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首页> 外文期刊>The Journal of Antibiotics: An International Journal >In vitro and in vivo antimicrobial activity of TS2037, a novel aminoglycoside antibiotic
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In vitro and in vivo antimicrobial activity of TS2037, a novel aminoglycoside antibiotic

机译：体外和体内抗菌活性Ts2037，一种新型氨基糖苷类抗生素

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摘要

To overcome serious methicillin-resistant Staphylococcus aureus (MRSA) and Pseudomonas aeruginosa infections, we synthesized TS2037, 5,4 ''-diepi-arbekacin, a novel aminoglycoside antibiotic, and evaluated its biological properties. TS2037 showed broad-range, as well as robust antibacterial activities against Gram-positive and Gram-negative bacteria. The MIC50 and MIC90 of TS2037 against clinical isolates of MRSA (n = 54) were both 0.25 mu g/mL, and no resistant strain was observed. The MIC50 and MIC90 of TS2037 against clinical isolates of P. aeruginosa (n = 54) were 1 and 4 mu g/mL, respectively. TS2037 and arbekacin, anti-MRSA aminoglycoside, were more stable against AAC(6')-APH(2 ''), aminoglycoside-6'-N-acetyltransferase and 2 ''-O-phosphotransferase, produced by resistant S. aureus than gentamicin. Therapeutic efficacies of TS2037 in the mouse models of systemic infection with MRSA were superior to those of arbekacin, vancomycin, and linezolid. The efficacy of TS2037 against systemic infection caused by P. aeruginosa producing AAC(6')-II was superior to those of arbekacin and amikacin. In the nephrotoxicity risk screening, the release of free N-acetyl-beta-D-glucosaminidase from the kidney epithelial cell line after treatment with TS2037 at 2.5 and 5.0 mu M were 2.0 and 2.1 (U/L), respectively, which were about two times higher than those of arbekacin. In conclusion, TS2037 exhibited the most potent antibacterial activity among aminoglycosides tested against both MRSA and P. aeruginosa in vitro and in vivo, although its nephrotoxicity risk remains to be improved.
机译：为了克服严重的耐甲氧西林金黄色葡萄球菌（MRSA）和铜绿假单胞菌感染，我们合成了新型氨基糖苷类抗生素TS2037，5,4'-diepi arbekacin，并对其生物学特性进行了评估。TS2037对革兰氏阳性和革兰氏阴性细菌具有广泛的抗菌活性。TS2037对临床分离的MRSA（n=54）的MIC50和MIC90均为0.25μg/mL，未观察到耐药菌株。TS2037对临床分离的铜绿假单胞菌（n=54）的MIC50和MIC90分别为1和4μg/mL。抗MRSA氨基糖苷类药物TS2037和阿贝卡星对耐药金黄色葡萄球菌产生的AAC（6’）-APH（2’）、氨基糖苷-6’-N-乙酰转移酶和2’-O-磷酸转移酶比庆大霉素更稳定。TS2037在MRSA全身感染小鼠模型中的治疗效果优于阿贝卡星、万古霉素和利奈唑胺。TS2037对产生AAC（6’-II）的铜绿假单胞菌引起的全身感染的疗效优于阿贝卡星和阿米卡星。在肾毒性风险筛查中，经2.5和5.0μM的TS2037处理后，肾上皮细胞系释放的游离N-乙酰-β-D-氨基葡萄糖苷酶分别为2.0和2.1（U/L），约为阿贝卡星的两倍。总之，TS2037在体外和体内抗MRSA和铜绿假单胞菌的氨基糖苷类药物中表现出最强的抗菌活性，尽管其肾毒性风险仍有待提高。

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