Iwahi T, Satoh H, Nakao M, Iwasaki T, Yamazaki T, Kubo K, Tamura T, Imada A
Research and Development Division, Takeda Chemical Industries, Ltd., Osaka, Japan.
Antimicrob Agents Chemother. 1991 Mar;35(3):490-6. doi: 10.1128/AAC.35.3.490.
The activities of various types of antiulcer agents against Helicobacter pylori (formerly called Campylobacter pylori) strains were determined by an agar dilution method. Among the compounds tested, two benzimidazole proton pump inhibitors, lansoprazole (AG-1749) and omeprazole, were found to have significant activities against this organism. The activity of lansoprazole was comparable to that of bismuth citrate, with MICs ranging from 3.13 to 12.5 micrograms/ml, and fourfold more potent than that of omeprazole. A major metabolite and two acid-converted rearrangement products of lansoprazole also exhibited good activities comparable or superior to that of the parent compound. Exposure to lansoprazole of H. pylori growing in a liquid medium led to an extensive loss of viability without a reduction in culture turbidity and produced an aberrant bacterial morphology characterized by the irregular constriction of cells and the collapse of cell surface structures. The antibacterial activity of lansoprazole and its related compounds was selective against H. pylori; common aerobic and anaerobic bacteria and Campylobacter jejuni were not inhibited by 100 micrograms/ml.
采用琼脂稀释法测定了各类抗溃疡药物对幽门螺杆菌（原称幽门弯曲菌）菌株的活性。在所测试的化合物中，发现两种苯并咪唑质子泵抑制剂，兰索拉唑（AG - 1749）和奥美拉唑，对该菌具有显著活性。兰索拉唑的活性与枸橼酸铋相当，最低抑菌浓度（MIC）范围为3.13至12.5微克/毫升，比奥美拉唑强四倍。兰索拉唑的一种主要代谢产物和两种酸转化重排产物也表现出良好的活性，与母体化合物相当或更优。在液体培养基中生长的幽门螺杆菌暴露于兰索拉唑后，导致活力大幅丧失，但培养物浊度未降低，并产生异常的细菌形态，其特征为细胞不规则收缩和细胞表面结构塌陷。兰索拉唑及其相关化合物的抗菌活性对幽门螺杆菌具有选择性；普通需氧菌、厌氧菌和空肠弯曲菌在100微克/毫升浓度下未受抑制。
