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1.
Artigo | IMSEAR | ID: sea-203799

RESUMO

According to one pot microwave assisted synthesis, the versatile precursor 2- aminothiazole was prepared and utilized for the construction of new thiazole hybrids targeting MCF7 cell lines. 2‐amino thiazole was condensed with corresponding aldehydes to yield Schiff’sbase (2) intermediates followed by the diazo coupling reaction furnished the designed hybrids(3) contains azo-methine and diazo linkages in its structures. The newly synthesizedcompounds were confirmed on the basis of IR and H1NMR spectral analytical data. All thesynthesized compounds were evaluated for their in-vitro cytotoxicity activity against MCF-7celllines using MTT assay method. The obtained results revealed the more promising compoundsof the synthesised series, 3B and 3H with CTC50 value of 17.77±0.31μg/ml, 17.83±1.14 μg/ml.

2.
Artigo em Inglês | IMSEAR | ID: sea-176851

RESUMO

In recent years azo functionalized polymeric hydrogels are very interesting; it is due to their promising applications in various fields especially in the colon drug delivery. 4-Hydroxyphenylazo-3-N-(4-hydroxyphenyl) maleimide (HPM) was synthesized and used for development of hydrogels by free radical polymerization with acrylamide (Am) and N,N-methylene bis acrylamide. Synthesized poly(Am-co-HPM) (PAH) hydrogels were used for encapsulation of 5-fluorouracil (5-FU) an anticancer drug. Structural, thermal, morphological and drug distribution of PAH hydrogels were characterized by Fourier transform infrared spectroscopy, scanning electron microscopy and X-ray diffraction techniques, respectively. Maximum percentage of encapsulation efficiency i.e. 78.25±1.3 was observed for AZ1 PAH hydrogels. 5-FU release studies were performed by in vitro method in simulated gastro intestinal fluids (pH 1.2 & 7.4). To support the 5-FU release mechanism from PAH hydrogels, swelling and deswelling kinetics were studied in doubly distilled water.

3.
Braz. j. pharm. sci ; 48(4): 659-665, Oct.-Dec. 2012. ilus, tab
Artigo em Inglês | LILACS | ID: lil-665862

RESUMO

Sickle cell disease promotes hemolytic anemia and occlusion of small blood vessels due to the presence of high concentrations of hemoglobin S, resulting in increased production of reactive oxygen species and decreased antioxidant defense capacity. The aim of this study was to evaluate the protective action of a standardized extract of Ginkgo biloba (EGb 761), selected due to its high content of flavonoids and terpenoids, in erythrocytes of patients with sickle cell anemia (HbSS, SS erythrocytes) subjected to oxidative stress using tert-butylhydroperoxide or 2,2-azobis-(amidinepropane)-dihydrochloride, in vitro. Hemolysis indexes, reduced glutathione, methemoglobin concentrations, lipid peroxidation, and intracellular reactive oxygen species were determined. SS erythrocytes displayed increased rates of oxidation of hemoglobin and membrane lipid peroxidation compared to normal erythrocytes (HbAA, AA erythrocytes), and the concentration of EGb 761 necessary to achieve the same antioxidant effect in SS erythrocytes was at least two times higher than in normal ones, inhibiting the formation of intracellular reactive oxygen species (IC50 of 13.6 µg/mL), partially preventing lipid peroxidation (IC50 of 242.5 µg/mL) and preventing hemolysis (IC50 of 10.5 µg/mL). Thus, EGb 761 has a beneficial effect on the oxidative status of SS erythrocytes. Moreover, EGb 761 failed to prevent oxidation of hemoglobin and reduced glutathione at the concentrations examined.


A doença falciforme promove anemia hemolítica e oclusão dos pequenos vasos, causados pela presença de altas concentrações de hemoglobina S, cujas consequências incluem a produção aumentada de espécies reativas de oxigênio e diminuição da capacidade de defesa antioxidante. O objetivo desse estudo foi avaliar a ação protetora de um extrato padronizado de Ginkgo biloba (EGb 761), selecionado devido ao seu alto conteúdo de flavonóides e terpenóides, em eritrócitos de pacientes com anemia falciforme (HbSS, eritrócitos SS) submetidos ao estresse oxidativo usando terc-butil-hidroperóxido e 2,2-azobis-(amidinopropano)-diidrocloreto, in vitro. Índices de hemólise, glutationa reduzida, concentração de metemoglobina, peroxidação lipídica e espécies reativas de oxigênio foram determinados. Eritrócitos de pacientes com anemia falciforme apresentaram taxas aumentadas de oxidação da hemoglobina e peroxidação lipídica e a concentração de EGb 761 necessária para atingir o mesmo efeito antioxidante foi pelo menos duas vezes maior em relação aos eritrócitos normais (HbAA, eritrócitos AA), inibindo a formação de espécies reativas de oxigênio (IC50 de 13.6 µg/mL), prevenindo parcialmente a peroxidação lipídica (IC50 de 242.5 µg/mL) e prevenindo a hemólise (IC50 de 10.5 µg/mL). Portanto, EGb 761 possui um efeito benéfico no estado oxidativo dos eritrócitos SS. Entretanto, o EGb 761 não preveniu a oxidação da hemoglobina e da glutationa reduzida, nas concentrações examinadas.


Assuntos
Humanos , Estresse Oxidativo/imunologia , Ginkgo biloba/classificação , Eritrócitos/classificação , Anemia Falciforme/classificação , Compostos Azo/farmacocinética
4.
Chinese Journal of Laboratory Medicine ; (12)2001.
Artigo em Chinês | WPRIM | ID: wpr-582404

RESUMO

0 05, The reference inteval ( ?2s ) was 0 70~1 15 mmol/L ( n =67) Conclusions This method is simple, sensitive, rapid and accurate,and suitable for the routine manual or automatic analysis of magnesium in serum

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