Sox T E, Olson C A
Sharon Woods Technical Center, Procter and Gamble Company, Cincinnati, Ohio 45241.
Antimicrob Agents Chemother. 1989 Dec;33(12):2075-82. doi: 10.1128/AAC.33.12.2075.
Bismuth subsalicylate (BSS) is a compound without significant aqueous solubility that is widely used for the treatment of gastrointestinal disorders. BSS was able to bind bacteria of diverse species, and these bound bacteria were subsequently killed. A 4-log10 reduction of viable bacteria occurred within 4 h after a 10 mM aqueous suspension of BSS was inoculated with 2 x 10(6) Escherichia coli cells per ml. Binding and killing were dependent on the levels of inoculated bacteria, and significant binding but little killing of the exposed bacteria occurred at an inoculum level of 2 x 10(9) E. coli per ml. Intracellular ATP decreased rapidly after exposure of E. coli to 10 mM BSS and, after 30 min, was only 1% of the original level. Extracellular ATP increased after exposure to BSS, but the accumulation of extracellular ATP was not sufficient to account for the loss of intracellular ATP. The killing of bacteria exposed to BSS may have been due to cessation of ATP synthesis or a loss of membrane integrity. Bactericidal activity of BSS was also investigated in a simulated gastric juice at pH 3. Killing of E. coli at this pH was much more rapid than at pH 7 and was apparently due to salicylate released by the conversion of BSS to bismuth oxychloride. It is proposed that the binding and killing observed for BSS contribute to the efficacy of this compound against gastrointestinal infections such as traveler's diarrhea.
碱式水杨酸铋（BSS）是一种水溶性不佳的化合物，广泛用于治疗胃肠道疾病。BSS能够结合多种细菌，这些被结合的细菌随后会被杀死。在每毫升接种2×10⁶个大肠杆菌细胞的10 mM BSS水悬浮液接种后4小时内，活菌数量减少了4个对数级。结合和杀灭作用取决于接种细菌的数量，在每毫升接种2×10⁹个大肠杆菌的接种水平下，暴露细菌发生了显著的结合但几乎没有杀灭。大肠杆菌暴露于10 mM BSS后，细胞内ATP迅速下降，30分钟后仅为原始水平的1%。暴露于BSS后细胞外ATP增加，但细胞外ATP的积累不足以解释细胞内ATP的损失。暴露于BSS的细菌的杀灭可能是由于ATP合成停止或膜完整性丧失。还在pH 3的模拟胃液中研究了BSS的杀菌活性。在该pH值下大肠杆菌的杀灭比在pH 7时快得多，显然是由于BSS转化为氯氧化铋释放出的水杨酸盐所致。有人提出，观察到的BSS的结合和杀灭作用有助于该化合物对诸如旅行者腹泻等胃肠道感染的疗效。
