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In this investigation, 4-antipyrinecarboxaldhyde was reacted with methyl hydrazinecarbodithioate to afford the carbodithioate derivative 3. The as-prepared carbodithioate derivative 3 is considered to be a key molecule for the preparation of new antipyrine-1,3,4-thiadiazole-based molecules (4–9) through its reaction with the appropriate hydrazonoyl halides. Furthermore, a typical Biginelli three-component cyclocondensation reaction involving ethyl acetoacetate, 4-antipyrinecarboxaldhyde, and thiourea under the standard conditions is carried out in the presence of sulfuric acid to afford the corresponding antipyrine–pyrimidine hybrid molecule (10). The latter was submitted to react with hydrazine monohydrate to provide the corresponding hydrazide derivative (11) which, under reaction with ethyl acetoacetate in refluxing ethanol containing catalytic amount of acetic acid, afforded the corresponding derivative (12). The structure of the newly synthesized compounds was affirmed by their spectral and microanalytical data. We also screened for their antimicrobial potential (ZOI and MIC) and conducted a kinetic study. Additionally, the mechanism of biological action was assessed by a membrane leakage assay and SEM imaging technique. Moreover, the biological activities and the binding modes of these compounds were further supplemented by an in silico docking study against E. coli β-carbonic anhydrase. The amount of cellular protein released by E. coli is directly correlated to the concentration of compound 9, which was found to be 177.99 µg/mL following treatment with 1.0 mg/mL of compound 9. This finding supports compound 9's antibacterial properties and explains how the formation of holes in the E. coli cell membrane results in the release of proteins from the cytoplasm. The newly synthesized compounds represent acceptable antimicrobial activities with potential action against E. coli β-carbonic anhydrase. The docking studies and antimicrobial activity test proved that compound (9) declared a greater activity than the other synthesized compounds. [ABSTRACT FROM AUTHOR]

The exacerbation of climatic changes helped to increase the risk of plant diseases in the world. The novelty of this study lies in the manufacture of therapeutic nutrients using nanotechnology with strong effectiveness against plant disease. Based on this concept, we mycosynthesized bimetallic ZnO-CuO nanoparticles (NPs), alternatives to reduce the spread of Vicia faba Fusarium wilt disease, which is one of the world's most imperative cultivated crops. The article's uniqueness comes in the utilization of ZnO-CuO nanoparticles to carry out two crucial tasks: therapeutic nutrients and managing Fusarium disease. To evaluate the resistance of infected plants, disease index (DI), photosynthetic pigments, osmolytes, oxidative stress and yield parameters were assessed. NPs of ZnO, CuO, and ZnO-CuO were mycosynthesized using a biomass filtrate of Aspergillus fumigatus OQ519856. DI reached 87.5%, due to Fusarium infection, and, as a result, a severe decrease in growth characters, photosynthetic pigments, total soluble carbohydrates, and proteins as well as yield parameters was observed. Infected plants produced more of the studied metabolites and antioxidants. On the other hand, the treatment with CuO-ZnO NPs led to a great decline in the DI by 22.5% and increased the protection by 74.28%. A clear improvement in growth characters, photosynthetic pigments and a high content of carbohydrates and proteins was also observed in both healthy and infected plants as a result of CuO-ZnO NPs treatment. Remarkably, CuO-ZnO NPs significantly increased the yield parameters, i.e., pods/plant and pod weight, by 146.1% and 228.8%, respectively. It could be suggested that foliar application of NPs of ZnO, CuO, and ZnO-CuO could be commercially used as antifusarial agents and strong elicitors of induced systemic resistance. [ABSTRACT FROM AUTHOR]

One of the most hazardous diseases that influences human health globally is microbial infection. Therefore, bimetallic nanoparticles have received much attention for controlling microbial infections in the current decade. In the present study, bimetallic selenium–silver nanoparticles (Se-Ag NPs) were effectively biosynthesized using watermelon rind WR extract through the green technique for the first time. UV-visible spectroscopy, transmission electron microscopy (TEM), and energy dispersive X-ray spectroscopy (EDX) methods were used to characterize the produced NPs. The results indicated that the bimetallic Se-Ag NPs had synergistic antimicrobial activity at low concentrations, which helped to reduce the toxicity of Ag NPs after the bimetallic Se-Ag NPs preparation and increase their great potential. Se-Ag NPs with sizes ranging from 18.3 nm to 49.6 nm were detected by TEM. Se-Ag NP surfaces were uniformly visible in the SEM picture. The cytotoxicity of bimetallic Se-Ag NPs was assessed against the Wi38 normal cell line to check their safety, where the IC50 was 168.42 µg/mL. The results showed that bimetallic Se-Ag NPs had antibacterial action against Candida albicans, Escherichia coli, Pseudomonas aeruginosa, Klebsiella oxytoca, Bacillus subtilis, and Staphylococcus aureus with a minimum inhibitory concentration (MIC) of 12.5 to 50 µg/mL. Additionally, bimetallic Se-Ag NPs had promising anticancer activity toward the MCF7 cancerous cell line, where the IC50 was 21.6 µg/mL. In conclusion, bimetallic Se-Ag NPs were biosynthesized for the first time using WR extract, which had strong antibacterial, antifungal and anticancer properties. [ABSTRACT FROM AUTHOR]

