Antimicrobial peptides (AMPs) represent the first defense line against infection when organisms are infected by pathogens. These peptides are generally good targets for the development of antimicrobial agents. Peptide amide analogs of Ixosin-B, an antimicrobial peptide with amino acid sequence of QLKVDLWGTRSGIQPEQHSSGKSDVRRWRSRY, were designed, synthesized and examined for antimicrobial activities against Escherichia coli, Staphylococcus aureus, and Pseudomonas aeruginosa. Within the peptides synthesized, we discovered an 11-mer peptide, KRLRRVWRRWR-amide, which exhibited potent antimicrobial activity while very little hemolytic activity in human erythrocytes was observed even at high dose level (100 μM). With further modifications, this peptide could be developed into a potent antimicrobial agent in the future.
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http://dx.doi.org/10.1016/j.bmcl.2012.04.018 | DOI Listing |
Biochemistry
January 2025
Department of Biochemistry, Genetics and Microbiology, Faculty of Natural and Agricultural Sciences, University of Pretoria, Pretoria 0002, South Africa.
C-terminal amidation of antimicrobial peptides (AMPs) is a frequent minor modification used to improve antibacterial potency, commonly ascribed to increased positive charge, protection from proteases, and a stabilized secondary structure. Although the activity of AMPs is primarily associated with the ability to penetrate bacterial membranes, hitherto the effect of amidation on this interaction has not been understood in detail. Here, we show that amidation of the scorpion-derived membranolytic peptide AamAP1-Lys produces a potent analog with faster bactericidal activity, increased membrane permeabilization, and greater Gram-negative membrane penetration associated with greater conformational flexibility.
View Article and Find Full Text PDFMicrobiol Spectr
January 2025
Department of Microbiology, University of Massachusetts, Amherst, Massachusetts, USA.
Unlabelled: is an acid-fast, aerobic, non-motile, and biofilm-forming bacterium. The increasing prevalence of mycobacterial infections makes it necessary to find new methods to combat the resistance of bacteria to conventional antibiotics. is an emerging pathogen that is intrinsically drug resistant due to several factors, including an impermeable cell envelope, drug efflux pumps, target-modifying enzymes, and the ability to form thick, robust biofilms.
View Article and Find Full Text PDFAntimicrob Agents Chemother
January 2025
Department of Molecular Biology and Microbiology, Case Western Reserve University School of Medicine, Cleveland, Ohio, USA.
Foremost in the design of new β-lactamase inhibitors (BLIs) are the boronic acid transition state inhibitors (BATSIs). Two highly potent BATSIs being developed are S02030 and MB076 strategically designed to be active against cephalosporinases and carbapenemases, especially KPC. When combined with cefepime, S02030 and MB076 demonstrated potent antimicrobial activity against laboratory and clinical strains of expressing a variety of class A and class C β-lactamases, including and .
View Article and Find Full Text PDFJ Sci Food Agric
January 2025
University of Agricultural Sciences, Bengaluru, India.
Background: The edible seeds of Ocimum gratissimum and Ocimum basilicum were found to be a potent source of phytochemicals with noteworthy antioxidant, antidiabetic, and antimicrobial properties. This study aimed to investigate the impact of germination and extraction solvents (ethanol (EtOH), distilled water) on the therapeutic properties exhibited and the ability of seed extracts to act as natural food preservatives.
Results: The EtOH extracts of germinated O.
ChemistryOpen
January 2025
School of Chemistry and Physics, University of KwaZulu-Natal, P/Bag X54001, Westville, Durban, 4000, South Africa.
Quinazolines/quinazolin-4-ones are significant nitrogen-containing heterocycles that exist in various natural products and synthetic scaffolds with diverse medicinal and pharmacological applications. Researchers across the globe have explored numerous synthetic strategies to develop safer and more potent quinazoline/quinazolinone analogues, particularly for combating cancer and microbial infections. This review systematically examines scholarly efforts toward understanding this scaffold's synthetic pathways and medicinal relevance, emphasizing the role of metal and non-metal catalysts and other reagents in their synthesis.
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