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1.
J Educ Health Promot ; 12: 229, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-37727408

RESUMO

BACKGROUND: Higher education institutions are adapting and innovating like never before to provide highly individualized learning environments for both traditional and non-traditional students. This seismic upheaval in the higher education landscape is being observed across the world. The present study aimed to evaluate the effectiveness of a blended learning approach on nursing students' self-directed learning readiness. MATERIALS AND METHODS: This study is a quasi-experimental approach in which a non-equivalent control group was used in a post-test design. A comparison was carried out with two separate semester cohort students representing the control and intervention groups which had 24 and 30 students, respectively. This study included first-year nursing students that enrolled in a course called "Anatomy and Physiology" course of nursing education at a private university. The control group received all their teaching face-to-face, and the intervention group used information technology and prescribed activities in their online e-book. The self-directed learning readiness (SDLR) tool measures the learners' readiness in self-directed learning in both groups. This scale comprises three subscales which are "self-management," "desire for learning," and "self-control." An independent-samples t-test was conducted to compare self-directed learning readiness in the control and intervention groups. Data were analyzed using IBM SPSS Statistics 25 software to measure the independent t-test. RESULTS: The self-directed readiness scores were significantly higher in the intervention group with P = 0.019. The intervention group showed a higher mean value on the subscales of self-management and self-control, which demonstrated a significant difference with P values of 0.018 and 0.028, respectively. The subscale desire for learning was insignificant with a P value of 0.166. CONCLUSION: This study concluded that the overall results demonstrate that incorporating blended learning using e-books for anatomy and physiology courses in nursing education can contribute to students' readiness for self-directed learning. Specifically, the blended learning teaching and learning strategy had a positive impact on nursing students' capacity for self-management and self-control.

2.
Dalton Trans ; 52(9): 2735-2748, 2023 Feb 28.
Artigo em Inglês | MEDLINE | ID: mdl-36749193

RESUMO

We present the combustion-based synthesis of BiFeO3 (BFO) and Gd:BiFeO3 perovskite nanoparticles. XRD analysis demonstrates that the undoped BFO (x = 0) perovskite sample shows a single perovskite phase with a rhombohedral structure. However, increase in the Gd3+ content from x = 0.05 and 0.15 to 0.25 led to the occurrence of a structural phase transformation from rhombohedral (BiFeO3) to orthorhombic (Bi2Fe4O9). With an increase in the Gd-dopant the average crystallite size of rhombohedral structures increased from 16 to 23 nm. The perovskite samples were examined using XPS, which confirmed the presence of Bi3+, Gd3+, Fe2+, and O2+ ions. FT-IR spectroscopy indicated the existence of elemental functional groups in the synthesized perovskite nanoparticles. Furthermore, the direct band gap measured by DRS reduced from 2.16 to 2.0 eV as the Gd concentration increased. The nanoparticles of the BFO perovskite had an uneven shape, a tendency to agglomerate, and fused grains with defined grain boundaries. At ambient temperature, both the undoped and Gd:BFO perovskite nanoparticles exhibit a ferromagnetic characteristic. It was found that the BET surface area of the undoped and Gd-doped BFO perovskite nanoparticles varied progressively from 4.38 to 33.52 m2 g-1. The catalytic oxidation studies conducted in a batch reactor under air conditions revealed that the synthesized catalysts, in particular, Gd:BFO (x = 0.25), exhibited higher conversion and selectivity efficiencies for glycerol (con. 100% and sel. 99.5%, respectively).