An excessive accumulation of crystal violet dye in the human body results in an accelerated heart rate, tetraplegia, eye irritation, and long-term damage to the transparent mucous membrane that protects the eyeballs. Accordingly, in this paper, sodium manganese silicate/sodium manganese silicate hydroxide hydrate was easily fabricated as a novel type of nanostructures for the successful disposal of crystal violet dye from aqueous solutions. The formed sodium manganese silicate/sodium manganese silicate hydroxide hydrate nanostructures after the hydrothermal treatment of the gel produced from the interaction of Mn(II) ions with Si(IV) ions at 180 °C for 6, 12, 18, and 24 h were abbreviated as MS1, MS2, MS3, and MS4, respectively. The XRD showed that the average crystallite size of the MS1, MS2, MS3, and MS4 samples is 8.38, 7.43, 4.25, and 8.76 nm, respectively. The BET surface area of the MS1, MS2, MS3, and MS4 samples is 41.58, 46.15, 58.25, and 39.69 m2/g, respectively. The MS1, MS2, MS3, and MS4 samples consist of spherical and irregular shapes with average grain sizes of 157.22, 88.06, 43.75, and 107.08 nm, respectively. The best adsorption conditions of the crystal violet dye employing the MS1, MS2, MS3, and MS4 products were achieved at pH = 8, contact time = 140 min, and solution temperature = 298 kelvin. The linear pseudo-2nd-order model as well as the linear Langmuir isotherm better describe the disposal of the crystal violet dye using the MS1, MS2, MS3, and MS4 adsorbents. The studied thermodynamic parameters indicated that the disposal of the crystal violet dye employing the MS1, MS2, MS3, and MS4 adsorbents is spontaneous, exothermic, and chemical. The maximum disposal capacities of the MS1, MS2, MS3, and MS4 adsorbents towards crystal violet dye are 342.47, 362.32, 411.52, and 310.56 mg/g, respectively. [ABSTRACT FROM AUTHOR]

It is essential to remove rhodamine 6G and acid orange 10 dyes from contaminated water because they can induce cancer and irritate the lungs, skin, mucous, membranes, and eyes. Hence, in the current work, the Pechini sol–gel method was used for the facile synthesis of ZrO2/CdMn2O4/CdO as novel nanocomposites at 600 and 800 °C. The synthesized nanocomposites were used as novel adsorbents for the efficient removal of rhodamine 6G and acid orange 10 dyes from aqueous media. The nanocomposites, which were synthesized at 600 and 800 °C, were abbreviated as EK600 and EK800, respectively. The synthesized nanocomposites were characterized by EDS, XRD, N2 adsorption/desorption analyzer, and FE-SEM. The patterns of XRD showed that the average crystal size of the EK600 and EK800 nanocomposites is 68.25 and 85.32 nm, respectively. Additionally, the images of FE-SEM showed that the surface of the EK600 nanocomposite consists of spherical, polyhedral, and rod shapes with an average grain size of 99.36 nm. Additionally, the surface of the EK800 nanocomposite consists of polyhedral and spherical shapes with an average grain size of 143.23 nm. In addition, the BET surface area of the EK600 and EK800 nanocomposites is 46.33 and 38.49 m2/g, respectively. The optimal conditions to achieve the highest removal of rhodamine 6G and acid orange 10 dyes are pH = 8, contact time = 24 min, and temperature = 298 kelvin. The greatest removal capacity of the EK600 and EK800 adsorbents towards rhodamine 6G dye is 311.53 and 250.63 mg/g, respectively. Additionally, the greatest removal capacity of the EK600 and EK800 adsorbents towards acid orange 10 dye is 335.57 and 270.27 mg/g, respectively. The removal of rhodamine 6G and acid orange 10 dyes using the EK600 and EK800 adsorbents is spontaneous, exothermic, follows the Langmuir adsorption isotherm, and fits well with the pseudo-first-order kinetic model. [ABSTRACT FROM AUTHOR]

