Nilius M, Bode G, Lehnhardt G, Malfertheiner P
Department of Internal Medicine II, University of Ulm, Germany.
Eur J Clin Invest. 1991 Oct;21(5):551-7. doi: 10.1111/j.1365-2362.1991.tb01409.x.
Inhibition of H. pylori urease was studied by means of electron-microscopy and electrophoretic methods using different urease inhibitors, such as acetohydroxamic-acid (AHA), L-ascorbic acid (AsA), copper ions, a combination of L-ascorbic acid with copper ions and UV light. AHA in two different concentrations and AsA at a concentration of 0.1 mg ml-1 showed incomplete inhibition of H. pylori urease activity in our electrophoretic experiments. Only membrane-bound activity was inhibited with AHA but not the activity localized within the cytoplasma as demonstrated by electron-microscopy. AsA at a concentration of 0.5 mg ml-1 and the combination of copper ions (1 microgram ml-1) with AsA completely inhibited the urease activity as demonstrated by electron-microscopy and electrophoretic experiments. Cu2+ ions in high concentrations (100 micrograms ml-1) and UV light exposure for more than 4 h induced a complete disintegration of H. pylori. Electrophoresis showed no active protein after UV light exposure of 2 h. Different urease inhibitors tested in this study showed dose-dependent inhibitory effects on H. pylori urease in vitro.
采用电子显微镜和电泳方法，使用不同的尿素酶抑制剂，如乙酰氧肟酸（AHA）、L-抗坏血酸（AsA）、铜离子、L-抗坏血酸与铜离子的组合以及紫外线，研究幽门螺杆菌尿素酶的抑制作用。在我们的电泳实验中，两种不同浓度的AHA和浓度为0.1 mg/ml的AsA对幽门螺杆菌尿素酶活性表现出不完全抑制。如电子显微镜所示，AHA仅抑制膜结合活性，而不抑制细胞质内的活性。电子显微镜和电泳实验表明，浓度为0.5 mg/ml的AsA以及铜离子（1微克/毫升）与AsA的组合完全抑制了尿素酶活性。高浓度（100微克/毫升）的Cu2+离子和超过4小时的紫外线照射导致幽门螺杆菌完全解体。电泳显示，紫外线照射2小时后没有活性蛋白。本研究中测试的不同尿素酶抑制剂在体外对幽门螺杆菌尿素酶显示出剂量依赖性抑制作用。
