Department of Microbiology, Immunology and Pathology, Rocky Mountain Regional Center of Excellence for Biodefense and Emerging Infectious Diseases Research, Colorado State University, Fort Collins, CO 80523-0922, USA.
Int J Antimicrob Agents. 2011 Aug;38(2):157-9. doi: 10.1016/j.ijantimicag.2011.03.019. Epub 2011 May 18.
Burkholderia pseudomallei is an intrinsically antibiotic-resistant Category B priority pathogen and the aetiological agent of melioidosis. Treatment of B. pseudomallei infection is biphasic and lengthy in order to combat the acute and chronic phases of the disease. Acute-phase treatment preferably involves an intravenous cephalosporin (ceftazidime) or a carbapenem (imipenem or meropenem). In this study, the anti-B. pseudomallei efficacy of a new monosulfactam, BAL30072, was tested against laboratory strains 1026b and 1710b and several isogenic mutant derivatives as well as a collection of clinical and environmental B. pseudomallei strains from Thailand. More than 93% of the isolates had minimal inhibitory concentrations (MICs) in the range 0.004-0.016 μg/mL. For the laboratory strain 1026b, the MIC of BAL30072 was 0.008 μg/mL, comparable with the MICs of 1.5 μg/mL for ceftazidime, 0.5 μg/mL for imipenem and 1 μg/mL for meropenem. Time-kill curves revealed that BAL30072 was rapidly bactericidal, killing >99% of bacteria in 2 h. BAL30072 activity was not significantly affected by efflux, it was only a marginal substrate of PenA β-lactamase, and activity was independent of malleobactin production and transport and the ability to transport pyochelin. In summary, BAL30072 has superior in vitro activity against B. pseudomallei compared with ceftazidime, meropenem or imipenem and it is rapidly bactericidal.
类鼻疽伯克霍尔德菌是一种固有抗生素耐药的 B 类优先病原体,也是类鼻疽病的病原体。治疗类鼻疽伯克霍尔德菌感染需要进行两阶段且漫长的治疗,以对抗疾病的急性和慢性阶段。急性阶段的治疗最好使用静脉注射头孢菌素(头孢他啶)或碳青霉烯类药物(亚胺培南或美罗培南)。在这项研究中,测试了一种新的单磺酰胺 BAL30072 对实验室菌株 1026b 和 1710b 以及几个同源突变衍生物以及来自泰国的一组临床和环境类鼻疽伯克霍尔德菌菌株的抗类鼻疽伯克霍尔德菌疗效。超过 93%的分离株的最小抑菌浓度(MIC)在 0.004-0.016 μg/mL 范围内。对于实验室菌株 1026b,BAL30072 的 MIC 为 0.008 μg/mL,与头孢他啶的 MIC(1.5 μg/mL)、亚胺培南的 MIC(0.5 μg/mL)和美罗培南的 MIC(1 μg/mL)相当。时间杀伤曲线显示 BAL30072 具有快速杀菌作用,在 2 小时内杀死了>99%的细菌。BAL30072 的活性不受外排的显著影响,它只是 PenAβ-内酰胺酶的一个边缘底物,其活性与马勒菌素的产生和转运以及对吡咯啉的转运能力无关。总之,与头孢他啶、美罗培南或亚胺培南相比,BAL30072 对类鼻疽伯克霍尔德菌具有优越的体外活性,且具有快速杀菌作用。