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Cytotoxicity and Cellular Accumulation of Palladium(II) Complexes of Tetracyclines
Author(s) -
de Paula Flávia C. S.,
Guerra Wendell,
Silva Iara R.,
Silveira Josianne N.,
Botelho Françoise Vasconcelos,
Vieira Leda Q.,
PereiraMaia Elene C.
Publication year - 2008
Publication title -
chemistry and biodiversity
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.427
H-Index - 70
eISSN - 1612-1880
pISSN - 1612-1872
DOI - 10.1002/cbdv.200890193
Subject(s) - chemistry , intracellular , incubation , cytotoxic t cell , cytotoxicity , viability assay , k562 cells , in vitro , biochemistry
We studied the cytotoxic effect and the uptake of Pd II complexes of doxycycline (Dox), [Pd(Dox)Cl 2 ] ( 1 ), and tetracycline (Tc), [Pd(Tc)Cl 2 ] ( 2 ), in chronic myelogenous leukemia cells. The effect of the compounds on macrophage viability was also investigated. Compound 1 is more effective than compound 2 in inhibiting the growth of K562 cells with the IC 50 values of 14.44 and 34.54 μ M , respectively. There is a good correlation between cell‐growth inhibition and intracellular metal concentrations, determined by inductively coupled plasma atomic emission spectroscopy (ICP‐AES). Incubation of the cells with equitoxic concentrations of both compounds yields approximately the same intracellular Pd concentration. At the IC 50 doses, intracellular concentration is ca. 33×10 −16 mol/cell for both compounds 1 and 2 . This suggests that more [Pd(Tc)Cl 2 ] is needed to produce a cytotoxic effect, because it enters cells more slowly. Both compounds up to 16 μ M did not affect the viability of mouse peritoneal macrophages after a 48‐h incubation. After 72 h of incubation, the IC 50 values are 22 for [Pd(Dox)Cl 2 ] and 40 μ M for [Pd(Tc)Cl 2 ]. Therefore, the cytotoxic effect in cancer cells exhibited by both compounds is higher than their effect in macrophages.