COMPARATIVE IN-VITRO EXOENZYME-SUPPRESSING ACTIVITIES OF AZITHROMYCIN AND OTHER MACROLIDE ANTIBIOTICS AGAINST PSEUDOMONAS-AERUGINOSA
COMPARATIVE IN-VITRO EXOENZYME-SUPPRESSING ACTIVITIES OF AZITHROMYCIN AND OTHER MACROLIDE ANTIBIOTICS AGAINST PSEUDOMONAS-AERUGINOSA
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DOI：
10.1128/aac.38.3.528
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发表时间：
1994-03-01
影响因子：
4.9
通讯作者：
YAMAGUCHI, K
中科院分区：
文献类型：
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作者：
MIZUKANE, R;HIRAKATA, Y;YAMAGUCHI, K
测定了新的15元大环内酯类抗生素阿奇霉素(AZM)对铜绿假单胞菌产生外毒素A、总蛋白水解酶、弹性蛋白酶和磷脂酶C的抑制作用，并与红霉素(EHL)、罗红霉素(RXM)和罗吉霉素(RKM)进行了比较。测定了培养物中铜绿假单胞菌PA103或B16与这些大环内酯类抗生素亚MIC接触对外源酶产生的影响。AZM对铜绿假单胞菌PA103产生的胞外和胞内外毒素A的抑制作用强于EM，在浓度为4~32mU g/ml时，对铜绿假单胞菌B16产生的总蛋白酶、弹力酶和磷脂酶C的抑制作用强于EM、RXM和RKM。AZM能有效地抑制外毒素A和总蛋白产量，但对铜绿假单胞菌的生长和总蛋白产量无明显影响。此外，在浓度为4微克/毫升时，AZM对其他铜绿假单胞菌产生的胞外酶的抑制作用强于EM。这些结果表明，AZM、EM、RXM和RKM分别对胞外酶的产生具有抑制作用，而不是抑菌作用，并且在这些大环内酯类化合物中，AZM的毒力抑制作用最强。
The inhibitory effects of azithromycin (AZM), a new 15-membered macrolide antibiotic, on the production of exotoxin A, total protease, elastase, and phospholipase C by Pseudomonas aeruginosa were determined, and the virulence-suppressing effects of AZ?(l were compared,vith those of erythromycin (Ehl), roxithromycin (RXM), and rokitamycin (RKM). The effect of exposure of P. aeruginosa PA103 or B16 in cultures to sub-MICs of these macrolide antibiotics on the production of exoenzymes was determined. AZM suppressed the in vitro production of extracellular and intracellular exotoxin A by P. aeruginosa PA103 more than did EM, even at a concentration of only 2 mu g/ml. At concentrations of between 4 and 32 mu g/ml, AZM also inhibited total protease, elastase, and phospholipase C production by P. aeruginosa B16 more than did EM, RXM, and RKM. AZM was effective in suppressing exotoxin A and total protease production through 24 h of incubation in the presence of drug at sub-MICs, but it had no significant effect on either the growth of P. aeruginosa or its total protein production. Moreover, at a concentration of 4 mu g/ml, AZM suppressed exoenzyme production by other strains of P. aeruginosa more than did EM. These findings indicate that AZM, EM, RXM, and RKM each has an inhibitory effect on exoenzyme production separate from the antimicrobial effect and that, of these macrolides, AZM has the strongest virulence-suppressing effect.