Examining the quaternary ammonium chitosan Schiff base-ZnO nanocomposite's potential as protective therapy for rats' cisplatin-induced hepatotoxicity.

BACKGROUND: Despite cisplatin's long history as a cornerstone in cancer therapy, both acquired chemoresistance and significant impacts on healthy tissues limit its use. Hepatotoxicity is one of its side effects. Adjunct therapies have shown promise in not only attenuating liver damage caused by cisplatin but also in enhancing the efficacy of chemotherapy. In this context, a new quaternary ammonium chitosan Schiff base (QACSB) was synthesized and applied as an encapsulating agent for the in-situ synthesis of QACSB-ZnO nanocomposite. MATERIAL AND METHODS: Thirty male albino rats were classified into Group 1 (control) distilled water, Group 2 (Cisplatin-treated) (12 mg/kg, i.p), and Group 3 (QACSB-ZnO NCs/cisplatin-treated) (150 mg/kg/day QACSB-ZnO NCs, i.p) for 14 days + a single dose of cisplatin. Liver functions, tissue TNF-α, MDA, and GSH were measured as well as histopathological and immunohistochemical studies were performed. RESULTS: The QACSB-ZnO NCs significantly restore liver functions, tissue TNF-α, MDA, and GSH levels (p < 0.001). Histopathological examination showed patchy necrosis in the cisplatin-treated group versus other groups. The QACSB-ZnO NCs showed a weak TGF-ß1 (score = 4) and a moderate Bcl-2 immunohistochemistry expression (score = 6) versus the CP group. CONCLUSIONS: QACSB-ZnO NCs have been shown to protect the liver from cisplatin-induced hepatotoxicity.

Ziziphus spina-christi L. extract attenuates bleomycin-induced lung fibrosis in mice via regulating TGF-ß1/SMAD pathway: LC-MS/MS Metabolic profiling, chemical composition, and histology studies.

Ancient Egyptians (including Bedouins and Nubians) have long utilized Ziziphus spina-christi (L.), a traditional Arabian medicinal herb, to alleviate swellings and inflammatory disorders. It is also mentioned in Christian and Muslim traditions. Ziziphus spina-christi L. (Family: Rhamnaceae) is a plentiful source of polyphenols, revealing free radical scavenging, antioxidant, metal chelating, cytotoxic, and anti-inflammatory activities. Herein, different classes of the existing bioactive metabolites in Z. spina-christi L. were detected using liquid chromatography-tandem mass spectrometry (LC-MS/MS) for the first time. The study also aimed to assess the anti-inflammatory and antifibrotic properties of Z. spina-christi L. extract against bleomycin-induced lung fibrosis in an experimental mouse model. 32 male Swiss Albino mice were assigned into 4 groups; the first and second were the normal control group and the bleomycin positive control (single 2.5 U/kg bleomycin intratracheal dose). The third and fourth groups received 100 and 200 mg/kg/day Z. spina-christi L. extract orally for 3 weeks, 2 weeks before bleomycin, and 1 week after. The bioactive metabolites in Z. spina-christi L. extract were identified as phenolic acids, catechins, flavonoids, chalcones, stilbenes, triterpenoid acids, saponins, and sterols. The contents of total phenolic compounds and flavonoids were found to be 196.62 mg GAE/gm and 33.29 mg QE/gm, respectively. In the experimental study, histopathological examination revealed that lung fibrosis was attenuated in both Z. spina-christi L.- treated groups. Z. spina-christi L. extract downregulated the expression of nuclear factor kappa B (NF-κB) p65 and decreased levels of the inflammatory markers tumor necrosis factor-alpha (TNF-α), monocyte chemoattractant protein-1 (MCP-1), and c-Jun N-terminal kinase (JNK) in lung tissue. Z. spina-christi L. also downregulated the expression of the fibrotic parameters collagen-1, alpha-smooth muscle actin (α-SMA), transforming growth factor-beta 1 (TGF-ß1), matrix metalloproteinase-9 (MMP-9) and SMAD3, with upregulation of the antifibrotic SMAD7 in lung tissue. Overall, the present study suggests a potential protective effect of Z. spina-christi L. extract against bleomycin-induced lung fibrosis through regulation of the TGF-ß1/SMAD pathway.

