Mouse Fibroblast Cell Line Research Articles

A novel polyurethane-based silver foam dressing with superior antimicrobial action for management of infected chronic wounds.

Wound healing is a complex and dynamic process supported by several cellular events. Around 13 million individuals globally suffer from chronic wounds yearly, for which dressings with excellent antimicrobial activity and cell viability (>70%, as per ISO 10993) are needed. Excessive use of silver can cause cytotoxicity and has been linked to increasing antimicrobial resistance.In this study, HDI Ag foam was synthesized using a safer hexamethylene diisocyanate-based prepolymer (HDI prepolymer) instead of commonly used diisocyanates like TDI and MDI and substantially lower Ag content than that incorporated in other Ag foams. In vitro characteristics of the HDI Ag foam were evaluated in comparison with leading clinically-used foam-based dressings. All dressings underwent a detailed characterization in accordance with industrially accepted BS EN 13726 standards. The HDI Ag foam exhibited highest antimicrobial efficiency against Staphylococcus aureus and Pseudomonas aeruginosa (static condition), with the lowest amount of Ag (0.2 wt%) on the wound contact surface. The extracts from HDI Ag foam showed superior cell viability (>70%), when tested on the L929 mouse fibroblast cell line. Measurements of moisture vapour transmission, fluid handling, physico-chemical and mechanical properties ensured that the HDI foam was clinically acceptable for chronic wound patients.&#xD.

Cytotoxic potential of Hemp seed oil and molecular docking studies with inflammatory markers of diabetic cardiomyopathy

Present study was to assess the potential cytotoxic effects of commercially available Hemp seed oil and the effectiveness of its compounds in inhibiting inflammatory markers associated with diabetic cardiomyopathy. The bioactive components of Hemp seed oil were analysed using gas chromatography coupled with mass spectrometry (GC–MS). To evaluate the oil's cytotoxic properties, a modified 3-(4, 5-dimethylthiazol-2-yl)-2, 5-diphenyltetrazolium (MTT) assay was conducted on L929 cells (a mouse fibroblast cell line). Furthermore, an in vivo antiangiogenic assessment of the oil was performed using the chick chorioallantoic membrane (CAM) model, following a laboratory-standardized protocol. Docking and simulation studies were carried out to examine the binding and stability of the oil's compounds with inflammatory markers relevant to diabetic cardiomyopathy. The GC–MS analysis revealed that hemp seed oil contains several compounds, including Cannabidiol, Benzenemethanaminium, Dronabinol, Cannabinol, and Squalene. The cytotoxicity assessment on L929 cells demonstrated that Hemp seed oil did not exhibit any harmful effects at a concentration of 2.5 - 5 mg/mL. The CAM model confirmed the presence of antiangiogenic properties in Hemp seed oil, as evidenced by the inhibition of vascular patterns and blood vessel dissolution in the eggs. Additionally, docking and molecular dynamics (MD) simulations indicated that Benzenemethanaminium and Cannabielsoin exhibited the highest inhibitory efficacy and stability when interacting with IL-1β and C-reactive protein, respectively. This study suggests that Hemp seed oil possesses anti-inflammatory and anti-angiogenic properties, making it a potential herbal remedy for patients with diabetic cardiomyopathy.

Fabrication and evaluation of four combinations of pullulan-based biopolymeric, microporous scaffolds impregnated with peppermint oil for management of partial thickness burn wounds and accelerated tissue regeneration

