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首页> 外文期刊>Drug Design, Development and Therapy >Potential Allylpyrocatechol Derivatives as Antibacterial Agent Against Oral Pathogen of S. sanguinis ATCC 10,556 and as Inhibitor of MurA Enzymes: in vitro and in silico Study
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Potential Allylpyrocatechol Derivatives as Antibacterial Agent Against Oral Pathogen of S. sanguinis ATCC 10,556 and as Inhibitor of MurA Enzymes: in vitro and in silico Study

机译：潜在的烯丙基丙酰衍生物作为抗菌剂的抗菌剂免受S.Sanguinis ATCC 10,556和Mura酶的抑制剂：体外和硅研究

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Background: Streptococcus sanguinis is Gram-positive bacteria that contribute to caries. Many antibacterial agents are resistant against bacteria so that the discovery of new antibacterial agents is a crucial issue. Mechanism of antibacterial agents by disrupting cell wall bacteria is a promising target to be developed. One of the enzymes contributing to the cell wall is MurA enzyme. MurA is an enzyme catalyzing the first step of peptidoglycan biosynthesis in the cell wall formation. Inhibiting MurA is an effective and efficient way to kill the bacteria. Source of bioactive compounds including the antibacterial agent can be found in natural product such as herbal plant. Piper betle L. was reported to contain active antibacterial compounds. However, there is no more information on the antibacterial activity and molecular mechanism of P. betle ’s compound against S. sanguinis . Purpose: The study aims to identify antibacterial constituents of P. betle L. and evaluate their activities through two different methods including in vitro and in silico analysis. Materials and Methods: The antibacterial agent was purified by bioactivity-guided isolation with combination chromatography methods and the chemical structure was determined by spectroscopic methods. The in vitro antibacterial activity was evaluated by disc diffusion and dilution methods while the in silico study of a compound binds on the MurA was determined using PyRx program. Results: The antibacterial compound identified as allylpyrocatechol showed inhibitory activity against S. sanguinis with an inhibition zone of 11.85 mm at 1%, together with MIC and MBC values of 39.1 and 78.1 μg/mL, respectively. Prediction for molecular inhibition mechanism of allylpyrocatechols against the MurA presented two allylpyrocatechol derivatives showing binding activity of ? 5.4, stronger than fosfomycin as a reference with the binding activity of ? 4.6. Conclusion: Two allylpyrocatechol derivatives were predicted to have a good potency as a novel natural antibacterial agent against S. sanguinis through blocking MurA activity that causes disruption of bacterial cell wall.
机译：背景：链球菌血管球菌是克阳性细菌，为龋齿有助于龋齿。许多抗菌剂对细菌有抗性，因此发现新的抗菌剂是至关重要的问题。通过破坏细胞壁细菌的抗菌剂机理是待开发的靶向靶标。贡献对细胞壁的一种酶是Mura酶。 Mura是一种催化肽聚糖生物合成在细胞壁形成中的第一步。抑制穆拉是杀死细菌的有效和有效的方法。包括抗菌剂的生物活性化合物来源可以在天然产品如草药植物中找到。据报道吹笛剂浸渍剂L.含有活性抗菌化合物。然而，不再有关于对S.Suganguinis的抗菌活性和分子机制的信息。目的：该研究旨在鉴定P.Petle L的抗菌成分。并通过两种不同的方法评估其活性，包括体外和硅分析。材料和方法：通过组合色谱方法通过生物活性引导分离纯化抗菌剂，并通过光谱法测定化学结构。通过盘扩散和稀释方法评价体外抗菌活性，而使用Pyrx程序测定硅藻的化合物的硅研究。结果：被鉴定为烯丙基吡酰脲的抗菌化合物对S. anguinis的抑制活性显示为11.85mm的抑制区，分别与39.1和78.1μg/ ml的MIC和MBC值。烯丙基吡罗基酚对尤拉的分子抑制机制的预测呈现出两种烯丙基吡啶醇衍生物，其显示有结合活性？ 5.4，比Fosfomycin更强，作为具有结合活动的引用？ 4.6。结论：预计两种烯丙基吡罗基酚衍生物通过阻断细菌细胞壁破坏的静脉活性，含有良好的天然抗菌剂。

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