Carboxymethyl-imidazolium O-vanillin Schiff base grafted into NH2-tagged MIL-101 (Cr) for effective removal of cupric ions from aqueous effluents.

A novel adsorbent (MIL-CMIVSB) was fabricated by modification of H2N-MIL-101(Cr) with carboxymethyl-imidazolium O-vanillin Schiff base. The MIL-CMIVSB's physicochemical characteristics were examined using the pertinent characterization methods. NH2-MIL-101(Cr) has a BET surface area of 1492.4 m2g-1, while MIL-CMIVSB adsorbent had 1278.7 m2g-1. Batch adsorption experiments examined the MIL-CMIVSB's cupric ion adsorption capacity from aqueous solutions at different adsorbent doses (0.1-3 mg), pH (2.0-10.0), contact times (0-240 min), metal ion initial concentrations (10-300 mg/L), and temperatures (298-308 K). The optimum conditions were 1 mg/mL of MIL-CMIVSB adsorbent, 46 min adsorption time, pH 7, 100 ppm initial cupric ion concentration, and 303 K temperature. MIL-CMIVSB effectively and selectively removes cupric ions with an adsorption capability of 359.05 ± 12.06 mg/g. The nonlinear Liu isotherm governed Cu(II) sorption performance on MIL-CMIVSB (KL = 0.257 ± 0.01 mg/g, R2 = 0.99892) and pseudo-2nd-order kinetically (k2 = 0.00116 × 10-4 g/mg min, R2 = 0.99721).

Synthesis of new quaternized chitosan Schiff bases and their N-alkyl derivatives as antimicrobial and anti-biofilm retardants in membrane technology.

New quaternized salicylidene chitosan Schiff bases (QSCSBs) and their N-octyl derivatives (OQCs) have been synthesized and characterized, aiming to develop innovative antimicrobial and anti-biofilm agents. This research holds immense potential, as these compounds could be utilized as anti-biofouling additives in membrane technology in the future. The synthesis involved the modification of low molecular-weight-chitosan (LMC) through simultaneous Schiff base formation and quaternization processes to create QSCSBs. Subsequently, QSCSBs were catalytically reduced to form quaternized N-benzyl chitosan (QBCs) intermediates, which then underwent nucleophilic substitution reactions affording N-octyl quaternized chitosans (OQCs). Characterization techniques such as elemental, spectral, and microscopic analyses were used to confirm the successful synthesis of these materials. As membrane technology relies on surface charge, QSCSBs and OQCs with large zeta potentials could be used as positively charged additives. Moreover, SEM image revealed the regular distribution of pores and voids across the additives' surfaces raises intriguing questions about their implications for membrane performance. Meanwhile, the superior antibacterial and antibiofilm potential of these materials, particularly QSCSB2 and OQC2, indicate that the utilization of these compounds as anti-biofouling additives in membrane technology could significantly improve the performance and longevity of membranes used in various applications such as water treatment and desalination.

Exploring the chondroitin sulfate nanogel's potential in combating nephrotoxicity induced by cisplatin and doxorubicin-An in-vivo study on rats.

In this study, we aim to unveil the potential of itaconyl chondroitin sulfate nanogel (ICSNG) in tackling chronic kidney diseases triggered by the administration of CDDP and doxorubicin (Adriamycin, ADR). To that end, the new drug delivery system (ICSNG) was initially prepared, characterized, and loaded with the target drugs. Thereafter, the in-vivo studies were performed using five equally divided groups of 100 male Sprague-Dawley (SD) rats. Biochemical evaluation and immunohistochemistry studies have revealed the renal toxicity and the ameliorative effects of ICSNG on renal function. When ICSNG-based treatments were contrasted with the CDDP and ADR infected groups, they significantly increased paraoxonase-1 (PON-1), superoxide dismutase (SOD), catalase (CAT) and albumin activity and significantly decreased nitric oxide (NO), tumor necrosis factor alpha (TNF-α), creatinine, urea, and cyclooxygenase-2 (COX-2) activity (p < 0.001). The findings of the current study imply that ICSNG may be able to lessen renal inflammation and damage in chronic kidney disorders brought on by the administration of CDDP and ADR. Interestingly, according to the estimated selectivity indices, the ICSNG-encapsulated drugs have demonstrated superior selectivity for cancer MCF-7 cells, over healthy HSF cells, in comparison to the bare drugs.

