Menkes病治療薬の開発をめざしたジスルフィラム—銅錯体の可溶化

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タイトル別名
  • Development of a Therapeutic Agent for Menkes Disease: Solubilization of a Copper-Disulfiram Complex
  • Menkes病治療薬の開発をめざしたジスルフィラム : 銅錯体の可溶化
  • Menkesビョウ チリョウヤク ノ カイハツ オ メザシタ ジスルフィラム : ドウ サクタイ ノ カヨウカ

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  Menkes disease (MD) is a neurodegenerative disorder characterized by copper deficiency. It is caused by defective intestinal absorption of copper resulting from a deficiency of a copper-transporting ATPase, ATP7A. We investigated the effects of combination therapy with copper and disulfiram, a known lipophilic chelator. We synthesized a copper-disulfiram complex (Cu-DSF) and determined its crystal structure by X-ray crystallographic analysis. Unfortunately, Cu-DSF was not orally bioavailable due to its lipophilicity. We therefore planned to use cyclodextrin as a solubilizing agent to increase the water solubility of Cu-DSF. After comparisons of the effects of cyclodextrins (α, β, γ), it was found that addition of β-cyclodextrin (β-CyD) increased the solubility of Cu-DSF. Moreover, the modified β-CyD, hydroxypropyl-β-cyclodextrin, was yet more effective as a solubilizing agent. For the development of a convenient method to determine the concentration of Cu-DSF included by β-cyclodextrins, a standard curve based on UV-visible(VIS) absorption was derived.<br>

収録刊行物

  • 薬学雑誌

    薬学雑誌 135 (3), 493-499, 2015-03-01

    公益社団法人 日本薬学会

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