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1.
Chem Biodivers ; 17(2): e1900659, 2020 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-31995280

RESUMO

Breast Cancer (BCa) is the most often diagnosed cancer among women who were in the late 1940's. Breast cancer growth is largely dependent on the expression of estrogen and progesterone receptor. Breast cancer cells may have one, both, or none of these receptors. The treatment for breast cancer may involve surgery, hormonal therapy (Tamoxifen, an aromatase inhibitor, etc.) and oral chemotherapeutic drugs. The molecular docking technique reported the findings on the potential binding modes of the 2-(2-bromo-3-nitrophenyl)-5-phenyl-1,3,4-oxadiazole derivatives with the estrogen receptor (PDB ID: 3ERT). The 1,3,4-oxadiazole derivatives 4a-4j have been synthesized and described by spectroscopic method. 2-(2-Bromo-6-nitrophenyl)-5-(4-bromophenyl)-1,3,4-oxadiazole (4c) was reconfirmed by single-crystal XRD. All the compounds have been tested in combination with generic Imatinib pharmaceutical drug against breast cancer cell lines isolated from Caucasian woman MCF-7, MDA-MB-453 and MCF-10A non-cancer cell lines. The compounds with the methoxy (in 4c) and methyl (in 4j) substitution were shown to have significant cytotoxicity, with 4c showing dose-dependent activation and decreased cell viability. The mechanism of action was reported by induced apoptosis and tested by a DNA enzyme inhibitor experiment (ELISA) for Methyl Transferase. Molecular dynamics simulations were made for hit molecule 4c to study the stability and interaction of the protein-ligand complex. The toxicity properties of ADME were calculated for all the compounds. All these results provide essential information for further clinical trials.


Assuntos
Antineoplásicos/síntese química , Desenho de Fármacos , Oxidiazóis/química , Antineoplásicos/metabolismo , Antineoplásicos/farmacologia , Apoptose/efeitos dos fármacos , Sítios de Ligação , Neoplasias da Mama/metabolismo , Neoplasias da Mama/patologia , Linhagem Celular Tumoral , DNA (Citosina-5-)-Metiltransferase 1/antagonistas & inibidores , DNA (Citosina-5-)-Metiltransferase 1/metabolismo , Ensaios de Seleção de Medicamentos Antitumorais , Inibidores Enzimáticos/química , Inibidores Enzimáticos/metabolismo , Inibidores Enzimáticos/farmacologia , Receptor alfa de Estrogênio/química , Receptor alfa de Estrogênio/metabolismo , Feminino , Humanos , Mesilato de Imatinib/farmacologia , Conformação Molecular , Simulação de Acoplamento Molecular , Oxidiazóis/metabolismo , Oxidiazóis/farmacologia , Relação Estrutura-Atividade
2.
Physiother Res Int ; 25(2): e1827, 2020 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-31880059

RESUMO

OBJECTIVES: To develop an adherence questionnaire specific to stroke and measure the level of adherence to home-based exercises among community-dwelling stroke survivors. METHODS: We developed and validated the "Stroke-Specific Measure of Adherence to Home-based Exercises" (SS-MAHE). We measured the exercise adherence among 92 community-dwelling stroke survivors in a cross-sectional study. RESULTS: The SS-MAHE has two sections covering (a) the dosage of prescribed exercises and (b) dosage of actual exercises done by the participants. It was found to be reliable with ICC score of 0.81 (95% CI, 0.44, 0.94, p = .001.) Adherence was measured by comparing prescribed exercises to the actual exercises performed at home. We rated participants as "adherent" if they were following more than 70% of the prescribed exercise dosage. In our sample of 92 stroke survivors, only 28% of participants were adherent to prescribed home-based exercises. CONCLUSION: SS-MAHE is a practical and reliable tool to measure adherence to home-based exercises after a stroke. Exercise adherence among stroke survivors is less than ideal. There is a need for strategies to specifically target exercise adherence in stroke survivors.


