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Table 3 Global and enantiomer specific inhibition of β-haematin aggregation

From: Differences in anti-malarial activity of 4-aminoalcohol quinoline enantiomers and investigation of the presumed underlying mechanism of action

Compound

Inhibition (%)

Enantiomer

Inhibition (%)

IC50 (mM)

CQ indexa

Chloroquine

77.8 ± 6.27b

-

NAc

0.85 ± 0.11

-

Mefloquine

6.1 ± 4.63

-

NDd

> > > 2

> > > 2.35

1

47.1 ± 7.84

(R)

49.8 ± 7.54

> 2

> 2.35

  

(S)

44.7 ± 7.58

> 2

> 2.35

2

49.1 ± 6.23

(R)

51.2 ± 7.03

1.90 ± 0.26

2.23

  

(S)

46.5 ± 4.1

> 2

> 2.35

3

50.2 ± 5.05

(R)

48.3 ± 3.68

> 2

> 2.35

  

(S)

51.8 ± 5.60

1.90 ± 0.21

2.23

4

59.3 ± 6.27*

(R)

60.8 ± 6.44

1.61 ± 0.17

1.89

  

(S)

57.8 ± 6.07

1.29 ± 0.13

1.52

5

57.6 ± 8.31**

(R)

53.6 ± 8.89

1.86 ± 0.31

2.19

  

(S)

61.7 ± 5.48

1.77 ± 0.16

2.08

6

50.6 ± 7.63

(R)

49.0 ± 7.95

> 2

> 2.35

  

(S)

52.2 ± 7.38

1.92 ± 0.27

2.26

  1. a: calculated as compound IC50/chloroquine IC50
  2. b: Results expressed as mean ± standard deviation of the inhibition witnessed for each compound at a 2 mM concentration.
  3. c: Not applicable
  4. d: Not determined
  5. *: Significantly higher than all other values in the same column except for chloroquine and compound 4 (p ≤ 0.0011)
  6. **: Significantly higher than values for mefloquine and compounds 1, 2, 3 and 6 (p < 0.02)