Tragacanth gum-based copper oxide nanoparticles: Comprehensive characterization, antibiofilm, antimicrobial and photocatalytic potentials.

Hereunder, we pioneered the synthesis of Copper Oxide nanoparticles (CuO NPs) utilizing Tragacanth gum (TG). The NPs were characterized using advanced techniques and assessed for different pharmaceutical and environmental perspectives. The successful formation of a colloidal NPs solution was confirmed by the appearance of a distinct black color and a distinct peak at 260 nm in UV-Visible spectrophotometry. The FTIR analysis unveiled a spectrum of functional groups responsible for the reduction and stabilization of CuO NPs. Dynamic Light Scattering (DLS) and Transmission Electron Microscopy (TEM) revealed size of NPs as 36.24 nm and 28 ±â€¯04 nm respectively. Energy Dispersive X-ray (EDX) Analysis indicated weight percentages of 70.38 % for Cu and 18.88 % for O, with corresponding atomic percentages. The X-ray Diffraction (XRD) analysis revealed the orthorhombic crystal structure of the prepared CuO NPs. Antimicrobial assessments through disc-diffusion assays demonstrated significant zones of inhibition (ZOI) against gram-positive bacterial strains (Bacillus Halodurans and Micrococcus leutus) and a gram-negative bacterial strain (E. coli). Against the fungal strain Aspergillus niger, a ZOI of 18.5 ±â€¯0.31 mm was observed. The NPs exhibited remarkable antioxidant potential determined through 2,2-Diphenyl-1-picrylhydrazyl (DPPH) and H2O2 scavenging assays. At a concentration of 3 mg/mL, the NPs demonstrated biofilm inhibition rates of 96 %, 90 %, 89.60 %, and 72.10 % against Micrococcus luteus, Bacillus halodurans, MRSA and E.coli respectively. Furthermore, the CuO NPs showed a high photocatalytic potential towards the degradation of safranin dye under sunlight irradiation. In conclusion, the findings underline the promising multifunctional properties of TG-based CuO NPs for different practical applications.

Obliteration of H. pylori infection through the development of a novel thyme oil laden nanoporous gastric floating microsponge.

Thyme oil (TO) is a valuable essential oil believed to possess a variety of bioactivities, including antibacterial, anticancer, and antioxidant properties. These attributes grant TO the excellent capability to treat a wide range of diseases, particularly the effective eradication of Helicobacter pylori infection in the stomach. However, its practical use is limited by its low stability under atmospheric conditions. Our current research aims to encapsulate TO in eudragit (EGT) microsponges to enhance its stability and improve its effectiveness against H. pylori. The TO microsponges were prepared using EGT as a polymer, polysorbate 80 as a stabilizer, and dichloromethane (DCM) as a solvent via the quasi-emulsion solvent evaporation method. The product yield, particle size, surface morphology, entrapment efficiency, drug-polymer interaction, in-vitro floating, and in-vitro drug release of the microsponges were evaluated. The most promising microsponge was tested against H. pylori ATCC 43504 strains. The results showed that the microsponges exhibited a high product yield (ranging from 41 % ± 0.75-81.27 % ± 1.13), excellent entrapment efficiency (ranging from 63.01 % ± 0.79-88.64 % ± 0.98), prolonged in-vitro floating time (more than 12 h) and sustained in-vitro drug release for 18 h (81.53 %). Scanning electron microscopy results indicated that the microsponges were spherical in shape with a spongy surface. The average particle size of the selected microsponges was determined to be 49.79 ± 1.4 µm, and their average pore size was measured to be 0.81 ± 0.14 µm. DSC study results revealed that TO was physically entrapped in the microsponges. In-vitro anti-H. pylori activity studies demonstrated that TO in microsponge was more effective against H. pylori than pure TO. In conclusion, the developed microsponges containing thyme oil provide a promising alternative for the efficient targeting and eradication of H. Pylori infection.

"The potential contribution of aquatic wildlife to antibiotic resistance dissemination in freshwater ecosystems: A review".

