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Table 1 GI50 and MIC values and ratios of salinomycin and monensin derivatives for T. brucei and HL-60 cells

From: In vitro activity of salinomycin and monensin derivatives against Trypanosoma brucei

 

T. brucei

HL-60

Selectivity

Compound

MIC (μM)a

GI50 (μM)b

MIC (μM)a

GI50 (μM)b

MIC ratioc

GI50 ratiod

Salinomycin

1

0.18 ± 0.06

1

0.44 ± 0.21

1

2.4

SAL-E1

10

3.08 ± 0.18

100

35.5 ± 2.4

10

11.4

SAL-E2

10

3.25 ± 0.26

100

34.6 ± 1.9

10

10.6

SAL-E3

10

3.10 ± 0.21

100

33.8 ± 3.5

10

10.9

SAL-E4

10

3.12 ± 0.08

100

32.9 ± 2.5

10

10.5

SAL-E5

10

3.21 ± 0.02

100

38.4 ± 4.2

10

11.0

SAL-E6

10

3.01 ± 0.06

> 100

> 100

> 10

> 33

SAL-E7

0.1–1e

0.057 ± 0.029

100

16.4 ± 1.9

100–1000

288

SAL-AM1

10

3.23 ± 0.21

100

38.9 ± 3.2

10

12.0

SAL-AM2

0.1

0.040 ± 0.007

100

14.5 ± 1.3

1000

363

SAL-AM3

10

2.94 ± 0.20

100

7.92 ± 1.95

10

2.7

SAL-AM4

10

2.69 ± 0.51

100

24.5 ± 3.7

10

9.1

SAL-AM5

10

2.69 ± 0.20

100

39.2 ± 1.6

10

14.6

Monensin

0.1

0.029 ± 0.002

10

1.48 ± 0.56

100

51

MON-E1

10

3.06 ± 0.06

100

34.1 ± 2.2

10

11.1

MON-E2

10

2.76 ± 0.10

100

25.3 ± 5.0

10

9.2

MON-E3

10

1.68 ± 0.56

100

20.3 ± 3.1

10

12.1

MON-UR1

1

0.31 ± 0.06

100

23.3 ± 6.6

100

75

Suraminf

0.1

0.035 ± 0.002

> 100

> 100

> 1000

> 2857

  1. aData shown are mean values of three independent experiments
  2. bData shown are mean values ± SD of three independent experiments
  3. cMIC ratio, MIC(HL-60)/MIC(T. brucei)
  4. dGI50 ratio, GI50(HL-60)/GI50(T. brucei)
  5. eAfter an incubation period of 72 h, in one of the three experiments a few motile trypanosomes were observed at a concentration of 0.1 μM (but none at 1 μM) while in the two other experiments no motile parasites were found at that concentration. Thus, a range of 0.1–1 μM as MIC value was assigned
  6. fReference control