RESUMO
The selective action of drugs in tumor cells is a major problem in cancer therapy. Most chemotherapy drugs act nonspecifically and damage both cancer and healthy cells causing various side effects. In this study, the preparation of a selective drug delivery system, which is able to act as a carrier for hydrophobic and anticancer drugs is reported. Amino-functionalized silica nanoparticles loaded with curcumin were successfully synthesized via sol-gel approach and duly characterized. Thereafter, the targeting ligand, folate, was covalently attached to amino groups of nanoparticle surface through amide bond formation. The cytotoxic effect of nanoparticles on prostate cancer cells line was evaluated and compared to normal cells line (prostate epithelial cell). Cytotoxicity experiments demonstrated that folate-functionalized nanoparticles were significantly cytotoxic to tumor cells, whereas normal cells were much less affected by the presence of these structures.
Assuntos
Antineoplásicos/farmacologia , Curcumina/farmacologia , Portadores de Fármacos/síntese química , Nanopartículas/química , Dióxido de Silício/química , Antineoplásicos/toxicidade , Linhagem Celular Tumoral , Curcumina/toxicidade , Dimetil Sulfóxido , Portadores de Fármacos/toxicidade , Ácido Fólico/análogos & derivados , Ácido Fólico/química , Ácido Fólico/toxicidade , Humanos , Nanopartículas/toxicidade , Tamanho da Partícula , Propilaminas/química , Propilaminas/toxicidade , Dióxido de Silício/síntese química , Dióxido de Silício/toxicidadeRESUMO
The trypanocidal activity of several 3-(4'-bromo-[1,1-biphenyl]-4-yl) -3-(4-X-phenyl)-N,N-dimethyl-2-propen-1-amine derivatives of the three evolutionary stages of Trypanosoma cruzi, namely the bloodstream trypomastigote form and both the proliferative epimastigote and amastigote forms, were studied. For both proliferative forms of T. cruzi, total lysis occurred at 10-60 microM for trypomastigotes at 40-200 muM. The following order of susceptibility was established: amastigotes > epimastigotes > trypomastigotes. The most were the bromo (X = g) and unsubstituted (X = b) compounds, which had 13- and 8-fold higher activity against trypomastigotes, respectively, than nifurtimox. Cytotoxicity in the Chinese hamster V-79 cell line, measured as inhibition of cell proliferation showed that all the compounds had the same range of IC50 (7.0-12.4 muM). The halogen (X = a,g,h) and the unsubstituted derivatives (X = b) were the least toxic in the series together with the compound (X = f).