3.
Anticancer Agents Med Chem ; 22(5): 933-942, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-34229589

RESUMO

BACKGROUND: Cancer disease is a serious concern globally. Global cancer occurrence is steadily increasing every year. There is always a persistent need to develop new anticancer drugs with reduced side effects or that act synergistically with the existing chemotherapeutics. OBJECTIVE: Benzoxazoles are fused bicyclic nitrogen and oxygen-containing heterocyclic compounds and are considered biologically privileged scaffolds. We designed a synthetic route to link the benzoxazoles with oxadiazole,s resulting in a better pharmacophore for anticancer activity. METHODS: A series of novel amide derivatives of benzoxazole linked 1,3,4-oxadiazoles (10 a-j) were synthesized and characterized by 1H NMR, 13C NMR, and mass spectroscopic techniques. The biological properties of the compounds were screened in vitro against four different tumor cell lines. RESULTS: The results suggest that the compound 10b having 3,4,5-trimethoxy substitution on the phenyl ring exhibited potent anticancer activity in three cell lines (A549 = 0.13 ± 0.014 µM, MCF-7 = 0.10 ± 0.013 µM and HT-29 = 0.22 ± 0.017 µM). Notably, among the synthesized derivatives, compounds 10b, 10c, 10f, 10g, and 10i exhibited potent anticancer activity than the control, with IC50 values in the range from 0.11 ± 0.02 to 0.93 ± 0.034 µM. Molecular docking simulation results showed that compounds were stabilized by hydrogen bond and π-π interactions with the protein. CONCLUSION: The molecules showed comparable binding affinities with standard Combretastatin-A4. The present research work is in a preliminary phase and needs further studies to take the synthesized compounds to the next level in the cancer research field.


Assuntos
Antineoplásicos , Oxidiazóis , Antineoplásicos/química , Benzoxazóis/farmacologia , Proliferação de Células , Desenho de Fármacos , Ensaios de Seleção de Medicamentos Antitumorais , Humanos , Simulação de Acoplamento Molecular , Estrutura Molecular , Oxidiazóis/química , Relação Estrutura-Atividade
4.
Bioorg Chem ; 116: 105377, 2021 11.
Artigo em Inglês | MEDLINE | ID: mdl-34670329

RESUMO

CDK4 & CDK6 are essential regulators of initial cell cycle phases and are always considered an exciting choice for anti-cancer therapy. In the present study, we presented the structure-based rational design & synthesis of a new class of 1,2,3-triazole tethered acridinedione derivatives (6a-l) as selective CDK4/6 inhibitors. Title molecules were prepared as a result of the rate-determining reaction between substituted derivatives of 1-Phenyl-1H-1,2,3-triazole-4-carbaldehydes and substituted dimedones, and the molecules were structurally characterized by IR, 1H,13C NMR, and MS spectral data. All molecules were screened for in-vitro cytotoxic potential against a group of human breast tumor cell lines of distinct origin with differential Rb expression status. Out of entire series of conjugated hexahydro acridinediones, 6g showed potent cytotoxic effect against MCF-7, BT-474, and SK-BR3 cell lines with IC50values 0.173 ±â€¯0.037, 0.117 ±â€¯0.025, and 0.136 ±â€¯0.027 µM, respectively. Further, CDK inhibition assays revealed that the compounds 6g and 6h selectively inhibit CDK4/6 over other CDK-parter complexes of the family against the selected cell line group except for MDA-MB468 cells. Furthermore, apoptotic evaluation and cell cycle analysis determined that compound 6g successfully triggered apoptosis in all examined cell lines except MDA-MB468 through blocking G1/S cell cycle transformation. In addition, compound 6g showed the highest in-vitro selectivity towards CDK4/6 inhibition, even compared with Abemaciclib, and it was also proved for favourable in-vivo pharmacokinetic properties in male albino mice. Furthermore, molecule 6g showed promising tumor growth suppression with lower adverse effects in MCF-7 xenograft mice models, which could competently be considered as a novel chemotherapeutic candidate for a further comprehensive preclinical study involving breast cancer therapy.


Assuntos
Acridinas/farmacologia , Antineoplásicos/farmacologia , Neoplasias da Mama/tratamento farmacológico , Inibidores de Proteínas Quinases/farmacologia , Retinoblastoma/tratamento farmacológico , Triazóis/farmacologia , Acridinas/síntese química , Acridinas/química , Antineoplásicos/síntese química , Antineoplásicos/química , Neoplasias da Mama/metabolismo , Neoplasias da Mama/patologia , Pontos de Checagem do Ciclo Celular/efeitos dos fármacos , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Quinase 4 Dependente de Ciclina/antagonistas & inibidores , Quinase 4 Dependente de Ciclina/metabolismo , Quinase 6 Dependente de Ciclina/antagonistas & inibidores , Quinase 6 Dependente de Ciclina/metabolismo , Relação Dose-Resposta a Droga , Feminino , Humanos , Modelos Moleculares , Estrutura Molecular , Fosforilação/efeitos dos fármacos , Inibidores de Proteínas Quinases/síntese química , Inibidores de Proteínas Quinases/química , Retinoblastoma/metabolismo , Retinoblastoma/patologia , Relação Estrutura-Atividade , Triazóis/química
5.
Mol Divers ; 25(4): 2017-2033, 2021 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-32361888

