Inhibition of Streptococcus mutans biofilm formation, extracellular polysaccharide production, and virulence by an oxazole derivative
Inhibition of Streptococcus mutans biofilm formation, extracellular polysaccharide production, and virulence by an oxazole derivative
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恶唑衍生物抑制变形链球菌生物膜形成、胞外多糖产生和毒力
DOI：
10.1007/s00253-015-7092-1
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发表时间：
2016-01-01
影响因子：
5
通讯作者：
Li, Yuqing
中科院分区：
文献类型：
--
作者：
Chen, Lulu;Ren, Zhi;Li, Yuqing
龋齿是一种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（Streptococcus mutans）是主要的致龋菌之一，其产生合成胞外多糖（EPS）的葡糖基转移酶（Gtfs）。EPS，尤其是水不溶性葡聚糖，通过允许细菌粘附在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、生物膜稳定性和结构完整性。需要确定新的替代品，选择性地抑制致龋生物，而不抑制口腔微生物居民。本研究的目的是探讨恶唑衍生物对S。由于恶唑及其衍生物通常表现出广泛和重要的生物活性，因此，恶唑及其衍生物对大鼠中变形杆菌生物膜的形成和龋齿的发展具有重要的作用。我们的数据表明，一种特殊的恶唑衍生物，命名为5H6，抑制S的形成。在体外，通过拮抗Gtfs，在不影响细菌生长的情况下，变形杆菌生物膜和阻止胞外多糖的合成。此外，局部应用该抑制剂可降低体内光滑面和沟面龋的发生率和严重程度，并降低S。与对照组相比，实验组大鼠牙菌斑中的变形杆菌含量显著降低（P < 0.05）。我们的研究结果表明，这种恶唑衍生物具有抑制生物膜形成和致龋性的能力。变异人
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.