- 期刊
Semicarbazide-sensitive Amine Oxidase Inhibitory Activity of Galacturonic Acid Hydroxamate
半乳糖醛酸羥肟酸具有抑制semicarbazide-敏感型胺酶活性
摘要
文獻報導，semicarbazide-敏感型胺酶(SSAO)在糖尿病患與心臟受損病患的血漿中有增加。SSAO催化氧化去胺反應，過程中產生過氧化氫，可能是細胞內產生氧化逆境來源之一。本研究發現，合成物之半乳糖醛酸羥肟酸(galA-nHOH)，而非原料之半乳糖醛酸，具有有效且濃度相關抑制商品化牛血漿或豬血漿來源之SSAO，抑制SSAO活性一半所需濃度分別為0.041及0.018 mM。利用電泳膠體活性染色技術，也顯示半乳糖醛酸羥肟酸抑制商品化來源之SSAO活性。半乳糖醛酸羥肟酸在0.03mM濃度下抑制牛血漿來源之SSAO之動力學研究，發現其V'(下標 max)及K'(下標m)數值都明顯降低。顯示半乳糖醛酸羥肟酸為混合型非競爭型抑制(mixed noncompetitive inhibition)，其競爭對象為SSAO反應基質與SSAO-基質複合體。
並列摘要
In the literature, semicarbazide-sensitive amine oxidase (SSAO) in plasma was elevated in diabetes mellitus and heart failure. SSAO catalyzed the oxidative deamination of various amines to produce hydrogen peroxide, which is one possible source of oxidative stresses. In this research, galacturonic acid hydroxamate (GalA-NHOH), but not GalA, effectively inhibited SSAO activities from bovine plasma and porcine plasma in a dose-dependent manner, and the IC50 values were 0.041 and 0.018 mM, respectively. The SSAO activities from bovine plasma and pig plasma were confirmed by the SSAO specific inhibitor of semicarbazide. Using AO activity staining in the 7.5% native-PAGE gels, it was also revealed that GalA-NHOH had inhibitory activities against SSAO from bovine plasma. GalA-NHOH showed mixed noncompetitive inhibition against bovine SSAO in respect to benzylamine (substrate) and benzylamine-SSAO (substrate-enzyme complex). It was found that the V'(subscript max) and K'(subscript m) values were reduced in the presence of GalA-NHOH (0.03 mM).
延伸閱讀
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