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1.
ACS Omega ; 9(16): 18566-18575, 2024 Apr 23.
Artigo em Inglês | MEDLINE | ID: mdl-38680340

RESUMO

We generated novel elven 1,2,3,6-tetrahydrophthalimides and tetrahydroquinazoline derivatives from 1,2,3,6-tetrahydrophthalic anhydride (1) in response to our interest in using the anhydrides to produce heterocyclic nitrogen compounds. The elemental and spectral analyses of the produced compounds validated the recommended configurations and MOE 2014.09 (Molecular Operating Environment) computations were used to perform their in silico analysis. The synthesized compounds have been analyzed and put through various experiments, including in vitro and in silico methods to assess their biological activity against Escherichia coli Penicillin-Binding Protein 3 (PBP3) and Staphylococcus aureus Penicillin-Binding Protein 2 (PBP2), among these compounds showing promising data as antibacterial drugs.

2.
RSC Adv ; 14(16): 11443-11451, 2024 Apr 03.
Artigo em Inglês | MEDLINE | ID: mdl-38595714

RESUMO

The present work aims at design and synthesis of a congeneric series of small hybrids 5 and 6a-i featuring the privileged quinoline scaffold tethered with 2-(arylamido)cinnamide moiety as potential anticancer tubulin polymerization inhibitors. Most of the synthesized hybrids 5 and 6a-i significantly inhibited the growth of the HepG2 cell line, with IC50 ranged from 2.46 to 41.31 µM. In particular, 2-(3,4,5-trimethoxybenzamido)-4-methoxycinnamide-quinoline hybrid 6e displayed potent IC50 value toward the examined cell line, and hence chosen for further mechanistic investigations. It is noteworthy that the antiproliferative action of compound 6e highly correlated well with its ability to inhibit tubulin polymerization. In addition, the most potent hybrid 6e demonstrated a significant modification in the cellular cycle distribution, in addition to provoke of apoptotic death within the tested HepG2 cell line. Furthermore, the mechanistic approach was confirmed by a substantial upregulation in the quantity of active caspase 9 by 5.81-fold relative to untreated control cells.

3.
J Clin Exp Hepatol ; 13(6): 1008-1016, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-37975051

RESUMO

Background: Hepatocellular carcinoma (HCC) is the most common primary malignant tumor of the liver. Aim: This study aimed to assess serum human telomerase enzyme (hTERT) levels and their relation to the progression of liver disease. Also, it aimed to assess the effect of hepatitis C virus (HCV) core protein on memory T-cells in HCV patients with or without HCC and the correlation between memory cell phenotype and the progression of the disease in the same patients. Methods: HTERT level in serum was assessed through relative quantitative RT-PCR. Flow cytometric analysis was used to assess T-cell responsiveness (as IFN- γ secretion) before and after stimulation with HCV core protein and the memory CD8+ cell phenotype using several differentiation markers. Results: HTERT was found to be increased in a stepwise manner upon comparing its level in controls, chronic hepatitis patients, cirrhotic patients, and HCC patients. T-cells showed a similar manner of stepwise decrease in response (decreased IFN- γ secretion) in HCC patients compared to HCV patients without HCC and controls. Also, late differentiated memory cells (CD8+, CD27-, CD28-, CD45RA+, and CCR7-) were depleted in HCC patients compared to HCV patients without HCC. Conclusion: These results suggest a negative correlation between hTERT and IFN- γ secretion by T-cells in HCV patients and that this relationship, along with the depletion of late differentiated memory cells, could help the progression of liver disease to HCC.

4.
Biol Psychol ; 182: 108645, 2023 09.
Artigo em Inglês | MEDLINE | ID: mdl-37596151

RESUMO

Early irritability, a transdiagnostic vulnerability for psychopathology, is associated with alterations in neural reactivity to emotional stimuli and reward; however, associations between childhood irritability and neural markers of risk may be mitigated by the quality of caregiving youth receive. We examined longitudinal relationships between irritability in childhood and young adolescents' neural activity of regions typically associated with emotion regulation and reward processing during processing of maternal feedback and tested whether these associations were moderated by youth's perceptions of the parent-child relationship quality. Eighty-one adolescents (Mage = 11.1 years) listened to maternal critical and praising feedback while undergoing functional magnetic resonance imaging. Age 3 irritability, assessed observationally, was negatively associated with age 11 neural reactivity to maternal criticism in a cluster in the right dorsolateral prefrontal cortex (dlPFC), particularly for youths who reported more positive maternal parenting. Given the role of the dlPFC activation in the effortful processing of emotional stimuli, decreased activation may reflect disengagement from negatively valenced interpersonal feedback in the context of a positive caregiving environment, thereby mitigating psychopathology risk associated with irritability.


