【摘要】 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。更多还原

【Abstract】 As a noncompetitive inhibitor of pig gastric H+/K+-ATPase, indomethacin inhibited the H+ transportation function of the enzyme, leading to not only the obvious dissipation of H+/K+-ATPase-gene-rated H+ gradients, but also the deceasing of the H+ gradient formation ability of the enzyme. 4% of indomethacin was able to penetrate into the lipid bilayer of H+/ K+-ATPase vesicles at 0.15mg/ml protein concentration, which showed an influence of indomethacin to the membrane. Indome-thacin reduced the membrane fluidity of H+/K+-ATPase vesicles significantly. It also damaged the conformation of membrane protein extraordinarily, which was evidenced by decreasing the intrinsic fluorescence of H+/K+-ATPase. From the results, we suggest that the effect of indomethacin on H+/K+-ATPase is taken place by its inhibition on H+/K+-ATPase protein, as well as by its influence on the membrane lipid bilayer of H+/K+-ATPase vesicles.更多还原