemic Agents; D008070:Lipopolysaccharides; D004144:Diosgenin; D007052:Ibuprofen