Assuntos
Regulação Emocional , Humor Irritável , Adolescente , Humanos , Criança , Pré-Escolar , Retroalimentação , Relações Pais-Filho , Poder Familiar
5.
Sci Rep ; 13(1): 12176, 2023 07 27.
Artigo em Inglês | MEDLINE | ID: mdl-37500657

RESUMO

Dyslipidemia, steatohepatitis and insulin resistance are among the components of metabolic syndrome (MS). Nutraceuticals containing chitosan, beta-sitosterol and/or ferulic acid and their nanostructures could have a potential role for management of MS. The aim of the present study was to assess the efficacy of the aforementioned nutraceuticals in treatment of MS in rat and their interaction with atorvastatin, a hypolipidemic drug. The two nutraceuticals and their nanostructures were prepared and the nanostructures were assessed by transmission electron microscope and Fourier-Transform Infra-red Spectrometry. MS was induced in rats by feeding high fructose-high fat diet (HFFD). Different groups of rats fed HFFD and treated with the different nutraceuticals, atorvastatin and atorvastatin in combination with different nutraceuticals, control fed on balanced diet and control consumed HFFD without treatments were run. Plasma glucose, lipid profile, aminotransferases activity, total antioxidant capacity, malondialdehyde, urea, creatinine, insulin, high sensitivity C-reactive protein, and adiponectin were assessed along with calculation of insulin resistance. Liver fat and histopathology were investigated. All nutraceuticals in original and nanostructures showed beneficial effects in the treatment of MS, superiority was ascribed to nutraceuticals composed of chitosan and ferulic acid in both forms. A more promising treatment of MS belonged to atorvastatin administered with the different nutraceuticals.


Assuntos
Quitosana , Resistência à Insulina , Síndrome Metabólica , Ratos , Animais , Quitosana/farmacologia , Quitosana/uso terapêutico , Atorvastatina/uso terapêutico , Suplementos Nutricionais , Dieta Hiperlipídica/efeitos adversos , Frutose
6.
Orphanet J Rare Dis ; 18(1): 52, 2023 03 13.
Artigo em Inglês | MEDLINE | ID: mdl-36907859

RESUMO

BACKGROUND: Tay-Sachs disease (TSD), an autosomal recessively inherited neurodegenerative lysosomal storage disease, reported worldwide with a high incidence among population of Eastern European and Ashkenazi Jewish descent. Mutations in the alpha subunit of HEXA that encodes for the ß-hexosaminidase-A lead to deficient enzyme activity and TSD phenotype. This study is the first to highlight the HEXA sequence variations spectrum in a cohort of Egyptian patients with infantile TSD. RESULTS: This study involved 13 Egyptian infant/children patients presented with the infantile form of TSD, ten of the 13 patients were born to consanguineous marriages. ß-hexosaminidase-A enzyme activity was markedly reduced in the 13 patients with a mean activity of 3 µmol/L/h ± 1.56. Sanger sequencing of the HEXA' coding regions and splicing junctions enabled a detection rate of ~ 62% (8/13) in our patients revealing the molecular defects in eight patients; six homozygous-mutant children (five of them were the product of consanguineous marriages) and two patients showed their mutant alleles in heterozygous genotypes, while no disease-causing mutation was identified in the remaining patients. Regulatory intragenic mutations or del/dup may underlie the molecular defect in those patients showing no relevant pathogenic sequencing variants or in the two patients with a heterozygous genotype of the mutant allele. This research identified three novel, likely pathogenic variants in association with the TSD phenotype; two missense, c.920A > C (E307A) and c.952C > G (H318D) in exon 8, and a single base deletion c.484delG causing a frameshift E162Rfs*37 (p.Glu162ArgfsTer37) in exon 5. Three recurrent disease-causing missense mutations; c.1495C > T (R499C), c.1511G > A(R504H), and c.1510C > T(R504C) in exon 13 were identified in five of the eight patients. None of the variants was detected in 50 healthy Egyptians' DNA. Five variants, likely benign or of uncertain significance, S3T, I436V, E506E, and T2T, in exons 1, 11,13, & 1 were detected in our study. CONCLUSIONS: For the proper diagnostics, genetic counseling, and primary prevention, our study stresses the important role of Next Generation Sequencing approaches in delineating the molecular defect in TSD-candidate patients that showed negative Sanger sequencing or a heterozygous mutant allele in their genetic testing results. Interestingly, the three recurrent TSD associated mutations were clustered on chromosome 13 and accounted for 38% of the HEXA mutations detected in this study. This suggested exon 13 as the first candidate for sequencing screening in Egyptian patients with infantile TSD. Larger studies involving our regional population are recommended, hence unique disease associated pathogenic variations could be identified.


