In vitro and in vivo evaluation of chitosan-alginate/gentamicin wound dressing nanofibrous with high antibacterial performance

Wound dressings based on nanofiber polymer scaffolds with good antimicrobial performance and skin reconstruction ability are promising options to thwart wound infection and accelerate wound healing. This paper reports on the synthesis via electrospinning of chitosan-alginate (CS-Alg) nanofiber dressings with various amounts of gentamicin (Gn; 0–10 wt%) as a drug delivery system. Smooth and continuous nanofibers with no obvious beads were created, with increases in the amount of Gn resulting in reduced fiber diameter. Antimicrobial tests showed the Gn-loaded nanofibers had good antibacterial performance as indicated by the inhibition of bacterial growth. CS-Alg nanofibers loaded with higher Gn concentrations exhibited greater antibacterial performance than those with lower Gn concentrations. In vitro cell culture studies demonstrated that CS-Alg wound dressings with 1–3% Gn improved L929 cell attachment and proliferation more than wound dressings with higher Gn concentrations. In vivo experiments revealed that Cs-Alg nanofibers loaded with 3% Gn significantly enhanced skin regeneration in a Balb/C mice model by stimulating the formation of a thicker dermis, increasing collagen deposition, and increasing the formation of new blood vessels and hair follicles. Collectively, Gn-loaded CS-Alg wound dressings can be considered a good candidate for drug delivery systems and skin regeneration applications.     

Synthesis and antibacterial activity of methylated N-(4-N,N-dimethylaminocinnamyl) chitosan chloride

The methylated chitosan containing different aromatic moieties were synthesized by two steps, the reductive amination and the methylation. The chemical structures of all methylated derivatives, methylated N-(4-N,N-dimethylaminocinnamyl) chitosan chloride (MDMCMCh), methylated N-(4-pyridylmethyl) chitosan chloride (MPyMeCh), and N,N,N-trimethyl chitosan chloride (TMChC) were characterized by ATR-FTIR and ¹H NMR spectroscopy. The molecular weights of the methylated chitosan derivatives were determined by gel permeation chromatography. The results revealed that the molecular weights of chitosan and N-aryl chitosan derivatives could be reduced by the methylation process. The degree of N-substitution (DS) and the degree of quaternization (DQ) were calculated by ¹H NMR ranged from 50% to 76%, and 28% to 82%, respectively. The water solubility of the methylated chitosan derivatives decreased with increasing concentration and pH. The antibacterial studies of these methylated chitosan derivatives were carried out by using minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) methods against Escherichia coli ATCC 25922 (Gram-negative) and Staphylococcus aureus ATCC 6538 (Gram-positive) bacteria. It was found that the MDMCMCh showed higher antibacterial activity than TMChC while MPyMeCh exhibited reduced antibacterial activity against both bacteria at the same DQ level. In comparison to each of the chemical structure, it was found that the antibacterial activity was not only dependent on the DQ but it was also dependent on the positively charged location and the molecular weight.     

Biosynthesis of Bixa orellana seed extract mediated silver nanoparticles with moderate antioxidant,antibacterial and antiproliferative activity