Burn injuries are common in both civilian and military settings and cause severe morbidity and mortality. The present study aimed to develop microporous bioactive scaffolds from the natural polysaccharide, pullulan, combined individually with Gelatin (Gel)/ Alginate (Alg)/ Chitosan (Ch)/ Carboxy-methyl cellulose (CMC), and crosslinked with glutaraldehyde to form a polymeric network. The objective was to evaluate and compare their efficacy in healing second degree partial-thickness burn wounds. The scaffolds were also impregnated with peppermint oil (PEO) to provide potential analgesic and cooling effects. Scaffolds were characterized using FTIR, TGA and SEM analysis to understand the intra-and intermolecular interactions and morphological characteristics. In vitro parameters like fluid uptake ability, biodegradation and hemolytic index were also assessed. Biocompatibility studies, including cell adhesion, migration and proliferation, were conducted using L929 mouse fibroblast cell lines. The in vivo efficacy was evaluated in Sprague Dawley rats inflicted with second degree burns to assess and compare wound retraction across different experimental groups. Histology, immunohistochemistry along with gram and picrosirius staining studies were also performed. The average pore size of all biopolymeric scaffold combinations ranged between 25.6-298μm. All four test combinations were non-hemolytic, with hemolytic indices between 0.3-2.9. Wound retraction studies in rats clearly indicated that among the four test combinations studied, Pu/Gel/PEO scaffold not only reduced local inflammation faster but also accelerated dermal regeneration in comparison to positive control as well as other test combinations (viz., Pu/Alg/PEO, Pu/Ch/PEO, and Pu/CMC/PEO). Immunohistochemistry results corroborated animal efficacy findings and demonstrated enhanced expression level of epidermal growth factor and fibroblast growth factor-2 in Pu/Gel/PEO scaffold treated group. Picrosirius staining also revealed enhanced collagen deposition in Pu/Gel/PEO scaffold treated group. The study findings suggest that biopolymeric scaffolds made from pullulan combined with gelatin and PEO (Pu/Gel/PEO) could serve as a promising substrate for skin regeneration template for second degree burns.

STRUCTURAL, MORPHOLOGICAL AND MAGNETIC PROPERTIES OF FUNCTIONALIZED MANGANESE IRON OXIDE NANOPARTICLES FOR BIOLOGICAL APPLICATIONS

The chitosan functionalized MnFe2O4 nanoparticles were synthesized using thermal decomposition method. The morphological, structural and magnetic properties of obtained chitosan functionalized magnetic nanoparticles were studied to assess the feasibility for biomedical applications. The crystallite size of nanoparticles observed using XRD was 15nm. Functional group attachment to surface of nanoparticles was analyzed using FTIR. Particle size of nanoparticles was studied by TEM analysis and it showed that particles were roughly spherical. Thermal stability and bonding strength of ligands to the surface of material was determined using TGA. The magnetization of chitosan functionalized nanoparticles observed by VSM is 56emu/g and VSM showed no coercivity and remanence existence, stipulating the super-paramagnetic behavior. The cell viability of chitosan functionalized nanoparticles was above 85% at concentration up to the 1.0mg mL-1 on mouse fibroblast cell line i.e. L929 cell line. These studies revealed that, MnFe2O4 nanoparticles are potential materials for biomedical applications.

Synthesis and Characterization of Ti-13Ta-6Sn Foams Produced Using Mechanical Alloying, the Space Holder Method and Plasma-Assisted Sintering

Highly porous titanium foams are great candidates for replacing bone structures with a low elastic modulus owing to their ability to avoid the stress shielding effect. However, the production of highly porous foams (>70 vol.%) with well-distributed, stable, and predictable porous architectures using powder compaction and space holders is challenging. In this study, pure titanium powder and mechanically alloyed Ti-13Ta-6Sn were mixed with 50, 70, and 80 vol.% KCl powders as a space holder, cold-compacted, and sintered in a plasma-assisted sintering reactor to produce highly porous foams. The space holder was completely removed using heat and plasma species collisions prior to sintering. A Ti-13Ta-6Sn alloy powder with α, β, and metastable FCC-γ phases was synthesized. The characteristics of the alloyed powder, mixing step, and the resulting sintered samples were compared to those of CP-Ti. After sintering, the alloy exhibited α and β phases and a reduced elastic modulus. Foams with an elastic modulus in the range of the cortical and trabecular bones were obtained. The results showed the effects of the space holder volume fractions on the volume fraction, size, distribution, interconnectivity, and shape of the pores. The Ti-13Ta-6Sn foams exhibited a uniform open-celled porous architecture, lower elastic modulus, higher yield strength, and higher passivation resistance than CP-Ti. Ti-13Ta-6Sn exhibited a nontoxic effect for the mouse fibroblast cell line.

3D Printing of Biocompatible and Antibacterial Silica-Silk-Chitosan-Based Hybrid Aerogel Scaffolds Loaded with Propolis.