Chemotherapeutic Activity of Imidazolium-Supported Pd(II) o-Vanillylidene Diaminocyclohexane Complexes Immobilized in Nanolipid as Inhibitors for HER2/neu and FGFR2/FGF2 Axis Overexpression in Breast Cancer Cells.

Two bis-(imidazolium-vanillylidene)-(R,R)-diaminocyclohexane ligands (H2(VAN)2dach, H2L1,2) and their Pd(II) complexes (PdL1 and PdL2) were successfully synthesized and structurally characterized using microanalytical and spectral methods. Subsequently, to target the development of new effective and safe anti-breast cancer chemotherapeutic agents, these complexes were encapsulated by lipid nanoparticles (LNPs) to formulate (PdL1LNP and PdL2LNP), which are physicochemically and morphologically characterized. PdL1LNP and PdL2LNP significantly cause DNA fragmentation in MCF-7 cells, while trastuzumab has a 10% damaging activity. Additionally, the encapsulated Pd1,2LNPs complexes activated the apoptotic mechanisms through the upregulated P53 with p < 0.001 and p < 0.05, respectively. The apoptotic activity may be triggered through the activity mechanism of the Pd1,2LNPs in the inhibitory actions against the FGFR2/FGF2 axis on the gene level with p < 0.001 and the Her2/neu with p < 0.05 and p < 0.01. All these aspects have triggered the activity of the PdL1LNP and PdL2LNP to downregulate TGFß1 by p < 0.01 for both complexes. In conclusion, LNP-encapsulated Pd(II) complexes can be employed as anti-cancer drugs with additional benefits in regulating the signal mechanisms of the apoptotic mechanisms among breast cancer cells with chemotherapeutic-safe actions.

Silver nanoparticles formulation of Marrubium alysson L. phenolic extract potentiates cytotoxicity through apoptosis with molecular docking study as Bcl-2 inhibitors.

Crude or semi-purified extracts of plants can play a significant role as antitumor agents. They were used as stabilizing and reducing agents in the preparation of silver nanoparticles (AgNPs) that allows these particles to have more efficient cytotoxic activity. In the current study, the extract of Marrubium alysson L., a plant of common occurrence in Egypt was used to synthesize AgNPs for the first time, where comparison of anticancer activity of crude and phenolic extracts with the AgNPs were extensively studied against cancer cell lines PC-3 and HCT-116. Interestingly, AgNPs of the crude extract exhibited promising cytotoxicity with IC50 values of 10.4 and 16.3 µg/ml, while AgNPs of the phenolic extract exhibited very potent cytotoxicity with IC50 values of 2.66 and 1.34 µg/ml compared to Doxorubicin (as a standard reference drug) that exhibited IC50 values of 5.13 and 4.36 µg/ml, respectively against the tested cells. Additionally, AgNPs of the phenolic extract induced apoptosis in HCT-116 with a higher ratio than in PC-3 cells. It induced apoptosis in PC-3 cells by 79.3-fold change, while it induced total colon apoptotic cell death by 228.3-fold change compared to untreated control. Finally, the apoptotic activity of AgNPs of the phenolic extract in the treated PC-3 and HCT-116 cells was confirmed using RT-PCR. As a result, AgNPs of the phenolic extract could be considered a promising anticancer candidate through apoptosis-induction.Communicated by Ramaswamy H. Sarma.

A New Saponin (Zygo-albuside D) from Zygophyllum album Roots Triggers Apoptosis in Non-Small Cell Lung Carcinoma (A549 Cells) through CDK-2 Inhibition.

