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索利霉素(CEM-101)的抗菌特性:一种新型氟酮内酯类药物对葡萄球菌和肠球菌的活性。

Antimicrobial characterisation of solithromycin (CEM-101), a novel fluoroketolide: activity against staphylococci and enterococci.

机构信息

JMI Laboratories, 345 Beaver Kreek Centre, Suite A, North Liberty, IA 52317, USA.

出版信息

Int J Antimicrob Agents. 2011 Jan;37(1):39-45. doi: 10.1016/j.ijantimicag.2010.08.021.

DOI:10.1016/j.ijantimicag.2010.08.021
PMID:21075602
Abstract

Solithromycin (CEM-101) is a novel fluoroketolide with high potency against Gram-positive and Gram-negative bacteria commonly associated with community-acquired respiratory tract infections and skin and skin-structure infections. In this study, solithromycin and comparator antimicrobials were tested against a contemporary collection of Staphylococcus aureus, coagulase-negative staphylococci, Enterococcus faecalis, Enterococcus faecium and other Enterococcus spp. collected in the SENTRY Antimicrobial Surveillance Program. Solithromycin was active against S. aureus [minimum inhibitory concentration for 50% of the organisms (MIC(50))=0.12 μg/mL] and was two-fold more active than telithromycin (MIC(50)=0.25 μg/mL). Solithromycin was more potent against methicillin (oxacillin)-susceptible S. aureus [MIC(50)=0.06 μg/mL and MIC for 90% of the organisms (MIC(90))=0.12 μg/mL) compared with methicillin (oxacillin)-resistant S. aureus (MIC(50)=0.12 μg/mL and MIC(90)>16 μg/mL). Solithromycin activity was reduced amongst heterogeneous vancomycin-intermediate S. aureus and vancomycin-resistant S. aureus (MIC(50)>16 μg/mL). Against strains with defined susceptibilities to erythromycin, clindamycin and telithromycin, solithromycin showed potent inhibition against all combinations (MIC(50)=0.06 μg/mL) except those with non-susceptibility to telithromycin (>2 μg/mL) (MIC(50)>16 μg/mL). The solithromycin MIC(50) for E. faecium (1 μg/mL) was four-fold higher than the MIC(50) for E. faecalis (0.25 μg/mL). In summary, solithromycin demonstrated high potency against many Staphylococcus and Enterococcus spp. isolated from contemporary infections worldwide.

摘要

索利霉素(CEM-101)是一种新型氟酮内酯,对革兰氏阳性和革兰氏阴性细菌具有高度活性,这些细菌通常与社区获得性呼吸道感染和皮肤及皮肤结构感染有关。在这项研究中,索利霉素和对照抗菌药物对 SENTRY 抗菌监测计划中收集的当代金黄色葡萄球菌、凝固酶阴性葡萄球菌、粪肠球菌、屎肠球菌和其他肠球菌属的分离株进行了测试。索利霉素对金黄色葡萄球菌具有活性[对 50%的微生物的最小抑菌浓度(MIC50)为 0.12μg/ml],比泰利霉素(MIC50)更具活性(0.25μg/ml)。与耐甲氧西林(苯唑西林)金黄色葡萄球菌(MIC50=0.12μg/ml,MIC90>16μg/ml)相比,索利霉素对甲氧西林(苯唑西林)敏感的金黄色葡萄球菌(MIC50=0.06μg/ml,MIC90=0.12μg/ml)的活性更强。异质性万古霉素中介金黄色葡萄球菌和万古霉素耐药金黄色葡萄球菌(MIC50>16μg/ml)的索利霉素活性降低。对于对红霉素、克林霉素和泰利霉素具有明确敏感性的菌株,索利霉素对所有组合均显示出强大的抑制作用(MIC50=0.06μg/ml),除了对泰利霉素(>2μg/ml)不敏感的组合(MIC50>16μg/ml)之外。粪肠球菌的索利霉素 MIC50(1μg/ml)是屎肠球菌的 MIC50(0.25μg/ml)的四倍。总的来说,索利霉素对来自全球当代感染的许多金黄色葡萄球菌和肠球菌属表现出高度的活性。

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