Exploring the quorum sensing inhibition of isolated chrysin from Penicillium chrysogenum DXY-1

2021 ◽  
Vol 111 ◽  
pp. 104894
Author(s):  
Aiping Chang ◽  
Qiaomei He ◽  
Li Li ◽  
Xiaodan Yu ◽  
Shiwei Sun ◽  
...  
2017 ◽  
Vol 17 (17) ◽  
pp. 1915-1927 ◽  
Author(s):  
Israel Castillo-Juarez ◽  
Luis Esau Lopez-Jacome ◽  
Gloria Soberon-Chavez ◽  
Maria Tomas ◽  
Jintae Lee ◽  
...  

2011 ◽  
Vol 8 (2) ◽  
pp. 133-137 ◽  
Author(s):  
Zoltan Gabor Varga ◽  
Mira Agnes Szabo ◽  
Zsuzsanna Schelz ◽  
Erno Szegedi ◽  
Leonard Amaral ◽  
...  

Antibiotics ◽  
2021 ◽  
Vol 10 (3) ◽  
pp. 321
Author(s):  
Shekh Sabir ◽  
Tsz Tin Yu ◽  
Rajesh Kuppusamy ◽  
Basmah Almohaywi ◽  
George Iskander ◽  
...  

The quorum sensing (QS) system in multi-drug-resistant bacteria such as P. aeruginosa is primarily responsible for the development of antibiotic resistance and is considered an attractive target for antimicrobial drug discovery. In this study, we synthesised a series of novel selenourea and thiourea-containing dihydropyrrol-2-one (DHP) analogues as LasR antagonists. The selenium DHP derivatives displayed significantly better quorum-sensing inhibition (QSI) activities than the corresponding sulphur analogues. The most potent analogue 3e efficiently inhibited the las QS system by 81% at 125 µM and 53% at 31 µM. Additionally, all the compounds were screened for their minimum inhibitory concentration (MIC) against the Gram-positive bacterium S. aureus, and interestingly, only the selenium analogues showed antibacterial activity, with 3c and 3e being the most potent with a MIC of 15.6 µM.


2021 ◽  
Vol 11 (1) ◽  
Author(s):  
Arpit Shukla ◽  
Gaurav Shukla ◽  
Paritosh Parmar ◽  
Baldev Patel ◽  
Dweipayan Goswami ◽  
...  

AbstractThere persists a constant threat from multidrug resistance being acquired by all human pathogens that challenges the well-being of humans. This phenomenon is predominantly led by Pseudomonas aeruginosa which is already resistant to the current generations of antibiotic by altering its metabolic pathways to survive. Specifically for this microbe the phenomenon of quorum sensing (QS) plays a crucial role in acquiring virulence and pathogenicity. QS is simply the cross talk between the bacterial community driven by signals that bind to receptors, enabling the entire bacterial microcosm to function as a single unit which has led to control P. aeruginosa cumbersome even in presence of antibiotics. Inhibition of QS can, therefore, be of a significant importance to curb such virulent and pathogenic strains of P. aeruginosa. Natural compounds are well known for their antimicrobial properties, of which, information on their mode of action is scarce. There can be many antimicrobial phytochemicals that act by hindering QS-pathways. The rationale of the current study is to identify such natural compounds that can inhibit QS in P. aeruginosa driven by LasR, PhzR, and RhlR dependent pathways. To achieve this rationale, in silico studies were first performed to identify such natural compounds which were then validated by in vitro experiments. Gingerol and Curcumin were identified as QS-antagonists (QSA) which could further suppress the production of biofilm, EPS, pyocyanin, and rhamnolipid along with improving the susceptibility to antibiotics.


2020 ◽  
Vol 21 (24) ◽  
pp. 9512
Author(s):  
Alfredo Fuentes-Gutiérrez ◽  
Everardo Curiel-Quesada ◽  
José Correa-Basurto ◽  
Alberto Martínez-Muñoz ◽  
Alicia Reyes-Arellano

Quorum sensing is a communication system among bacteria to sense the proper time to express their virulence factors. Quorum sensing inhibition is a therapeutic strategy to block bacterial mechanisms of virulence. The aim of this study was to synthesize and evaluate new bioisosteres of N-acyl homoserine lactones as Quorum sensing inhibitors in Chromobacterium violaceum CV026 by quantifying the specific production of violacein. Five series of compounds with different heterocyclic scaffolds were synthesized in good yields: thiazoles, 16a–c, thiazolines 17a–c, benzimidazoles 18a–c, pyridines 19a–c and imidazolines 32a–c. All 15 compounds showed activity as Quorum sensing inhibitors except 16a. Compounds 16b, 17a–c, 18a, 18c, 19c and 32b exhibited activity at concentrations of 10 µM and 100 µM, highlighting the activity of benzimidazole 18a (IC50 = 36.67 µM) and 32b (IC50 = 85.03 µM). Pyridine 19c displayed the best quorum sensing inhibition activity (IC50 = 9.66 µM). Molecular docking simulations were conducted for all test compounds on the Chromobacterium violaceum CviR protein to gain insight into the process of quorum sensing inhibition. The in-silico data reveal that all 15 the compounds have higher affinity for the protein than the native AHL ligand (1). A strong correlation was found between the theoretical and experimental results.


2020 ◽  
Vol 104 (11) ◽  
pp. 5025-5037
Author(s):  
Wei-Jia Cheng ◽  
Jin-Wei Zhou ◽  
Ping-Ping Zhang ◽  
Huai-Zhi Luo ◽  
Shi Tang ◽  
...  

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