Biosynthesis of metallic silver nanoparticles (AgNPs) has gained much interest and offers an attractive alternate to physical and chemical approaches. In recent year several safe, easy, cost-effective, reproducible, and environmentally friendly synthesis approaches for silver nanoparticles have been developed. In this research work, a simple, cheap, and unexplored method was applied on green synthesis of AgNPs using secondary metabolites extracted from Bixa orellana seeds. The seeds are rich of flavonoids and phenolic compounds which presumably responsible for the fast reduction and stabilization of silver ion into silver nanoparticles. The biosynthesis process is very likely to be able to reduce silver ions under simple physiological conditions. The surface plasmon resonance (SPR) that was appeared at 420 nm in UV–vis spectrum, had confirmed the formation of AgNPs. Moreover, the functional groups in secondary metabolite that act as reducing, capping and stabilizing agents for silver nanoparticles, are identified by Fourier transform infrared (FTIR) spectra. An X-ray diffraction analysis generated four peaks for Bixa orellana seed extract mediated AgNPs positioned at 2θ angles of 38.1°, 44.2°, 64.6°, and 77.5° corresponding to crystal planes (1 1 1), (2 0 0), (2 2 0), and (3 1 1). Field emission scanning electron microscope (FESEM) and transmission electron microscopy (TEM) images confirmed the formation of nanosized silver particles. The z-average of the synthesized particles measured by dynamic light scattering (DLS) was found to be 92.9 nm. AgNPs synthesized exhibited remarkable antioxidant activity, antibacterial and antiproliferative activity against human breast (MCF-7) cell line. On the basis of our results, we conclude that biologically synthesized AgNPs exhibited favorable characteristics and have the potential to be used in biomedical fields.     

Synthesis of new water soluble diorganotin(IV) complexes with hydrazones derived from Girard-T reagent as antibacterial and anticancer agents

Three new water-soluble organotin complexes R₂Sn(5-BrSalGT)Cl [R = Ph, Me] and Ph₂Sn(2-OHNaphGT)Cl have been synthesized by the reaction of R₂SnCl₂ (R = Ph or Me) with Schiff bases derived from condensation of Girard-T reagent with 5-bromosalicylaldehyde and 2-naphthaldehyde, (5-BrH₂SalGT)Cl (1) and (2-OHH₂NaphGT)Cl (2). The synthesized compounds have been investigated by elemental analysis, conductometric measurements, IR, ¹H NMR, and ¹¹⁹Sn NMR spectroscopy. These data show that the deporotonated ligand is coordinated to Sn(IV) via ONO atoms and six-coordinate zwitterionic complexes are formed. The ligands and their complexes were investigated for their in vitro toxicity against Gram-positive (Bacillus subtilis and Staphylococcus aureus) and Gram-negative (Escherichia coli and Pseudomonas aeruginosa) bacteria. The results show remarkable antibacterial activity against the studied bacteria. All complexes exhibit more inhibitory effects than the parent ligand. The anticancer activity of all compounds were also performed on HN5 cell line and (2-OHH₂NaphGT)Cl with concentration of 1 mg mL^?1 was found to show higher anticancer activity than other compounds.     

新型磷钨酸盐的合成、表征及其抑菌性能研究

甲壳低聚糖具有广谱抗菌性,对日常生活中特别是食品中一些常见的细菌、霉菌、酵母菌具有抑制作用,在抗菌抑菌方面具有很好前景[1]。杂多化合物是一类以氧原子桥联的多核配合物,由杂多阴离子、反荷阳离子及结晶水构成。一般具有大的分子体积、高分子量、好的电子和质子的传输作用和贮备能力、高的热稳定性等方面的独特性质[2]。20世纪80年代末,Yamase等[3]报道了Keggin结构钨系杂多化合物具有抗艾滋病毒活性,从而掀起了多酸化合物药物化学应用研究的高潮[4-8]。本文采用液相法将磷钨酸引入甲壳低聚糖中,合成了新型磷钨酸盐。对该盐进行红外…     

Synthesis,crystal structure,and antibacterial activity of two new mononuclear nickel(II) complexes of a NNS Schiff base

Two new mononuclear nickel(II) complexes, [Ni(L)(N₃)] (1) and [Ni(L)₂(NCS)₂] (2), where HL = 2-{[phenyl(pyridin-2-yl)methylidene]amino}benzenethiol, a tridentate Schiff base derived from 2-aminothiophenol and 2-benzoylpyridine, have been prepared and characterized. The syntheses of 1 and 2 have been achieved by the reaction of equimolar amounts of nickel perchlorate and HL in the presence of azide and thiocyanate, respectively. The complexes have been characterized by microanalytical, spectroscopic, single-crystal X-ray diffraction, and other physicochemical studies. Structural studies reveal that 1 and 2 adopt two different geometries, distorted square planar in 1 and octahedral in 2. The two mononuclear complex units are held together by π…π or C–H…π weak intermolecular interactions to develop supramolecular networks in their solid states. The antibacterial activity of 1, 2 and their constituent Schiff base has been tested against some gram(+) and gram(?) bacteria.     

