A new generation of triazine-based coupling reagents (TBCRs), designed according to the concept "superactive esters", was obtained by treatment 4-(4,6-dimethoxy-1,3,5-triazin-2-yl)-4-methylmorpholinium (DMTMM) chloride with lithium or silver tetrafluoroborate. The structure tetrafluoroborate confirmed X-ray diffraction. Activation carboxylic acids using this reagent proceeds via triazine ester". successfully used for synthesis Z-, Boc-, and Fmoc-protected dipeptides derived from natural...

Cellular drug delivery can improve efficacy and render intracellular pathogens susceptible to compounds that cannot permeate cells. The transport of physiologically active across membranes into target cells be facilitated by cell-penetrating peptides (CPPs), such as oligoarginines. Here, we investigated whether the fosmidomycin improved combination with CPP octaarginine. Fosmidomycin is an antibiotic inhibits second reaction in nonmevalonate pathway isoprenoid biosynthesis, essential for...

Hydrogel materials based on sodium alginate find versatile applications in regenerative medicine and tissue engineering due to their unique properties, such as biocompatibility biodegradability, the possibility of customization mechanical terms individual requirements separate clinical applications. These materials, however, have numerous limitations area biological activity. In order eliminate limitations, is popularly applied combination with added gelatin, which represents a product...

In light of searching for new breast cancer therapies, DNA-targeted small molecules were rationally designed to simultaneously bind DNA and inhibit human dihydrofolate reductase (hDHFR). Fourteen arylidene-hydrazinyl-1,3-thiazoles (5–18) synthesised their dual groove binding potential in vitro hDHFR inhibition performed. Two compounds, 5 11, proved efficacy. Molecular docking molecular dynamics simulations performed those active derivatives explore mode stability interactions inside DHFR...

Abstract A collection of N ‐triazinylammonium sulfonates, designed according to the concept “superactive esters”, was obtained by treatment ammonium sulfonates with 2‐chloro‐4,6‐dimethoxy‐1,3,5‐triazine. The structure tertiary amine as well sulfonate anion influenced their reactivity and stability in , ‐dimethylformamide (DMF) solution. reagents were successfully used solution‐ solid‐phase synthesis Z‐, Boc‐, Fmoc‐protected peptides containing natural unnatural sterically hindered amino...

Algae are employed commonly in cosmetics, food and pharmaceuticals, as well feed production biorefinery processes. In this study, post-fermentation leachate from a biogas plant which exploits stillage maize silage was utilized culture medium for Chlorella vulgaris. The content of polyphenols hydrophilic extracts the vulgaris biomass determined, were evaluated their antioxidant activity (DPPH assay), antibacterial (against Escherichia coli, Lactobacillus plantarum, Staphylococcus aureus,...

Carbon-based nanomaterials (CBN) are currently used in many biomedical applications. The research includes optimization of single grain size and conglomerates pure detonated nanodiamond (DND), modified particles graphene oxide (GO) order to compare their bactericidal activity against food pathogens. Measurement zeta potential was performed using the Dynamic Light Scattering (DLS) method. Surface morphology evaluated a Scanning Electron Microscope (SEM) confocal microscope. X-ray diffraction...

Antibiofilm strategies may be based on the prevention of initial bacterial adhesion, inhibition biofilm maturation or eradication. N-acetyl-L-cysteine (NAC), widely used in medical treatments, offers an interesting approach to destruction. However, many Eubacteria strains are able enzymatically decompose NAC molecule. This is first report action two hybrid materials, NAC-Si-1 and NAC-Si-2, against bacteria isolated from a water environment: Agrobacterium tumefaciens, Aeromonas hydrophila,...

A thorough study of the exosomal proteomic cargo may enable identification proteins that play an important role in cancer development. The aim this was to compare protein profiles serum exosomes derived from non-small lung (NSCLC) patients and healthy volunteers (control) using high-performance liquid chromatography coupled mass spectrometry (HPLC-MS) method identify potentially new diagnostic and/or prognostic biomarkers. Proteins exclusively identified NSCLC control groups were analyzed...