Phytochemical study of the ethyl acetate root extract of Zygophyllum album has resulted in the isolation of a new saponin, Zygo-albuside D (1), along with two known compounds; (3-O-[ß-D-quinovopyranosyl]-quinovic acid) (2), which is first reported in the root, and catechin (3), first reported in the genus. Their chemical structures were established by NMR and high-resolution mass spectrometry (HRMS). The new saponin (1) exhibited promising cytotoxicity with IC50 values of 3.5 and 5.52 µM on A549 and PC-3 cancer cell lines, respectively, compared to doxorubicin with IC50 values of 9.44 and 11.39 µM on A549 and PC-3 cancer cell lines, respectively. While it had an IC50 value of 46.8 µM against WISH cells. Investigating apoptosis-induction, compound 1 induced total apoptotic cell death in A549 lung cancer cells by 32-fold; 21.53% compared to 0.67% in the untreated control cells. Finally, it upregulated the pro-apoptotic genes and downregulated the antiapoptotic gene using gene expression levels. Compound 1 exhibited remarkable CDK-2 target inhibition by 96.2% with an IC50 value of 117.6 nM compared to Roscovitine. The molecular docking study further confirmed the binding affinity of compound 1 as CDK2 and Bcl2 inhibitors that led to apoptosis induction in A549 cancer cells. Hence, this study highlights the importance of compound 1 in the design of a new anticancer agent with specific mechanisms.

Deciphering Molecular Aspects of Potential α-Glucosidase Inhibitors within Aspergillus terreus: A Computational Odyssey of Molecular Docking-Coupled Dynamics Simulations and Pharmacokinetic Profiling.

Hyperglycemia, as a hallmark of the metabolic malady diabetes mellitus, has been an overwhelming healthcare burden owing to its high rates of comorbidity and mortality, as well as prospective complications affecting different body organs. Available therapeutic agents, with α-glucosidase inhibitors as one of their cornerstone arsenal, control stages of broad glycemia while showing definitive characteristics related to their low clinical efficiency and off-target complications. This has propelled the academia and industrial section into discovering novel and safer candidates. Herein, we provided a thorough computational exploration of identifying candidates from the marine-derived Aspergillus terreus isolates. Combined structural- and ligand-based approaches using a chemical library of 275 metabolites were adopted for pinpointing promising α-glucosidase inhibitors, as well as providing guiding insights for further lead optimization and development. Structure-based virtual screening through escalating precision molecular docking protocol at the α-glucosidase canonical pocket identified 11 promising top-docked hits, with several being superior to the market drug reference, acarbose. Comprehensive ligand-based investigations of these hits' pharmacokinetics ADME profiles, physiochemical characterizations, and obedience to the gold standard Lipinski's rule of five, as well as toxicity and mutagenicity profiling, proceeded. Under explicit conditions, a molecular dynamics simulation identified the top-stable metabolites: butyrolactone VI (SK-44), aspulvinone E (SK-55), butyrolactone I 4''''-sulfate (SK-72), and terrelumamide B (SK-173). They depicted the highest free binding energies and steadiest thermodynamic behavior. Moreover, great structural insights have been revealed, including the advent of an aromatic scaffold-based interaction for ligand-target complex stability. The significance of introducing balanced hydrophobic/polar moieties, like triazole and other bioisosteres of carboxylic acid, has been highlighted across docking, ADME/Tox profiling, and molecular dynamics studies for maximizing binding interactions while assuring safety and optimal pharmacokinetics for targeting the intestinal-localized α-glucosidase enzyme. Overall, this study provided valuable starting points for developing new α-glucosidase inhibitors based on nature-derived unique scaffolds, as well as guidance for prospective lead optimization and development within future pre-clinical and clinical investigations.

Alginate-chitosan-microencapsulated tyrosols/oleuropein-rich olive mill waste extract for lipopolysaccharide-induced skin fibroblast inflammation treatment.