The aim of this study is to design a therapeutic enhanced three-dimensional (3D) silk fibroin (SF)-based scaffold containing propolis (Ps)-loaded chitosan (CH) nanocarriers. To this aim, we initially synthesized a hybrid gel-based ink by a synergistic sol-gel and self-assembly approach and then processed the resulting gels by microextrusion-based 3D printing followed by supercritical drying to obtain 3D hybrid aerogel scaffolds. Ps was utilized to enhance the final scaffold's bactericidal efficacy and cell responsiveness. For the synthesis of the scaffold, two Ps loading methods (in preprint and postprinting steps) were investigated in order to optimize the Ps drug quantities in the scaffold and maximize the antibacterial properties of scaffold. In the postprinting Ps loading step, the hybrid silica-oxidized SF (SFO)-CH hydrogel ink was 3D printed into a construct with an interconnected porous structure, and then, Ps was loaded into the printed construct. In the preprint loading method, PS was incorporated into the SF and a hydrolyzed silane solution prior to gelation. The morphological studies demonstrate that the addition of Ps encapsulated CH nanoparticles (NPs) into the hydrogel solution improved the porosity of the developed scaffolds. The rheological analysis of the designed gel ink with and without Ps loading and the release kinetics were studied. The antimicrobial results show that the Ps-loaded scaffolds in the postprinting step exhibited superior antibacterial activity against Escherichia coli (E. coli) and Staphylococcus aureus (S. aureus) strains compared to a preprinted Ps-loaded scaffold. Direct and indirect in vitro cytotoxicity tests also confirmed the designed Ps-loaded scaffold biocompatibility toward a mouse fibroblast (L929) cell line. We demonstrated that the scaffold formulated by propolis-loaded chitosan NPs can enhance the migration and proliferation of L929 fibroblast cells. The obtained results prove the promise of the designed 3D printed silica-SFO-CH-Ps scaffolds as a potent 3D scaffold to mediate tissue regeneration but also as an antibacterial highly porous matrix to support wound healing.

Antiviral respiratory masks with plasma-functionalized polypropylene textiles for optimal adsorption of antiviral substance

During the COVID-19 pandemic, face masks were the first line of defense against the spread of infection. However, infectious viruses may remain on medical textiles, potentially serving as an additional source of infection. Due to their chemical inertness, many textiles cannot be enhanced with antiviral functionalities. Through treatment with low-pressure gaseous plasma, we have activated the surface of a medical-grade melt-blown, non-woven polypropylene textile so that it can absorb sodium dodecyl sulfate, an antimicrobial surfactant. Within two hours of contact time, the functionalized textile has been able to inactivate over 7 log10 PFU mL−1 of bacteriophage phi6, a surrogate of enveloped viruses such as SARS-CoV-2, and it has retained its antiviral properties for over 100 days. The functionalized material has not disrupted facial mask filtration efficiency or breathability. In addition, the in vitro biocompatibility testing in accordance with ISO 10993-5 for testing of medical devices has demonstrated that the selected formulation causes no adverse effects on the mouse fibroblast cell line L-929. With the treatment processes that have been completed within seconds, the method seems to have great potential to produce antiviral textiles against future outbreaks.

Design, synthesis, biological evaluation and molecular docking study of thiadiazole-isatin hybrid analogues as potential anti-diabetic and anti-bacterial agents

We have synthesized thiadiazole-isatin hybrid analogues (1–20), characterized through different spectroscopic techniques such as 1HNMR, 13CNMR, HREI-MS, and evaluated against α-glucosidase and α-amylase enzymes. All analogues showed potent inhibitory potentials, having an IC50 values ranged from 22.08 ± 0.09 to 54.03 ± 0.07 μM (against α-amylase) and 19.03 ± 0.04 to 50.03 ± 0.02 μM (α-glucosidase) when compared with the standard drug acarbose (IC50 = 22.07 ± 0.02 μM for α-amylase and IC50 = 18.01 ± 0.06 μM for α-glucosidase respectively). Among the series, analogues 13 (IC50 = 19.03 ± 0.04 and 22.08 ± 0.09 μM), 12 (IC50 = 21.03 ± 0.07 and 24.03 ± 0.07 μM), and 5 (IC50 = 22.02 ± 0.03 and 26.02 ± 0.04 μM) were identified as the most active inhibitors. The structure–activity relationship was carried out, mainly associated with the nature, number, position, and electron-donating and electron-withdrawing effects of the substituent (s) on the phenyl ring. With the help of molecular docking, the binding interaction of the most active analogues within the active site of enzymes was confirmed. Almost twelve compounds were also screened for antibacterial potential, and few were found to be effective against Bacillus subtilis. All compounds were verified for cytotoxicity against the 3 T3 mouse fibroblast cell line and detected non-toxic.