Assuntos
Doença de Tay-Sachs , Cadeia alfa da beta-Hexosaminidase , Humanos , Cadeia alfa da beta-Hexosaminidase/química , Cadeia alfa da beta-Hexosaminidase/genética , beta-N-Acetil-Hexosaminidases/genética , Egito , Hexosaminidase A/genética , Mutação , Doença de Tay-Sachs/genética , Lactente
7.
Antibiotics (Basel) ; 12(2)2023 Jan 25.
Artigo em Inglês | MEDLINE | ID: mdl-36830157

RESUMO

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.

8.
Int J Gen Med ; 16: 141-150, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-36659914

RESUMO

Background: Proton pump inhibitors (PPIs) are the most effective agents for managing acid-related disorders. However, inappropriate prescribing of PPIs is becoming an issue of concern. Objective: This study aimed to assess the appropriate utilization of PPIs in terms of indication, dose, frequency, and route of administration during admission and discharge. Furthermore, direct costs associated with inappropriate PPI use were calculated. Methods: A descriptive cross-sectional study was conducted at the internal medicine department of a tertiary hospital in Palestine from January 1, 2021, to June 30, 2021. The medical records of patients aged 18 years or older, hospitalized for 48 hours or more, and receiving oral or intravenous (IV) PPIs during their stay were collected and evaluated for the appropriateness of PPIs prescribed according to clinical guidelines. Results: Of 262 patients, 80.2% had an appropriate indication for prophylaxis (67.6%) or treatment (12.6%). A total of 230 patients were prescribed IV pantoprazole.182 (79.1%) had an appropriate indication, whereas 122/182 (67%) received IV PPI instead of oral without an appropriate indication. Of the 32 patients who received 20 mg of oral omeprazole, 28 (87.5%) had an appropriate indication, dose, and route of administration, whereas 16/28 (57.1%) had an inappropriate frequency. At discharge, 32.5% of patients were discharged with unnecessary PPI prescriptions. The total direct cost of inappropriate PPI Indications and route of administration in 188 patients over six months was $1518. Conclusion: This study showed that most patients received a PPI for an appropriate indication with the correct dose. However, a high prevalence of inappropriate IV pantoprazole administration was observed, resulting in the highest costs, demonstrating the importance of correctly ordering IV medications. Adherence to clinical guidelines, such as those of the American College of Gastroenterology (ACG), will improve the appropriateness of PPI prescribing, prevent complications, and reduce healthcare costs.