Modification of fumed silica surface with different sulfonamides via a postsynthesis method and their application as antibacterial agents

The surface of nanosized fumed silica (FSi) was modified with different amine groups by the use of silylating agents. The obtained propylamine, propylpiperazine, and propyl-p-phenylenediamine–modified FSi were treated with different sulfonyl chlorides to gain sulfonamide-modified FSi compounds. These compounds were characterized by various techniques including Fourier transform infrared spectroscopy, thermogravimetric analysis, differential thermal analysis, scanning electron microscopy, and energy-dispersive X-ray spectroscopy (EDX), confirming the grafted sulfonamides on the FSi surface. Sulfonamide-modified surfaces are efficient catalysts for the Michael addition-based syntheses and coupling reactions. Furthermore, the antibacterial tests showed that these modified FSi compounds have antibacterial activities and thus are useful materials for preparing antibacterial silicone-based compounds such as silicone glue and oil.     

Biosynthesis of ZnO nanoparticles through extract from Prosopis juliflora plant leaf: Antibacterial activities and a new approach by rust-induced photocatalysis

Rust-induced photocatalytic and antibacterial activities of ZnO nanoparticles derived from Prosopis juliflora leaf extracts by biosynthesis using the hydrothermal method at 170 °C are reported in this study. The characterization has been accomplished by various methods such as XRD, DRS, FT-IR, SEM, TEM, EDAX, and PL spectra. XRD exhibits that ZnO has a hexagonal wurtzite structure with a preferred orientation of 101 planes. The functional groups, which are present in the leaf extracts, are responsible for corresponding peaks in FT-IR spectra. The FESEM images of the synthesized nanoparticles show the morphology sphere like structure. ZnO particle size of 65 nm has been observed from HR-TEM analysis. The elemental composition has a good agreement with the biosynthesized ZnO nanoparticles. The antibacterial activities have been carried out in vitro assays against four different pathogens viz Escherichia coli (E. coli), Rhodococcus rhodochrous (R. rhodochrous), Bacillus subtilis (B. subtilis) and Vibrio cholera (V. Cholera) against a standard (streptomycin sulfate). Furthermore, the Photocatalytic ability of the titled nanoparticles has been experimented from the rust solution with methylene blue and degradation under UV radiation of 99%. The proposed mechanism is based on scavenger studies and it is investigated during the photo degradation of Methylene blue. The catalytic amount and recovery of photocatalyst have also been studied in detail.     

Synthesis,characterization, and anticancer activity of some metal complexes with a new Schiff base ligand

A new Schiff base ligand, 2-((E)-((4-(((E)-benzylidene)amino)phenyl)imino)methyl)-naphthalene-1-ol, was prepared by the reflux condensation of p-phenylenediamine with 2-hydroxy-1-naphthaldehyde and benzaldehyde. Metal complexes were prepared by reacting the ligand with metal salts: VCl₃, CrCl₃·6H₂O, MnCl₂·3H₂O, FeCl₃·6H₂O, CoCl₃·6H₂O, NiCl₂·6H₂O, CuCl₂·2H₂O, and ZnCl₂. The ligand and its metallic complexes were characterized by various techniques such as elemental analysis, AAS, NMR, IR, UV–Vis, TGA, DTA, XRD and TEM. The data confirmed that the ligand coordinated with the metal ions in a bidentate nature, bonding through its azomethine nitrogen atom and phenolic oxygen atom; this gave an octahedral geometry. The XRD patterns of the complexes indicated that they were of various structures: the Mn(II), Co(III), and Cu(II) complexes were triclinic, the ligand and Ni(II) complex were orthorhombic, the V(III) and Zn(II) complexes were hexagonal, the Cu(II) complex was monoclinic, and the Fe(II) complex was cubic. TEM analysis confirmed that the complexes were nanoscale in nature. The antibacterial and antifungal activities of the ligand and its complexes against Salmonella enterica serovar typhi and Candida albicans were investigated by the hole plate diffusion method. It was observed that the Co(II) and Zn(II) complexes had intermediate antibacterial activities, while the V(III) complex had the highest activity against C. albicans fungi. The in vitro anticancer activities of the ligand and its metal complexes were tested towards PC-3, SKOV3, and HeLa tumour cell lines, where they exhibited higher antitumour activities against these selected human cell lines than clinically used drugs such as cisplatin, estramustine, and etoposide.     