Antibiotic resistance (AR) is one of the major health threats of our time. The presence of antibiotics in the environment and their continuous release from sewage treatment plants, chemical manufacturing plants and animal husbandry, agriculture and aquaculture, result in constant selection pressure on microbial organisms. This presence leads to the emergence, mobilization, horizontal gene transfer and a selection of antibiotic resistance genes, resistant bacteria and mobile genetic elements. Under these circumstances, aquatic wildlife is impacted in all compartments, including freshwater organisms with partially impermeable microbiota. In this narrative review, recent advancements in terms of occurrence of antibiotics and antibiotic resistance genes in sewage treatment plant effluents source compared to freshwater have been examined, occurrence of antibiotic resistance in wildlife, as well as experiments on antibiotic exposure. Based on this current state of knowledge, we propose the hypothesis that freshwater aquatic wildlife may play a crucial role in the dissemination of antibiotic resistance within the environment. Specifically, we suggest that organisms with high bacterial density tissues, which are partially isolated from the external environment, such as fishes and amphibians, could potentially be reservoirs and amplifiers of antibiotic resistance in the environment, potentially favoring the increase of the abundance of antibiotic resistance genes and resistant bacteria. Potential avenues for further research (trophic transfer, innovative exposure experiment) and action (biodiversity eco-engineering) are finally proposed.

Physicochemical Properties and Biological Activities of Quinoa Polysaccharides.

Quinoa, known as the "golden grain" for its high nutritional value, has polysaccharides as one of its sources of important nutrients. However, the biological functions of quinoa polysaccharides remain understudied. In this study, two crude polysaccharide extracts of quinoa (Q-40 and Q-60) were obtained through sequential precipitation with 40% and 60% ethanol, with purities of 58.29% (HPLC) and 62.15% (HPLC) and a protein content of 8.27% and 9.60%, respectively. Monosaccharide analysis revealed that Q-40 contained glucose (Glc), galacturonic acid (GalA), and arabinose (Ara) in a molar ratio of 0.967:0.027:0.006. Q-60 was composed of xylose (xyl), arabinose (Ara), galactose, and galacturonic acid (GalA) with a molar ratio of 0.889:0.036:0.034:0.020. The average molecular weight of Q-40 ranged from 47,484 to 626,488 Da, while Q-60 showed a range of 10,025 to 47,990 Da. Rheological experiments showed that Q-40 exhibited higher viscosity, while Q-60 demonstrated more elastic properties. Remarkably, Q-60 showed potent antioxidant abilities, with scavenging rates of 98.49% for DPPH and 57.5% for ABTS. Antibacterial experiments using the microdilution method revealed that Q-40 inhibited the growth of methicillin-resistant Staphylococcus aureus (MRSA) and Escherichia coli (E. coli), while Q-60 specifically inhibited MRSA. At lower concentrations, both polysaccharides inhibited MDA (MD Anderson Cancer Center) cell proliferation, but at higher concentrations, they promoted proliferation. Similar proliferation-promoting effects were observed in HepG2 cells. The research provides important information in the application of quinoa in the food and functional food industries.

Discovery of Potential Anti-Microbial Molecules and Spectrum Correlation Effect of Ardisia crenata Sims via High-Performance Liquid Chromatography Fingerprints and Molecular Docking.

Ardisia crenata Sims, an important ethnic medicine, is recorded in the Chinese Pharmacopoeia for treating laryngeal diseases and upper respiratory tract infections. This study aimed to evaluate the antimicrobial effect of extracts and potential antimicrobial compounds of A. crenata Sims. It was found that the roots of A. crenata Sims have a potential inhibitory effect on Candida albicans and Aspergillus flavus, with MICs of 1.56 mg/mL and 0.39 mg/mL, and the leaves of A. crenata Sims have a potential inhibitory effect on Pseudomonas aeruginosa and Staphylococcus aureus, with MICs of 3.12 mg/mL and 6.77 mg/mL, respectively. Meanwhile, five compounds including one catechin and four bergenins were obtained from roots. These components were identified on the fingerprint spectrum, representing chromatographic peaks 16, 21, 22, 23, and 25, respectively. Among these, 11-ß-d-glucopyranosyl-bergenin and (-)-gallocatechin showed potential inhibition for Staphylococcus aureus and Pseudomonas aeruginosa with MIC of 0.26 and 0.33 mg/mL, respectively. The roots, stems, and leaves of A. crenata Sims are very similar in chemical composition, with large differences in content. Principal component analysis (PCA) and Hierarchical cluster analysis (HCA) showed that 16 batches of A. crenata Sims could be divided into four main production areas: Guizhou, Jiangsu, Guangxi, and Jiangxi. Furthermore, molecular docking results showed that 11-ß-d-glucopyranosyl-bergenin had a better affinity for Casein lytic proteinase P (ClpP), and (-)-gallocatechin possessed a strong affinity for LasA hydrolysis protease and LasB elastase. These findings suggest catechin and bergenins from A. crenata Sims can be used as antimicrobial activity molecules.