9.
Polymers (Basel) ; 14(19)2022 Sep 27.
Artigo em Inglês | MEDLINE | ID: mdl-36235997

RESUMO

The performance of photovoltaics with superstrate configuration is limited by the rigidity and low refractivity of a classical glass cover. In this work, two polyimides (PIs) and two copolyimides combined in the main chain cycloaliphatic moieties, aromatic sequences, chalcogen atoms, and having/lacking fluorine atoms, are proposed as shielding covers for solar cells. The samples containing small cycloaliphatic moieties displayed high transmittance above 80% at 550 nm. The refractive index values under changeable wavelengths and temperatures were shown to influence the magnitude of the reflection losses. At the sample interface with the transparent electrode, optical losses were reduced (~0.26%) in comparison to the classical glass (~0.97%). The samples with the best optical features were further subjected to a surface treatment to render the self-cleaning ability. For this, a new approach was used residing in irradiation with the diffuse coplanar surface barrier discharge (DCSBD), followed by spraying with a commercial substance. Scanning electron microscopy and atomic force microscopy scans show that the surface characteristics were changed after surface treatment, as indicated by the variations in root mean square roughness, surface area ratio, and surface bearing index values. The proposed PI covers diminish the optical losses caused by total internal reflection and soiling, owing to their adapted refractivity and superhydrophobic surfaces (contact angles > 150°), and open up new perspectives for modern photovoltaic technologies.

10.
Nat Commun ; 13(1): 6006, 2022 Oct 12.
Artigo em Inglês | MEDLINE | ID: mdl-36224249

RESUMO

Architected materials that actively respond to external stimuli hold tantalizing prospects for applications in energy storage, wearable electronics, and bioengineering. Molybdenum disulfide, an excellent two-dimensional building block, is a promising candidate for lithium-ion battery anode. However, the stacked and brittle two-dimensional layered structure limits its rate capability and electrochemical stability. Here we report the dewetting-induced manufacturing of two-dimensional molybdenum disulfide nanosheets into a three-dimensional foam with a structural hierarchy across seven orders of magnitude. Our molybdenum disulfide foam provides an interpenetrating network for efficient charge transport, rapid ion diffusion, and mechanically resilient and chemically stable support for electrochemical reactions. These features induce a pseudocapacitive energy storage mechanism involving molybdenum redox reactions, confirmed by in-situ X-ray absorption near edge structure. The extraordinary electrochemical performance of molybdenum disulfide foam outperforms most reported molybdenum disulfide-based Lithium-ion battery anodes and state-of-the-art materials. This work opens promising inroads for various applications where special properties arise from hierarchical architecture.

11.
Environ Res ; 215(Pt 2): 114303, 2022 12.
Artigo em Inglês | MEDLINE | ID: mdl-36116500

RESUMO

Steroid hormones as a class of emerging organic pollutant and high concern, due to their potential risks for human and environmental. Accurate analytical methods of steroid hormones are necessary in quantifying and monitoring. Biosensor is a promising technique. In this study, though part of 3α-HSD DNA to construct a regulatory plasmid and with the EGFP reporter gene to generate a reporter plasmid. Separately transformed into Escherichia coli strain BL21 and extracted the cell lysates as novel biosensor reagents. Analyzed the total amounts of steroid hormones in water, sediment, and soil samples using biosensor reagents, and compared these results with those obtained by HPLC. In summary, detection method using an EGFP reporter that can detect trace amounts of steroid hormones to reached fg/L. The optimal reaction time range and temperature were 30 min and 30 °C, respectively, while the most suitable organic solvent for the steroid hormone was 100% ethanol, up to 96-well plate format. This method is very suitable for high-throughput detection of environmental steroid hormone pollutants.


Assuntos
Técnicas Biossensoriais , Poluentes Ambientais , Técnicas Biossensoriais/métodos , DNA , Escherichia coli/genética , Etanol , Hormônios , Humanos , Indicadores e Reagentes , Solo , Solventes , Esteroides , Água
12.
Dev Psychopathol ; : 1-16, 2022 Aug 30.
Artigo em Inglês | MEDLINE | ID: mdl-36039979

RESUMO

Caregiving experiences are implicated in children's depression risk; however, children's neural reactivity to positive and negative feedback from mothers, a potential mediator of depression risk, is poorly understood. In a sample of 81 children (Mage = 11.12 years, SDage = 0.63), some of whom were recruited based on a maternal history of depression (n = 29), we used fMRI to characterize children's neural responses to maternal praise and criticism. Maternal history of depression was unrelated to children's brain activity during both the praise and criticism conditions; however, ROI analyses showed that children's self-reported depressive symptoms were negatively associated with functional activity in the left anterior insula and right putamen while hearing maternal criticism. Whole-brain analyses showed that children's depressive symptoms were positively associated with left inferior frontal gyrus activity while listening to maternal praise. These findings complement past work implicating these brain regions in the processing of emotionally salient stimuli, reward processing, and internal speech. Given associations between early depressive symptoms and later disorder, findings suggest that maladaptive neural processing of maternal feedback may contribute to children's early emerging risk for depression.

