An increasing number of multidrug-resistant pathogens is a serious problem modern medicine and new antibiotics are highly demanded. In this study, different n-alkyl acids (C2-C14) aromatic (benzoic trans-cinnamic) were conjugated to the N-terminus KR12 amide. The effect modification on antimicrobial activity (ESKAPE bacteria biofilm Staphylococcus aureus) cytotoxicity (human red blood cells HaCaT cell line) was examined. lipophilic modifications helicity studied by CD spectroscopy, whereas...

Summary Human infection by the vector‐borne protozoan Leishmania is responsible for substantial worldwide morbidity and mortality. The surface‐metalloprotease (leishmanolysin) of a virulence factor which contributes to variety functions including evasion complement‐mediated parasite‐killing host intramacrophage survival. We tested hypothesis that leishmanolysin serves protect parasites from cytolytic effects various antimicrobial peptides (AMPs) are important components innate immune system....

The secondary structure of proteins in unheated and heated whey protein isolate dispersions the surface tension solutions were investigated at different pH. Heating 80°C results an increase unordered structure. Nevertheless, difference between contents samples increases with increasing pH solution. At low concentrations decreased concentration to about 5 mg/ml. For solution, a similar trend was observed decrease protein. In both cases, curves depicting as function could be fitted exponential...

ABSTRACT Candida auris has increasingly become a global threat due to its wide range of antifungal resistances as well ability sustain outbreaks in clinical settings. Two lipopeptides, C14-NleRR-NH 2 (Nel) and C14-WRR-NH (WR), were evaluated against six fluconazole-resistant C. isolates. Both molecules showed good antimicrobial activity demonstrated by MIC determination, time-kill, microscopy experiments. The peptides able inhibit fungal growth, while sub-MIC concentrations the delayed...

Isothermal titration calorimetry (ITC), circular dichroism (CD) spectroscopy, and molecular dynamics simulations were applied to describe interactions between lipopeptides decavanadate ions ([V10O28]6−). The selected are conjugates of the amide KR12 peptide, smallest antimicrobial peptide derived from human cathelicidin LL-37, with lauric acid (C12-KR12) myristic (C14-KR12). smaller sizes C12-KR12 C14-KR12 compared proteins allow for rigorous characterization their non-covalent highly...

Candidiasis belongs to common fungal infections and is usually mild self-limiting. However, in patients with immunodeficiencies, it can transform into invasive high mortality. Long-term antifungal treatment lead the emergence of resistance. The problem further complicated by development biofilm resistant conventional antimicrobials. Due a limited choice available antifungals, novel active agents, such as antimicrobial peptides (AMPs), highly desirable. Human cathelicidin LL-37 an intensively...

Increasing drug resistance of common pathogens urgently needs discovery new effective molecules. Antimicrobial peptides are believed to be one the possible solutions this problem. One approaches for improvement biological properties is reversion sequence (retro analog concept). This research based on investigation antimicrobial activity against Gram-positive, Gram-negative bacteria, and fungi, hemolysis erythrocytes, interpretation circular dichroism spectra, measurement counter-ion content,...

We investigated cytotoxic activity of antimicrobial peptides different origin (both naturally occurring and synthetic), structure known mechanisms action against human histiocytic lymphoma cell line U937. The strongest U937 was shown by Pexiganan MSI-78, followed Citropin 1.1, Protegrin 1 a synthetic lipopeptide, N-α-palmitoyl-L-lysyl-L-lysine amide (Pal-Lys-Lys-NH₂). the more dependent on time incubation than concentration. Only for whose mode restricted to disruption electric potential...

Antimicrobial research is being focused to look for more effective therapeutics against antibiotic-resistant infections caused by methicillin-resistant Staphylococcus aureus (MRSA). In this direction, antimicrobial peptides (AMP) appear as promising tool.This study evaluated the activity of different AMPs (Citropin 1.1, Temporin A, Pexiganan, CA(1-7)M(2-9)NH2, Pal-KGK-NH2, Pal-KKKK-NH2, LL-37) human MRSA clinical isolates.The Minimum Inhibitory Concentration (MIC) was assessed each AMP;...

Antimicrobial peptides (AMPs) are compounds widely distributed in nature that display activity against a broad spectrum of pathogens. Amphibian skin, as an organ rich pharmacologically active peptides, appears to be interesting source novel AMPs. Aurein 1.2 (GLFDIIKKIAESF-NH2) is short 13-residue antimicrobial peptide primarily isolated from the skin secretions Australian bell frogs. In this study, alanine scan aurein was performed investigate effect each amino acid residue on its biological...