A novel metabolite of Streptomyces coeruleorubidus exhibits antibacterial activity against Streptococcus agalactiae through modulation of physiological performance, inflammatory cytokines, apoptosis, and oxidative stress-correlated gene expressions in Nile tilapia (Oreochromis niloticus).

Using the unique structures found in natural materials to produce new antibacterial drugs is crucial. Actinobacteria is well-known for its ability to produce naturally occurring chemicals with a variety of structural features that can be used as weapons against infectious bacteria. In the present study, the Streptomyces coeruleorubidus metabolites were characterized and their efficacy in suppressing Streptococcus agalactiae growth was carried out both in vitro and in vivo. The metabolites of S. coeruleorubidus were purified and identified as octasiloxane-hexadecamethyl (OHM). In vivo antibacterial activity of OHM revealed an inhibitory minimum concentration value of 0.5 µg/ml against S. agalactiae and induced ultrastructural cell changes revealed by scanning electron microscope. The safe concentration of OHM was determined as 0.8 mg/L for Nile tilapia. Four in vivo treatments were treated with 0 and 0.8 mg/L OHM and with or without challenge by S. agalactiae (1 × 107 CFU/mL) named control, OHM, S. agalactiae, and S. agalactiae + OHM groups. The OHM treatment improved the survival of Nile tilapia by 33.33% than S. agalactiae challenge group. Waterborne OHM treatment significantly mitigated the deleterious effects of S. agalactiae on hematological, hepato-renal functions, stress indicators, and antioxidant balance. OHM significantly alleviated nitric oxide levels, complement 3, IgM, and lysozyme activity, downregulation of liver antioxidant genes expression in S. agalactiae group. Furthermore, the addition of OHM to challenged fish with S. agalactiae-significantly reversed dramatic negative regulation of inflammatory, apoptosis, and immune related gene expression (caspase-3, bax, pcna, tnf-α, ifn-γ, il-8 il-1ß, il-10, tgf-ß, and bcl-2 in the Nile tilapia spleen. Additionally, the damaged hepatic and splenic structure induced by bacterial infection was restored with OHM treatment. Finally, S. coeruleorubidus metabolites (mainly OHM) revealed in vitro and in vivo antibacterial activity and showed alleviated effects on the physiological status of S. agalactiae infected tilapia.

Novel synthesis of new triazine sulfonamides with antitumor, anti-microbial and anti-SARS-CoV-2 activities.

Novel approach for synthesizing triazine sulfonamide derivatives is accomplished via reacting the sulfaguanidine derivatives with N-cyanodithioiminocarbonate. Further reaction of the novel triazine sulfonamide analogues with various secondary amines and anilines generated various substituted triazine sulfonamide analogues of promising broad-spectrum activities including anti-microbial, anti-tumor, and anti-viral properties. The in vitro anti-proliferative activities of most of the novel compounds were evaluated on the NCI-60 cell line panel. The antifungal and antibacterial activities of the compounds were also estimated. The anti-viral activity against SARS CoV-2 virus was performed using MTT cytotoxicity assay to evaluate the half-maximal cytotoxic concentration (CC50) and inhibitory concentration 50 (IC50) of a representative compound from the novel triazine sulfonamide category. Compound 3a demonstrated potent antiviral activity against SARS-CoV-2 with IC50 = 2.378 µM as compared to the activity of the antiviral drug remdesivir (IC50 = 10.11 µM). Our results indicate that, upon optimization, these new triazine sulfonamides could potentially serve as novel antiviral drugs.

Anti-Microbial Activities of Mussel-Derived Recombinant Proteins against Gram-Negative Bacteria.

