Antitumoral activity, isolation and identification of compounds actives of kielmeyera coriacea Mart &Zucc / Atividade antitumoral, isolamento e identificação dos principios ativos da Kielmeyera coriacea Mart &Zucc

AUTOR(ES)
DATA DE PUBLICAÇÃO

2008

RESUMO

Kielmeyera coriacea Mart. (Clusiacea), popularly known as Pau-Santo (Alves et aI., 2000), was one of the Cerrado species that showed significant antiproliferative activity in previous tests and therefore was selected for this study. Activity guided fractionation of the crude dichloromethane extract was undertaken to isolate and identify the active compounds involved with the antiproliferative activity. Df seven fractions separated, fraction F7 presented best antiproliferative activity, showed inhibition of growth and cell death for most cell lines with good correlation between concentration and effect, high potency and selectivity for breast, prostate, ovarian and breast resistant to multipledrugs. For in vivo evaluating, mice (balb /c) had i fibers (Hollow Fibers) containing human tumor lines implanted(Hollingshead et aI., 1995) - Breast, ovarian and ovarian resistant to multiple drugs. Thus, treatment with fraction 7, reduced the cellline densitybreast by 61% when the fibers were implanted in the abdomen (ip), whereas doxorubicin, the standard drug, showed reduction by 44%. With subcutaneous fibers, Fraction 7 showed reduction by 44%,which was the same value obtained by doxorubicin. With ovarian cancer lines, both Fraction 7 and doxorubicin showed significant inhibition only on abdomen fiber. The in vitro results were reproduced by in .viv experimentso, suggesting that the active compounds are able to achieve different body locations. Fractionation of fraction by column chromatography Fr7 provided three nain fractions. The most polar of the trhee fractions, Fr f3, produced grovyth inhibition and cell death for most celllines (in vitro), with good correlation between concentration and effect with selectivity for ovarian, breast and prostate. Cell line selectivity was observed for steroidal hormone type compounds. Analysis of Fr f3 demonstrated that this fraction is a mixture of oleaonic and ursolic acid type skeletons (Mahato e col., 1994, 1997). Subsequently, nitric oxide interference was evaluated for antitumor activity (Floyd et ai, 2007). Fraction 7 previously treated with L-NAME, an inhibitor of nitric oxide synthase enzyme, LPS (Iipopolysaccharide of E. coli), which stimulates the production of nitric oxide was assessed in vitro (breast). The results demonstrated reduction of was NO synthesis and stimulated by LPS, suggesting nitric oxide to be involved with the mechanism of action. Evaluation of fraction 7 on fibroblast proliferation proved not to be very cytotoxic to "normal" cells (Jorge, 2008)

ASSUNTO(S)

cancer cancer medicinal plants plantas medicinais

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