Oral Health CRC, Melbourne Dental School, Bio21 Institute, The University of Melbourne, Melbourne, Victoria, Australia.
Antimicrob Agents Chemother. 2014;58(1):378-85. doi: 10.1128/AAC.01375-13. Epub 2013 Oct 28.
Bacterial pathogens commonly associated with chronic periodontitis are the spirochete Treponema denticola and the Gram-negative, proteolytic species Porphyromonas gingivalis and Tannerella forsythia. These species rely on complex anaerobic respiration of amino acids, and the anthelmintic drug oxantel has been shown to inhibit fumarate reductase (Frd) activity in some pathogenic bacteria and inhibit P. gingivalis homotypic biofilm formation. Here, we demonstrate that oxantel inhibited P. gingivalis Frd activity with a 50% inhibitory concentration (IC50) of 2.2 μM and planktonic growth of T. forsythia with a MIC of 295 μM, but it had no effect on the growth of T. denticola. Oxantel treatment caused the downregulation of six P. gingivalis gene products and the upregulation of 22 gene products. All of these genes are part of a regulon controlled by heme availability. There was no large-scale change in the expression of genes encoding metabolic enzymes, indicating that P. gingivalis may be unable to overcome Frd inhibition. Oxantel disrupted the development of polymicrobial biofilms composed of P. gingivalis, T. forsythia, and T. denticola in a concentration-dependent manner. In these biofilms, all three species were inhibited to a similar degree, demonstrating the synergistic nature of biofilm formation by these species and the dependence of T. denticola on the other two species. In a murine alveolar bone loss model of periodontitis oxantel addition to the drinking water of P. gingivalis-infected mice reduced bone loss to the same level as the uninfected control.
与慢性牙周炎相关的常见细菌病原体是螺旋体密螺旋体和革兰氏阴性、蛋白水解物种牙龈卟啉单胞菌和坦纳拉福赛思菌。这些物种依赖于氨基酸的复杂无氧呼吸,驱虫药奥沙苯达唑已被证明可抑制一些病原菌的延胡索酸还原酶(Frd)活性,并抑制牙龈卟啉单胞菌同型生物膜形成。在这里,我们证明奥沙苯达唑抑制牙龈卟啉单胞菌 Frd 活性的 50%抑制浓度(IC50)为 2.2 μM,抑制坦纳拉福赛思菌浮游生长的最小抑菌浓度(MIC)为 295 μM,但对密螺旋体的生长没有影响。奥沙苯达唑处理导致 6 种牙龈卟啉单胞菌基因产物的下调和 22 种基因产物的上调。所有这些基因都是血红素可用性调控的一个调控子的一部分。编码代谢酶的基因表达没有发生大规模变化,表明牙龈卟啉单胞菌可能无法克服 Frd 抑制。奥沙苯达唑以浓度依赖的方式破坏了由牙龈卟啉单胞菌、坦纳拉福赛思菌和密螺旋体组成的多微生物生物膜的发育。在这些生物膜中,所有三种物种都受到相似程度的抑制,这表明这些物种生物膜形成的协同性质以及密螺旋体对其他两种物种的依赖性。在牙周炎的小鼠牙槽骨丢失模型中,奥沙苯达唑添加到感染牙龈卟啉单胞菌的小鼠饮用水中,可将骨丢失减少到与未感染对照组相同的水平。