The Ca2+ ion-driven emulsification-ionotropic gelation method produced chitosan-alginate microspheres (CAMSs) with a narrow particle size distribution (PSD). Particle size distribution and zeta potential studies, as well as spectral electron microscopy, were used to assess the microspheres' physicochemical properties and morphology. The tyrosols (hydroxytyrosol (HT), tyrosol (TY), and oleuropein (OE) were loaded into these microspheres using a polyphenol extract (PPE) from Koroneki olive mill waste (KOMW). The microencapsulation efficiency and loading capacity of microspheres for PPE were 98.8% and 3.9%, respectively. Three simulated fluids, including gastric (pH = 1.2), intestinal (pH = 6.8), and colonic (pH = 7.4), were used to examine how the pH of the releasing medium affected the ability of CAMSs to release bioactive phenols. At a severely acidic pH (1.2, SGF), PPE release is nearly halted, while at pH 6.8 (SCF), release is at its maximum. Additionally, the PPE-CAMPs have ameliorated the endogenous antioxidant content SOD, GST, GPx with significant values from 0.05 to 0.01 in the treated LPS/human skin fibroblast cells. The anti-inflammatory response was appeared through their attenuations activity for the released cytokines TNF-α, IL6, IL1ß, and IL 12 with levels significantly from 0.01 to 0.001. Microencapsulation of PPE by CAMPs significantly improved its antioxidant and anti-inflammatory capabilities.

Immobilization of ZnO-TiO2 Nanocomposite into Polyimidazolium Amphiphilic Chitosan Film, Targeting Improving Its Antimicrobial and Antibiofilm Applications.

This study presents a green protocol for the fabrication of a multifunctional smart nanobiocomposite (NBC) (ZnO-PIACSB-TiO2) for secure antimicrobial and antibiofilm applications. First, shrimp shells were upgraded to a polyimidazolium amphiphilic chitosan Schiff base (PIACSB) through a series of physicochemical processes. After that, the PIACSB was used as an encapsulating and coating agent to manufacture a hybrid NBC in situ by co-encapsulating ZnONPs and TiO2NPs. The physicochemical and visual characteristics of the new NBC were investigated by spectral, microscopic, electrical, and thermal methods. The antimicrobial indices revealed that the newly synthesized, PIACSB-coated TiO2-ZnO nanocomposite is an exciting antibiotic due to its amazing antimicrobial activity (MIC/MBC→0.34/0.68 µg/mL, 0.20/0.40 µg/mL, and 0.15/0.30 µg/mL working against S. aureus, E. coli, and P. aeruginosa, respectively) and antifungal capabilities. Additionally, ZnO-PIACSB-TiO2 is a potential fighter of bacterial biofilms, with the results being superior to those of the positive control (Cipro), which worked against S. aureus (only 8.7% ± 1.9 biofilm growth), E. coli (only 1.4% ± 1.1 biofilm growth), and P. aeruginosa (only 0.85% ± 1.3 biofilm growth). Meanwhile, the NBC exhibits excellent biocompatibility, as evidenced by its IC50 values against both L929 and HSF (135 and 143 µg/mL), which are significantly higher than those of the MIC doses (0.24-24.85 µg/mL) that work against all tested microbes, as well as the uncoated nanocomposite (IC50 = 19.36 ± 2.04 and 23.48 ± 1.56 µg/mL). These findings imply that the new PIACSB-coated nanocomposite film may offer promising multifunctional food packaging additives to address the customer demand for safe, eco-friendly food products with outstanding antimicrobial and antibiofilm capabilities.

Cost-effective removal of toxic methylene blue dye from textile effluents by new integrated crosslinked chitosan/aspartic acid hydrogels.

Chitosan/aspartic acid hydrogels were synthesized for MB dye removal from textile aqueous effluents with different ratios by gelation of chitosan with non-toxic gelling agent, crosslinker, glutaraldehyde (Glu). The obtained hydrogels were characterized by spectral and morphological techniques. The characterization techniques confirmed successful preparations and MB dye adsorption. Batch experiments were done to investigate the effects of adsorbent dose, pH, contact time, temperature, and initial MB dye concentration. The optimum conditions were: adsorbent dose 0.1 g, pH 5, contact time 30 min, and temperature 25 °C for Chitosan-Aspartic Acid Hydrogel 1 (CSAA-HG1) and adsorbent dose 0.4 g, pH 2, contact time 60 min, temperature 25 °C for Chitosan-Aspartic Acid Hydrogel 2 (CSAA-HG2). Adsorption capacity of newly hydrogels CSAA-HG1,2 was compared with each other. Adsorption efficiencies reached 99.85 % for CSAA-HG1 and 99.88 % for CSAA-HG2. MB dye adsorption on CSAA-HG1,2 followed Freundlich isotherm model (R2 = 0.94 and 0.92, respectively). Both adsorbents exhibited pseudo-second-order kinetics for MB dye adsorption (R2 = 1). The negative ΔHo indicated that the MB dye adsorption was exothermic, negative ΔGo confirmed that MB dye adsorption process was spontaneous and low values of ∆So indicated low degree of freedom, ordered MB dye molecules on CSAA-HG1,2 surfaces.