RESUMO

In an effort to discover potential cytotoxic agents, a series of novel (Z)-5-((1,3-diphenyl-1H-pyrazol-4-yl)methylene)-3-((1-substituted phenyl-1H-1,2,3-triazol-4-yl)methyl)thiazolidine-2,4-dione derivatives (8a-n) were designed and synthesized in various steps with acceptable reaction procedures with quantitative yields and characterized by 1H NMR, 13C NMR, IR, HRMS and ESI-MS spectra. These newly synthesized novel derivatives were screened for their in vitro cell viability/cytotoxic studies against human breast cancer cell line (MCF-7) with various concentrations of 0.625 µM, 1.25 µM, 2.5 µM, 5 µM and 10 µM, respectively. The biological interpretation assay outcome was demonstrated in terms of cell viability percentage reduction and IC50 values against standard reference drug cisplatin. Based on these results, most of the derivatives exhibited promising cytotoxic activity. Among them, particularly compounds 8j (R1 = OMe and R3 = NO2) and 8e (R3 = CF3) demonstrate remarkable cytotoxic activity with IC50 values 0.426 µM ± 0.455 and 0.608 µM ± 0.408, which are even better than the standard drug cisplatin 0.636 µM ± 0.458 and compounds 8m (R2 = OMe and R3 = OMe) and 8c (R3 = OMe) exhibited closely equivalent IC50 values to the standard drug with IC50 values 0.95 µM ± 0.32 and 0.976 µM ± 0.313 and rest of the compounds exhibits moderate cytotoxic activity. Moreover, molecular modeling studies and ADME calculations of the novel synthesized derivatives are in adequate consent with the pharmacological screening results.


Assuntos
Tiazolidinas
6.
Bioorg Chem ; 90: 103056, 2019 09.
Artigo em Inglês | MEDLINE | ID: mdl-31276952

RESUMO

11-Beta-Hydroxysteroid dehydrogenase-1(11ß-HSD1) inhibitors are one of the emerging classes of molecules to fight against diabetic complications. A novel series of 4-(1-substituted-1H-1,2,3-triazol-4-yl)-1,4-dihydropyridine derivatives were synthesized and evaluated for their anti-diabetic activity. Two compounds showed anti-diabetic activity very effectively. To clarify the mechanism of action of these compounds, the most potent compounds (5g and 5h) of the synthesized analogs were further studied by testing its 11-Beta Hydroxysteroid dehydrogenase-1 inhibitory activity through in vitro enzymatic experiments. The results showed that the 11ß-HSD1 inhibitory activity of compounds 5g and 5h was stable and efficient. Molecular docking studies revealed compounds 5g (-9.758) and 5h (-8.495) to have a stable binding patterns to the human 11-Beta-Hydroxysteroid dehydrogenase-1.


Assuntos
11-beta-Hidroxiesteroide Desidrogenase Tipo 1/antagonistas & inibidores , Diabetes Mellitus Experimental/tratamento farmacológico , Inibidores Enzimáticos/síntese química , Inibidores Enzimáticos/farmacologia , 11-beta-Hidroxiesteroide Desidrogenase Tipo 1/metabolismo , Animais , Diabetes Mellitus Experimental/enzimologia , Diabetes Mellitus Experimental/patologia , Camundongos , Modelos Moleculares , Simulação de Acoplamento Molecular , Relação Estrutura-Atividade
7.
Biomed Pharmacother ; 96: 742-749, 2017 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-29049977