13.
Molecules ; 27(14)2022 Jul 20.
Artigo em Inglês | MEDLINE | ID: mdl-35889493

RESUMO

A group of novel trimethoxyphenyl (TMP)-based analogues were synthesized by varying the azalactone ring of 2-(3,4-dimethoxyphenyl)-4-(3,4,5-trimethoxybenzylidene)oxazolone 1 and characterized using NMR spectral data as well as elemental microanalyses. All synthesized compounds were screened for their cytotoxic activity utilizing the hepatocellular carcinoma (HepG2) cell line. Compounds 9, 10 and 11 exhibited good cytotoxic potency with IC50 values ranging from 1.38 to 3.21 µM compared to podophyllotoxin (podo) as a reference compound. In addition, compounds 9, 10 and 11 exhibited potent inhibition of ß-tubulin polymerization. DNA flow cytometry analysis of compound 9 shows cell cycle disturbance at the G2/M phase and a significant increase in Annexin-V-positive cells compared with the untreated control. Compound 9 was further studied regarding its apoptotic potential in HepG2 cells; it decreased the level of MMP and Bcl-2 as well as boosted the level of p53 and Bax compared with the control HepG2 cells.


Assuntos
Antineoplásicos , Apoptose , Antineoplásicos/química , Linhagem Celular Tumoral , Proliferação de Células , Ensaios de Seleção de Medicamentos Antitumorais , Estrutura Molecular , Relação Estrutura-Atividade , Tubulina (Proteína)/metabolismo , Moduladores de Tubulina/farmacologia
14.
Sci Rep ; 12(1): 11839, 2022 07 12.
Artigo em Inglês | MEDLINE | ID: mdl-35821255

RESUMO

Cinnamon is a well-known natural spice and flavoring substance used worldwide. The objective of the present work is to explore the possible antitumor and immunomodulatory potencies of cinnamon essential oil (Cinn) on Ehrlich ascites carcinoma (EAC). A total of fifty female Swiss albino mice were sub-grouped into five groups (n = 10), namely, normal (a non-tumorized and non-treated) group; EAC-tumorized and non-treated group; Cinn (non-tumorized mice received Cinn, 50 mg/kg per body weight daily) group; a group of EAC-tumorized mice treated with Cinn and the final positive control group of EAC-tumorized mice received cisplatin. Eight compounds were identified from Cinn using UPLC-MS-Qtof and NMR analysis. Compared to EAC untreated group, Cinn successfully (P < 0.05) inhibited tumor growth by reducing tumor cell count (45%), viability (53%) and, proliferation accompanied by the inhibition of tumor growth rate. Moreover, a significant (P < 0.05) arrest in the cell cycle at G0/G1 phase was noticed following Cinn treatments (~ 24.5%) compared to EAC group. Moreover, Cinn markedly evoked an antitumor immune response by elevating the percentage of splenic T helper (CD3+CD4+) and T cytotoxic (CD3+CD8+) cells. It is noteworthy that Cinn treatments significantly restored different hematological alterations as well as liver and kidney functions in EAC-tumorized mice. In conclusion, results suggest that Cinn has a good antitumor and immunostimulatory potencies against Ehrlich ascites carcinoma in vivo. The mechanism underlying its antitumor activity may be attributed to its immunostimulatory effects which increase its potential as a promising anticancer candidate.


Assuntos
Antineoplásicos Fitogênicos , Carcinoma de Ehrlich , Óleos Voláteis , Animais , Antineoplásicos Fitogênicos/farmacologia , Ascite , Carcinoma de Ehrlich/patologia , Cromatografia Líquida , Cinnamomum zeylanicum , Feminino , Imunidade , Camundongos , Camundongos Endogâmicos , Óleos Voláteis/farmacologia , Óleos Voláteis/uso terapêutico , Espectrometria de Massas em Tandem
15.
Molecules ; 27(12)2022 Jun 20.
Artigo em Inglês | MEDLINE | ID: mdl-35745081

