scholarly journals Synthesis and 3D-QSAR of p-Hydroxybenzohydrazide Derivatives With Antimicrobial Activity Against Multidrug-Resistant Staphylococcus aureus

2010 ◽  
Vol 54 (1) ◽  
pp. 77-87 ◽  
Author(s):  
Ritesh P. Bhole ◽  
Kishore P. Bhusari
Marine Drugs ◽  
2021 ◽  
Vol 19 (8) ◽  
pp. 411
Author(s):  
Maxence Quemener ◽  
Marie Dayras ◽  
Nicolas Frotté ◽  
Stella Debaets ◽  
Christophe Le Meur ◽  
...  

Among the different tools to address the antibiotic resistance crisis, bioprospecting in complex uncharted habitats to detect novel microorganisms putatively producing original antimicrobial compounds can definitely increase the current therapeutic arsenal of antibiotics. Fungi from numerous habitats have been widely screened for their ability to express specific biosynthetic gene clusters (BGCs) involved in the synthesis of antimicrobial compounds. Here, a collection of unique 75 deep oceanic crust fungi was screened to evaluate their biotechnological potential through the prism of their antimicrobial activity using a polyphasic approach. After a first genetic screening to detect specific BGCs, a second step consisted of an antimicrobial screening that tested the most promising isolates against 11 microbial targets. Here, 12 fungal isolates showed at least one antibacterial and/or antifungal activity (static or lytic) against human pathogens. This analysis also revealed that Staphylococcus aureus ATCC 25923 and Enterococcus faecalis CIP A 186 were the most impacted, followed by Pseudomonas aeruginosa ATCC 27853. A specific focus on three fungal isolates allowed us to detect interesting activity of crude extracts against multidrug-resistant Staphylococcus aureus. Finally, complementary mass spectrometry (MS)-based molecular networking analyses were performed to putatively assign the fungal metabolites and raise hypotheses to link them to the observed antimicrobial activities.


2006 ◽  
Vol 50 (2) ◽  
pp. 806-809 ◽  
Author(s):  
Giuseppantonio Maisetta ◽  
Giovanna Batoni ◽  
Semih Esin ◽  
Walter Florio ◽  
Daria Bottai ◽  
...  

ABSTRACT The antimicrobial activity of human β-defensin 3 (hBD-3) against multidrug-resistant clinical isolates of Staphylococcus aureus, Enterococcus faecium, Pseudomonas aeruginosa, Stenotrophomonas maltophilia, and Acinetobacter baumannii was evaluated. A fast bactericidal effect (within 20 min) against all bacterial strains tested was observed. The presence of 20% human serum abolished the bactericidal activity of hBD-3 against gram-negative strains and reduced the activity of the peptide against gram-positive strains.


mBio ◽  
2019 ◽  
Vol 10 (5) ◽  
Author(s):  
Karine Loth ◽  
Agnès Vergnes ◽  
Cairé Barreto ◽  
Sébastien N. Voisin ◽  
Hervé Meudal ◽  
...  

ABSTRACT Big defensins, ancestors of β-defensins, are composed of a β-defensin-like C-terminal domain and a globular hydrophobic ancestral N-terminal domain. This unique structure is found in a limited number of phylogenetically distant species, including mollusks, ancestral chelicerates, and early-branching cephalochordates, mostly living in marine environments. One puzzling evolutionary issue concerns the advantage for these species of having maintained a hydrophobic domain lost during evolution toward β-defensins. Using native ligation chemistry, we produced the oyster Crassostrea gigas BigDef1 (Cg-BigDef1) and its separate domains. Cg-BigDef1 showed salt-stable and broad-range bactericidal activity, including against multidrug-resistant human clinical isolates of Staphylococcus aureus. We found that the ancestral N-terminal domain confers salt-stable antimicrobial activity to the β-defensin-like domain, which is otherwise inactive. Moreover, upon contact with bacteria, the N-terminal domain drives Cg-BigDef1 assembly into nanonets that entrap and kill bacteria. We speculate that the hydrophobic N-terminal domain of big defensins has been retained in marine phyla to confer salt-stable interactions with bacterial membranes in environments where electrostatic interactions are impaired. Those remarkable properties open the way to future drug developments when physiological salt concentrations inhibit the antimicrobial activity of vertebrate β-defensins. IMPORTANCE β-Defensins are host defense peptides controlling infections in species ranging from humans to invertebrates. However, the antimicrobial activity of most human β-defensins is impaired at physiological salt concentrations. We explored the properties of big defensins, the β-defensin ancestors, which have been conserved in a number of marine organisms, mainly mollusks. By focusing on a big defensin from oyster (Cg-BigDef1), we showed that the N-terminal domain lost during evolution toward β-defensins confers bactericidal activity to Cg-BigDef1, even at high salt concentrations. Cg-BigDef1 killed multidrug-resistant human clinical isolates of Staphylococcus aureus. Moreover, the ancestral N-terminal domain drove the assembly of the big defensin into nanonets in which bacteria are entrapped and killed. This discovery may explain why the ancestral N-terminal domain has been maintained in diverse marine phyla and creates a new path of discovery to design β-defensin derivatives active at physiological and high salt concentrations.


2019 ◽  
Vol 17 (1) ◽  
pp. 587-599 ◽  
Author(s):  
D TIRADO-TORRES ◽  
C A CHAN-KEB ◽  
R A PÉREZ-BALÁN ◽  
B AKE-CANCHÉ ◽  
M I GÓMEZ-SOLANO ◽  
...  

