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1.
J Pharm Pharmacol ; 70(9): 1262-1271, 2018 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-29956343

RESUMO

OBJECTIVES: This study sought to investigate the differences in the quality of dried ginger samples obtained from two places in Zambia, Lusaka and Copperbelt in terms of their secondary metabolite differences and heavy metals content. METHODS: Ten and eight batches of dried ginger obtained, respectively, from Lusaka and Copperbelt were analysed using untargeted Q/TOF-MS-based metabolomics and inductively coupled plasma optical emission spectroscopy (ICP-OES). KEY FINDINGS: The metabolomics approach yielded 11 differential metabolites that clearly discriminated between the samples from the two locations. Eight were found to be more abundant in the samples from Lusaka while three were present in greater amounts in the samples from Copperbelt. The results of the heavy metal content analysis for four selected elements, Cd, Pb, As and Cu, showed that the samples from Copperbelt recorded higher levels. However, all samples contained levels of the toxic metals, Cd and Pb above permissible limits, making them unwholesome for human consumption. CONCLUSIONS: The outcome of the heavy metal content analysis led us to speculate that abiotic stress as a result of these metals experienced by the ginger rhizomes during cultivation could have contributed to the metabolites abundance differences. Further studies are, however, recommended to verify this hypothesis.


Assuntos
Gengibre/metabolismo , Metabolômica/métodos , Metais Pesados/análise , Metais Pesados/metabolismo , Espectrometria de Massas em Tandem/métodos , Cromatografia Líquida de Alta Pressão/métodos , Humanos , Zâmbia
2.
Bioorg Med Chem Lett ; 27(4): 867-874, 2017 02 15.
Artigo em Inglês | MEDLINE | ID: mdl-28110871

RESUMO

Various 3-substituted 4-anilino-coumarin derivatives have been designed, synthesized and their anti-proliferative properties have been studied. The in vitro cytotoxicity screening was performed against MCF-7, HepG2, HCT116 and Panc-1 cancer cell lines by MTT assay. Most of the synthesized compounds exhibited comparable anti-proliferative activity to the positive control 5-Fluorouracil against these four tested cancer cell lines. Among the different substituents at C-3 position of coumarin scaffold, 3-trifluoroacetyl group showed the most promising results. Especially, compounds 33d (IC50=16.57, 5.45, 4.42 and 5.16µM) and 33e (IC50=20.14, 6.71, 4.62 and 5.62µM) showed excellent anti-proliferative activities on MCF-7, HepG2, HCT116 and Panc-1 cell lines respectively. In addition, cell cycle analysis and apoptosis activation revealed that 33d induced G2/M phase arrest and apoptosis in MCF-7 cells in a dose-dependent manner. Low toxicity of compounds 33d and 33e was observed against human umbilical vein endothelial cells (HUVECs), suggesting their acceptable safety profiles in normal cells. Furthermore, the results of in silico ADME studies indicated that both 33d and 33e exhibited good pharmacokinetic properties.


Assuntos
Antineoplásicos/síntese química , Cumarínicos/química , Desenho de Fármacos , Antineoplásicos/farmacologia , Apoptose/efeitos dos fármacos , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Cumarínicos/farmacologia , Dano ao DNA/efeitos dos fármacos , Ensaios de Seleção de Medicamentos Antitumorais , Pontos de Checagem da Fase G2 do Ciclo Celular/efeitos dos fármacos , Células HCT116 , Células Hep G2 , Células Endoteliais da Veia Umbilical Humana , Humanos , Pontos de Checagem da Fase M do Ciclo Celular/efeitos dos fármacos , Células MCF-7 , Relação Estrutura-Atividade
3.
Eur J Med Chem ; 118: 328-39, 2016 Aug 08.
Artigo em Inglês | MEDLINE | ID: mdl-27176944

RESUMO

The estrogen receptors have played important roles in breast cancer development and progression. Selective estrogen receptor modulators, such as Tamoxifen, have showed great benefits in the treatment and prevention of breast cancer. But the disadvantages of induction of endometrial cancer and drug resistance have limited their use. Multiple ligand which act at multiple biomolecular targets may exert favorable advantages of improved efficacy with lower incidence of side effects. In this work, we described the synthesis and evaluation of a series of 6-aryl-indenoisoquinolone derivatives as dual ERα and VEGFR-2 inhibitors. These compounds presented good ERα binding affinity and ERα antagonistic activity, as well as potent VEGFR-2 inhibitory potency. They also possessed excellent anti-proliferative activities against MCF-7, MDA-MB-231, Ishikawa and HUVEC cell lines. Further investigation of selective compound 21c showed that it was able to inhibit the activation of VEGFR-2 and the signaling transduction of Raf-1/MAPK/ERK pathway in MCF-7 cells.


Assuntos
Desenho de Fármacos , Receptor alfa de Estrogênio/metabolismo , Terapia de Alvo Molecular , Quinolonas/síntese química , Quinolonas/farmacologia , Receptor 2 de Fatores de Crescimento do Endotélio Vascular/antagonistas & inibidores , Inibidores da Angiogênese/síntese química , Inibidores da Angiogênese/química , Inibidores da Angiogênese/metabolismo , Inibidores da Angiogênese/farmacologia , Antineoplásicos/síntese química , Antineoplásicos/química , Antineoplásicos/metabolismo , Antineoplásicos/farmacologia , Técnicas de Química Sintética , Receptor alfa de Estrogênio/química , Regulação Neoplásica da Expressão Gênica/efeitos dos fármacos , Humanos , Células MCF-7 , Modelos Moleculares , Conformação Proteica , Quinolonas/química , Quinolonas/metabolismo , RNA Mensageiro/genética , RNA Mensageiro/metabolismo , Receptores de Progesterona/genética , Receptor 2 de Fatores de Crescimento do Endotélio Vascular/metabolismo
4.
Asian Pac J Trop Biomed ; 5(11): 921-927, 2015 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-32363148

RESUMO

Objective: To evaluate the scientific basis for the use of Kang 601 heji (K-601) as an anti-inflammatory and antipyretic agent using appropriate animal models. Methods: Carrageenan-induced rat paw and xylene-induced ear oedemas were models used to investigate anti-inflammatory actions of K-601. Lipopolysaccharide-induced pyrexia model was used to evaluate antipyretic activity in Wistar rats. The anti-inflammatory and antipyretic mechanisms were evaluated by detecting prostaglandins E2, nitric oxide, interleukin-1ß and tumour necrosis factor-α levels using appropriate reagents and ELISA kits. Results: The results revealed that K-601 reduced the level of inflammations in both anti-inflammatory models in a dose-dependent manner. The same was true for the antipyretic model. The possible mechanisms of actions were through the inhibition of prostaglandins E2, interleukin-1ß, tumour necrosis factor-α and nitric oxide. Conclusions: K-601 has proven anti-inflammatory and antipyretic actions. The findings provide a scientific basis for the use of K-601 as anti-inflammatory and antipyretic agent in traditional Chinese medicinal practice.

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