Green synthesis, characterization and biological activity analysis of silver nanoparticles from commercially available root powder of Picrorhiza kurroa Royle ex Benth.

Picrorhiza kurroa Royle ex Benth., a medicinal plant native to the alpine regions of the Himalayas, is renowned for its diverse therapeutic properties. Recently, green-synthesized silver nanoparticles have gained attention for their potential in pharmaceutical and industrial applications. In this study, silver nanoparticles (Pk-AgNPs) were synthesized using commercially available root powder of P. kurroa. The objective was to evaluate their potential biomedical applications by assessing their antioxidant properties and cytotoxicity. The Pk-AgNPs were characterized using Scanning Electron Microscopy (SEM) and Fourier-Transform Infrared Spectroscopy (FT-IR), which revealed their morphology and functional groups. The Total Antioxidant Capacity (TAC) of methanolic root extract of P. kurroa (PkRE) and the Pk-AgNPs was determined using the Phosphomolybdenum method. The results indicated that the antioxidant activity of PkRE was higher than that of the Pk-AgNPs. Moreover, the activity increased with concentration, ranging from 20 µg/mL to 120 µg/mL, demonstrating their capability to eliminate harmful free radicals. The cytotoxicity of PkRE and Pk-AgNPs was evaluated using the MTT assay against the SV40 T-antigen-containing HEK293T cell line, derived from human embryonic kidney 293 cells and the L929 cell line, a mouse fibroblast cell line. The results demonstrated dose-dependent cytotoxicity. L929 cells remained 100 % viable at concentration up to 200 µg/mL for PkRE and 100 µg/mL Pk-AgNPs. In contrast, HEK293T cells didn’t show 100 % viability even at a concentration of 50 µg/mL for both samples. This study highlights the potential use of PkRE and Pk-AgNPs as antioxidants. However, the cytotoxicity findings suggests that they may be harmful to humans if consumed orally, though they could be suitable for use in other organisms. This paves the way for further research into the application of AgNPs synthesized from P. kurroa in biomedical and pharmaceutical domains as well as in veterinary sciences.

A bioactive self-healing hydrogel wound-dressing based on Tragacanth gum: Structural and invitro biomedical investigations

The design and development of wound-dressing hydrogels with desirable therapeutic effects and proper mechanical and self-healing properties are crucial in the healthcare sector. This research aims to prepare a new self-healing hydrogel based on Tragacanth, polyvinyl alcohol, and borax to be used as a wound dressing, the hydrogel was first prepared through a simple and one-pot reaction. The efficiency of the resulting product was then assessed based on the rheological and self-healing tests as well as cellular tests on a mouse fibroblast cell line (L929) including toxicity and scratch tests as well as the investigation of the expression of TGFβ1, TGFβ2, and VEGF-A gens (using Real-time PCR). The synthesized hydrogel exhibited proper mechanical strength, high self-healing features, and no toxicity (cell viability >100 %). Rheological studies indicate that hydrogels with a higher borax content (PVA: B ratio of 5:1) exhibit a higher storage modulus across all frequencies. The presence of hydrogel improved the migration of the L929 cells and scratch healing. The hydrogel also caused a significant improvement in the expression of the growth factors of the genes (P < 0.001). Therefore, it can be concluded that the prepared wound dressing can actively contribute to wound healing, opening promising potentials in medical applications.

Cyanobacterial Ampholyte Hydrogels Developed by the Cationization of Sulfated Polysaccharides and Their Cell-Compatibility.