Many anti-microbial peptides (AMPs) and pro-apoptotic peptides are considered as novel anti-microbial agents, distinguished by their different characteristics. Nevertheless, AMPs exhibit certain limitations, including poor stability and potential toxicity, which hinder their suitability for applications in pharmaceutics and medical devices. In this study, we used recombinant mussel adhesive protein (MAP) as a robust scaffold to overcome these limitations associated with AMPs. Mussel adhesive protein fused with functional peptides (MAP-FPs) was used to evaluate anti-microbial activities, minimal inhibitory concentration (MIC), and time-kill kinetics (TKK) assays against six of bacteria strains. MAP and MAP-FPs were proved to have an anti-microbial effect with MIC of 4 or 8 µM against only Gram-negative bacteria strains. All tested MAP-FPs killed four different Gram-negative bacteria strains within 180 min. Especially, MAP-FP-2 and -5 killed three Gram-negative bacteria strain, including E. coli, S. typhimurium, and K. pneumoniae, within 10 min. A cytotoxicity study using Vero and HEK293T cells indicated the safety of MAP and MAP-FP-2 and -3. Thermal stability of MAP-FP-2 was also validated by HPLC analysis at an accelerated condition for 4 weeks. This study identified that MAP-FPs have novel anti-microbial activity, inhibiting the growth and rapidly killing Gram-negative bacteria strains with high thermal stability and safety.

Unrelenting Infection of Implanted Prosthetic Hip Joint by Corynebacterium striatum.

Non-diphtherial Corynebacterial (NDC) species, while previously considered as culture contaminants, are increasingly being implicated in clinical disease and identified as causes of opportunistic infections. In cases where they grow in pure cultures, isolated from a sterile site or repeated isolations from the same patient, NDC may be labeled as clinically significant. We report here a case of non-healing infection of one of the implanted devices in a case of bilateral total hip replacement, caused by multidrug-resistant Corynebacterium striatum. Adherence to infection prevention strategies is essential for the prevention of prosthetic implant infections.

Antarctic marine sediment as a source of filamentous fungi-derived antimicrobial and antitumor compounds of pharmaceutical interest.

Antarctica harbors a microbial diversity still poorly explored and of inestimable biotechnological value. Cold-adapted microorganisms can produce a diverse range of metabolites stable at low temperatures, making these compounds industrially interesting for biotechnological use. The present work investigated the biotechnological potential for antimicrobial and antitumor activity of filamentous fungi and bacteria isolated from marine sediment samples collected at Deception Island, Antarctica. A total of 89 microbial isolates were recovered from marine sediments and submitted to an initial screening for L-glutaminase with antitumoral activity and for antimicrobial metabolites. The isolates Pseudogymnoascus sp. FDG01, Pseudogymnoascus sp. FDG02, and Penicillium sp. FAD33 showed potential antiproliferative action against human pancreatic carcinoma cells while showing no toxic effect on non-tumor cells. The microbial extracts from unidentified three bacteria and four filamentous fungi showed antibacterial activity against at least one tested pathogenic bacterial strain. The isolate FDG01 inhibited four bacterial species, while the isolate FDG01 was active against Micrococcus luteus in the minimal inhibitory concentration of 0.015625 µg mL -1. The results pave the way for further optimization of enzyme production and characterization of enzymes and metabolites found and reaffirm Antarctic marine environments as a wealthy source of compounds potentially applicable in the healthcare and pharmaceutical industry.

Antileishmanial activity of cathelicidin and its modulation by Leishmania donovani in a CREM-dependent manner for establishing infection.

Concerns regarding toxicity and resistance of current drugs have been reported in visceral leishmaniasis. Anti-microbial peptides are considered as new promising candidates and amongst them, human cathelicidin hCAP18/LL-37 showed significant parasite killing on drug-sensitive and resistant Leishmania promastigotes, coupled with its apoptosis-inducing role. Administration of hCAP18/LL-37 in infected macrophages also decreased parasite survival and increased the host favorable cytokine IL-12. However, 1,25-dihydroxyvitamin D3 (VitD3)-induced endogenous hCAP18/LL-37 production was hampered in infected THP-1 cells. Infection also suppressed the VitD3-receptor (VDR), transcription factor of hCAP18/LL-37. cAMP response element modulator (CREM), the repressor of VDR, was induced in infection resulting in suppression of both VDR and cathelicidin expression. PGE2/cAMP/PKA axis was found to regulate CREM induction during infection and silencing CREM in infected cells and BALB/c mice led to decreased parasite survival. Present study thus documents the anti-leishmanial potential of cathelicidin and further identifies CREM as a repressor of cathelicidin in Leishmania infection.