The extracellular matrix (ECM) can be a convenient scaffold used in tissue engineering, regenerative medicine and pharmacy. synthetic cell should imitate the natural both composition architecture. study examined fibrous chitosan modified with fragments of human collagen I (10–15 amino acids) mimicking internal sphere native protein. surface fibers was by physical chemical methods to obtain polysaccharide-peptide conjugates, which may considered analogous complex glycosaminoglycans (GAG)...

Abstract Cell‐penetrating peptides (CPPs) are promising vehicles for delivery of drugs, antibiotics, proteins, nucleic acid derivatives, etc. into eukaryotic and prokaryotic target cells. To prevent premature degradation, CPPs consisting D ‐ or β ‐amino residues have been used. We present simple models the various modes physiologically active cargoes by CPPs, depending on nature their conjugation ( Fig. 1 ), we describe plasma stability oligoarginines (OAs) – 4 , most common unnatural CPPs....

Abstract After a survey of the special role, which amino acid proline plays in chemistry life, cell‐penetrating properties polycationic proline‐containing peptides are discussed, and widely unknown discovery by Giralt group ( J. Am. Chem. Soc. 2002 , 124 8876) is acknowledged, according to fluorescein‐labeled tetradecaproline slowly taken up rat kidney cells (NRK‐49F). Here, we describe details our previously mentioned Biodiversity 2004 1 1111) observation that hexa‐ β 3 ‐Pro derivative...

Catalytic systems based on bimetallic Pd-Au particles deposited SiO2 were prepared by ultrasonically assisted water impregnation and used in the hydrogenation of furfural obtained acidic hydrolysis waste biomass (brewery’s spent grain) aqueous phase. Pd-Au/SiO2 catalysts containing 50 g Pd 2–100 Au per 1 kg catalyst characterized high activity studied process and, depending Pd/Au ratio, selectivity to 2-methyloxolan-2-ol. The modification 5%Pd/SiO2 leads formation dispersed Au-Pd solid...

Pulcherrimin, a red iron chelate, is produced by some yeasts and bacteria. It plays important ecological roles in many ecosystems, including growth control, biofilm inhibition photoprotection. In this study, fifteen yeast strains of the genus Metschnikowia were characterized based on their production pulcherrimin. Yeast pulcherrimin was isolated its purity assessed using 1H nuclear magnetic resonance spectroscopy. Under experimental conditions, formation varied depending both tested culture...

A series of new analogs nitrogen mustards (4a–4h) containing the 1,3,5-triazine ring substituted with dipeptide residue were synthesized and evaluated for inhibition both acetylcholinesterase (AChE) β-secretase (BACE1) enzymes. The AChE inhibitory activity studies carried out using Ellman’s colorimetric method, BACE1 fluorescence resonance energy transfer (FRET). All compounds displayed considerable inhibition. most active against enzymes 4a, an concentration IC50 = 0.051 µM; 0.055 µM 9.00...

Bone tissue defects resulting from periodontal disease are often treated using guided regeneration (GTR). The barrier membranes utilized here should prevent soft infiltration into the bony defect and simultaneously support bone regeneration. In this study, we designed a degradable poly(l-lactide-co-glycolide) (PLGA) membrane that was surface-modified with cell adhesive arginine-glycine-aspartic acid (RGD) motifs. For novel method of manufacture, RGD motifs were coupled non-ionic amphiphilic...

Abstract Review with 101 refs. of progress in synthetic applications and properties P-acylphosphonium salts including acylation via salts, enantioselective using chiral phosphine ligands, nucleophilic (β)-oniovinylation, reaction involving vinyloges formed by treatment conjugated alkenoates or alkynoates phosphines.

Abstract Neurotensin(8–13) (NTS(8–13)) analogs with C‐ and/or N‐terminal β ‐amino acid residues and three DOTA derivatives thereof have been synthesized ( i.e. , 1 – 6 ). A virtual docking experiment showed almost perfect fit of one the 1,4,7,10‐tetraazacyclododecane‐1,4,7,10‐tetraacetic (DOTA) derivatives, 6a into a crystallographically identified receptor NTSR1 Fig. The affinities for receptors NTS are low, when determined cell‐membrane homogenates, while, NTSR1‐exhibiting cancer tissues,...