RESUMO

Polymorphonuclear neutrophils (PMNn) are the pivotal mediators of phagocytosis. In addition to neutropenia, impaired neutrophilic function is associated with pathological conditions and immuno-deficiencies. Henceforth, Immuno-stimulatory strategies targeting neutrophilic function are indeed powerful tools in combating obstinate infections. In appreciation towards the usefulness of herbal medicines in therapeutic scenario, the present study was carried out to analyse the immuno-stimulatory effect of Cuscuta epithymum, Ipomoea batata and Euphorbia hirta using in-vitro and in-vivo rodent experimental models. Throughout the experimentation, phagocytosis was studied and expressed as phagocytotic index and percentage phagocytosis. Different extracts of these plants were initially screened for their potency to induce phagocytosis in PMNn and the methanolic fractions, which are effective, were considered for further experimentation.The phagocytosis stimulation by the methanolic extracts was compared with the standard Granulocyte Macrophage - Colony Stimulating Factor (GM-CSF) at a dose of 65ng/ml. Immunoblotting analysis shown that the methanolic extracts induce the phosphorylation of Syk which in turn phosphorylates GDP-RAC-1, hinting the possible mechanism of action. Following these in vitro investigations, the potency of methanolic extracts was assessed using rat model by performing carbon clearance assay, Delayed Type Hypersensitivity and antibody titre.The phosphorylation status of Syk and GDP-RAC-1 was also assessed in the edematous fluid collected from the right hind paw. In vivo findings were in agreement with the in vitro findings by presenting an improved immune response and increased phosphorylation of Syk and GDP-RAC-1. Conclusively, this study provides the initial insights into the therapeutic implications of the tropical plants in inducing phagocytosis.


Assuntos
Cuscuta/imunologia , Euphorbia/imunologia , Guanosina Difosfato/metabolismo , Ipomoea batatas/imunologia , Extratos Vegetais/imunologia , Quinase Syk/metabolismo , Proteínas rac1 de Ligação ao GTP/metabolismo , Adolescente , Adulto , Animais , Humanos , Camundongos , Neutrófilos/efeitos dos fármacos , Neutrófilos/imunologia , Fagocitose/efeitos dos fármacos , Fagocitose/imunologia , Fosforilação/efeitos dos fármacos , Fosforilação/imunologia , Plantas Medicinais/imunologia , Ratos , Ratos Wistar , Adulto Jovem
8.
J Fluoresc ; 26(2): 703-7, 2016 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-26753757

RESUMO

A simple method for the synthesis of fluorescent zinc chalcogenide (ZnO, ZnS and ZnSe) nanoparticles directly in the transparent PMMA and PS polymer matrices were reported. Highly dispersed small spherical ZnO nanoparticles (3-5 nm) was obtained by hydrothermal reaction of PMMA/PS-Zn(acac)2H2O in toluene. ZnS and ZnSe nanoparticles were prepared by heterogeneous stirring of PMMA/PS-Zn(acac)2H2O in toluene with aqueous solution of thiourea or NaHSe. Interestingly, ZnO and ZnS-PMMA thin film showed strong fluorescence quenching upon exposure to ammonia.

9.
Neuroscience ; 245: 136-47, 2013 Aug 15.
Artigo em Inglês | MEDLINE | ID: mdl-23618759

RESUMO

Sleep is a universal phenomenon in vertebrates, and its loss affects various behaviors. Independent studies have reported that sleep loss increases anxiety; however, the detailed mechanism is unknown. Because sleep deprivation increases noradrenalin (NA), which modulates many behaviors and induces patho-physiological changes, this study utilized zebrafish as a model to investigate whether sleep loss-induced increased anxiety is modulated by NA. Continuous behavioral quiescence for at least 6s was considered to represent sleep in zebrafish; although some authors termed it as a sleep-like state, in this study we have termed it as sleep. The activity of fish that signified sleep-waking was recorded in light-dark, during continuous dark and light; the latter induced sleep loss in fish. The latency, number of entries, time spent and distance travelled in the light chamber were assessed in a light-dark box test to estimate the anxiety behavior of normal, sleep-deprived and prazosin (PRZ)-treated fish. Zebrafish showed increased waking during light and complete loss of sleep upon continuous exposure to light for 24h. PRZ significantly increased sleep in normal fish. Sleep-deprived fish showed an increased preference for dark (expression of increased anxiety), and this effect was prevented by PRZ, which increased sleep as well. Our findings suggest that sleep loss-induced anxiety-like behavior in zebrafish is likely to be mediated by NA's action on the α1-adrenoceptor.


