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作为猪胃H~+/K~+-ATPase的非竞争性抑制剂,消炎痛明显抑制H~+/K~+-ATPase泡囊的质子转运功能,造成质子泄漏。在0.15 mg/ml蛋白浓度下,4%的消炎痛结合于H~+/K~+-A- TPase泡囊上。它能渗入膜脂相并显著降低膜的流动性,并使H~+/K~+-ATPase内源荧光受到淬灭。从实验结果看来,消炎痛对猪胃H~+/K~+-ATPase质子转运功能的抑制来自对酶蛋白和膜结构影响两个方面,而非仅抑制酶蛋白本身的功能。
As a noncompetitive inhibitor of H ~ + / K ~ + -ATPase in porcine stomach, indomethacin obviously inhibited the proton transport function of H ~ + / K ~ + -ATPase vesicles and caused proton leakage. At a 0.15 mg / ml protein concentration, 4% of indomethacin binds to the H ~ + / K ~ + -A-TPase vesicles. It can penetrate into the membrane lipid phase and significantly reduce the membrane fluidity and quench the endogenous fluorescence of H ~ + / K ~ + -ATPase. It seems from the experimental results, indomethacin on pig stomach H ~ + / K ~ + -ATPase proton transport function inhibition from the two aspects of the enzyme protein and membrane structure, rather than just inhibit the enzyme protein itself.