Assuntos
Terapia por Exercício/psicologia , Cooperação do Paciente/psicologia , Autocuidado/psicologia , Reabilitação do Acidente Vascular Cerebral/psicologia , Sobreviventes/psicologia , Idoso , Estudos Transversais , Feminino , Humanos , Vida Independente , Índia , Masculino , Pessoa de Meia-Idade , Acidente Vascular Cerebral/psicologia , Reabilitação do Acidente Vascular Cerebral/métodos , Inquéritos e Questionários
3.
Environ Sci Pollut Res Int ; 26(24): 25154-25166, 2019 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-31256397

RESUMO

This study evaluated an enhancement of simultaneous polycyclic aromatic hydrocarbon (PAH) biodegradation and lipid accumulation by Rhodococcus opacus using biochar derived cheaply from biomass gasification effluent. The chemical, physical, morphological, thermal, and magnetic properties of the cheaply derived biochar were initially characterized employing different techniques, which indicated that the material is easy to separate, recover, and reuse for further application. Batch experiments were carried out to study biochar-aided PAH biodegradation by R. opacus clearly demonstrating its positive effect on PAH biodegradation and lipid accumulation by the bacterium utilizing the synthetic media containing 2-, 3- or 4-ring PAH compounds, at an initial concentration in the range 50-200 mg L-1, along with 10% (w/v) inoculum. An enhancement in PAH biodegradation from 79.6 to 92.3%, 76.1 to 90.5%, 74.1 to 88.2%, and 71.6 to 82.3% for naphthalene, anthracene, phenanthrene, and fluoranthene, respectively, were attained with a corresponding lipid accumulation of 68.1%, 74.2%, 72.4%, and 63% (w/w) of cell dry weight (CDW). From contact angle measurements carried out in the study, enhancement in PAH biodegradation and lipid accumulation due to the biochar was attributed to an improved bioavailability of PAH to the degrading bacterium.


Assuntos
Lipídeos/química , Naftalenos/química , Fenantrenos/química , Hidrocarbonetos Policíclicos Aromáticos/química , Rhodococcus/química , Biodegradação Ambiental , Biomassa , Carvão Vegetal , Hidrocarbonetos Policíclicos Aromáticos/metabolismo , Rhodococcus/metabolismo
4.
J Spinal Cord Med ; 41(4): 397-406, 2018 07.
Artigo em Inglês | MEDLINE | ID: mdl-29067867

RESUMO

OBJECTIVE: Spasticity following spinal cord injury (SCI) can impair function and affect quality of life. This study compared the effects of transcutaneous electrical nerve stimulation (TENS) and functional electrical stimulation (FES) on lower limb spasticity in patients with SCI. DESIGN: Double blind randomized crossover design. SETTING: Neuro-rehabilitation unit, Manipal University, India. PARTICIPANTS: Ten participants (age: 39 ± 13.6 years, C1-T11, 1-26 months post SCI) with lower limb spasticity were enrolled in this study. INTERVENTIONS: Participants were administered electrical stimulation with TENS and FES (duration - 30 minutes) in a cross over manner separated by 24 hours. OUTCOME MEASURES: Spasticity was measured using modified Ashworth scale (MAS) [for hip abductors, knee extensors and ankle plantar flexors] and spinal cord assessment tool for spastic reflexes (SCATS). Assessments were performed at baseline, immediately, 1 hour, 4 hours, and 24 hours post intervention. RESULTS: A between group analysis did not show statistically significant differences between FES and TENS (P > 0.05). In the within group analyses, TENS and FES significantly reduced spasticity up to 4 hours in hip adductors and knee extensors (P < 0.01). SCATS values showed significant reductions at 1 hour (P = 0.01) following TENS and 4 hours following FES (P = 0.01). CONCLUSION: A single session of electrical stimulation with FES and TENS appears to have similar anti-spasticity effects that last for 4 hours. The findings of this preliminary study suggest that both TENS and FES have the potential to be used as therapeutic adjuncts to relieve spasticity in the clinic. In addition, FES may have better effects on patients presenting with spastic reflexes.


Assuntos
Espasticidade Muscular/terapia , Traumatismos da Medula Espinal/terapia , Estimulação Elétrica Nervosa Transcutânea/métodos , Adulto , Feminino , Humanos , Masculino , Pessoa de Meia-Idade , Espasticidade Muscular/etiologia , Traumatismos da Medula Espinal/complicações , Estimulação Elétrica Nervosa Transcutânea/efeitos adversos
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