Electrospun L-Lysine/Amorphous Calcium Phosphate Loaded Core-Sheath Nanofibers for Managing Oral Biofilm Infections and Promoting Periodontal Tissue Repairment.

Introduction: Periodontitis, a chronic inflammatory disease prevalent worldwide, is primarily treated through GTR for tissue regeneration. The efficacy of GTR, however, remains uncertain due to potential infections and the intricate microenvironment of periodontal tissue. Herein, We developed a novel core-shell structure multifunctional membrane using a dual-drug-loaded coaxial electrospinning technique (Lys/ACP-CNF), contains L-lysine in the outer layer to aid in controlling biofilms after GTR regenerative surgery, and ACP in the inner layer to enhance osteogenic performance for accelerating alveolar bone repair. Methods: The biocompatibility and cell adhesion were evaluated through CCK-8 and fluorescence imaging, respectively. The antibacterial activity was assessed using a plate counting assay. ALP, ARS, and RT-qPCR were used to examine osteogenic differentiation. Additionally, an in vivo experiment was conducted on a rat model with acute periodontal defect and infection. Micro-CT and histological analysis were utilized to analyze the in vivo alveolar bone regeneration. Results: Structural and physicochemical characterization confirmed the successful construction of the core-shell fibrous structure. Additionally, the Lys/ACP-CNF showed strong antibacterial coaggregation effects and induced osteogenic differentiation of PDLSCs in vitro. The in vivo experiment confirmed that Lys/ACP-CNF promotes new bone formation. Conclusion: Lys/ACP-CNF rapidly exhibited excellent antibacterial activity, protected PDLSCs from infection, and was conducive to osteogenesis, demonstrating its potential application for clinical periodontal GTR surgery.

Polyphenolic compounds in the combat of foodborne infections - An update on recent evidence.

In recent years, the incidence of food-borne bacterial enteric diseases has increased worldwide causing significant health care and socioeconomic burdens. According to the World Health Organization, there are an estimated 600 million cases of foodborne illnesses worldwide each year, resulting in 420,000 deaths. Despite intensive efforts to tackle this problem, foodborne pathogenic microorganisms continue to be spread further. Therefore, there is an urgent need to find novel anti-microbial non-toxic compounds for food preservation. One way to tackle this issue may be the usage of polyphenols, which have received increasing attention in the recent years given their pleotropic health-promoting properties. This prompted us to perform a literature search summarizing studies from the past 10 years regarding the potential anti-microbial and disease-alleviating effects of plant-derived phenolic compounds against foodborne bacterial pathogens. The included 16 studies provide evidence that polyphenols show pronounced anti-bacterial and anti-oxidant effects against both Gram-positive and Gram-negative bacterial species. In addition, synergistic anti-microbial effects in combination with synthetic antibiotics were observed. In conclusion, phenolic compounds may be useful as natural anti-microbial agents in the food, agricultural, and pharmaceutical industries in the combat of foodborne infections.

Evidence that the loss of colonic anti-microbial peptides may promote dysbiotic Gram-negative inflammaging-associated bacteria in aging mice.

Introduction: Aging studies in humans and mice have played a key role in understanding the intestinal microbiome and an increased abundance of "inflammaging" Gram-negative (Gn) bacteria. The mechanisms underlying this inflammatory profile in the aging microbiome are unknown. We tested the hypothesis that an aging-related decrease in colonic crypt epithelial cell anti-microbial peptide (AMP) gene expression could promote colonic microbiome inflammatory Gn dysbiosis and inflammaging. Methods: As a model of aging, C57BL/6J mice fecal (colonic) microbiota (16S) and isolated colonic crypt epithelial cell gene expression (RNA-seq) were assessed at 2 months (mth) (human: 18 years old; yo), 15 mth (human: 50 yo), and 25 mth (human: 84 yo). Informatics examined aging-related microbial compositions, differential colonic crypt epithelial cell gene expressions, and correlations between colonic bacteria and colonic crypt epithelial cell gene expressions. Results: Fecal microbiota exhibited significantly increased relative abundances of pro-inflammatory Gn bacteria with aging. Colonic crypt epithelial cell gene expression analysis showed significant age-related downregulation of key AMP genes that repress the growth of Gn bacteria. The aging-related decrease in AMP gene expressions is significantly correlated with an increased abundance in Gn bacteria (dysbiosis), loss of colonic barrier gene expression, and senescence- and inflammation-related gene expression. Conclusion: This study supports the proposed model that aging-related loss of colonic crypt epithelial cell AMP gene expression promotes increased relative abundances of Gn inflammaging-associated bacteria and gene expression markers of colonic inflammaging. These data may support new targets for aging-related therapies based on intestinal genes and microbiomes.