Sacran is a cyanobacterial supergiant polysaccharide with carboxylate and sulfate groups that exhibits antiallergic and antiinflammatory properties. However, its high anionic functions restrict cell compatibility. Quaternary ammonium groups were substituted to form sacran ampholytes, and the cell compatibility of the cationized sacran hydrogels was evaluated. The cationization process involved the reaction of N-(3-chloro-2-hydroxypropyl)trimethylammonium chloride with the primary amine or hydroxyl groups of sacran. The degree of cationization ranged from 32 to 87% for sugar residues. Hydrogels of sacran ampholytes were prepared by annealing their dried sheets by thermal cross-linking; these hydrogels exhibited anisotropic expansion properties. The water contact angle on the hydrogels decreased from 26.5 to 15.3° with an increase in the degree of cationization, thereby enhancing hydrophilicity. The IC50 values of sacran ampholytes decreased with an increased degree of cationization, resulting in a reduction in cytotoxicity toward the L-929 mouse fibroblast cell line. This reduction was associated with an increase in the cell proliferation density after 3 days of incubation. Scanning electron microscopy images showed fibroblast intercellular connections. Therefore, the sacran ampholyte hydrogel exhibited increased hydrophilicity and cell compatibility, which is beneficial for various biomedical applications.

Mystery of the Passerini Reaction for the Synthesis of the Antimicrobial Peptidomimetics against Nosocomial Pathogenic Bacteria.

The first example of applying salicylaldehyde derivatives, as well as coumarin with the formyl group at the C8 position in its structure, as carbonyl partners in a three-component Passerini reaction, is presented. As a result of research on the conditions of the Passerini reaction, the important role of the hydroxyl group in the salicylaldehyde used in the course of the multicomponent reaction was revealed. When an aldehyde with an unprotected hydroxyl group is used, only two-component α-hydroxy amide products are obtained. In contrast, the use of acylated aldehyde results in three-component α-acyloxy amide products with high efficiency. The developed protocol gives access to structurally diversified peptidomimetics with good yield. The compounds were also evaluated as antimicrobial agents against selected strains of nosocomial pathogenic bacteria. The structure-activity relationship revealed that inhibitory activity is strongly related to the presence of the trifluoromethyl group (CF3) or the methyl group at the C4 position in an unsaturated lactone ring of the coumarin scaffold. MIC and MBC studies were carried out on eight selected pathogenic bacteria strains (Gram-positive pathogenic Staphylococcus aureus strain (ATCC 23235), as well as on Gram-negative E. coli (K12 (ATCC 25404), R2 (ATCC 39544), R3 (ATCC 11775), and R4 (ATCC 39543)), Acinetobacter baumannii (ATCC 17978), Pseudomonas aeruginosa (ATCC 15442), and Enterobacter cloacae (ATCC 49141) have shown that the tested compounds show a strong bactericidal effect at low concentrations. Among all agents investigated, five exhibit higher antimicrobial activity than those observed for commonly used antibiotics. It should be noted that all the compounds tested showed very high activity against S. aureus, which is the main source of nosocomial infections that cause numerous fatalities. Additionally, the cytotoxicity of sixteen derivatives was measured with the use of the MTT test on BALB/c3T3 mouse fibroblast cell lines. The cytotoxicity studies revealed that the tested substances exert a similar or lower effect on cell proliferation than that observed for commonly used antibiotics within the range of therapeutic doses. A parallel MTT assay using ciprofloxacin, bleomycin, and cloxacillin showed that these antibiotics are more cytotoxic when tested in mammalian cells, and cell viability is in the range of 85.0-89.9%. Furthermore, we have shown that the studied coumarin-based peptidomimetics, depending on their structural characteristics, are nonselective and act efficiently against various Gram-positive and Gram-negative pathogens, which is of great importance for hospitalised patients.

Identification of monoclonal antibodies from naive antibody phage-display libraries for protein detection in formalin-fixed paraffin-embedded tissues

Most antibodies used in immunohistochemistry (IHC) have been developed by animal immunization. We wanted to explore naive antibody repertoires displayed on filamentous phages as a source of full-length antibodies for IHC on Formalin-Fixed and Paraffin-Embedded (FFPE) tissues. We used two isogenic mouse fibroblast cell lines that express or not human HER2 to generate positive and negative FFPE pseudo-tissue respectively. Using these pseudo-tissues and previously described approaches based on differential panning, we isolated very efficient antibody clones, but not against HER2. To optimize HER2 targeting and tissue specificity, we first performed 3–4 rounds of in vitro panning using recombinant HER2 extracellular domain (ECD) to enrich the phage library in HER2 binders, followed by one panning round using the two FFPE pseudo-tissues to retain binders for IHC conditions. We then analyzed the bound phages using next-generation sequencing to identify antibody sequences specifically associated with the HER2-positive pseudo-tissue. Using this approach, the top-ranked clone identified by sequencing was specific to the HER2-positive pseudo-tissue and showed a staining pattern similar to that of the antibody used for the clinical diagnosis of HER2-positive breast cancer. However, we could not optimize staining on other tissues, showing that specificity was restricted to the tissue used for selection and screening. Therefore, future optimized protocols must consider tissue diversity early during the selection by panning using a wide collection of tissue types.