2019 ◽  
Vol 75 (02) ◽  
pp. 6211-2019
Author(s):  
ERHAN KEYVAN ◽  
HIDAYET TUTUN

The occurrence of multidrug-resistant Staphylococcus aureus is an important causative agent of mastitis in cattle and of foodborne diseases. It is a worldwide concern, making it essential to develop alternative treatments to fight against the bacteria. Thus, the aim of this study is to determine the ability of carvacrol to inhibit the growth of S. aureus isolated from bulk tank milk in Turkey’s Burdur Province. All strains (n = 31) were used to investigate the antimicrobial activity of carvacrol, including the methicillin-resistant S. aureus and strains from the American Type Culture Collection and England’s National Collection of Type Cultures. The minimum inhibitory concentration (MIC) values were determined via a microdilution method, and the antimicrobial susceptibility profiles via a disk diffusion method. Antibiotic resistance was detected in 20 strains (64.5%). Multidrug resistance was observed in 8 strains (25.8%). Carvacrol exhibited strong antimicrobial activity, with MIC value at 0.058-0.234 mg/ml, in the microdilution method. Inhibition zones of carvacrol were in the range of 19 to 45 mm. The results of this study emphasize the promising role of carvacrol among new antibacterial agents that can combat S. aureus strains.


mBio ◽  
2016 ◽  
Vol 7 (2) ◽  
Author(s):  
George G. Zhanel ◽  
James A. Karlowsky

ABSTRACT Clay minerals are naturally occurring layered phyllosilicates which consist of fine particles and possess antimicrobial activity. In a recent article, Behroozian et al. obtained Kisameet clay (KC) from Kisameet, from the central coast of British Columbia, Canada, northwest of Vancouver and assessed its antimicrobial activity versus 16 selected ESKAPE pathogens ( Enterococcus faecium , Staphylococcus aureus , Klebsiella pneumoniae , Acinetobacter baumannii , Pseudomonas aeruginosa , and Enterobacter spp.) possessing a variety of different resistance profiles [S. Behroozian, S. L. Svensson, and J. Davies, mBio 7(1):e01842-15, 2016, http://dx.doi.org/10.1128/mBio.01842-15]. KC demonstrated complete bacterial eradication of Klebsiella pneumoniae , Acinetobacter baumannii , Pseudomonas aeruginosa , and Staphylococcus aureus within 24 h. For Enterobacter spp., the organisms were eradicated with 1% KC within 5 h, while for Enterococcus faecium , it took 48 h to kill all organisms. Although many questions need to be answered, these exciting findings highlight the importance of testing natural substances/products from around the globe to assess whether they possess antimicrobial activity and potential for usage as topical, oral, or systemic agents for the treatment of multidrug-resistant pathogens.


2021 ◽  
Vol 12 (6) ◽  
pp. 7523-7531

Phytochemical studies on Croton species have identified the presence of secondary metabolites responsible for a wide variety of pharmacological activities, among them antimicrobial activity. Research for new substances with antimicrobial activity derived from natural products can give a major contribution to human health worldwide by finding more efficient and fewer toxic formulas in the race against pathogenic microorganisms' resistance. Among bacterial pathogens, Staphylococcus aureus species, despite being present in the skin and nasal mucosa, can cause many infections and diseases. These opportunists reach debilitated people in hospitals and are challenging to treat. Here, we performed the structural characterization, determination of antibiotic activity, and MepA efflux pump inhibition potential against S. aureus of the chalcone (2E, 4E) -1- (2-hydroxy-3,4,6-trimethoxyphenyl)-5-phenylpenta-2,4-dien-1-one, derived from natural products 2-hydroxy-3,4,6-trimethoxyacetophenone isolated from Croton anisodontus and cinnamaldehyde. The chalcone was synthesized by the Claisen-Schmidt condensation. In addition, microbiological tests were performed to investigate the antibacterial activity, modulator potential, and efflux pump inhibition against the S. aureus multi-resistant strains. MIC values obtained to chalcone were not clinically relevant (MIC ≥ 1024 µg/mL). However, chalcone hampers the binding of the antibiotic to the binding site of the MepA efflux pump. It acts as a competitive inhibitor, being expelled from the bacteria in place of the antibiotic and potentiating ciprofloxacin's action against multidrug-resistant bacterial strains of K2068. Therefore, chalcone can be used as a base for substance design with antibiotic modifying activity.


2018 ◽  
Vol 33 (24) ◽  
pp. 3587-3591 ◽  
Author(s):  
Barbara Kot ◽  
Kamila Wierzchowska ◽  
Małgorzata Piechota ◽  
Paweł Czerniewicz ◽  
Grzegorz Chrzanowski

2019 ◽  
Vol 48 (31) ◽  
pp. 11822-11828 ◽  
Author(s):  
Payal Srivastava ◽  
Manjulika Shukla ◽  
Grace Kaul ◽  
Sidharth Chopra ◽  
Ashis K. Patra

Two curcumin conjugated ruthenium(ii) polypyridyl complexes, [Ru(NN)2(cur)](PF6) (1, 2), were systematically exploited for their antimicrobial activity in vitro and in vivo and potential selectivity against multidrug resistant S. aureus strains.


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