Table 2.
Compounds | Dose (mg) | HPLC analyses (ng/mL)a | Cytotoxic activity (% cells of control)c | DNA migration (% DNA in tail) | |||
---|---|---|---|---|---|---|---|
A-549 | TR-146 | A-549 | TR-146 | A-549 | TR-146 | ||
RCS-4 | 0.0 | 0.0 | 0.0 | 96.17 ± 5.46 | 97.87 ± 2.12 | 2.22 ± 0.75 | 2.03 ± 0.54 |
5.0 | n.d.b | 1358.0 | 86.33 ± 3.81 | 84.93 ± 2.87 | 8.10 ± 2.91* | 6.98 ± 4.21* | |
0.0 | 0.0 | 0.0 | 94.67 ± 4.93 | 83.33 ± 1.53 | 3.72 ± 0.78 | 3.55 ± 1.09 | |
20.0 | n.d.b | 2987.0 | 81.50 ± 2.27 | 82.80 ± 2.52 | 10.1 ± 3.20* | 7.04 ± 1.89* | |
XLR-11 | 0.0 | 0.0 | 0.0 | 95.50 ± 3.42 | 97.87 ± 2.12 | 1.76 ± 0.71 | 1.63 ± 0.47 |
5.0 | 2010.0 | 1847.0 | 89.33 ± 9.35 | 87.60 ± 2.30 | 3.79 ± 1.07* | 4.94 ± 2.03* | |
0.0 | 0.0 | 0.0 | 95.60 ± 3.53 | 91.00 ± 6.25 | 2.60 ± 1.01 | 2.44 ± 0.90 | |
20.0 | 3030.0 | 4390.0 | 81.83 ± 3.54 | 84.47 ± 4.15 | 5.71 ± 1.42* | 4.68 ± 1.24* |
Numbers indicate means ± SDs of data obtained with three parallel cultures per experimental point in a representative experiment. From each culture, 3 slides were made and 50 cells were evaluated per slide
* Significant differences from the corresponding control (unexposed) cultures (Student’s t test, p ≤ 0.05). In each experiment, positive controls were included; i.e., cells were exposed for 5 min on ice H2O2 (50 µM); in all these experiments, significant induction of DNA migration was observed (data not shown)
aValues indicate means of four measurements. 104 cells per insert were sonicated with 1000 µL MeOH; subsequently, the concentrations of the drug were determined (see “Materials and methods” section)
b n.d. not determined
cCytotoxicity was evaluated by use of trypan blue exclusion method. Numbers (%) indicate the ratio of cells with clear cytoplasm (cells without membrane damage) to total number of evaluated cells