Synthesis of Diosgenin-Ibuprofen Derivatives and Their Activities against Insulin-Dependent Diabetes Mellitus
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概要
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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.
著者
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Xing Zhihua
Laboratory Of Ethnopharmacology Institute For Nanobiomedical Technology And Membrane Biology Regener
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He Yang
Laboratory Of Ethnopharmacology Institute For Nanobiomedical Technology And Membrane Biology Regener
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Huang Wen
Laboratory Of Ethnopharmacology Institute For Nanobiomedical Technology And Membrane Biology Regener
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Zhang Rui
Laboratory of Ethnopharmacology, Institution for Nanobiomedical Technology and Membrane Biology, Regenerative Medicinal Research Center, West China Hospital, West China Medical School, Sichuan University
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He Yang
Laboratory of Ethnopharmacology, Institution for Nanobiomedical Technology and Membrane Biology, Regenerative Medicinal Research Center, West China Hospital, West China Medical School, Sichuan University
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Xin Guang
Laboratory of Ethnopharmacology, Institution for Nanobiomedical Technology and Membrane Biology, Regenerative Medicinal Research Center, West China Hospital, West China Medical School, Sichuan University
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Wang Yanyan
Laboratory of Ethnopharmacology, Institution for Nanobiomedical Technology and Membrane Biology, Regenerative Medicinal Research Center, West China Hospital, West China Medical School, Sichuan University
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Guo Xiurong
Laboratory of Ethnopharmacology, Institution for Nanobiomedical Technology and Membrane Biology, Regenerative Medicinal Research Center, West China Hospital, West China Medical School, Sichuan University
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Huang Baozhan
Laboratory of Ethnopharmacology, Institution for Nanobiomedical Technology and Membrane Biology, Regenerative Medicinal Research Center, West China Hospital, West China Medical School, Sichuan University
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Du Dan
Laboratory of Ethnopharmacology, Institution for Nanobiomedical Technology and Membrane Biology, Regenerative Medicinal Research Center, West China Hospital, West China Medical School, Sichuan University
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He Shiliang
Laboratory of Ethnopharmacology, Institution for Nanobiomedical Technology and Membrane Biology, Regenerative Medicinal Research Center, West China Hospital, West China Medical School, Sichuan University
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Zhao Hang
State Key Laboratory of Oral Diseases, West China Hospital of Stomatology, Sichuan University
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Chen Qianming
State Key Laboratory of Oral Diseases, West China Hospital of Stomatology, Sichuan University
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Huang Wen
Laboratory of Ethnopharmacology, Institution for Nanobiomedical Technology and Membrane Biology, Regenerative Medicinal Research Center, West China Hospital, West China Medical School, Sichuan University
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Xing Zhihua
Laboratory of Ethnopharmacology, Institution for Nanobiomedical Technology and Membrane Biology, Regenerative Medicinal Research Center, West China Hospital, West China Medical School, Sichuan University
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