Zinc(II) complexes with allixin-derivatives as oral therapeutics for type 2 diabetes (特集:糖尿病と金属) Zinc(II) complexes with allixin-derivatives as oral therapeutics for type 2 diabetes

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During the investigation on the development of Zn(II) complexes with a blood glucose-lowering effect in experimental diabetic animals, we found a potent bis(maltolato)Zn(II) complex (Zn(ma)<SUB>2</SUB>) which exhibited an excellent blood glucose lowering effects in a type 2 diabetic animal model by daily intraperitoneal (<I>i.p.</I>) injections. In order to find orally active Zn(II) complexes in treating type 2 diabetic mellitus, we examined the <I>in vitro</I> and <I>in vivo</I> structure-activity relationships of Zn(II) complexes by using bis(3-hydroxypyronato)Zn(II) complex (Zn(3hp)<SUB>2</SUB>) as a leading compound. Zn(II) complex (Zn(alx)<SUB>2</SUB>) with allixin (Halx) isolated from garlic, exhibited the relatively high <I>in vitro</I> insulin-mimetic activity, as determined by the inhibition of free fatty acid (FFA)-release in isolated rat adipocytes treated with epinephrine. The insulin-mimetic activity of Zn(II) complexes examined strongly correlated with the partition coefficient of the ligand, indicating that the activity of Zn(II) complexes depends on the lipophilicity of the ligand. In type 2 diabetic KKA<SUP>y</SUP> mice, Zn(alx)<SUB>2</SUB> exhibited higher anti-diabetic activity than Zn(ma)<SUB>2</SUB> by daily <I>i.p.</I> injections for 2 weeks. In addition, daily oral administrations of Zn(alx)<SUB>2</SUB> lowered the high blood glucose levels in KKA<SUP>y</SUP> mice, however the effect was not so high. In order to find more active Zn(II) complexes than Zn(alx)<SUB>2</SUB>, three Zn(alx)<SUB>2</SUB>-related complexes were newly prepared and a Zn(II) complex (Zn(tanm)<SUB>2</SUB>) with 1,6-dimethyl-3-hydroxy-5-methoxy-2-pentyl-1,4-dihydropyridine-4-thionato was found to have extremely high <I>in vitro</I> insulin-mimetic activity.

収録刊行物

  • Biomedical research on trace elements  

    Biomedical research on trace elements 17(1), 17-24, 2006-04-01 

    Japan Society for Biomedical Research on Trace Elements

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各種コード

  • NII論文ID(NAID)
    10018127407
  • NII書誌ID(NCID)
    AN10423256
  • 本文言語コード
    ENG
  • 資料種別
    REV
  • ISSN
    0916717X
  • NDL 記事登録ID
    7927375
  • NDL 雑誌分類
    ZS8(科学技術--医学--解剖学・生理学・生化学)
  • NDL 請求記号
    Z19-3255
  • データ提供元
    CJP書誌  NDL  J-STAGE 
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