Biocompatible Co-organic Composite Thin Film Deposited by VHF Plasma-Enhanced Atomic Layer Deposition at a Low Temperature.

Although metal-organic thin films are required for many biorelated applications, traditional deposition methods have proven challenging in preparing these composite materials. Here, a Co-organic composite thin film was prepared by plasma-enhanced atomic layer deposition (PEALD) with cobaltocene (Co(Cp)2) on polydimethylsiloxane (PDMS), using two very high frequency (VHF) NH3 plasmas (60 and 100 MHz), for use as a tissue culture scaffold. VHF PEALD was employed to reduce the temperature and control the thickness and composition. In the result of the VHF PEALD process, the Young's modulus of the Co-organic composite thin film ranged from 82.0 ± 28.6 to 166.0 ± 15.2 MPa, which is similar to the Young's modulus of soft tissues. In addition, the deposited Co ion on the Co-organic composite thin film was released into the cell culture media under a nontoxic level for the biological environment. The proliferation of both L929, the mouse fibroblast cell line, and C2C12, the mouse myoblast cell line, increased to 164.9 ± 23.4% during 7 days of incubation. Here, this novel bioactive Co-organic composite thin film on an elastic PDMS substrate enhanced the proliferation of L929 and C2C12 cell lines, thereby expanding the application range of VHF PEALD in biological fields.

Dual phage-incorporated electrospun polyvinyl alcohol-eudragit nanofiber matrix for rapid healing of diabetic wound infected by Pseudomonas aeruginosa and Staphylococcus aureus.

Diabetic wound healing remains a healthcare challenge due to co-occurring multidrug-resistant (MDR) bacterial infections and the constraints associated with sustained drug delivery. Here, we integrate two new species of phages designated as PseuPha1 and RuSa1 respectively lysing multiple clinical MDR strains of P. aeruginosa and S. aureus into a novel polyvinyl alcohol-eudragit (PVA-EU†) nanofiber matrix through electrospinning for rapid diabetic wound healing. PVA-EU† evaluated for characteristic changes that occurred due to electrospinning and subjected to elution, stability and antibacterial assays. The biocompatibility and wound healing ability of PVA-EU† were assessed through mouse fibroblast cell line NIH3T3, followed by validation through diabetic mice excision wound co-infected with P. aeruginosa and S. aureus. The electrospinning resulted in the incorporation of ~ 75% active phages at PVA-EU†, which were stable at 25°C for 30days and at 4°C for 90days. PVA-EU† showed sustained release of phages for 18h and confirmed to be detrimental to both mono- and mixed-cultures of target pathogens. The antibacterial activity of PVA-EU† remained unaltered in the presence of high amounts of glucose, whereas alkaline pH promoted the activity. The matrix exerted no cytotoxicity on NIH3T3, but showed significant (p < 0.0001) wound healing in vitro and the process was rapid as validated through a diabetic mice model. The sustained release, quick wound closure, declined abundance of target MDR bacteria in situ and histopathological signs of recovery corroborated the therapeutic efficacy of PVA-EU†. Taken together, our data signify the potential application of PVA-EU† in the rapid treatment of diabetic wounds without the aid of antibiotics.

A dual responsive bis-thiophene affixed thiosemicarbazide based chemosensor for colorimetrically Hg2+ and fluorometrically Cu2+ ions and their applications in live cell imaging

In this work, we developed a fast and straightforward colorimetric and photoluminescent chemosensor probe (P1), featuring bis-thiophene-thiosemicarbazide moieties as its signaling and binding unit. This probe exhibited rapid sensitivity to Hg2+ and Cu2+ ions in a semi-aqueous medium, resulting in distinct colorimetric and photoluminescent changes. In the presence of Cu2+, P1 displayed an impressive 50-fold increase in photoluminescence (PL) at 450 nm (with excitation at 365 nm). The probe P1 formed a 1:1 complex with Hg2+ and Cu2+ ions, featuring association constant values of 4.04 × 104 M−1 and 1.25 × 103 M−1, respectively. P1 has demonstrated its efficacy in the analysis of real samples, yielding promising results. Additionally, the probe successfully visualized copper ions on a mouse fibroblast cell line (NIH3T3), highlighting its potential as an intracellular probe for copper ion detection.

