Nagata K, Takagi E, Tsuda M, Nakazawa T, Satoh H, Nakao M, Okamura H, Tamura T
Department of Bacteriology, Hyogo College of Medicine, Japan.
Antimicrob Agents Chemother. 1995 Feb;39(2):567-70. doi: 10.1128/AAC.39.2.567.
The proton pump inhibitors omeprazole and lansoprazole and its acid-activated derivative AG-2000, which are potent and specific inhibitors of urease of Helicobacter pylori (K. Nagata, H. Satoh, T. Iwahi, T. Shimoyama, and T. Tamura, Antimicrob. Agents Chemother. 37:769-774, 1993), inhibited the growth of H. pylori. The growth was inhibited not only in urease-positive clinical isolates but also in their urease-negative derivatives which had no urease polypeptides. AG-1789, a derivative of lansoprazole with no inhibitory activity against H. pylori urease, also inhibited the growth of both strains even more strongly than the urease inhibitors lansoprazole and AG-2000. Furthermore, the antibacterial activity of omeprazole and lansoprazole was not affected by glutathione or dithiothreitol, which completely abolished the inhibitory activity of lansoprazole against H. pylori urease. These results indicated that the inhibitory action of these compounds against the growth of H. pylori was independent from the inhibitory action against urease.
质子泵抑制剂奥美拉唑和兰索拉唑及其酸活化衍生物AG - 2000是幽门螺杆菌脲酶的强效特异性抑制剂(K. Nagata、H. Satoh、T. Iwahi、T. Shimoyama和T. Tamura,《抗菌药物与化疗》37:769 - 774,1993),它们能抑制幽门螺杆菌的生长。不仅脲酶阳性的临床分离株的生长受到抑制,而且其无脲酶多肽的脲酶阴性衍生物的生长也受到抑制。AG - 1789是兰索拉唑的一种衍生物,对幽门螺杆菌脲酶无抑制活性,但它对这两种菌株生长的抑制作用甚至比脲酶抑制剂兰索拉唑和AG - 2000更强。此外,奥美拉唑和兰索拉唑的抗菌活性不受谷胱甘肽或二硫苏糖醇的影响,而这两种物质能完全消除兰索拉唑对幽门螺杆菌脲酶的抑制活性。这些结果表明,这些化合物对幽门螺杆菌生长的抑制作用与对脲酶的抑制作用无关。