RESUMO

A novel series of amides based TMP moiety was designed, synthesized and evaluated for their antiproliferative as well as enzyme inhibition activity. Compounds 6a and 6b showed remarkable cytotoxic activity against HepG2 cells with IC50 values 0.65 and 0.92 µM, respectively compared with SAHA and CA-4 as reference compounds. In addition, compound 6a demonstrated good HDAC-tubulin dual inhibition activity as it showed better HDAC activity as well as anti-tubulin activity. Moreover, compound 6a exhibited G2/M phase arrest and pre-G1 apoptosis as demonstrated by cell cycle analysis and Annexin V assays. Further apoptosis studies demonstrated that compound 6a boosted the level of caspase 3/7. Caspase 3/7 activation and apoptosis induction were evidenced by decrease in mitochondrial permeability suggesting that activation of caspase 3/7 may occur via mitochondrial apoptotic pathway.


Assuntos
Amidas , Antineoplásicos , Amidas/farmacologia , Antineoplásicos/farmacologia , Apoptose , Caspase 3/metabolismo , Linhagem Celular Tumoral , Proliferação de Células , Desenho de Fármacos , Ensaios de Seleção de Medicamentos Antitumorais , Células Hep G2 , Humanos , Relação Estrutura-Atividade
16.
J Patient Exp ; 9: 23743735221089698, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-35434298

RESUMO

This qualitative phenomenological study examined the impact of the COVID-19 pandemic on the lives of patients living with chronic pain. Patients referred to an intensive interdisciplinary pain management program between June 2020 to June 2021 were asked, "How did the COVID-19 pandemic affect your life?" as part of their interdisciplinary assessment. Ninety patients (50 Veterans, 40 civilians) provided comments to this question, which were independently organized into themes using an inductive approach by 4 researchers. Nine main themes emerged: (1) changed psychological state, (2) minimal to no effect, (3) affected personal life activities, (4) changes in accessing care, (5) changes in work/education situation, (6) changes in family dynamics, (7) experiencing more annoyances, (8) COVID-19 pandemic is a barrier to making positive changes, and (9) got COVID-19. Themes are consistent with topics of interest in light of this ongoing, global stressor. Most commonly reported themes reflected changes in psychological well-being and changes in access to care, highlighting similarities between life with chronic pain and life under the pandemic for this group.

17.
Molecules ; 27(5)2022 Mar 02.
Artigo em Inglês | MEDLINE | ID: mdl-35268750

RESUMO

1,4-Bis(p-tolylamino)-6,7-dichloroanthraquinone 1 when reacted with di(sodiothio)-maleonitrile 2 afforded heterocyclic thianone compound, 5,12-dioxo-5,12-dihydroanthro[2,3-b][1,4]dithiine-2,3-dicarbonitrile 3. Using lithium/pentanol and acetic acid, the dicarbonitrile product 3 was cyclotetramerized, yielding the matching tetra 5,12-dioxo-5,12-dihydroanthro[2,3-b][1,4]dithiine-porphyrazine dye compound (2H-Pz) 4a. The dicarbonitrile molecule was a ring-shaped metallic product utilizing metallic salt and quinoline, yielding the corresponding tetra 5,12-dioxo-5,12-dihydroanthro[2,3-b][1,4]dithiine-porphyrazinato-metal II dyes (M-Pz), M = Zn, Co, or Ni 4b-d. The produced compounds' elemental analysis investigation, Infrared, and nuclear magnetic resonance spectrum information accord with the structures attributed to them. The cyclotetramerization and complexation reactions are ensured by the molecular weight and metal load of the produced products. The inclusion of electron-donating groups resulted in a lower optical band gap of the produced dye sensitizers, with "push-pull" promotion of about 1.55 eV. The prepared substituted porphyrazines reveal high absorption in the UV-VIS region, which could be of potential value as a building block for novel electronic and optical materials as well as a sensor for technology. This is considered for improving solar cell absorption. The absorption bands of the synthesized porphyrazine dyes extend beyond 800 nm, so these dyes could be useful in various optoelectronic applications.

