In vitro anti-Helicobacter pylori activity of Extractum liquiritiae, glycyrrhizin and its metabolites

被引:91
作者
Krausse, R
Bielenberg, J
Blaschek, W
Ullmann, U
机构
[1] Univ Hosp Schleswig Holstein, Inst Med Microbiol & Virol, D-24105 Kiel, Germany
[2] Raphael Pharm, Westerhorn, Germany
[3] Univ Kiel, Dept Pharmaceut Biol, Inst Pharm, D-24098 Kiel, Germany
关键词
Helicobacter; liquorice; glycyrrhetinic acid; novel derivatives;
D O I
10.1093/jac/dkh287
中图分类号
R51 [传染病];
学科分类号
100401 ;
摘要
Objectives: To investigate the in vitro activity of Extractum liquiritiae (EL), glycyrrhizic acid (GL), glycyrrhetinic acid (GA) and a novel lipophilic derivative of glycyrrhetinic acid monoglucuronide (GAMG), acetylated GAMG (aGAMG), against 29 Helicobacter pylori strains. Methods: The MIC of each compound was determined by the agar dilution method, and the killing kinetics were monitored in brain heart infusion broth (similar to10(6)-10(7) cfu/mL) at 0, 4, 24, 48, 72 and 96 h. Results: GA was the most potent compound (MIC50 /90, 50/100 mg/L), inhibiting 79.3% of the strains at MIC less than or equal to50 mg/L. Clarithromycin-resistant strains were susceptible at 12.5 and 25 mg/L, and metronidazole-resistant strains at 25-50 and at 200 mg/L. The MIC distribution (mg/L) of aGAMG was less than or equal to6.25 (29.2%), 50 (4.2%), 100-200 (12.5%) and greater than or equal to400 (54.1%). EL and GL were less active (MICs >400 mg/L). GA exhibited rapid, concentration and strain-dependent bactericidal activity. Conclusions: The potent in vitro activity of GA against H. pylori provides a further explanation for its beneficial effect on peptic ulcers. Its effectiveness against clarithromycin-resistant strains provides hope that it can form the basis for an alternative therapeutic agent against H. pylori.
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页码:243 / 246
页数:4
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