Journal
BRAZILIAN JOURNAL OF MEDICAL AND BIOLOGICAL RESEARCH
Volume 40, Issue 10, Pages 1399-1402Publisher
ASSOC BRAS DIVULG CIENTIFICA
DOI: 10.1590/S0100-879X2006005000159
Keywords
lapachol; amino-lapachol derivatives; cytotoxicity; DNA-topoisomerase; DNA-interactions
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The cytotoxic activity of amino (3a-e), aza-1-antraquinone (4a-e) lapachol derivatives against Ehrlich carcinoma and human K562 leukemia cells was investigated. Cell viability was determined using MTT assay, after 48 (Ehrlich) or 96 h (K562) of culture, and vincristine (for K562 leukemia) and quercetin (for Ehrlich carcinoma) were used as positive controls. The results showed dose-dependent growth-inhibiting activities and that the amino derivatives were active against the assayed cells, whereas the 4a-e derivatives were not. The allylamine derivative 3a was the most active against Ehrlich carcinoma, with IC50 = 16.94 +/- 1.25 mu M, and against K562 leukemia, with IC50 = 14.11 +/- 1.39 mu M. The analogous lawsone derivative, 5a, was also active against Ehrlich carcinoma (IC50 = 23.89 +/- 2.3 mu M), although the 5d and 5e derivatives showed lower activity. The interaction between 3a-d and calf thymus DNA was investigated by fluorimetric titration and the results showed a hyperchromic effect indicating binding to DNA as presented of ethidium bromide, used as positive control. The inhibitory action on DNA-topoisomerase II-alpha was also evaluated by a relaxation assay of supercoiled DNA plasmid, and the etoposide (200 mu M) was used as positive control. Significant inhibitory activities were observed for 3a-d at 200 mu M and a partial inhibitory action was observed for lapachol and methoxylapachol.
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