Background
Methods
Plant materials
Extraction and UPLC-ELSD-PDA-MS analysis
Antiparasitic assay
Cytotoxicity assay
Phylogenetic analysis of screening activities
General compound isolation procedures
Extraction and isolation of alkaloids from Berberis thunbergii
Extraction and isolation of triterpenes from Eugenia rigida
Results and discussion
Fraction or COMBI | Primary (% activity) | Secondary (EC50, μg/mL) | |||||
---|---|---|---|---|---|---|---|
μg/mL | MAR3D7a
| MARK1b
| HEK293c
| BJd
| MAR3D7a
| MARK1b
| |
f8/c9 | 23.68 | 43.4 | 37 | 2.15 | −0.85 | ||
f9/c8 | 35.75 | 95.2 | 80.2 | 2.52 | 6.63 | 8.15 | 7.57 |
f10/c7 | 23.68 | 97.4 | 95 | 8.13 | 4.91 | 0.53 | 0.63 |
f11/c6 | 14.39 | 96.9 | 96.5 | 5.29 | 0 | 2.02 | 3.6 |
f12/c5 | 8.37 | 92.8 | 93.4 | 7.42 | 0.7 | 0.61 | 0.81 |
f13/c5 | 5.57 | 92 | 92.4 | 3.59 | 0.45 | 0.39 | 0.45 |
f14/c4 | 5.11 | 89.9 | 96 | 5.05 | −0.48 | 0.86 | 2.07 |
f15/c4 | 7.43 | 84.9 | 97.6 | 6.94 | 0.56 | 1.11 | 10.61 |
f16/c3 | 11.14 | 84.4 | 93.7 | 10.1 | 1.13 | 0.21 | 4.77 |
f17/c2 | 6.96 | 95.7 | 94.6 | 1.09 | 1.48 | 1.66 | 1.7 |
f18/c2 | 5.11 | 76.9 | 39 | 3.12 | −0.94 | ||
f19/c1 | 4.18 | 35.6 | 21.2 | 1.29 | 0.64 |
UPLC-ELSD-PDA-MS analysis of B. thunbergii-active COMBIs
UPLC-ELSD-PDA-MS analysis of Eugenia rigida-active COMBIs
Compound isolation from Berberis thunbergii and Eugenia rigida
Anti-malarial compounds isolated from Berberis thunbergii and Eugenia rigida
Sample | Unit |
P. falciparum EC50
| Sample |
P. falciparum EC50
| ||
---|---|---|---|---|---|---|
3D7 | K1 | 3D7 | K1 | |||
BT-EtOHa
| μg/mL | NTg
| NT | ER-EtOHh
| >100 | >100 |
BT-P-Ab
| μg/mL | 0.25 | 0.291 | ER-MeOHi
| 2 | 1.37 |
BT-P-Bc
| μg/mL | 0.23 | 0.19 | ER-Hexj
| >100 | >100 |
BT-P–Cd
| μg/mL | NT | NT | ER-Hex-33-52k
| 1 | 0.6 |
BT-P-De
| μg/mL | 10 | 10 | ER-Hex-53-60l
| 0.7 | 0.6 |
7 + 8
f
| μg/mL | 100 | 0.42 | ER-EtOAcm
| >100 | >100 |
1
| μM | 0.46 | 0.44 |
11
| 7.7 | 4.0 |
9
| μM | 0.035 | 0.15 |
12
| NT | NT |
10
| μM | NT | NT |
13
| 0.3 | 1.1 |