循环 ((Pro-Tyr) 类循环二酸中的基组对它们的抗QS活性和自我组装的影响
Li Li1, Zuxian Xu1, Ruipin Cao1
1Fujian-Taiwan Science and Technology Cooperation Base of Biomedical Materials and Tissue Engineering, Engineering Research Center of Industrial Biocatalysis, Fujian Provincial Key Laboratory of Advanced Materials Oriented Chemical Engineering, Fujian Provincial Key Laboratory of Polymer Materials, College of Chemistry and Materials Science, Fujian Normal University, Fuzhou 350007, China.
iScience
|June 26, 2023
概括
基基团增强循环二的抗定数感应和抗生物膜活性对抗Pseudomonas aeruginosa. 这些修改改进了自我组装和基因调节,为新的抗QS化合物设计提供了洞察力.
科学领域:
- 微生物学 微生物学
- 生物化学 生物化学
- 药用化学 医学化学
背景情况:
- 定数感应 (QS) 是一种细胞间通信系统,对细菌毒性至关重要.
- 循环二被研究为潜在的QS抑制剂.
- 了解结构-活动关系是开发有效的抗QS剂的关键.
研究的目的:
- 研究基对循环二的抗QS和抗生物膜特性的影响.
- 为了比较cyclo (L-Pro-L-Tyr),cyclo (L-Hyp-L-Tyr) 和cyclo (L-Pro-L-Phe) 与Pseudomonas aeruginosa PAO1.1的活性.
- 为了阐明这些化合物的结构功能关系.
主要方法:
- 循环二的合成和表征.
- 通过测量毒性因子抑制来评估抗QS活性.
- 对抗生物膜形成能力的评估.
- 基因表达分析QS系统 (las和rhl).
- 与QS受体蛋白 LasR. 的结合性研究.
主要成果:
- 环 (L-Pro-L-Phe),缺乏基,显示出更高的毒性因子抑制,但较弱的生物膜抑制.
- 赛克洛 (L-Pro-L-Tyr) 和赛克洛 (L-Hyp-L-Tyr) 抑制了las和rhl QS系统,而赛克洛 (L-Pro-L-Phe) 主要影响了rhl和pqs系统.
- 所有与LasR结合的,其中循环 ((L-Pro-L-Phe) 表现出较低的亲和力.
- 基组显著增强了的自我组装特性.
结论:
- 基团对于这些循环二的强有力的抗QS和抗生物膜活性至关重要.
- 基团的存在和位置影响了QS抑制的机制.
- 增强的自我组装与改善的抗QS和抗生物膜有效性相关.
- 这些发现为设计改性循环二作为抗QS疗法提供了基础.
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