Department of Microbiology and Immunology, University at Buffalo, State University of New York, Buffalo, New York, United States of America.
PLoS One. 2012;7(8):e43514. doi: 10.1371/journal.pone.0043514. Epub 2012 Aug 15.
The fight against antibiotic resistance is one of the most significant challenges to public health of our time. The inevitable development of resistance following the introduction of novel antibiotics has led to an urgent need for the development of new antibacterial drugs with new mechanisms of action that are not susceptible to existing resistance mechanisms. One such compound is HAMLET, a natural complex from human milk that kills Streptococcus pneumoniae (the pneumococcus) using a mechanism different from common antibiotics and is immune to resistance-development. In this study we show that sublethal concentrations of HAMLET potentiate the effect of common antibiotics (penicillins, macrolides, and aminoglycosides) against pneumococci. Using MIC assays and short-time killing assays we dramatically reduced the concentrations of antibiotics needed to kill pneumococci, especially for antibiotic-resistant strains that in the presence of HAMLET fell into the clinically sensitive range. Using a biofilm model in vitro and nasopharyngeal colonization in vivo, a combination of HAMLET and antibiotics completely eradicated both biofilms and colonization in mice of both antibiotic-sensitive and resistant strains, something each agent alone was unable to do. HAMLET-potentiation of antibiotics was partially due to increased accessibility of antibiotics to the bacteria, but relied more on calcium import and kinase activation, the same activation pathway HAMLET uses when killing pneumococci by itself. Finally, the sensitizing effect was not confined to species sensitive to HAMLET. The HAMLET-resistant respiratory species Acinetobacter baumanii and Moraxella catarrhalis were all sensitized to various classes of antibiotics in the presence of HAMLET, activating the same mechanism as in pneumococci. Combined these results suggest the presence of a conserved HAMLET-activated pathway that circumvents antibiotic resistance in bacteria. The ability to activate this pathway may extend the lifetime of the current treatment arsenal.
对抗抗生素耐药性是当今公共卫生面临的最大挑战之一。新型抗生素引入后,耐药性的不可避免发展导致迫切需要开发具有新作用机制的新型抗菌药物,这些药物不易受到现有耐药机制的影响。HAMLET 就是这样一种化合物,它是一种来自人乳的天然复合物,通过不同于常见抗生素的机制杀死肺炎链球菌(肺炎球菌),并且不易产生耐药性。在这项研究中,我们表明亚致死浓度的 HAMLET 增强了常见抗生素(青霉素、大环内酯类和氨基糖苷类)对肺炎球菌的作用。通过 MIC 测定和短时间杀伤试验,我们大大降低了杀死肺炎球菌所需的抗生素浓度,特别是对于 HAMLET 存在下落入临床敏感范围的抗生素耐药菌株。使用体外生物膜模型和体内鼻咽定植模型,HAMLET 和抗生素的联合使用完全消除了抗生素敏感和耐药菌株在小鼠中的生物膜和定植,而每种药物单独使用都无法做到这一点。HAMLET 增强抗生素的作用部分归因于抗生素对细菌的可及性增加,但更依赖于钙内流和激酶激活,这是 HAMLET 单独杀死肺炎球菌时所使用的相同激活途径。最后,这种增敏作用不仅限于对 HAMLET 敏感的物种。在 HAMLET 存在的情况下,对 HAMLET 耐药的呼吸道物种鲍曼不动杆菌和卡他莫拉菌对各种类别的抗生素都变得敏感,激活了与肺炎球菌相同的机制。这些结果表明存在一种保守的 HAMLET 激活途径,可以绕过细菌中的抗生素耐药性。激活这种途径的能力可能会延长当前治疗武器库的使用寿命。