Citron Diane M, Warren Yumi A, Tyrrell Kerin L, Merriam Vreni, Goldstein Ellie J C
R. M. Alden Research Laboratory, Culver City, CA 90230, USA.
J Antimicrob Chemother. 2009 May;63(5):972-6. doi: 10.1093/jac/dkp037. Epub 2009 Feb 24.
The aim of this study was to determine the anaerobic spectrum of activity of REP3123, a novel diaryldiamine that inhibits bacterial methionyl-tRNA synthetases in Gram-positive bacteria.
Fifty recent clinical isolates of Clostridium difficile from patients diagnosed with C. difficile infection and 223 other intestinal normal flora anaerobes were tested for their susceptibility to REP3123 and four or five comparator agents by the agar dilution method using supplemented Brucella agar with 5% laked sheep blood.
All strains of C. difficile were inhibited by 0.5-1 mg/L REP3123, including those resistant to moxifloxacin and clindamycin. REP3123 lacked activity against many normal flora anaerobes in the gut, including Clostridium ramosum, bifidobacteria, lactobacilli of the Lactobacillus casei-rhamnosus-plantarum group and Gram-negative anaerobes.
REP3123 demonstrated good potency against C. difficile, but limited activity against many other intestinal anaerobic species, thus, in theory, maintaining the colonization resistance barrier.
本研究旨在确定REP3123（一种新型二芳基二胺，可抑制革兰氏阳性菌中的细菌甲硫氨酰 - tRNA合成酶）的厌氧活性谱。
采用添加5%脱纤维羊血的布氏琼脂，通过琼脂稀释法，对50株近期从诊断为艰难梭菌感染的患者中分离出的艰难梭菌临床菌株以及223株其他肠道正常菌群厌氧菌进行了对REP3123和四或五种对照药物的敏感性测试。
所有艰难梭菌菌株均被0.5 - 1 mg/L的REP3123抑制，包括那些对莫西沙星和克林霉素耐药的菌株。REP3123对肠道中的许多正常菌群厌氧菌缺乏活性，包括多枝梭菌、双歧杆菌、干酪乳杆菌 - 鼠李糖乳杆菌 - 植物乳杆菌组的乳杆菌以及革兰氏阴性厌氧菌。
REP3123对艰难梭菌显示出良好的效力，但对许多其他肠道厌氧菌种的活性有限，因此，从理论上讲，维持了定植抗性屏障。
