Inhibition of Streptococcus mutans Biofilms by the Natural Stilbene Piceatannol Through the Inhibition of Glucosyltransferases.
Inhibition of Streptococcus mutans Biofilms by the Natural Stilbene Piceatannol Through the Inhibition of Glucosyltransferases.
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DOI：
10.1021/acsomega.8b00367
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发表时间：
2018-07-31
期刊：
影响因子：
4.1
通讯作者：
Velu SE
中科院分区：
文献类型：
--
作者：
Nijampatnam B;Zhang H;Cai X;Michalek SM;Wu H;Velu SE
口腔生物膜的去除涉及使用广谱抗菌剂，其根除致病性和保护性口腔微生物物种。理想的龋齿治疗剂应该能够选择性地抑制由变形链球菌引起的致病生物膜。S.变形菌胞外葡糖基转移酶（Gtfs），特别是GtfB和GtfC，主要合成水不溶性葡聚糖，其有助于生物膜的结构支架。通过我们对GtfC催化结构域的对接研究确定的铅芪是一种天然产物，称为piceatannol，其抑制S。以剂量依赖性方式抑制变形链球菌生物膜的形成，对变形链球菌的生长抑制具有相当大的选择性。变形链球菌和链球菌。使用Octet RED针对GtfB和GtfC两者进行云杉烷醇的结合动力学分析，其产生低微摩尔KD值。白皮杉醇抑制S.在体内果蝇模型和龋齿的大鼠模型中的变形杆菌定殖。
Removal of oral biofilms involves the use of broad-spectrum antimicrobials, which eradicate both pathogenic and protective oral commensal species. Ideal therapeutics for dental caries should be able to selectively inhibit pathogenic biofilms caused by Streptococcus mutans. S. mutans extracellular glucosyltransferases (Gtfs), particularly GtfB and GtfC, synthesize predominantly water-insoluble glucans, which contribute to the structural scaffold of biofilms. The lead stilbene identified through our docking study against the catalytic domain of GtfC is a natural product known as piceatannol, which inhibited S. mutans biofilm formation in a dose-dependent manner, with considerable selectivity over growth inhibition of S. mutans and commensal streptococci. Binding kinetic analysis of piceatannol was performed using Octet RED against both GtfB and GtfC, which produced low micromolar KD values. Piceatannol inhibited S. mutans colonization in an in vivo drosophila model and a rat model of dental caries.
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影响因子：
2.7
作者：
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