Health-promoting benefits of lentils: Anti-inflammatory and anti-microbial effects.

This paper describes how lentils (Lens culinaris species) can positively affect health by reducing inflammation, providing antioxidants, and displaying antimicrobial properties. Lentils are rich in proteins, essential amino acids, minerals, and fibers, making them a valuable source of nutrition, particularly in low and middle-income countries. Lentils have many health benefits, including positive effects on diabetes management, support for cardiovascular health, and antioxidative properties. The antioxidative properties of lentils, attributed to their phenolic content, and their ability to inhibit inflammation-related enzymes are also discussed. We discuss the potential of lentils as a dietary tool in promoting immunity, reducing disease burdens, and preventing nutritional deficiencies. Overall, lentils are a highly nutritious food with various health benefits, including anti-inflammatory and antimicrobial effects. The fiber and protein content in lentils make them beneficial for weight management, blood sugar regulation, and supporting overall gut health. Furthermore, the slow rate at which lentils affect blood sugar levels, due to their low glycemic index, can be advantageous for individuals with diabetes.

Structure and ligand binding in the putative anti-microbial peptide transporter protein, YejA.

YejABEF is an ATP-binding cassette transporter that is implicated in the sensitivity of Escherichia coli to anti-microbial peptides, the best-characterized example being microcin C, a peptide-nucleotide antibiotic that targets aspartyl-tRNA synthetase. Here the structure of the extracellular solute binding protein, YejA, has been determined, revealing an oligopeptide-binding protein fold enclosing a ligand-binding pocket larger than those of other peptide-binding proteins of known structure. Prominent electron density in this cavity defines an undecapeptide sequence LGEPRYAFNFN, an observation that is confirmed by mass spectrometry. In the structure, the peptide interactions with the protein are mediated by main chain hydrogen bonds with the exception of Arg5 whose guanidinium side chain makes a set of defining polar interactions with four YejA residues. More detailed characterization of purified recombinant YejA, by a combination of ESI and MALDI-mass spectrometry as well as thermal shift assays, reveals a set of YejA complexes containing overlapping peptides 10-19 residues in length. All contain the sequence LGEPRYAFN. Curiously, these peptides correspond to residues 8-26 of the mature YejA protein, which belong to a unique N-terminal extension that distinguishes YejA from other cluster C oligopeptide binding proteins of known structure. This 35-residue extension is well-ordered and packs across the surface of the protein. The undecapeptide ligand occupies only a fraction of the enclosed pocket volume suggesting the possibility that much larger peptides or peptide conjugates could be accommodated, though thermal shift assays of YejA binding to antimicrobial peptides and peptides unrelated to LGEPRYAFNFN have not provided evidence of binding. While the physiological significance of this 'auto-binding' is not clear, the experimental data suggest that it is not an artefact of the crystallization process and that it may have a function in the sensing of periplasmic or membrane stress.

Unlocking the Pharmacological Potential of Benzimidazole Derivatives: A Pathway to Drug Development.

Heterocyclic molecules have garnered a massive interest in medicinal chemistry. They are heterocyclic compounds that have gained significance due to their diverse variety of pharmacological activities. Benzimidazole is a heterocyclic compound consisting of benzene and imidazole rings. The ease of synthesis and the structural versatility of benzimidazole make it a promising scaffold for drug development. Many biological actions of benzimidazole derivatives have been well documented, including antibacterial, antiviral, anticancer, anti-inflammatory, antitubercular, and anthelmintic properties. The mechanism of action of benzimidazole derivatives varies with their chemical structure and target enzyme. This review has explored numerous methods for producing benzimidazole derivatives as well as a broad range of pharmacological activities. SAR investigations are also discussed in this review as they provide crucial details regarding the essential structural qualities that benzimidazole derivatives must have in order to be biologically active, which could aid in the rational design of new drug candidates. Benzimidazole scaffold is an exclusive structure in drug design and discovery. Many new pharmaceutical drugs containing benzimidazole are anticipated to be available within the next ten years as a result of the extensive therapeutic applications of benzimidazole and its derivatives. This review inspired many researchers to develop more biologically active compounds bearing benzimidazole, expanding the scope of finding a remedy for other diseases. From this study, we concluded that 2-substituted benzimidazole was considered more extensively by researchers.