Comparison of the ameliorative roles of crab chitosan nanoparticles and mesenchymal stem cells against cisplatin-triggered nephrotoxicity.

AIM: In the present investigation, we compared the effects of mesenchymal stem cells extracted from bone marrow (BMSCs) and crab chitosan nanoparticles (CCNPs) on renal fibrosis in cisplatin (CDDP)-induced kidney injury rats. MATERIAL AND METHODS: 90 male Sprague-Dawley (SD) rats were divided into two equal groups and alienated. Group I was set into three subgroups: the control subgroup, the CDDP-infected subgroup (acute kidney injury), and the CCNPs-treated subgroup. Group II was also divided into three subgroups: the control subgroup, the CDDP-infected subgroup (chronic kidney disease), and the BMSCs-treated subgroup. Through biochemical analysis and immunohistochemical research, the protective effects of CCNPs and BMSCs on renal function have been identified. RESULTS: CCNPs and BMSC treatment resulted in a substantial rise in GSH and albumin and a decrease in KIM-1, MDA, creatinine, urea, and caspase-3 when compared to the infected groups (p < 0.05). CONCLUSION: According to the current research, chitosan nanoparticles and BMSCs may be able to reduce renal fibrosis in acute and chronic kidney diseases caused by CDDP administration, with more improvement of kidney damage resembling normal cells after CCNPs administration.

Therapeutic potential and protection enhancement of mesenchymal stem cell against cisplatin-induced nephrotoxicity using hyaluronic acid-chitosan nanoparticles as an adjuvant.

A newly synthesized nanoplatform of hyaluronic acid and chitosan nanoparticles (HA/CNPs) was applied to improve the therapeutic efficacy and protection of bone marrow mesenchymal stem cells (BM-MSCs) against cisplatin (CDDP)-induced nephrotoxicity in rats. CDDP administration causes significant increases in levels of serum creatinine (SCr), urea, and KIM-1 coupled with significant albumin level falls, as indicative of acute renal dysfunction. Moreover, the level of the antioxidant enzyme (GSH) was significantly decreased, while the levels of lipid peroxidation (MDA) and inflammatory (IL-6) and apoptotic (caspase-3) markers were significantly increased, indicating a decline in the kidney's antioxidant defense and increased inflammation. In contrast, when rats were pre-treated with either MSCs or MSCs-HA/CNPs before receiving CDDP, the levels of SCr, urea, KIM-1, MDA, IL-6, and caspase-3 were significantly decreased with simultaneous significant rises in GSH and albumin, impelling a great improvement in the antioxidant and anti-inflammatory defenses of the kidney as well as its functions. Intriguingly, MSCs-HA/CNPs were more effective against caspase-3 than MSCs alone, revealing the high anti-apoptotic capability of HA/CNPs. This finding suggests that HA/CNPs could effectively protect MSCs from oxidative stress and apoptosis and thus increase their stability and longevity.

Integration of Chemoinformatics and Multi-Omics Analysis Defines ECT2 as a Potential Target for Cancer Drug Therapy.

