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. 2016 Feb;23(6):520–577. doi: 10.2174/0929867323666151223095839

Table 17. Banyu eukaryotic and prokaryotic biochemical and cellular data for enantiomers 116 and 125 and in vivo antitumor activities in 3 murine models. Etoposide and ciprofloxacin were used as controls.

In vitro or in vivo assay 14
etopo-side
15
cipro-floxacin
E. coli gyrase DNA supercoiling IC50 (μg/ml)a 0.2 1.0 * 1.0
L1210 topo II DNA relaxation IC50 (μg/ml)a 1.5 24 4.4 > 50
L1210 topo II induction of DNA cleavage
IC50 (μg/ml)a
1.2 > 12 ½ as active vs of (-)-BO *
L1210 topo II induction of DNA cleavable complex formation in intact cells IC50 (μg/ml)a 3-17 fold increase vs control over range
0.10 to 28 μg/ml
minimal complex formation at 9 μg/ml ½ as active vs of (-)-BO *
P388 cytotoxicity
CC50 (μg/ml)a
0.004 0.50 0.004 *
L1210 cytotoxicity
CC50 (μg/ml)a
0.017 1.7 0.020 *
Antitumor activity i.p.-implanted murine leukaemia P388
0.313mg/kg/day i.p.
Survival days mean: 16.4b * 22.2b *
T/C%c 146 * 198 *
Antitumor activity on i.p.-implanted murine leukaemia L1210
0.313mg/kg/day i.p.
Survival days mean: 21.2d * 31.4d *
T/C%: 155 * 229 *
Antitumor activity on s.c.-implanted colon 26 solid tumor
1.25 mg/kg/day s.c.
Tumor weight mean (g): 0.00e * 1.28e *
% inhibition 100 * 63 *

aValues originally reported as μM were converted to μg/ml for this table; bcontrol = 11.2 days; cRatio (%) of survival time of drug treated animals to control; dcontrol = 13.7 days; econtrol tumor weight mean = 3.46g.