Lim Taehyeong, Ham Soyoung, Kim Han-Shin, Yang Ji-Eun, Lim Hyunwoong, Park Hee-Deung, Byun Youngjoo
College of Pharmacy, Korea University, 2511 Sejong-ro, Sejong 30019, Republic of Korea.
School of Civil, Environmental and Architectural Engineering, Korea University, 145 Anam-ro, Seongbuk-gu, Seoul 02841, Republic of Korea.
ACS Omega. 2024 Dec 11;9(51):50281-50299. doi: 10.1021/acsomega.4c06281. eCollection 2024 Dec 24.
(), a Gram-negative opportunistic pathogen, produces virulent factors and forms biofilms through a quorum sensing (QS) mechanism. Modulating QS networks is considered an effective strategy for treating infections. Particularly, the system, one of the QS networks, can be a potential target in treating patients with chronic infections. We previously discovered that gingerol acts as a RhlR antagonist of . Based on the chemical structure of gingerol, we have designed and synthesized gingerol derivatives by introducing various functional groups in the middle and tail regions. A comprehensive structure-activity relationship study showed that compound substituted with phenyl group in the tail region was the most potent in various biological assessments, such as RhlR binding affinity, gene expression, and virulence factor production of . Furthermore, compound decreased the biofilm formation and pathogenicity of . Interestingly, compound also influenced system in addition to the system. Taken together, compound can be utilized as a potent compound for controlling infection.
（）是一种革兰氏阴性机会致病菌，通过群体感应（QS）机制产生毒力因子并形成生物膜。调节QS网络被认为是治疗感染的有效策略。特别是，QS网络之一的系统可能是治疗慢性感染患者的潜在靶点。我们之前发现姜辣素可作为的RhlR拮抗剂。基于姜辣素的化学结构，我们通过在中间和尾部区域引入各种官能团设计并合成了姜辣素衍生物。一项全面的构效关系研究表明，在尾部区域被苯基取代的化合物在各种生物学评估中最有效，例如RhlR结合亲和力、基因表达以及的毒力因子产生。此外，化合物降低了的生物膜形成和致病性。有趣的是，化合物除了影响系统外，还影响系统。综上所述，化合物可作为控制感染的有效化合物。