Assuntos
Ansiedade/fisiopatologia , Atividade Motora/fisiologia , Receptores Adrenérgicos alfa 1/fisiologia , Privação do Sono/fisiopatologia , Sono/fisiologia , Vigília/fisiologia , Animais , Ansiedade/psicologia , Escuridão , Luz , Privação do Sono/psicologia , Peixe-Zebra
10.
Bioorg Med Chem Lett ; 21(14): 4138-40, 2011 Jul 15.
Artigo em Inglês | MEDLINE | ID: mdl-21689936

RESUMO

A new series of 3-phenyl-N-[3-(4-phenylpiperazin-1yl)propyl]-1H-pyrazole-5-carboxamide derivatives were synthesized and investigated their anti-inflammatory activities using carrageenan-induced rat paw edema model in vivo. All the synthesized compounds were found to be potent anti-inflammatory agents.


Assuntos
Amidas/química , Anti-Inflamatórios não Esteroides/síntese química , Pirazóis/química , Amidas/síntese química , Amidas/uso terapêutico , Animais , Anti-Inflamatórios não Esteroides/química , Anti-Inflamatórios não Esteroides/uso terapêutico , Carragenina/toxicidade , Edema/induzido quimicamente , Edema/tratamento farmacológico , Ratos
11.
Artigo em Inglês | MEDLINE | ID: mdl-17913572

RESUMO

The metal complexes of Cu(II), Ni(II) and Co(II) with Schiff bases of 3-(2-hydroxy-3-ethoxybenzylideneamino)-5-methyl isoxazole [HEBMI] and 3-(2-hydroxy-5-nitrobenzylidene amino)-5-methyl isoxazole [HNBMI] which were obtained by the condensation of 3-amino-5-methyl isoxazole with substituted salicylaldehydes have been synthesized. Schiff bases and their complexes have been characterized on the basis of elemental analysis, magnetic moments, molar conductivity, thermal analysis and spectral (IR, UV, NMR and Mass) studies. The spectral data show that these ligands act in a monovalent bidentate fashion, co-ordinating through phenolic oxygen and azomethine nitrogen atoms. Chelates of Co(II), Ni(II) appear to be octahedral and Cu(II) appears to be distorted octahedral. To investigate the relationship between formation constants of binary complexes and antimicrobial activity, the dissociation constants of Schiff bases and stability constants of their binary metal complexes have been determined potentiometrically in aqueous solution at 30+/-1 degrees C and at 0.1 M KNO3 ionic strength and discussed. Antimicrobial activities of the Schiff bases and their complexes were screened. The structure-activity correlation in Schiff bases and their metal(II) complexes are discussed, based on the effect of their stability constants. It is observed that the activity enhances upon complexation and the order of activity is in accordance with stability order of metal ions.


Assuntos
Antibacterianos/química , Antibacterianos/farmacologia , Isoxazóis/química , Metais Pesados/química , Metais Pesados/farmacologia , Antibacterianos/síntese química , Aspergillus niger/efeitos dos fármacos , Escherichia coli/efeitos dos fármacos , Ligantes , Espectroscopia de Ressonância Magnética , Magnetismo , Espectrometria de Massas , Metais Pesados/síntese química , Testes de Sensibilidade Microbiana , Microquímica/métodos , Nitratos/química , Concentração Osmolar , Compostos de Potássio/química , Potenciometria/métodos , Pseudomonas aeruginosa/efeitos dos fármacos , Rhizoctonia/efeitos dos fármacos , Bases de Schiff/química , Espectrofotometria Infravermelho , Espectrofotometria Ultravioleta , Relação Estrutura-Atividade , Temperatura , Termogravimetria , Água/química
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