Background
Methods
Plant selection and collection
Plant extraction and structure elucidation
Reagents and materials
Extraction and fractionation
Evaluation of biological activities
In vitro screening of Sorindeia juglandifolia extracts against Plasmodium falciparum W2
In vitro screening of Sorindeia juglandifolia extracts against Plasmodium falciparum field isolates
Blood sampling and purification of Plasmodium falciparum isolates
Evaluation of antiplasmodial activity
Assessment of falcipain-2 inhibition by plant extracts
In vivo assessment of 2,3,6-trihydroxy benzoic acid against Plasmodium berghei
Evaluation of the suppressive effect of the compound
Evaluation of the curative effect of the compound
Evaluation of the acute toxicity of active extracts
Results and discussion
Phytochemical investigation of the fruit extract of Sorindeia juglandifolia
In vitro activity of Sorindeia juglandifolia extracts against Plasmodium falciparum W2 and recombinant falcipain-2
Fractions /Compounds | Solvent system | P. falciparum W2- IC50±SD (μg/ml) | Falcipain-2 IC50±SD (μg/ml) |
---|---|---|---|
SJFR1 | 6.24±1.01 | 8.22±1.09 | |
SJFR2 | Hex:EtOAc 10% | 11.55±2.45 | 6.02±3.81 |
SJFR3 |
>10
|
>10
| |
SJFR4 |
>10
| 21.90 ±1.85 | |
SJFR5 | Hex:EtOAc 25% |
>10
|
>10
|
SJFR6 |
>10
|
>10
| |
SJFR7 |
>10
|
>10
| |
SJFR8 | 2.76±0.08 |
>10
| |
SJFR9 | 2.30±0.97 | 5.42±0.65 | |
SJFR10 | Hex:EtOAc 50/50 | 2.46±0.29 |
>10
|
SJFR11 |
>10
|
>10
| |
SJFR12 |
>10
|
>10
| |
SJFR13 |
>10
|
>10
| |
SJFR14 |
>10
|
>10
| |
SJFR15 | Hex:EtOAc 75% |
>10
| 17.31±2.51 |
SJFR16 |
>10
|
>10
| |
SJFR17 | 8.47±0.41 | 1.12±0.16 | |
SJFR18 | EtOAc 100% |
>10
| 1.14±0.10 |
CQ | 0.05±0.01 | ||
ART | 0.007±0.01 | ||
E64 | ND | 0.049±0.003 | |
2,3,6-trihydroxy benzoic acid (1) | 16.47±0.47 μM | 35.41±22.37μM | |
2,3,6-trihydroxy methyl benzoate (2) | 13.04±1.63 μM | 6.09±0.87 μM |
In vitro activity of Sorindeia juglandifolia extracts against field strains of Plasmodium falciparum
In vivo activity of 2,3,6-trihydroxy benzoic acid against Plasmodium berghei B
Drug dose (mg/kg) | Mean % Suppression/Inhibition | |
---|---|---|
Suppressive test
| ||
10 | 22.73 | |
30 | 35.95 |
c
SD50 = 44.9 ± 1.6 mg/kg |
50 | 53.66 | |
100 | 69.63 | |
Quinine sulfate (24 mg/kg) | 71.34 | |
Curative test
| ||
10 | 20.95 | |
30 | 41.00 |
c
ED50= 42.2 ± 1.6 mg/kg |
50 | 57.27 | |
100 | 66.40 | |
Quinine sulfate (24 mg/kg) | 89.50 |