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Bioorg Chem ; 87: 876-887, 2019 06.
Artigo em Inglês | MEDLINE | ID: mdl-30538052

RESUMO

Fluorescent labeling is a widely-used approach in the study of intracellular processes. This method is becoming increasingly popular for studying small bioactive molecules of natural origin; it allows us to estimate the vital intracellular changes which occur under their influence. We propose a new approach for visualization of the intracellular distribution of triterpene acids, based on fluorescent labeling by fluoresceine isothiocyanate. As a model compound we took the most widely-used and best-studied acid in the ursane series - ursolic acid, as this enabled us to compare the results obtained during our research with the available data, in order to evaluate the validity of the proposed method. Experimental tracing of the dynamics of penetration and distribution of the labeled ursolic acid has shown that when the acid enters the cell, it initially localizes on the inner membranes where the predicted target Akt1/protein kinase B - a protein that inhibits apoptosis - is located.


Assuntos
Antineoplásicos/farmacologia , Corantes Fluorescentes/farmacologia , Isotiocianatos/farmacologia , Triterpenos/farmacologia , Antineoplásicos/síntese química , Antineoplásicos/química , Apoptose/efeitos dos fármacos , Proliferação de Células/efeitos dos fármacos , Relação Dose-Resposta a Droga , Ensaios de Seleção de Medicamentos Antitumorais , Corantes Fluorescentes/síntese química , Corantes Fluorescentes/química , Humanos , Isotiocianatos/química , Células MCF-7 , Microscopia Confocal , Modelos Moleculares , Conformação Molecular , Relação Estrutura-Atividade , Triterpenos/química , Ácido Ursólico
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