Bactericidal, anti-biofilm, anti-oxidant potency and catalytic property of silver nanoparticles embedded into functionalised chitosan gel.

Chitosan is a versatile biocompatible polysaccharide which has attracted great attention for gel synthesis. Its reducing character is specifically exploited for nanoparticle synthesis via green approach. A silver nanocomposite synthesized using this gel, with a novel gelling agent 2,4,6-trihydroxy benzaldehyde, was found to be a promising candidate for several applications including anti-bacterial, anti-biofilm and anti-oxidant activity as well as catalysis. The nanocomposite was well characterized using various spectroscopic and microscopic techniques such as IR, TGA, XRD, XPS, SEM and TEM. The nanocomposite exhibited high bactericidal activity against both S. aureus and E. coli. Further, it was evaluated for anti-biofilm forming property and its potency as antioxidant agent. The nanocomposite served as a catalyst for degradation of Methyl Orange and Rhodamine B at high concentrations (in the range of mM) with a catalytic efficiency of 98.58 % and 99.56 % within 3 min and 5 min respectively.

Recent developments on the synthesis of biologically active glycohybrids.

The exploration of hybridization emerges as a potent tool in advancing drug discovery research, with a significant emphasis on carbohydrate-containing hybrid scaffolds. Evidence indicates that linking carbohydrate molecules to privileged bioactive scaffolds enhances the bioactivity of drug molecules. This synergy results in a diverse range of activities, making carbohydrate scaffolds pivotal for synthesizing compound libraries with significant functional and structural diversity. Beyond their synthesis utility, these scaffolds offer applications in screening bioactive molecules, presenting alternative avenues for drug development. This comprehensive review spanning 2015 to 2023 focuses on synthesized glycohybrid molecules, revealing their bioactivity in areas such as anti-microbial, anti-cancer, anti-diabetic, anti-inflammatory activities, enzyme inhibition and pesticides. Numerous novel glycohybrids surpass positive control drugs in biological activity. This focused study not only highlights the diverse bioactivities of glycohybrids but also underscores their promising role in innovative drug development strategies.

Freeze-drying of bupivacaine lipospheres: preparation, characterization, and evaluation of anti-microbial properties.

PURPOSE: To prepare freeze-dried bupivacaine lipospheres intended for topical application in burn injuries. The aim was improving the storage stability and developing a prolonged release pattern to tackle the adverse reactions resulting from the frequent administration of bupivacaine. METHODS: The lipospheres were prepared by hot-melt dispersion method employing bupivacaine base at 1.5 and 3%w/w, tristearin 6% w/w as the core while dipalmitoyl phosphatidylcholine (DPPC) and soy phosphatidylcholine (SPC) as the coat at 0.75, 1.5 and 3% w/w. The lotion was then freeze-dried and cryoprotected by sucrose 3% w/w. Evaluation was carried out through loading and release analysis, storage study, particle characterization including morphology, zeta potential and particle size as well as anti-microbial assessment. RESULTS: The highest loading, (87.6 ± 0.1%), was achieved using bupivacaine 3% and SPC 0.75%. After 6 months of storage at 4 ͦC, the loading in the lotion and the freeze-dried samples were 17.4 ± 0.2 and 87.2 ± 0.3%, respectively. In vitro dissolution test demonstrated 94.5% and 95% of bupivacaine release from lotion and freeze-dried samples, after 24 h. The respective zeta potential of -1.30 and 26 mV was recorded for lotion and solid-state bupivacaine. Micromeritic evaluation of freeze-dried powder exhibited particle size of 35.23 ± 2.02 µm and highly-wrinkled-irregular morphology without detectable needle structures related to drug free crystals. The powder had rapid reconstitution property and antibacterial activity. CONCLUSION: Freeze- drying holds a promising potential to improve the storage stability of bupivacaine lipospheres with well- preserved release pattern and particle properties for further topical application.