Surface modified niosomal quercetin with cationic lipid: an appropriate drug delivery system against Pseudomonas aeruginosa Infections

The Increase in infections caused by resistant strains of Pseudomonas aeruginosa poses a formidable challenge to global healthcare systems. P. aeruginosa is capable of causing severe human infections across diverse anatomical sites, presenting considerable therapeutic obstacles due to its heightened drug resistance. Niosomal drug delivery systems offer enhanced pharmaceutical potential for loaded contents due to their desirable properties, mainly providing a controlled-release profile. This study aimed to formulate an optimized niosomal drug delivery system incorporating stearylamine (SA) to augment the anti-bacterial and anti-biofilm activities of quercetin (QCT) against both standard and clinical strains of P. aeruginosa. QCT-loaded niosome (QCT-niosome) and QCT-loaded SA- niosome (QCT-SA- niosome) were synthesized by the thin-film hydration technique, and their physicochemical characteristics were evaluated by field emission scanning electron microscopy (FE-SEM), zeta potential measurement, entrapment efficacy (EE%), and in vitro release profile. The anti-P. aeruginosa activity of synthesized niosomes was assessed using minimum inhibitory and bactericidal concentrations (MICs/MBCs) and compared with free QCT. Additionally, the minimum biofilm inhibitory and eradication concentrations (MBICs/MBECs) were carried out to analyze the ability of QCT-niosome and QCT-SA-niosome against P. aeruginosa biofilms. Furthermore, the cytotoxicity assay was conducted on the L929 mouse fibroblasts cell line to evaluate the biocompatibility of the formulated niosomes. FE-SEM analysis revealed that both synthesized niosomal formulations exhibited spherical morphology with different sizes (57.4 nm for QCT-niosome and 178.9 nm for QCT-SA-niosome). The EE% for cationic and standard niosomal formulations was reported at 75.9% and 59.6%, respectively. Both formulations showed an in vitro sustained-release profile, and QCT-SA-niosome exhibited greater stability during a 4-month storage time compared to QCT-niosome. Microbial experiments indicated that both prepared formulations had higher anti-bacterial and anti-biofilm activities than free QCT. Also, the QCT-SA-niosome exhibited greater reductions in MIC, MBC, MBIC, and MBEC values compared to the QCT-niosome at equivalent concentrations. This study supports the potential of QCT-niosome and QCT-SA-niosome as effective agents against P. aeruginosa infections, manifesting significant anti-bacterial and anti-biofilm efficacy alongside biocompatibility with L929 cell lines. Furthermore, our results suggest that optimized QCT-niosome with cationic lipids could efficiently target P. aeruginosa cells with negligible cytotoxic effect.

Exploring anticancer and antibacterial activities of two self-assembling units: Band gap calculations, DFT studies, and polymorphism of a carbohydrazone ligand

The synthesis and physicochemical characterization of a novel self-assembling unit 1,3-bis(4-hydroxyphenylmethylideneamino)guanidine hydrochloride (H5L1) and polymorphic crystal structures of an analogous proligand 1,5-bis(4-hydroxybenzaldehyde) carbohydrazone (H4L2. DMF & H4L2. H2O) are reported. The crystal systems of H4L2. DMF and H4L2. H2O are monoclinic with C2/c and P21/c space groups. The intermolecular contacts are calculated by Hirshfeld surface analyses, which reveal that H···H interactions have a maximum contribution in the total Hirshfeld surfaces in both the crystal structures. The study also signifies that hydrogen bonding interactions are dominant in the crystal lattice of H4L2. H2O, while the C–H∙∙∙π interactions are also significant in H4L2. DMF lattice. Density functional theory is used for optimizing geometry and calculating quantum chemical parameters. Theoretical frontier molecular energy gaps in the gas phase for H5L1 and H4L2 are found to be 3.49 and 4.09 eV respectively. The solid-state band gaps of H5L1 and H4L2 are determined experimentally using the Kubelka-Munk model and are found to be 2.72 and 2.43 eV respectively, which is indicative of strong intermolecular association in the solid lattice of H4L2. ADME properties are estimated to predict the drug-likeness of the compounds. In vitro antibacterial activity study reveals that the diaminoguanidine based proligand is a more efficient inhibitor against Gram-positive Staphylococcus aureus and Gram-negative Escherichia coli bacterial species. Also, in vitro study of the compounds against human breast cancer MCF-7 cells shows that with the increase in the concentrations of the compounds the percentage of cell viability decreases, which indicates the anticancer potentials of both compounds. The IC50 values of H5L1 and H4L2 against MCF-7 cell lines (205.62 and 247.31 µg/mL) are also found to be better compared to the same (274.59 and 375.45 µg/mL) against the non-cancerous Mouse Fibroblast (L929) cell lines.