A new series of 4-((7-methoxyquinolin-4-yl) amino)-N-(substituted) benzenesulfonamide 3(a–s) was synthesized via the reaction of 4-chloro-7-methoxyquinoline 1 with various sulfa drugs. The structural elucidation was verified based on spectroscopic data analysis. All the target compounds were screened for their antimicrobial activity against Gram-positive bacteria, Gram-negative bacteria, and unicellular fungi. The results revealed that compound 3l has the highest effect on most tested bacterial and unicellular fungal strains. The highest effect of compound 3l was observed against E. coli and C. albicans with MIC = 7.812 and 31.125 µg/mL, respectively. Compounds 3c and 3d showed broad-spectrum antimicrobial activity, but the activity was lower than that of 3l. The antibiofilm activity of compound 3l was measured against different pathogenic microbes isolated from the urinary tract. Compound 3l could achieve biofilm extension at its adhesion strength. After adding 10.0 µg/mL of compound 3l, the highest percentage was 94.60% for E. coli, 91.74% for P. aeruginosa, and 98.03% for C. neoformans. Moreover, in the protein leakage assay, the quantity of cellular protein discharged from E. coli was 180.25 µg/mL after treatment with 1.0 mg/mL of compound 3l, which explains the creation of holes in the cell membrane of E. coli and proves compound 3l's antibacterial and antibiofilm properties. Additionally, in silico ADME prediction analyses of compounds 3c, 3d, and 3l revealed promising results, indicating the presence of drug-like properties. [ABSTRACT FROM AUTHOR]

Simple Summary: In this study, we have developed CD44 and folate receptor-targeting multi-functional dual drug-loaded nanoparticles. This comprises hyaluronic acid (HA) and folic acid (FA) conjugated to 2-deoxy glucose (2DG) and a shell linked to a dichloroacetate (DCA) and magnesium oxide (MgO) core (2DG@DCA@MgO; DDM) to enhance the localized chemo-radiotherapy for effective breast cancer (BC) treatment. The physicochemical properties of nanoparticles including stability, selectivity, responsive release to pH, cellular uptake, and anticancer efficacy were comprehensively examined. Mechanistically, we identified multiple component signal pathways as important regulators of BC metabolism and mediators for the inhibitory effects exerted by DDM. Nanoparticles exhibited sustained DDM release properties in bio-relevant media, which was responsive to acidic pH providing edibility to the control of drug release from nanoparticles. DDM-loaded and HA–FA-functionalized nanoparticles exhibited increased selectivity and uptake by BC cells. Cell-based assays indicated that the functionalized DDM significantly suppressed cancer cell growth and boosted radiotherapy (RT) efficacy via inducing cell cycle arrest, enhancing apoptosis, and modulating glycolytic and OXPHOS pathways. Accordingly, the inhibition of glycolysis/OXPHOS by DDM and RT treatment may result in cancer metabolic reprogramming via a novel PI3K/AKT/mTOR/P53NF-κB/VEGF pathway in BC cells. Therefore, the dual targeting of glycolysis/OXPHOS pathways is suggested as a promising antitumor strategy. Globally, breast cancer (BC) poses a serious public health risk. The disease exhibits a complex heterogeneous etiology and is associated with a glycolytic and oxidative phosphorylation (OXPHOS) metabolic reprogramming phenotype, which fuels proliferation and progression. Due to the late manifestation of symptoms, rigorous treatment regimens are required following diagnosis. Existing treatments are limited by a lack of specificity, systemic toxicity, temporary remission, and radio-resistance in BC. In this study, we have developed CD44 and folate receptor-targeting multi-functional dual drug-loaded nanoparticles. This composed of hyaluronic acid (HA) and folic acid (FA) conjugated to a 2-deoxy glucose (2DG) shell linked to a layer of dichloroacetate (DCA) and a magnesium oxide (MgO) core (2DG@DCA@MgO; DDM) to enhance the localized chemo-radiotherapy for effective BC treatment. The physicochemical properties of nanoparticles including stability, selectivity, responsive release to pH, cellular uptake, and anticancer efficacy were thoroughly examined. Mechanistically, we identified multiple component signaling pathways as important regulators of BC metabolism and mediators for the inhibitory effects elicited by DDM. Nanoparticles exhibited sustained DDM release properties in a bio-relevant media, which was responsive to the acidic pH enabling eligibility to the control of drug release from nanoparticles. DDM-loaded and HA–FA-functionalized nanoparticles exhibited increased selectivity and uptake by BC cells. Cell-based assays revealed that the functionalized DDM significantly suppressed cancer cell growth and improved radiotherapy (RT) through inducing cell cycle arrest, enhancing apoptosis, and modulating glycolytic and OXPHOS pathways. By highlighting DDM mechanisms as an antitumor and radio-sensitizing reagent, our data suggest that glycolytic and OXPHOS pathway modulation occurs via the PI3K/AKT/mTOR/NF-κB/VEGFlow and P53high signaling pathway. In conclusion, the multi-functionalized DDM opposed tumor-associated metabolic reprogramming via multiple signaling pathways in BC cells as a promising targeted metabolic approach. [ABSTRACT FROM AUTHOR]

