Department of Internal Medicine, Chung-Ang University Hospital, Chung-Ang University College of Medicine, Seoul, Korea.
Gut Liver. 2013 Nov;7(6):655-60. doi: 10.5009/gnl.2013.7.6.655. Epub 2013 Aug 14.
BACKGROUND/AIMS: A worldwide increase in amoxicillin resistance in Helicobacter pylori is having an adverse effect on eradication therapy. In this study, we investigated the mechanism of the amoxicillin resistance of H. pylori in terms of amino acid substitutions in penicillin-binding protein 1 (PBP1).
In total, 150 H. pylori strains were isolated from 144 patients with chronic gastritis, peptic ulcers, or stomach cancer. The minimum inhibitory concentrations (MICs) of the strains were determined with a serial 2-fold agar dilution method. The resistance breakpoint for amoxicillin was defined as >0.5 µg/mL.
Nine of 150 H. pylori strains showed amoxicillin resistance (6%). The MIC values of the resistant strains ranged from 1 to 4 µg/mL. A PBP1 sequence analysis of the resistant strains revealed multiple amino acid substitutions: Val16→Ile, Val45→Ile, Ser414→Arg, Asn562→Tyr, Thr593→Ala, Gly595→Ser, and Ala599→Thr. The natural transformation of these mutated genes into amoxicillin-sensitive strains was performed in two separate pbp1 gene segments. A moderate increase in the amoxicillin MIC was observed in the segment that contained the penicillin-binding motif of the C-terminal portion, the transpeptidase domain.
pbp1 mutation affects the amoxicillin resistance of H. pylori through the transfer of the penicillin-binding motif.
背景/目的:全球范围内幽门螺杆菌对阿莫西林的耐药性不断增加,对根除治疗产生了不良影响。本研究旨在从青霉素结合蛋白 1(PBP1)的氨基酸取代角度探讨幽门螺杆菌阿莫西林耐药的机制。
共从 144 例慢性胃炎、消化性溃疡和胃癌患者中分离出 150 株幽门螺杆菌。采用倍比琼脂稀释法测定菌株的最小抑菌浓度(MIC)。阿莫西林耐药的折点定义为>0.5μg/ml。
150 株幽门螺杆菌中有 9 株(6%)表现出阿莫西林耐药性。耐药株的 MIC 值范围为 1-4μg/ml。耐药株 PBP1 序列分析显示多个氨基酸取代:Val16→Ile、Val45→Ile、Ser414→Arg、Asn562→Tyr、Thr593→Ala、Gly595→Ser 和 Ala599→Thr。将这些突变基因自然转化为阿莫西林敏感株,分别在两个单独的 pbp1 基因片段中进行。在含有 C 端青霉素结合基序和转肽酶结构域的片段中,阿莫西林 MIC 值中度增加。
pbp1 突变通过转移青霉素结合基序影响幽门螺杆菌的阿莫西林耐药性。