Chemical,spectroscopic characterization,and in vitro antibacterial studies of a new gold(I) complex with N-acetyl-L-cysteine

A new gold(I) complex with N-acetyl-L-cysteine was synthesized and characterized by chemical and spectroscopic techniques. The elemental and thermal analyses of the solid compound fit to the composition AuC₅H₈NO₃S · 0.75H₂O. Solid-state ¹³C-nuclear magnetic resonance (SSNMR) and infrared (IR) analyses indicate the coordination of the ligand to Au(I) through sulfur. The insolubility of the complex in both polar and non-polar solvents supports a polymeric structure. The antibacterial activity of the complex was evaluated by antibiogram assays using the disc diffusion method. The compound showed effective antibacterial activity against Staphylococcus aureus (Gram positive) and Escherichia coli (Gram negative) bacterial cells.     

Cytocompatibility and antibacterial activity of a PHBV membrane with surface-immobilized water-soluble chitosan and chondroitin-6-sulfate

A water-soluble chitosan (WSC)/chondroitin-6-sulfate (ChS) polyelectrolyte complex (PEC) is covalently immobilized onto the surface of poly(3-hydroxybutyric acid-co-3-hydroxyvaleric acid) (PHBV) membranes via ozone-induced oxidation and poly(acrylic acid) (PAA) graft polymerization. To characterize the modified membranes, X-ray photoelectron spectroscopy (XPS) and water contact angle measurements are performed. It is shown that by coupling WSC as a spacer, the amount of ChS immobilized can be significantly increased. The water contact angle decreases with the amount of PAA, WSC, and ChS immobilized, which indicates the improving hydrophilicity. After WSC- and PEC-immobilization modification, the PHBV membranes possess antibacterial activity against S. aureus, E. coli, P. aeruginosa, and Methicilin resistant Staphylococus aureus (MRSA). According to the L929 fibroblast cell growth inhibition index, the as-prepared PHBV membranes are non-cytotoxic. In addition, the in-vitro evaluation of L929 fibroblast attachment, proliferation, and viability of PEC-immobilized PHBV membranes are ascertained to be superior to those of immobilized WSC or ChS alone. The overall results demonstrate that WSC/ChS PEC immobilization can not only improve the hydrophilicity and cytocompatibility of the PHBV membrane, but also endows antibacterial activity. [GRAPH: SEE TEXT] The bacterial survival ratio of as-prepared PHBV membranes (n=3).     

Syntheses, structural and antimicrobial studies of a new N-allylamide of monensin A and its complexes with monovalent metal cations

A new N-allylamide of monensin A (M-AM2) was synthesized and its capacity to form complexes with Li⁺, Na⁺ and K⁺ cations was studied by ESI MS, ¹H and ¹³C NMR, FTIR spectroscopy and PM5 semi-empirical methods. ESI mass spectrometry indicates that M-AM2 forms complexes with Li⁺, Na⁺ and K⁺ of exclusively 1:1 stoichiometry which are stable up to cv=70 V, and the formation of 1:1 complexes between M-AM2 and Na⁺ cations is strongly favoured. Above cv=90 V we observe fragmentation of the respective complexes involving several dehydration steps. The spectroscopic studies show that the structures of the M-AM2 and its complexes with Li⁺, Na⁺ and K⁺ cations are stabilized by intramolecular hydrogen bonds in which the OH groups are always involved. The data also demonstrate that the CO amide group is engaged in the complexation process of each cation. However with the K⁺ cation we also found a structure in which this CO amide group does not participate in the complexation to a significant extent. The in vitro biological tests of M-AM2 amide show its good activity towards some strains of Gram-positive bacteria (Giz 13-19 mm; MIC 25-100 μg/ml).     