Cancers are a major challenge to health worldwide. Spinel ferrites have attracted attention due to their broad theranostic applications. This study aimed at investigating the antimicrobial, antibiofilm, and anticancer activities of ebselen (Eb) and cerium-nanoparticles (Ce-NPs) in the form of ZnCexFe2−XO4 on human breast and colon cancer cell lines. Bioassays of the cytotoxic concentrations of Eb and ZnCexFe2−XO4, oxidative stress and inflammatory milieu, autophagy, apoptosis, related signalling effectors, the distribution of cells through the cell-cycle phases, and the percentage of cells with apoptosis were evaluated in cancer cell lines. Additionally, the antimicrobial and antibiofilm potential have been investigated against different pathogenic microbes. The ZOI, and MIC results indicated that ZnCexFe2−XO4; X = 0.06 specimen reduced the activity of a wide range of bacteria and unicellular fungi at low concentration including P. aeruginosa (9.5 mm; 6.250 µg/mL), S. aureus (13.2 mm; 0.390 µg/mL), and Candida albicans (13.5 mm; 0.195 µg/mL). Reaction mechanism determination indicated that after ZnCexFe2−xO4; X = 0.06 treatment, morphological differences in S.aureus were apparent with complete lysis of bacterial cells, a concomitant decrease in the viable number, and the growth of biofilm was inhibited. The combination of Eb with ZFO or ZnCexFe2−XO4 with γ-radiation exposure showed marked anti-proliferative efficacy in both cell lines, through modulating the oxidant/antioxidant machinery imbalance, restoring the fine-tuning of redox status, and promoting an anti-inflammatory milieu to prevent cancer progression, which may be a valuable therapeutic approach to cancer therapy and as a promising antimicrobial agent to reduce the pathogenic potential of the invading microbes. [ABSTRACT FROM AUTHOR]

Cancers are a major challenge to health worldwide. Spinel ferrites have attracted attention due to their broad theranostic applications. This study aimed at investigating the antimicrobial, antibiofilm, and anticancer activities of ebselen (Eb) and cerium-nanoparticles (Ce-NPs) in the form of ZnCe x Fe 2-X O 4 on human breast and colon cancer cell lines. Bioassays of the cytotoxic concentrations of Eb and ZnCe x Fe 2-X O 4 , oxidative stress and inflammatory milieu, autophagy, apoptosis, related signalling effectors, the distribution of cells through the cell-cycle phases, and the percentage of cells with apoptosis were evaluated in cancer cell lines. Additionally, the antimicrobial and antibiofilm potential have been investigated against different pathogenic microbes. The ZOI, and MIC results indicated that ZnCe x Fe 2-X O 4 ; X = 0.06 specimen reduced the activity of a wide range of bacteria and unicellular fungi at low concentration including P. aeruginosa (9.5 mm; 6.250 µg/mL), S. aureus (13.2 mm; 0.390 µg/mL), and Candida albicans (13.5 mm; 0.195 µg/mL). Reaction mechanism determination indicated that after ZnCe x Fe 2-x O 4 ; X = 0.06 treatment, morphological differences in S. aureus were apparent with complete lysis of bacterial cells, a concomitant decrease in the viable number, and the growth of biofilm was inhibited. The combination of Eb with ZFO or ZnCe x Fe 2-X O 4 with γ-radiation exposure showed marked anti-proliferative efficacy in both cell lines, through modulating the oxidant/antioxidant machinery imbalance, restoring the fine-tuning of redox status, and promoting an anti-inflammatory milieu to prevent cancer progression, which may be a valuable therapeutic approach to cancer therapy and as a promising antimicrobial agent to reduce the pathogenic potential of the invading microbes.