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1.
Molecules ; 29(4)2024 Feb 07.
Artigo em Inglês | MEDLINE | ID: mdl-38398517

RESUMO

Obesity is a source of significant pathologies and deadly diseases, including heart disease, diabetes, and cancer. One of the most intriguing strategies in the hunt for new anti-obesity medications is the inhibition of pancreatic lipase (PL). This study presents a novel application of short α and ß-mixed peptides as pancreatic lipase inhibitors. These peptides were synthesized in the solution phase and characterized using FTIR and 1H-NMR. L-proline is present in a high percentage of natural anti-lipase peptides and was used as a ß-amino acid in this study to enhance anti-lipase activity and proteolytic stability. Moreover, L-α-proline was converted to ß-amino acid derivatives using the Arndt-Eistert method with the advantage of stereo control at the α-carbon. The synthesized peptides with anti-lipase activity are N-Boc-ß-Pro-Gly-OBz (93%), N-Boc-O-Bz-Tyr-ß-Pro-ß-Pro-Gly-OBz (92%), N-Boc-O-Bz-Tyr-ß-Pro-COOH (91%), N-Boc-Phe-ß-Pro-OCH3 (90%), and N-Boc-O-Bz-Tyr-ß-Pro-OCH3 (89%). These peptides may function as lead molecules for further modification to more significant molecules, which can help control obesity.


Assuntos
Peptídeos , Prolina , Humanos , Peptídeos/farmacologia , Peptídeos/química , Aminoácidos , Lipase , Obesidade
2.
Sci Rep ; 14(1): 578, 2024 01 05.
Artigo em Inglês | MEDLINE | ID: mdl-38182627

RESUMO

Microorganism contamination on substrate surfaces is arousing increasingly concern as a serious health issue. In this research work, antimicrobial water-based acrylic paint containing silver nanoparticles (Ag NPs) was prepared using the facile Ag+ in situ reduction process, in which AgNO3 and reducing agent sodium acrylate were refluxed with acrylic polymeric solution to obtain an antimicrobial and antifungal polymeric material for substrate coating. The Synthesized antimicrobial and antifungal water-based acrylic paint were characterized by different spectroscopic techniques. The FTIR and UV-Visible spectroscopic analyses were investigated to study the water-based acrylic paint structure as well as the significant impact of Ag NPs on the paint matrix. The UV-Visible and FTIR Spectra peak shows successful integration of Ag NPs within the polymer matrix without altering the core functional groups of the paint. The water based acrylic paint exhibited a strong antimicrobial activity, revealed substantial inhibition zones against all four strains of Gram negative represented by Escherichia coli, Acinetobacter baumannii, Klebsiella pneumoniae and Gram-positive represented by Bacillus cereus. The coated film on substrate also shows great inhibition zone which exhibit a strong antimicrobial activity. Moreover, water based acrylic paint also exhibited a great antifungal activity, revealed substantial zone of inhibition against the Aspergillus niger, Aspergillus terreus and Rhizopus arrhizus fungal strains. Also, the coated film showed the best adhesion at 50% and 80% solution of polymeric coating sample as compared to pure or very dilute sample coating. This innovative approach has the potential to revolutionize varies industries from healthcare to construction.


Assuntos
Nanopartículas Metálicas , Nanoestruturas , Antifúngicos/farmacologia , Prata/farmacologia , Escherichia coli , Água
3.
Curr Top Med Chem ; 22(13): 1046-1067, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-34961445

RESUMO

The rapid emergence of multidrug-resistant bacterial strains highlights the need for the development of new antimicrobial compounds/materials to address associated healthcare challenges. Meanwhile, the adverse side effects of conventional antibiotics on human health urge the development of new natural product-based antimicrobials to minimize the side effects. In this respect, we concisely review the recent scientific contributions to develop natural product-based nano-antibiotics. The focus of the review is on the use of flavonoids, peptides, and cationic biopolymer functionalized metal/metal oxide nanoparticles as efficient tools to hit the MDR bacterial strains. It summarizes the most recent aspects of the functionalized nanoparticles against various pathogenic bacterial strains for their minimal inhibitory concentrations and mechanism of action at the cellular and molecular levels. In the end, the future perspectives to materialize the in vivo applications of nano-antimicrobials are suggested based on the available research.


Assuntos
Anti-Infecciosos , Produtos Biológicos , Antibacterianos/farmacologia , Antibacterianos/uso terapêutico , Anti-Infecciosos/farmacologia , Bactérias , Farmacorresistência Bacteriana Múltipla , Humanos , Testes de Sensibilidade Microbiana
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