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胡椒碱二羟基衍生物（PL-18）对群体感应和生物膜的抑制作用

quorum sensing and biofilm attenuation by a di-hydroxy derivative of piperlongumine (PL-18).

作者信息

Schlichter Kadosh Yael, Muthuraman Subramani, Nisaa Khairun, Ben-Zvi Anat, Karsagi Byron Danit Lisa, Shagan Marilou, Brandis Alexander, Mehlman Tevie, Gopas Jacob, Saravana Kumar Rajendran, Kushmaro Ariel

机构信息

Avram and Stella Goldstein-Goren Department of Biotechnology Engineering, Ben Gurion University of the Negev, Beer Sheva, Israel.

Chemistry Division, Vellore Institute of Technology, Chennai, India.

出版信息

Biofilm. 2024 Jul 18;8:100215. doi: 10.1016/j.bioflm.2024.100215. eCollection 2024 Dec.

DOI:10.1016/j.bioflm.2024.100215
PMID:39148892
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC11326495/
Abstract

Bacterial communication, Quorum Sensing (QS), is a target against virulence and prevention of antibiotic-resistant infections. 16 derivatives of Piperlongumine (PL), an amide alkaloid from L., were screened for QS inhibition. PL-18 had the best QSI activity. PL-18 inhibited the and QS systems of . PL-18 inhibited pyocyanin and rhamnolipids that are QS-controlled virulence elements. Iron is an essential element for pathogenicity, biofilm formation and resilience in harsh environments, its uptake was inhibited by PL-18. Pl-18 significantly reduced the biofilm biovolume including in established biofilms. PL-18-coated silicon tubes significantly inhibited biofilm formation. The transcriptome study of treated showed that PL-18 indeed reduced the expression of QS and iron homeostasis related genes, and up regulated sulfur metabolism related genes. Altogether, PL-18 inhibits QS, virulence, iron uptake, and biofilm formation. Thus, PL-18 should be further developed against bacterial infection, antibiotic resistance, and biofilm formation.

摘要

细菌通讯，即群体感应（QS），是对抗毒力和预防抗生素耐药性感染的一个靶点。对胡椒碱（PL）的16种衍生物进行了筛选，PL是一种来自长蒌的酰胺生物碱，用于检测其对群体感应的抑制作用。PL-18具有最佳的群体感应抑制（QSI）活性。PL-18抑制了铜绿假单胞菌的las和rhl群体感应系统。PL-18抑制了由群体感应控制的毒力因子绿脓菌素和鼠李糖脂。铁是致病性、生物膜形成以及在恶劣环境中的恢复力所必需的元素，其摄取受到PL-18的抑制。PL-18显著降低了生物膜生物体积，包括已形成的生物膜。涂有PL-18的硅胶管显著抑制了生物膜的形成。对经处理的铜绿假单胞菌进行的转录组研究表明，PL-18确实降低了群体感应和铁稳态相关基因的表达，并上调了硫代谢相关基因。总之，PL-18抑制群体感应、毒力、铁摄取和生物膜形成。因此，PL-18应进一步开发用于对抗细菌感染、抗生素耐药性和生物膜形成。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/473d/11326495/81c7b50fe169/gr7.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/473d/11326495/1ae230fc91ef/gr6.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/473d/11326495/81c7b50fe169/gr7.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/473d/11326495/563cfcf4f71d/gr1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/473d/11326495/87195f0a4c5c/gr2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/473d/11326495/56edd32c345d/gr3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/473d/11326495/c479855b3f87/gr4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/473d/11326495/0980fbfaf77e/gr5.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/473d/11326495/1ae230fc91ef/gr6.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/473d/11326495/81c7b50fe169/gr7.jpg

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