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首页> 外文期刊>Antimicrobial agents and chemotherapy. >In Vitro and In Vivo Activities of Tigecycline (GAR-936), Daptomycin, and Comparative Antimicrobial Agents against Glycopeptide-Intermediate Staphylococcus aureus and Other Resistant Gram-Positive Pathogens.
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In Vitro and In Vivo Activities of Tigecycline (GAR-936), Daptomycin, and Comparative Antimicrobial Agents against Glycopeptide-Intermediate Staphylococcus aureus and Other Resistant Gram-Positive Pathogens.

机译：替加环素（GAR-936），达托霉素和比较抗微生物剂对糖肽中间性金黄色葡萄球菌和其他抗革兰氏阳性病原菌的体外和体内活性。

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Tigecycline (GAR-936) and daptomycin are potent antibacterial compounds in advanced stages of clinical trials. These novel agents target multiply resistant pathogenic bacteria. Daptomycin is principally active against gram-positive bacteria, while tigecycline has broad-spectrum activity. When tested by the standard protocols of the National Committee for Clinical Laboratory Standards in Mueller-Hinton broth II, tigecycline was more active than daptomycin (MICs at which 90% of isolates tested are inhibited, 0.12 to 1 and 0.5 to 16 microg/ml, respectively) against staphylococcal, enterococcal, and streptococcal pathogens. Daptomycin demonstrated a stepwise increase in activity corresponding to an increase in the supplemental concentration of calcium. When tested in base Mueller-Hinton broth supplemented with 50 mg of calcium per liter, daptomycin demonstrated improved activity (MIC(90)s, 0.015 to 4 microg/ml). The activity of daptomycin, however, equaled that of tigecycline against the glycopeptide-intermediate Staphylococcus aureus (GISA) strains only when the test medium was supplemented with excess calcium (75 mg/liter). Tigecycline and daptomycin demonstrated in vivo efficacies against GISA, methicillin-resistant S. aureus, and methicillin-susceptible S. aureus strains in an intraperitoneal systemic murine infection model. These data suggest that tigecycline and daptomycin may offer therapeutic options against clinically relevant resistant pathogens for which current alternatives for treatment are limited.
机译：Tigecycline（GAR-936）和达托霉素在临床试验的晚期阶段是有效的抗菌化合物。这些新型药物靶向多重耐药病原菌。达托霉素主要对革兰氏阳性细菌具有活性，而替加环素具有广谱活性。当根据国家临床实验室标准委员会的标准规程在Mueller-Hinton肉汤II中进行测试时，替加环素比达托霉素具有更高的活性（MIC抑制了90％的分离株，分别为0.12和1和0.5至16微克/毫升，分别针对葡萄球菌，肠球菌和链球菌病原体。达托霉素表现出逐步增加的活性，对应于钙的补充浓度的增加。当在每升补充50 mg钙的基础Mueller-Hinton肉汤中进行测试时，达托霉素显示出更高的活性（MIC（90）s，0.015至4 microg / ml）。但是，达托霉素对糖中间肽金黄色葡萄球菌（GISA）菌株的活性相当于替加环素，仅当测试培养基中添加了过量的钙（75 mg / l）时才如此。 Tigecycline和达托霉素在腹膜内全身鼠感染模型中证明了对GISA，耐甲氧西林金黄色葡萄球菌和耐甲氧西林金黄色葡萄球菌菌株的体内功效。这些数据表明，替加环素和达托霉素可提供针对临床相关耐药性病原体的治疗选择，而目前针对这些病原体的替代治疗方法受到限制。

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