Epithelial cell transforming 2 (ECT2) is a potential oncogene and a number of recent studies have correlated it with the progression of several human cancers. Despite this elevated attention for ECT2 in oncology-related reports, there is no collective study to combine and integrate the expression and oncogenic behavior of ECT2 in a panel of human cancers. The current study started with a differential expression analysis of ECT2 in cancerous versus normal tissue. Following that, the study asked for the correlation between ECT2 upregulation and tumor stage, grade, and metastasis, along with its effect on patient survival. Moreover, the methylation and phosphorylation status of ECT2 in tumor versus normal tissue was assessed, in addition to the investigation of the ECT2 effect on the immune cell infiltration in the tumor microenvironment. The current study revealed that ECT2 was upregulated as mRNA and protein levels in a list of human tumors, a feature that allowed for the increased filtration of myeloid-derived suppressor cells (MDSC) and decreased the level of natural killer T (NKT) cells, which ultimately led to a poor prognosis survival. Lastly, we screened for several drugs that could inhibit ECT2 and act as antitumor agents. Collectively, this study nominated ECT2 as a prognostic and immunological biomarker, with reported inhibitors that represent potential antitumor drugs.

Cross-linked quaternized polyethersulfone-amino crystalline nanocellulose composite membrane for enhanced phosphate removal from wastewater.

Cross-linked quaternized polyethersulfone (QPES) hybrid mixed polymer membranes (MPMs) loading amino crystalline nanocellulose (ACNC) were successfully fabricated and applied for phosphate removal. The successful production of novel materials was validated by microscopic, spectral, and microanalytical methods. When compared to the native QPES membrane, the primary qualities of QPES hybrid membranes (hydrophilicity, porosity, permeability, antifouling) have been greatly improved overall. In addition, the surface zeta potential (SZP) and ion exchange capacity (IEC) measurements demonstrated the high positive surface charge densities of MPMs, which is beneficial for phosphate uptake. Phosphate adsorption by these membranes was studied at different temperatures, contact times, and initial phosphate concentrations using batch experiments, to investigate the optimal conditions for phosphate uptake. The MPMs showed excellent adsorption capacities with maximal removal capacities in the range of 68.8-87.95 %. Phosphate adsorption on MPMs was regulated primarily by the Sips isotherm model with multilayer adsorption capabilities and exhibited pseudo-second order kinetics (R2 = 0.9951-0.9976). The positive ΔH° and ΔS° values are indicative of the endothermic nature of phosphate adsorption and randomness increase. The negative ΔG° value indicates the spontaneousity of phosphate adsorption. Phosphate removal effectiveness of the membranes was maintained following recovery and regeneration with NaOH.

Synthesis and Characterization of New Lutidinium Ionic Liquid-Supported Vanadylsalicylaldoxime Complex for Catalytic Application in Epoxidation Reaction.

A new chelating task-specific ionic liquid (TSIL), lutidinium-based salicylaldoxime (LSOH), and its square pyramidal vanadyl(II) complex (VO(LSO)2 ) have been successfully synthesized and structurally characterized using elemental (CHN), spectral, and thermal analyses. The catalytic activity of the lutidinium-salicylaldoxime complex (VO(LSO)2 ) in the alkene epoxidation reactions was studied under various reaction conditions, such as solvent effect, alkene/oxidant molar ratio, pH, reaction temperature, reaction time, and the catalyst dose. The results demonstrated that the CHCl3 solvent, 1 : 3 of the cyclohexene/H2 O2 ratio, pH 8, temperature of 340 K, and catalyst dose of 0.012 mmol are assigned as the optimum conditions for achieving maximum catalytic activity for VO(LSO)2 . Moreover, the VO(LSO)2 complex has the potential for application in the effective and selective epoxidation of alkenes. Notably, under optimal VO(LSO)2 conditions, cyclic alkenes convert more efficiently to their corresponding epoxides than linear alkenes.

New Ionic Liquid Microemulsion-Mediated Synthesis of Silver Nanoparticles for Skin Bacterial Infection Treatments.

This work reports a new approach for the synthesis of extremely small monodispersed silver nanoparticles (AgNPs) (2.9-1.5) by reduction of silver nitrate in a new series of benzyl alkyl imidazolium ionic liquids (BAIILs)-based microemulsions (3a-f) as media and stabilizing agents. Interestingly, AgNPs isolated from the IILMEs bearing the bulkiest substituents (tert-butyl and n-butyl) (3f) displayed almost no nanoparticle agglomeration. In an in vitro antibacterial test against ESKAPE pathogens, all AgNPs-BAIILs had potent antibiotic activity, as reflected by antibacterial efficiency indices. Furthermore, when compared to other nanoparticles, these were the most effective in preventing biofilm formation by the tested bacterial strains. Moreover, the MTT assay was used to determine the cytotoxicity of novel AgNPs-BAIILs on healthy human skin fibroblast (HSF) cell lines. The MTT assay revealed that novel AgNPs-BAIILs showed no significant toxic effects on the healthy cells. Thus, the novel AgNPs-BAIILs microemulsions could be used as safe antibiotics for skin bacterial infection treatments. AgNPs isolated from BAIIL (3c) was found to be the most effective antibiotic of the nanoparticles examined.

