RESUMEN
A series of variously functionalized selenium-containing compounds were purposely synthesized and evaluated against a panel of cancer cell lines. Most of the compounds showed an interesting cytotoxicity profile with compound 5 showing a potent activity on MCF7 cells. The ethyl amino derivative 5 acts synergistically with cis-platin and inhibits the GST enzyme with a potency that well correlates with the cytotoxicity observed in MCF7 cells. A computational analysis suggests a possible binding mode on the GST enzyme. As the main outcome of the present study, the ethyl amino derivative 5 emerged as a valid lead compound for further, future developments.
Asunto(s)
Antineoplásicos , Proliferación Celular/efectos de los fármacos , Inhibidores Enzimáticos , Glutatión Transferasa/antagonistas & inhibidores , Proteínas de Neoplasias/antagonistas & inhibidores , Compuestos de Organoselenio , Compuestos de Selenio , Antineoplásicos/síntesis química , Antineoplásicos/química , Antineoplásicos/farmacología , Citotoxinas/síntesis química , Citotoxinas/química , Citotoxinas/farmacología , Inhibidores Enzimáticos/síntesis química , Inhibidores Enzimáticos/química , Inhibidores Enzimáticos/farmacología , Glutatión Transferasa/metabolismo , Células HeLa , Células Endoteliales de la Vena Umbilical Humana , Humanos , Células K562 , Células MCF-7 , Proteínas de Neoplasias/metabolismo , Compuestos de Organoselenio/síntesis química , Compuestos de Organoselenio/química , Compuestos de Organoselenio/farmacología , Compuestos de Selenio/síntesis química , Compuestos de Selenio/química , Compuestos de Selenio/farmacologíaRESUMEN
Newly synthesized carbosilane copper dendrimers (CCD) with chloride and nitrate surface groups seem to be good candidates to be used as gene and drug carriers in anti-cancer therapy, due to their properties such as size and surface charge. Copper attached to the nanoparticles is an important element of many biological processes and recently their anti-cancer properties have been widely examined. Zeta size and potential, transmission electron microscopy (TEM), circular dichroism (CD), analysis of haemolytic activity, and fluorescence anisotropy techniques were used to characterize copper dendrimers. Additionally, their cytotoxic properties toward normal (PBMC) and cancer (1301; HL-60) cells were examined. All tested dendrimers were more cytotoxic against cancer cells in comparison with normal cells.