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1.
Bioorg Chem ; 128: 106085, 2022 11.
Artigo em Inglês | MEDLINE | ID: mdl-35964502

RESUMO

Since breast cancer is the commonly cause of death among women around the world, diagnosis at the early stages is significantly important to prevent the metastasis of the cancer. Among the various growth factors that are involved in angiogenesis, vascular endothelial growth factor (VEGF) is believed to be the most important factor. Overexpressed VEGF receptor on tumors surface, is particularly interesting for cancer cells targeting purposes. In this study, citric acid dendrimer conjugated with VEGF antagonist peptide was synthesized. The obtained product was confirmed by FT-IR, TEM, DLS, and EDS. In vitro cytotoxicity assay showed no toxicity on normal cells and indicated the notably dose-dependence toxicity on cancer cells. Box-Behnken software as a computational method was used to determine the optimum amount of radiolabeling parameters. Optimized parameters for reducing agent, dendrimer-anti-VEGF, and time were 1.4 mg, 17.5 mg, and about 30 min respectively. Radiochemical purity of radio-labeled conjugated dendrimer was determined about 90 percent. SPECT imaging was done to observe the in vivo accumulation of dendrimer-anti-VEGF in the tumor site. Images showed high accumulation of radio-tracer in the tumor region. All in all, obtained results confirmed our hypothesis that the dendrimer-anti-VEGF can be a good radio-tracer for diagnosis of cancer.


Assuntos
Neoplasias da Mama , Dendrímeros , Neoplasias da Mama/diagnóstico por imagem , Neoplasias da Mama/tratamento farmacológico , Linhagem Celular Tumoral , Feminino , Humanos , Espectroscopia de Infravermelho com Transformada de Fourier , Fator A de Crescimento do Endotélio Vascular , Fatores de Crescimento do Endotélio Vascular
2.
Saudi J Biol Sci ; 29(8): 103353, 2022 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-35800144

RESUMO

Due to the growth of diabetic mellitus (DM) and diabetic nephropathy as a significant complication for diabetic patients, study on effective treatment with fewer side effects has been fascinated. In this study for the first time carvedilol effects on both function and structure of kidney in diabetic nephropathy treatment were evaluated. Diabetes was induced by injection of streptozotocin (STZ) intravenously in rats and three groups including control, diabetic, and treatment with carvedilol were considered. Biochemical parameters such as, blood glucose level, BUN, creatinine, uric acid, Na+, K+ was determined. Results showed that glucose (516 to 291 mg/dl), BUN (42 to 21.67 mg/dl), creatinine (0.75 to 0.6 mg/dl), uric acid (4.45 to 1.36 mg/dl), and K+ (7.433 to 5.433 mEq/l) level reduced. Decrease in glucose, BUN, creatinine, uric acid, and K+ and increase in Na+ level (138 to 146.33 mEq/l) confirmed therapeutic effect of carvedilol. Furthermore, the histopathological study was done for each group. Histopathological results confirmed the data obtained by biochemical parameters. For further investigation, SPECT imaging with 99mTc-DMSA, which is a gold standard in diabetic nephropathy detection, was done. SPECT imaging showed that accumulation of 99mTc-DMSA was increased in treated group (5 to 25 kcpm) which means the improvement in renal structure in the treated group compare to the diabetic group (5 kcpm). Finally, obtained results confirmed our hypothesis that carvedilol had a therapeutic effect on diabetic nephropathy.

3.
Bioorg Chem ; 115: 105204, 2021 10.
Artigo em Inglês | MEDLINE | ID: mdl-34325217

RESUMO

In this study for the first time, high efficient, eco-friendly and novel Dy2O3/ZnO-Au ternary nanocomposites (Dy/ZnO-AuNCs) were prepared in presence of pomegranate fruit (PF) extract as capping and reducing agents (Dy/ZnO-AuNCs@PF). The influence of various parameters such as basic agents, reducing agents, sonication power, and sonication time were performed to reach the optimum condition. The formation of the products was characterized by FT-IR, HRTEM, XRD, FE-SEM, TEM, EDX and DRS techniques. The XRD and TEM analysis showed that the morphology and crystallite size of nanocomposites were spherical morphology and 85-90 nm, respectively. The obtained Dy/ZnO-AuNCs@PF were investigated as a nanocatalyst for degradation of erythrosine (ES) as anionic dye and basic violet 10 (BV10) as cationic dye under UV and visible light irradiations. The Dy/ZnO-AuNCs@PF exhibited higher photodegradation against ES (89.6%) and BV10 (91.3%) than pure Dy2O3 (63.1% for ES, 66.5% for BV10) and Dy2O3/ZnO (64.5% for ES, 70.8% for BV10) under UV irradiation. It was found that gold nanoparticles have significant effect on Dy/ZnO-AuNCs@PF catalytic performance for decomposition of organic pollutants. In addition, Dy/ZnO-AuNCs@PF showed excellent in-vitro antibacterial activity against A. baumannii, S. aureus and P. mirabilis with MIC and MBC values of (5, 80 mg/ml), (5, 40 mg/ml) and (2.5, 20 mg/ml), respectively. Generally, according to its excellent antibacterial and catalytic activity, Dy/ZnO-AuNCs@PF can be used in biomedical and environmental applications.


Assuntos
Antibacterianos/farmacologia , Disprósio/farmacologia , Ouro/farmacologia , Nanocompostos/química , Extratos Vegetais/farmacologia , Óxido de Zinco/farmacologia , Acinetobacter baumannii/efeitos dos fármacos , Antibacterianos/síntese química , Antibacterianos/química , Catálise , Relação Dose-Resposta a Droga , Disprósio/química , Frutas/química , Ouro/química , Química Verde , Testes de Sensibilidade Microbiana , Estrutura Molecular , Processos Fotoquímicos , Extratos Vegetais/síntese química , Extratos Vegetais/química , Punica granatum/química , Proteus mirabilis/efeitos dos fármacos , Staphylococcus aureus/efeitos dos fármacos , Relação Estrutura-Atividade , Óxido de Zinco/química
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