Synthesis,characterization, density functional theory studies and antibacterial activity of a new Schiff base dioxomolybdenum(VI) complex with tryptophan as epoxidation catalyst

A cis ‐dioxomolybdenum(VI) complex was prepared with MoO₂(acac)₂ and a Schiff base ligand (2‐((2‐hydroxybenzylidene)amino)‐3‐(1H ‐indol‐3‐yl)propanoic acid) derived from salicylaldehyde and l ‐tryptophan in ethanol and designated as [MoO₂(Sal‐Tryp)(EtOH)]. It was characterized using several techniques including thermogravimetric and elemental analyses and mass, Fourier transform infrared and UV–visible spectroscopies. Theoretical calculations were performed using density functional theory for studying the molecular structure. An in vitro antibacterial activity evaluation showed that [MoO₂(Sal‐Tryp)EtOH] complex exhibits good inhibitory effects against Gram‐positive (Bacillus subtilis , Staphylococcus aureus ) and Gram‐negative (Escherichia coli , Pseudomonas aeruginosa ) bacteria in comparison to standard antibacterial drugs. It was also found that [MoO₂(Sal‐Tryp)EtOH] complex successfully catalyses the epoxidation of cyclooctene, norbornene, cyclohexene, styrene, α‐methylstyrene and trans ‐stilbene, with 45–100% conversions and 64–100% selectivities. Based on the obtained results, the heterogeneity and reusability of the catalyst seem promising.     

Comparison of mouse plasma and brain tissue homogenate sample pretreatment methods prior to high‐performance liquid chromatography for a new 1,2,4‐triazole derivative with anticonvulsant activity

The focus of the study was to develop a bio‐analytical assay for a 1,2,4‐triazole derivative from plasma and brain tissue homogenate samples. The goal was to compare analytical techniques that facilitate high accuracy with simplified sample processing. In this study, commonly used standard protein precipitation and solid‐phase extraction methods utilizing C₁₈ and cartridges of Hybrid technology were compared in terms of their ability for sample pretreatment and removal of biological matrices before high‐performance liquid chromatography quantification. Fast classical reversed‐phase chromatography on a C₁₈ column paired with selective sample preparation using Hybrid solid‐phase extraction technology resulted in the most precise bio‐analytical determination of the hydrophobic 1,2,4‐triazole derivative in both biological samples studied. The obtained recovery values were above 95% with the coefficient of variation lower than 5%.     

Synthesis, Characterization, Crystal Structure and Antibacterial Activities of a Nickel(Ⅱ) Complex with 2''-(2-Thienylidene)-hydroxybenzoylhydrazide

In the ethanol solvent, a nickel(Ⅱ) complex Ni(C12H10N2O2S)2 upon reaction of 2'-(2-thienylidene)-hydroxybenzoylhydrazide with nickel acetate was synthesized, and its structure was characterized by IR, UV, elemental analysis and X-ray diffraction analysis. The crystal belongs to monoclinic system, space group C2/c with a = 22.052(3), b = 5.9681(6), c = 18.522(2) (A), β = 110.679(4)° , V = 2280.6(4) (A)3, Z = 4, Mr = 551.27, μ = 1.606 mm-1, Dc = 1.075 g/cm3, F(000) = 1136 and Rint = 0.0556. The nickel(Ⅱ) atom in the compound is four-coordinated with two nitrogen atoms from amide and two oxygen atoms from keto group. The biological activities have been measured, show- ing the compound exhibits better anti-bacterial activity than the ligand.