The evaluation of cytotoxic activity of planar pentadentate ligand 2 ',2 '''-(2,6-pyridindiyldiethylidyne) dioxamohydrazide dihydrate (H(2)Lx2H(2)O) and its metal coordination complexes; Pitfalls in the use of the MTT-assay
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In this study we have investigated, for the first time to our knowledge, the antineoplastic activity of a planar pentadentate ligand (H2L&BULL; 2H(2)O = 2', 2"'-(2,6-pyridindiyldiethylidyne)dioxamohydrazide dihydrate) and some of its metal coordination complexes [Cu(L)(H2O)]&BULL; H2O, [Cu(HL)(H2O)]ClO4, [Co(L)(H2O)(2)]&BULL; 6H(2)O, [Co(H2L)(H2O)(MeOH)](ClO4)(2) and [Fe(L)(H2O)(2)]ClO4&BULL; 3H(2)O, as well as of inorganic salts CuCl2&BULL; 2H(2)O, CoCl2&BULL; 6H(2)O and FeCl3&BULL; 6H(2)O of corresponding metal ions. The antiproliferative activity of these compounds was examined in a human melanoma cell line FemX with exposure time of 48 hours by performing two cytotoxicity tests: 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay and sulforhodamine B (SRB) assay. Among these substances, the ligand H2L&BULL; 2H(2)O expressed the greatest antineoplastic activity IC50 = 45.40 μ M, while the IC50 of others Could not be determined by SRB assay in the examined ran...ge of concentrations due to their low activity. FeCl3&BULL; 6H(2)O showed stimulatory activity. We have found remarkable discrepancies between the results obtained by MTT assay and SRB assay that influence IC50 value as well as other measures of cytotoxicity, which led to the conlusion of uncertainty of using the MTT assay in evaluation of antineoplastic activity of organometalic complexes and inorganic metal salts.
Keywords:2,6-diacetylpyridine / 2 ',2 '''-(2,6-pyridindiyldiethylidyne)dioxamohydrazide dihydrate / metal coordination complexes / MTT / SRB / FemX / cytotoxic activity
Source:Journal of Experimental and Clinical Cancer Research, 2005, 24, 1, 63-68
- Apsit Assoc Prom Stud Immunol Tumor, Rome