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1.
Dalton Trans ; 50(30): 10369-10373, 2021 Aug 04.
Artigo em Inglês | MEDLINE | ID: mdl-34308466

RESUMO

To avoid the side effects of the current popular platinum-based anticancer drugs, researchers have made tireless attempts to design appropriate GSH-resistant Ru(ii)-arene complexes. In this regard, luminescent ruthenium(ii)-p-cymene-imidazophenanthroline complexes were developed as promising highly cytoselective cancer theraputic agents for HeLa and Caco-2 cells.


Assuntos
Rutênio , Células CACO-2 , Cimenos , Humanos , Fenol
2.
Int J Mol Sci ; 20(12)2019 Jun 23.
Artigo em Inglês | MEDLINE | ID: mdl-31234585

RESUMO

Hypertension is one of the growing risk factors for the progression of long-term memory loss. Hypertension-mediated memory loss and treatment remain not thoroughly elucidated to date. Plant-based natural compounds are an alternative solution to treating human diseases without side effects associated with commercial drugs. This study reveals that bioactive peptides extracted from soy hydrolysates mimic hypertension-mediated memory loss and neuronal degeneration and alters the memory molecular pathway in spontaneously hypertensive rats (SHR). The SHR animal model was treated with bioactive peptide VHVV (10 mg/kg/oral administration) and angiotensin-converting-enzyme (ACE) inhibitors (5 mg/kg/oral administration) for 24 weeks. We evaluated molecular level expression of brain-derived neurotrophic factor (BDNF), cAMP response element binding protein (CREB), and survival markers phospho-protein kinase B (P-AKT) and phosphoinositide 3-kinase (PI3K) after 24 weeks of treatment for SHR in this study. Western blotting, hematoxylin and eosin (H&E) staining, and immunohistochemistry showed long-term memory loss and neuronal degeneration in SHR animals. Bioactive peptide VHVV-treated animals upregulated the expression of long-term memory-relate proteins and neuronal survival. Spontaneously hypertensive rats treated with oral administration of bioactive peptide VHVV had activated CREB-mediated downstream proteins which may reduce hypertension-mediated long-term memory loss and maintain neuronal survival.


Assuntos
Biomarcadores , Memória de Longo Prazo/efeitos dos fármacos , Peptídeos/farmacologia , Inibidores da Enzima Conversora de Angiotensina/farmacologia , Animais , Barreira Hematoencefálica/metabolismo , Fator Neurotrófico Derivado do Encéfalo/metabolismo , Córtex Cerebral/efeitos dos fármacos , Córtex Cerebral/metabolismo , Proteína de Ligação ao Elemento de Resposta ao AMP Cíclico/metabolismo , Hipertensão/tratamento farmacológico , Hipertensão/etiologia , Hipertensão/metabolismo , Imuno-Histoquímica , Neurônios/efeitos dos fármacos , Neurônios/metabolismo , Peptídeos/química , Ratos , Ratos Endogâmicos SHR , Transdução de Sinais
3.
Drug Dev Ind Pharm ; 45(4): 577-586, 2019 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-30663427

RESUMO

The present study was aimed to develop Annona muricata fruit extract loaded solid lipid nanoparticles (SLNs) and explore its cytotoxic potential in vitro model of breast cancers. Extract loaded SLNs were successfully prepared by high-pressure homogenization followed by ultrasonication method and optimized using 23 full factorial design. The extract loaded SLNs were characterized using different parameters such as particle size (PS), % entrapment efficiency (EE), zeta potential (ZP) and % cumulative drug release (CDR). The SLNs formulation was optimized on the basis of software analysis with an overall desirability factor. The PS and %EE of the optimized formulation were found to be 134.8 nm and 83.26%, respectively. The optimized formulation showed a CDR of 79.83% up to 48 h. In vitro cytotoxicity efficacy of extract loaded SLNs was determined using MTT and Apoptosis assay and compared to that of a free extract. The SLNs showed a notable apoptotic effect and better efficacy to kill MCF7 cancer cells as compared to free extract. Thus, extract loaded SLNs could be an alternative dosage form which possibly controls therapeutic action with reducing side effect.


Assuntos
Annona/química , Antineoplásicos Fitogênicos/administração & dosagem , Portadores de Fármacos/química , Extratos Vegetais/administração & dosagem , Antineoplásicos Fitogênicos/isolamento & purificação , Antineoplásicos Fitogênicos/farmacocinética , Apoptose/efeitos dos fármacos , Neoplasias da Mama/tratamento farmacológico , Neoplasias da Mama/patologia , Sobrevivência Celular/efeitos dos fármacos , Liberação Controlada de Fármacos , Ensaios de Seleção de Medicamentos Antitumorais , Feminino , Frutas/química , Humanos , Lipídeos/química , Células MCF-7 , Nanopartículas/química , Tamanho da Partícula , Extratos Vegetais/isolamento & purificação , Extratos Vegetais/farmacocinética
4.
Nanomaterials (Basel) ; 9(12)2019 Dec 16.
Artigo em Inglês | MEDLINE | ID: mdl-31888164

RESUMO

In this study, we reported the synthesis and characterization of a novel hyperbranched polymer (HBPs) tris[(4-phenyl)amino-alt-4,8-bis(5-(2-ethylhexyl)thiophen-2-yl)benzo[1,2-b;4,5-b']dithiophene] (PTPABDT) composed of benzo[1,2-b:4,5-b']dithiophene (BDT) and triphenyleamine (TPA) constituent subunits by A3 + B2 type Stille's reaction. An estimated optical band gap of 1.69 eV with HOMO and LUMO levels of -5.29 eV and -3.60 eV, respectively, as well as a high thermal stability up to 398 °C were characterized for the synthesized polymer. PTPABDT fabricated as an encapsulated top gate/bottom contact (TGBC), organic field effect transistors (OFET) exhibited a p-type behavior with maximum field-effect mobility (µmax) and an on/off ratio of 1.22 × 10-3 cm2 V-1 s-1 and 7.47 × 102, respectively.

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