Koga T, Kawada H, Utsui Y, Domon H, Ishii C, Yasuda H
Biological Research Laboratories, Sankyo Co., Ltd, Tokyo, Japan.
J Antimicrob Chemother. 1996 May;37(5):919-29. doi: 10.1093/jac/37.5.919.
Recently, some antiulcer agents have been reported to have antibacterial activity against Helicobacter pylori, which is highly associated with gastritis and peptic ulcers. In-vitro and in-vivo activity of plaunotol, a cytoprotective antiulcer agent, against H. pylori was investigated. Antibacterial activity of plaunotol against a standard strain (NCTC 11637) and 14 clinical isolates was compared with those of other cytoprotective antiulcer agents: benexate, sofalcone, teprenone, cetraxate, and gefarnate, by an agar dilution method. The MIC50 and MIC90 of plaunotol against 15 strains were 6.25 and 12.5 mg/L, respectively, making it the most potent of the cytoprotective antiulcer agents. The bactericidal effect of plaunotol was investigated using an in-vitro killing assay. Plaunotol at concentrations of more than 6 mg/L induced a rapid reduction of culture turbidity, with an extensive loss of viability, within 30 min. Observation by scanning electron microscopy revealed that plaunotol caused autolysis and treated cells were deformed. In-vivo activity of plaunotol against H. pylori was examined in a nude mouse gastritis model. Plaunotol significantly decreased the number of H. pylori in the stomach of nude mice. In addition, the antiulcer agent enhanced the antibacterial activity of amoxycillin or clarithromycin in the infection model.
最近，有报道称一些抗溃疡药物对幽门螺杆菌具有抗菌活性，而幽门螺杆菌与胃炎和消化性溃疡高度相关。对具有细胞保护作用的抗溃疡药物普劳诺托针对幽门螺杆菌的体外和体内活性进行了研究。通过琼脂稀释法，将普劳诺托对标准菌株（NCTC 11637）和14株临床分离株的抗菌活性与其他具有细胞保护作用的抗溃疡药物：贝奈酯、索法酮、替普瑞酮、西曲酸酯和吉法酯进行了比较。普劳诺托对15株菌株的MIC50和MIC90分别为6.25和12.5 mg/L，使其成为最有效的具有细胞保护作用的抗溃疡药物。使用体外杀菌试验研究了普劳诺托的杀菌效果。浓度超过6 mg/L的普劳诺托在30分钟内导致培养物浊度迅速降低，活力大量丧失。扫描电子显微镜观察显示，普劳诺托导致自溶，处理后的细胞变形。在裸鼠胃炎模型中检测了普劳诺托对幽门螺杆菌的体内活性。普劳诺托显著降低了裸鼠胃中幽门螺杆菌的数量。此外，在感染模型中，该抗溃疡药物增强了阿莫西林或克拉霉素的抗菌活性。
