Chen Lulu, Ren Zhi, Zhou Xuedong, Zeng Jumei, Zou Jing, Li Yuqing
State Key Laboratory of Oral Diseases, West China Hospital of Stomatology, Sichuan University, Chengdu, 610041, People's Republic of China.
Department of Pediatric Dentistry, West China Hospital of Stomatology, Sichuan University, Chengdu, People's Republic of China.
Appl Microbiol Biotechnol. 2016 Jan;100(2):857-67. doi: 10.1007/s00253-015-7092-1. Epub 2015 Nov 3.
Dental caries, a biofilm-related oral disease, is a result of disruption of the microbial ecological balance in the oral environment. Streptococcus mutans, which is one of the primary cariogenic bacteria, produces glucosyltransferases (Gtfs) that synthesize extracellular polysaccharides (EPSs). The EPSs, especially water-insoluble glucans, contribute to the formation of dental plaque, biofilm stability, and structural integrity, by allowing bacteria to adhere to tooth surfaces and supplying the bacteria with protection against noxious stimuli and other environmental attacks. The identification of novel alternatives that selectively inhibit cariogenic organisms without suppressing oral microbial residents is required. The goal of the current study is to investigate the influence of an oxazole derivative on S. mutans biofilm formation and the development of dental caries in rats, given that oxazole and its derivatives often exhibit extensive and pharmacologically important biological activities. Our data shows that one particular oxazole derivative, named 5H6, inhibited the formation of S. mutans biofilms and prevented synthesis of extracellular polysaccharides by antagonizing Gtfs in vitro, without affecting the growth of the bacteria. In addition, topical applications with the inhibitor resulted in diminished incidence and severity of both smooth and sulcal surface caries in vivo with a lower percentage of S. mutans in the animals' dental plaque compared to the control group (P < 0.05). Our results showed that this oxazole derivative has the capacity to inhibit biofilm formation and cariogenicity of S. mutans.
龋齿是一种与生物膜相关的口腔疾病,是口腔环境中微生物生态平衡被破坏的结果。变形链球菌是主要的致龋菌之一,它产生合成细胞外多糖(EPSs)的葡糖基转移酶(Gtfs)。EPSs,尤其是水不溶性葡聚糖,通过使细菌黏附于牙齿表面并为细菌提供免受有害刺激和其他环境攻击的保护,有助于牙菌斑的形成、生物膜的稳定性和结构完整性。需要鉴定出能选择性抑制致龋生物而不抑制口腔常驻微生物的新型替代物。鉴于恶唑及其衍生物通常表现出广泛且具有药理学重要性的生物活性,本研究的目的是调查一种恶唑衍生物对变形链球菌生物膜形成及大鼠龋齿发展的影响。我们的数据表明,一种名为5H6的特定恶唑衍生物在体外通过拮抗Gtfs抑制了变形链球菌生物膜的形成并阻止了细胞外多糖的合成,而不影响细菌的生长。此外,与对照组相比,用该抑制剂进行局部应用导致体内光滑面和沟裂面龋齿的发生率和严重程度降低,动物牙菌斑中变形链球菌的百分比更低(P < 0.05)。我们的结果表明,这种恶唑衍生物具有抑制变形链球菌生物膜形成和致龋性的能力。