A Bisphenolic Honokiol Analog Outcompetes Oral Antimicrobial Agent Cetylpyridinium Chloride via a Membrane-Associated Mechanism
A Bisphenolic Honokiol Analog Outcompetes Oral Antimicrobial Agent Cetylpyridinium Chloride via a Membrane-Associated Mechanism
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DOI：
10.1021/acsinfecdis.9b00190
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发表时间：
2020-01-01
影响因子：
5.3
通讯作者：
Kozlowski, Marisa C.
中科院分区：
文献类型：
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作者：
Ochoa, Cristian;Solinski, Amy E.;Kozlowski, Marisa C.
针对变形链球菌是减少龋齿的主要焦点，龋齿是世界上最常见的疾病之一。此前，我们的研究小组发现了一种有效的杀菌联芳基化合物，其灵感来自天然产物honoklane。在此，构效关系（SAR）的研究，以确定结构的关键抑制图案概述。此外，机制研究表明，细菌膜破坏是细菌生长抑制的中心。在此过程中，发现类似物C2表现出比市售抗微生物氯化十六烷基吡啶（CPC）好4倍的治疗指数，使其成为口腔护理的可行替代品。
Targeting Streptococcus mutans is the primary focus in reducing dental caries, one of the most common maladies in the world. Previously, our groups discovered a potent bactericidal biaryl compound that was inspired by the natural product honokiol. Herein, a structure activity relationship (SAR) study to ascertain structural motifs key to inhibition is outlined. Furthermore, mechanism studies show that bacterial membrane disruption is central to the bacterial growth inhibition. During this process, it was discovered that analog C2 demonstrated a 4-fold better therapeutic index compared to the commercially available antimicrobial cetylpyridinium chloride (CPC) making it a viable alternative for oral care.