18.
Pharmaceuticals (Basel) ; 15(3)2022 Mar 20.
Artigo em Inglês | MEDLINE | ID: mdl-35337173

RESUMO

The first outbreak in Wuhan, China, in December 2019 was reported about severe acute coronaviral syndrome 2 (SARS-CoV-2). The global coronavirus disease 2019 (COVID-19) pandemic in 2020 resulted in an extremely high potential for dissemination. No drugs are validated in large-scale studies for significant effectiveness in the clinical treatment of COVID-19 patients, despite the worsening trends of COVID-19. This study aims to design a simple and efficient cyclo-condensation reaction of 6-aminouracil derivatives 2a-e and isatin derivatives 1a-c to synthesize spiro-oxindoles 3a-d, 4a-e, and 5a-e. All compounds were tested in vitro against the SARS-CoV-2. Four spiro[indoline-3,5'-pyrido[2,3-d:6,5-d']dipyrimidine derivatives 3a, 4b, 4d, and 4e showed high activities against the SARS-CoV-2 in plaque reduction assay and were subjected to further RNA-dependent-RNA-polymerase (RdRp) and spike glycoprotein inhibition assay investigations. The four compounds exhibited potent inhibitory activity ranging from 40.23 ± 0.09 to 44.90 ± 0.08 nM and 40.27 ± 0.17 to 44.83 ± 0.16 nM, respectively, when compared with chloroquine as a reference standard, which showed 45 ± 0.02 and 45 ± 0.06 nM against RdRp and spike glycoprotein, respectively. The computational study involving the docking studies of the binding mode inside two proteins ((RdRp) (PDB: 6m71), and (SGp) (PDB: 6VXX)) and geometrical optimization used to generate some molecular parameters were performed for the most active hybrids.

19.
Infect Drug Resist ; 15: 545-554, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-35221699

RESUMO

PURPOSE: The developed resistance of pathogenic microorganisms towards the currently used antimicrobial agents requires the fast search for newer potent antimicrobials. One of the most important ways to combat the previously mentioned disaster is the use of natural alternatives like medicinal plants. Our study aimed to estimate the anti-inflammatory property, and antibacterial effects of probiotics Lactiplantibacillus plantarum and ethanol extracts of Lawsonia inermis leaves against Staphylococcus aureus when they were used separately or collectively as synergism. MATERIAL AND METHODS: Experimentally induced infected wound model in mice was created and divided into 10 groups then treated for two days by L. plantarum and L. inermis individually or in combination, followed by biochemical assays. The antibacterial, anti-inflammatory, and wound healing activity were evaluated through histopathological sections taken before and after treatment. RESULTS: Our results revealed that L. plantarum and L. inermis mixture could inhibit growth of S. aureus and decrease the minimal inhibitory concentration (MIC) of L. plantarum to 2 mg/mL. The mixture decreased level of both interleukin 6 (IL-6) and interferon-alpha (TNF-α) to a level near the normal uninfected group. Histopathological study showed that animals treated with both L. plantarum and L. inermis had achieved almost 90% healing. CONCLUSION: These results suggest that L. plantarum and L. inermis mixture has synergistic effect on healing of infected wound.

20.
Luminescence ; 37(3): 399-407, 2022 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-34984799

RESUMO

In this work, a comparative study was made of different magnesium ion content incorporated into hydroxyapatite (HAP) and modified with selenite ions, with the aim to develop the degradation performance of methylene blue. Although the dopant metal (Mg2+ ) was present at a relatively low ratio, it induced a change in the microstructure, morphology, surface area, external surface charge, particle size, and degradation performance. The effect of magnesium and selenium binary doping on microstructure and degradation of methylene blue was evaluated. The external surface charge measured by zeta potential clarified that the highest negativity was -11.8 mV and this was accomplished in 1.0 Mg/Se-HAP. Furthermore, the roughness average increased from 36.8 nm, reaching 59.2 nm upon the addition of Mg(II). Moreover, transmission electron microscope micrographs showed that compositions were formed as rod shapes. The process of degradation was optimized, showing effectiveness in methylene blue degradation of 62.4% after 150 min of exposure to visible light. Electrostatic attraction and H-bonding, and coordination played vital roles in the adsorption process. The recyclability of the as-prepared compositions demonstrated that the effectiveness had been reduced to ~54.2% after five times of re-use.


Assuntos
Azul de Metileno , Poluentes Químicos da Água , Adsorção , Durapatita , Íons , Magnésio , Azul de Metileno/química , Poluentes Químicos da Água/análise
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