Molecular and Biological Investigation of Isolated Marine Fungal Metabolites as Anticancer Agents: A Multi-Target Approach.

Cancer is the leading cause of death globally, with an increasing number of cases being annually reported. Nature-derived metabolites have been widely studied for their potential programmed necrosis, cytotoxicity, and anti-proliferation leading to enrichment for the modern medicine, particularly within the last couple of decades. At a more rapid pace, the concept of multi-target agents has evolved from being an innovative approach into a regular drug development procedure for hampering the multi-fashioned pathophysiology and high-resistance nature of cancer cells. With the advent of the Red Sea Penicillium chrysogenum strain S003-isolated indole-based alkaloids, we thoroughly investigated the molecular aspects for three major metabolites: meleagrin (MEL), roquefortine C (ROC), and isoroquefortine C (ISO) against three cancer-associated biological targets Cdc-25A, PTP-1B, and c-Met kinase. The study presented, for the first time, the detailed molecular insights and near-physiological affinity for these marine indole alkaloids against the assign targets through molecular docking-coupled all-atom dynamic simulation analysis. Findings highlighted the superiority of MEL's binding affinity/stability being quite in concordance with the in vitro anticancer activity profile conducted via sulforhodamine B bioassay on different cancerous cell lines reaching down to low micromolar or even nanomolar potencies. The advent of lengthy structural topologies via the metabolites' extended tetracyclic cores and aromatic imidazole arm permitted multi-pocket accommodation addressing the selectivity concerns. Additionally, the presence decorating polar functionalities on the core hydrophobic tetracyclic ring contributed compound's pharmacodynamic preferentiality. Introducing ionizable functionality with more lipophilic characters was highlighted to improve binding affinities which was also in concordance with the conducted drug-likeness/pharmacokinetic profiling for obtaining a balanced pharmacokinetic/dynamic profile. Our study adds to the knowledge regarding drug development and optimization of marine-isolated indole-based alkaloids for future iterative synthesis and pre-clinical investigations as multi-target anticancer agents.

Analysis of Marrubiin in Marrubium alysson L. Extract Using Advanced HPTLC: Chemical Profiling, Acetylcholinesterase Inhibitory Activity, and Molecular Docking.

The main purpose of this work is to investigate the phytochemical composition of Marrubium alysson L. non-polar fraction. GC/MS analysis was used to evaluate the plant extract's saponifiable and unsaponifiable matter. Although M. alysson L. lipoidal matter saponification produced 30.3% of fatty acid methyl esters and 69.7% of unsaponifiable matter. Phytol was the most dominant substance in the unsaponifiable materials. Notably, marrubiin which is one of the most prominent metabolites of Marrubium alysson L. was not detected through our adopted GC/MS technique. Thus, further characterization was proceeded through simple and rapid HPTLC analysis which successfully managed to identify marrubiin. Based on the regression equation, the concentration of marrubiin in M. alysson L. extract was 14.09 mg/g of dry extract. Concerning acetylcholinesterase inhibitory activity, both the crude M. alysson L. total methanolic extract and the non-polar fraction displayed reasonable inhibitory activity against acetylcholinesterase (AChE), whereas the pure compound marrubiin was considered to be the most effective and potent AChE inhibitor, with an IC50 value of 52.66 (µM). According to the molecular docking studies, potential sites of interaction between the pure chemical marrubiin and AChE were examined. The results show that Tyr124 on AChE residue was critical to the activity of the aforementioned drug. Based on the depicted marrubin AChE inhibition activity and reported safety profile, this chemical metabolite is considered as a promising lead compound for further pre-clinical investigation as well as drug development and optimization.