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含色氨酸的环二肽的群体感应抑制活性。

Anti-Quorum-Sensing Activity of Tryptophan-Containing Cyclic Dipeptides.

机构信息

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.

出版信息

Mar Drugs. 2022 Jan 19;20(2):85. doi: 10.3390/md20020085.

DOI:10.3390/md20020085
PMID:35200615
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC8924889/
Abstract

Quorum sensing (QS) can regulate the pathogenicity of bacteria and the production of some virulence factors. It is a promising target for screening to find anti-virulence agents in the coming post-antibiotics era. Cyclo (-Trp--Ser), one variety of cyclic dipeptides (CDPs), isolated from a marine bacterium , exhibited anti-QS activity against CV026 and PAO1. Unlike the CDPs composed of phenylalanine or tyrosine, the anti-QS activity has been widely studied; however, cyclo (-Trp--Ser) and derivatives, containing one tryptophan unit and one non-aromatic amino acid, have not been systematically explored. Herein, the cyclo (-Trp--Ser) and seven derivatives were synthesized and evaluated. All tryptophane-contained CDPs were able to decrease the production of violacein in CV026 and predicted as binding within the same pocket of receptor protein CviR, but in lower binding energy compared with the natural ligand CHSL. As for PAO1, owning more complicated QS systems, these CDPs also exhibited inhibitory effects on pyocyanin production, swimming motility, biofilm formation, and adhesion. These investigations suggested a promising way to keep the tryptophan untouched and make modifications on the non-aromatic unit to increase the anti-QS activity and decrease the cytotoxicity, thus developing a novel CDP-based anti-virulence agent.

摘要

群体感应 (QS) 可以调节细菌的致病性和一些毒力因子的产生。在即将到来的后抗生素时代，QS 是筛选抗毒力药物的有前途的靶点。从海洋细菌中分离得到的环状二肽 (CDP) 之一，环 (-Trp--Ser)，对 CV026 和 PAO1 表现出抗 QS 活性。与由苯丙氨酸或酪氨酸组成的 CDP 不同，抗 QS 活性已被广泛研究；然而，环 (-Trp--Ser) 和含有一个色氨酸单元和一个非芳香族氨基酸的衍生物尚未得到系统的探索。在此，合成并评价了环 (-Trp--Ser) 和七个衍生物。所有含色氨酸的 CDP 都能够降低 CV026 中紫霉素的产生，并预测与受体蛋白 CviR 结合在相同的口袋中，但与天然配体 CHSL 相比，结合能较低。对于 PAO1，由于其具有更复杂的 QS 系统，这些 CDP 还对绿脓菌素的产生、泳动性、生物膜形成和黏附具有抑制作用。这些研究表明，保持色氨酸不变，对非芳香族单元进行修饰，以提高抗 QS 活性并降低细胞毒性，从而开发出一种新型基于 CDP 的抗毒力药物，这是一种很有前途的方法。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/22ea/8924889/87aaadd08de9/marinedrugs-20-00085-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/22ea/8924889/2a69ba248a24/marinedrugs-20-00085-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/22ea/8924889/265513a6c21d/marinedrugs-20-00085-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/22ea/8924889/2d6d7626dfd0/marinedrugs-20-00085-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/22ea/8924889/737e371e6f87/marinedrugs-20-00085-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/22ea/8924889/5494083eb314/marinedrugs-20-00085-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/22ea/8924889/a18207c4824b/marinedrugs-20-00085-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/22ea/8924889/87aaadd08de9/marinedrugs-20-00085-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/22ea/8924889/2a69ba248a24/marinedrugs-20-00085-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/22ea/8924889/265513a6c21d/marinedrugs-20-00085-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/22ea/8924889/2d6d7626dfd0/marinedrugs-20-00085-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/22ea/8924889/737e371e6f87/marinedrugs-20-00085-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/22ea/8924889/5494083eb314/marinedrugs-20-00085-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/22ea/8924889/a18207c4824b/marinedrugs-20-00085-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/22ea/8924889/87aaadd08de9/marinedrugs-20-00085-g006.jpg

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