Overview: The global spread of antibiotic resistance represents a serious threat for public health. Aim: We evaluated the efficacy antimicrobial peptide LL-37 as agent against multidrug-resistant Escherichia coli. Results: showed good activity mcr-1 carrying, extended spectrum β-lactamase- and carbapenemase-producing E. coli (minimum inhibitory concentration, MIC, from 16 to 64 mg/l). Checkerboard assays demonstrated synergistic effect LL-37/colistin combination all tested strains, further...

Protease inhibition has become a possible new approach in inflammatory bowel disease (IBD) therapy. A serine exopeptidase, dipeptidyl peptidase IV (DPP IV), is responsible for the inactivation of incretin hormone, glucagon-like peptide 2 (GLP-2), potent stimulator intestinal epithelium regeneration and growth. Recently, we showed that novel analog endomorphin-2, Tyr-Pro-D-ClPhe-Phe-NH₂ (EMDB-1) blocker DPP an inhibitory effect on gastrointestinal (GI) smooth muscle contractility....

The minimum inhibitory concentrations (MICs), the minimal fungicidal (MFCs), fungal biomass (FB) and hyphal viability employing dye 3-4,5 dimethyl- 2-thiazolyl- 2,5- diphenyl- 2H tetrazolium bromide (MTT) were used to compare in vitro effects of fluconazole (FLU) with those N-terminal palmitoyl-lipidated peptide, Pal-Lys-Lys-NH(2) (PAL), a tea tree oil component, gamma-Terpinene (TER), against several clinical isolates Microsporum canis Trichophyton rubrum. In general, FLU PAL MICs...

Pharmacological treatment and/or maintenance of remission in inflammatory bowel disease [IBD] is currently one the biggest challenges field gastroenterology. Here we aimed to assess anti-inflammatory effect and mechanism action sialorphin, natural blocker endogenous opioid peptide-degrading enzymes neprilysin [NEP] aminopeptidase N [APN], mouse models IBD changes expression these patients.We used two experimental colitis mice [2,4,6-trinitrobenzene sulphonic acid [TNBS]- dextran sulphate...

Antimicrobial research is being focused to look for more effective therapeutics against antibiotic-resistant infections such as those caused by methicillin-resistant Staphylococcus aureus (MRSA). In this regard, antimicrobial peptides (AMPs) appear be a promising solution. The aim of the present study was investigate potential activity temporin A, citropin 1.1, CA(1-7)M(2-9)NH2 and Pal-KGK-NH2 in synergistic MRSA biofilms developed on polystyrene surface (PSS) central venous catheter...

LL-37 is the only human antimicrobial peptide that belongs to cathelicidins. The aim of study was evaluate efficacy in management MRSA-infected surgical wounds mice.A wound on back adult male BALB/c mice made and inoculated with Staphylococcus aureus. Two control groups were formed (uninfected not treated, C0; infected C1) six contaminated respectively, with: teicoplanin, LL-37, given topically /or systemically. Histological examination VEGF expression micro-vessel density, bacterial...

The natural antimicrobial cationic peptide protegrin-1 displays a broad spectrum of activity and rapidly kills pathogens by interacting with their cell membrane. We investigated the structure-activity relationships three analogues: IB-367 (RGGLCYCRGRFCVCVGR-NH(2)), BM-1 (RGLCYCRGRFCVCVG-NH(2)) BM-2 (RGLCYRPRFVCVG-NH(2)). Our antifungal studies these peptides showed that was much more active than against Gram-positive bacteria fungi, whereas inactive. fourfold reduced haemolysis relative to...

Aim: The pharmacotherapy of inflammatory bowel disease is difficult and currently available treatments bring mostly poor unsatisfactory results. Results: purpose this work was the synthesis opiorphin, sialorphin, spinorphin a series their analogs in vitro characterization effect on degradation enkephalin by neutral endopeptidase aminopeptidase N. Consequently, we investigated vivo anti-inflammatory most active inhibitors selected studies (Pal-KKQRFSR & Pal-KKQHNPR). Putative inhibitor –...

Opiorphin and sialorphin are two recently discovered endogenous enkephalin‐degrading enzyme inhibitors. Our aim was to characterize their effect on the mouse ileum motility investigate role of glutamine in position 1. Opiorphin, sialorphin, analogs substituted 1 with pyroglutamic acid (pGlu) were synthesized by solid‐phase method using Fmoc chemistry. The peptides gastrointestinal (GI) characterized vitro assays model upper GI transit. but not analogs, significantly increased electrical...

Summary The occurrence of resistance or side effects in patients receiving antifungal agents leads to failure the treatment mycosis. aim this experimental study was investigate vitro IB ‐367 alone and combination with three standard drugs, fluconazole ( FLU ), itraconazole ITRA ) terbinafine TERB against 20 clinical isolates dermatophytes belonging species. Minimum inhibitory concentrations MIC s), minimal fungicidal MFC synergy test, time‐kill curves, fungal biomass FB hyphal damage using...