Cytotoxicity and bioavailability assessment from micellar system based Thiamine-Phospholipid complexes

Poor absorption (3–5 %) of thiamine hydrochloride (TH), is primarily concerned with impaired permeability across intestinal mucosa. To modulate the permeability of TH, a phospholipid (PL) interaction-based hydrophobic complex of thiamine was investigated. Using the solvent evaporation approach, thiamine-phospholipid complexes (TPCs) were prepared between free bases of thiamine and PLs in the weight ratio (1:1, 1:2, and 2:1) and characterized using FTIR, spectrophotometry, XRD, and conductometric methods. Electrical conductivity and partition coefficient studies demonstrated that TPCs were hydrophobic transformations formed via PL interaction with a free thiamine base. TPCs were embedded into the micellar system (Tween20/Ethanol), characterized by electrical conductivities and zeta-sizing studies, and exploited in its micellar delivery system design. TPC 1:1 & 1:2 had much lower conductivity than TH and its physical mixture (TH/PL) in the Tween20/Ethanol environment diluted with an aqueous phase. The average size of micellar systems loaded with TPC (10 % w/w) was within the range of 12–25 nm, and conductivity was in the range of 122-130µS/cm. In vitro release characterization from complexes and their micellar systems in HCl 1.2, phosphate buffer (PB) 6.8, and bidistilled water showed a delayed release pattern. TPC modulated the intestinal permeability of thiamine as revealed from ex vivo studies. TPC (1:1) and its micellar system produced significant differences in drug permeability (p < 0.001) compared to TH and physical mixture. Pharmacokinetic assessment of the micellar system of complexes in Wistar rats showed that the TPC (1:1) loaded micellar system produced a 2.4-fold enhancement of AUC(0−24) over (TH) followed by oral administration. Assessment of cell viability in mouse fibroblast cell line (L929) culture showed that TPC or micellar system did not inhibit cell growth and was safe at various concentration levels. TPc complexes developed using phospholipid complexation yield hydrophobic transformation in TH and their micellar system-based delivery modulates the intestinal permeability and bioavailability enhancement.

Evaluation of Antibiofilm, Antimicrobial, Cytotoxic and Antioxidant Effects of Some Wild Mushroom Species

In this study, ethanol extracts of some wild mushroom species, in the phylum Basidiomycota, [Armillaria mellea (Vahl) P. Kumm., Infundibulicybe geotropa (Bull.) Harmaja, Leucopaxillus gentianeus (Quél.) Kotl. and Trametes versicolor (L.) Lloyd] were tested for their antioxidant, antimicrobial, antibiofilm, and cytotoxic activities. Mushroom samples showed low antimicrobial activity on Enterococcus faecalis and Staphylococcus aureus, while biofilm inhibitory activity on test microorganisms ranging from 24.6% to 80.5%. At the end of the antioxidant activity studies A. mellea was the mushroom sample having the highest DPPH radical scavenging capacity (0.105±0.001 mg/mL) whereas T. versicolor was the one having the highest iron (III) ion reducing power (40.709±0.003 µg TE/100g). The highest polyphenol content was observed in T. versicolor (29.916±0.002 mg GAE/100g) samples, and the lowest in A. mellea (9.5±0.006 mg GAE/100g) samples. The cytotoxic effects of the samples were tested on MCF-7 and MDA-MB-231 (breast cancer) and L929 (mouse fibroblast) cell lines using the MTT method. As a result, it was observed that A. mellea and T. versicolor samples were more effective on MCF-7 cell line, A. mellea on MDA-MB-231 cell line.