@article{oai:fukuyama-u.repo.nii.ac.jp:00007074, author = {今村, 順茂 and 古賀, 利久 and 樋口, 敏幸 and 小田切, 優樹 and 杉野, 栄一 and 日比野, 俐}, journal = {福山大学薬学部研究年報, Annual report of the Faculty of Pharmacy & Pharmaceutical Sciences, Fukuyama University}, month = {}, note = {P(論文), ウサギ腎由来のカルボニル還元酵素によって触媒されるアセトヘキサミドの還元反応はケトン性薬剤ベフノロール,モペロン,レボブノロール,ダウノルビシン,ロキソプロフェンによって抑制された.ベフノロール,モペロン,レボブノロール,ダウノルビシンに対する酵素のVmax/Km値の対数値と酵素の抑制百分率の間には強い相関関係が観察され,アセトヘキサミドに関する酵素の競争的基質であると判明した.ケトン基薬剤であっても非ステロイド性坑炎症薬のロキソプロフェンに対するプロットは明らかに逆行していた.また,数種のケトン性非ステロイド性抗炎症薬も酵素によって抑制され,アセトヘキサミドの抑制を強く阻害した., The reduction of acetohexamide catalyzed by carbonyl reductase from rabbit kidney was inhibited by befunolol, moperone, levobunolol, daunorubicin and loxoprofen, which have a ketone group within their chemical structures and are substrates for the enzyme. A significant correlation was obserbed between the common logarithm of Vmax/Km values of enzyme for befunolol, moperone, levobunolol and daunorubicin and the percentage inhibition of the enzyme, confirming that these drugs are competitive substrates of the enzyme with respect to acetoxamide. However, the plot for loxoprofen, a nonsteroidal anti-inflammatory drug with a ketone group, was apparently distant from the regression line obtained. Although nonsteroidal anti-inflammatory drugs with a ketone group such as suprofen and fenbufen were not reduced by the enzyme, they strongly inhibited the reduction of acetohexamide catalyzed by the enzyme.}, pages = {56--57}, title = {ウサギ腎由来のカルボニル還元酵素により触媒されるアセトヘキサミドの還元反応におけるケトン性薬物の抑制効果に関する研究}, volume = {16}, year = {1998} }