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Table 1 Flavonoid IC50 values for growth inhibition of P. falciparum

From: Common dietary flavonoids inhibit the growth of the intraerythrocytic malaria parasite

Class

Major food sources [17]

Flavonoid

Chemical substitutions/modifications

In vitroantiplasmodial activity (IC50, μM)a

LogD (pH 7.0)b

    

3D7

7G8

 

Flavonols

Onions, kale, broccoli, apples, cherries, fennel, sorrel, berries, tea

Kaempferol

3, 5, 7, 4' – OH

33 ± 7

25 ± 2

2.40

  

Myricetin

3, 5, 7, 3', 4', 5' – OH

40 ± 10

76 ± 23

2.06

  

Quercetin

3, 5, 7, 3', 4' – OH

15 ± 5

14 ± 1

2.09

  

Isoquercitrin

3-gluc, 5, 7, 3', 4' – OH

66 ± 10

66 ± 18

1.59

Flavones

Parsley, thyme, celery, sweet red pepper

Acacetin

5, 7 – OH 4' – OCH3

> 100

13 ± 2

2.77

  

Apigenin

5, 7, 4' – OH

20 ± 3

13 ± 2

2.77

  

Baicalein

5, 6, 7 – OH

32 ± 1

21 ± 6

3.18

  

Chrysin

5, 7 – OH

18 ± 3

22 ± 4

2.79

  

Luteolin

5, 7, 3', 4' – OH

11 ± 1

12 ± 1

2.62

Flavanones

Citrus fruits, prunes

Naringenin

5, 7, 4' – OH, single bond between 2 and 3

> 125

71 ± 10

2.17

Isoflavones

Legumes

Genistein

5, 7, 4' – OH, B ring attached to 3

> 50

29 ± 5

1.53

Chloroquine

NA

NA

NA

0.006 ± 0.0003

0.084 ± 0.026

ND

  1. a Values are the means (± S.E.M.) of results from three independent experiments, each performed in duplicate or triplicate. Parasite susceptibility was measured in 96-well plates over 96 h using the [3H]hypoxanthine incorporation assay [19]. b LogD (the octanol-water distribution coefficient) was predicted using PrologD (Pallas for Windows version 2.1, CompuDrug International Inc.). Good cell permeability requires a logD value of 2–5 [20]. NA, not applicable; ND, not determined.