Background
Malaria in South America
Search methodology
Results
Natural products
Compound | Authors | Plant with the lowest IC50 | Type | IC50(P. falciparum strain) |
---|---|---|---|---|
1
|
Bowdichia virgiloides
|
Extracts
|
1.0 μg/mL
| |
Isolated substances
|
5 μg/mL (F32 and Indo)
| |||
-
|
Bowdichia virgiloides
|
Extracts
|
1 μg/mL (F32)
| |
2
|
Baccharis dracunculifolia
|
Extracts
|
13 μg/mL
| |
Isolated substances
|
0.8 μg/mL (W2 e D6)
| |||
3
|
Picrolemma spruce
|
Isolated substances
|
0.002 μM (K1)
| |
4
|
Holostylis reniformis
|
Isolated substances
|
0.20 μM (field isolate)
| |
-
|
Caesalpina pluviosa
|
Extracts
|
0.59 μg/mL (3D7)
| |
5
|
Piper peltatum
|
Isolated substances
|
0.05–2.11 μg/mL (M1)
| |
5
|
Pothomorphe peltata
|
Isolated substances
|
0.67 μM (K1)
| |
-
|
Remijia peruviana
|
Extracts
|
0.85 μg/mL (FcB2)
| |
-
|
Buddleja globosa
|
Extracts
|
8.9 μg/mL (K1)
| |
-
|
Caesalpina pluviosa
|
Extracts
|
8 μg/mL (D2)
| |
-
|
Caesalpina pluviosa
|
Extracts
|
3.4 μg/mL
| |
Isolated substances
|
Inactive (F32)
| |||
-
|
Rumex obtusifolius
|
Isolated substances
|
71 μg/mL
i
| |
-
|
Sparanttanthelium amazonum
|
Extracts
|
2 μg/mL (F32)
| |
-
|
Swietenia macrophylla
|
Extracts
|
73%
ii
| |
-
|
Tripodanthus acutifolis
|
Extracts
|
98%
iii
| |
-
|
Montrichardia linifera
|
Extracts
|
11.7 μg/mL (W2)
| |
-
|
Nectandra megapotamica
|
Extracts
|
28 μg/mL
| |
Isolated substances
|
3.8 μg/mL (D6)
| |||
-
|
Bidens pilosa
|
Extracts
|
3.1 μg/mL (D6)
| |
-
|
Remijia ferruginea
|
Extracts
|
48%
iv
| |
-
|
Matayba guianensis
|
Isolated substances
|
2.5 μg/mL (FcB1)
| |
-
|
Esenbeckia febrifuga
|
Extracts
|
15.5 μg/mL
| |
Isolated substances
|
75.3 μg/mL (W2)
| |||
-
|
Ouratea nitida
|
Extracts
|
51.04%
v
| |
-
|
Xylopia emarginata
|
Extracts
|
3.3 μg/mL (PA)
| |
-
|
Pentacalia desiderabilis
|
Isolated substances
|
7.82 μg/mL (K1)
| |
-
|
Bidens pilosa
|
Extracts
|
38%
vi
| |
-
|
Physalis angulata
|
Isolated substances
|
2.2 μM (W2)
| |
-
|
Cecropia pachystachya
|
Extracts
|
66%
4
| |
Isolated substances
|
58%
vii
| |||
-
|
Azorella compacta
|
Isolated substances
|
60%
viii
| |
-
|
Solanum nudum
|
Isolated substances
|
21 μM (FcB2)
| |
-
|
Siparuna aspera
|
Extracts
|
6.4 μg/mL (FCR-3)
| |
-
|
Minquartia guianensis
|
Extracts
|
4.2 μg/mL (FCR-3)
|
Medicinal chemistry
Compound | Authors | Target | Chemical class | Lowest IC50(strain) |
---|---|---|---|---|
6
| - | Pyrazolylnaphthoquinones, 5-aminoisoxazole | 0.11 μg/mL (K1) | |
7
| - | 1,4-naphthoquinones | 0.03 μM (FcB1) | |
8
| β-haematin | Thieno(2,3-b)quinoline | 74.42%1 | |
9
| Aspartyl protease | Hydroxyethylpiperazines | 4.6 μM (3D7) | |
10
| Aspartyl protease | Hydroxyethyylpiperazines | 5.1 μg/mL (W2) | |
11
| β-haematin | Piperazine, 3-acetylursolic acid | 0.08 μM (FcB1) | |
12
| Betulinic acid | 5.99 μM (W2) | ||
13
| - | Sesquiterpenes | 0.05 ng/mL (P. falciparum mefloquine resistant) | |
14
| - | Ozonides | 13.6 μg/mL | |
15
| Cysteine proteases | Semicarbazone, Thiosemicarbazone | 7.2 μM (W2) | |
16
| β-haematin | Benzimidazole-5-carbohydrazides | 8.43 μM | |
17
| Hypoxanthine-guanine phosphoribosyltransferase | 6-thiopurine Steroids | 82%1 | |
18
| β-haematin | Pyrazolo and pyrimido benzothiazine dioxide | 92.32%2 | |
19
| β-haematin | Benzothiazines | 78.17%2 | |
20
| Aspartyl protease | Thioetherhydroxyethyl, Sulfonamides | 15 μM (W2) | |
21
| β-haematin | Chlorovinyl sulfones | 0.025 μM (W2) | |
22
| β-haematin | Sulfonamide chalcones | 0.48 μM (W2) | |
23
| Glucose metabolism β-haematin | Sulfonylureas | 1.2 μM (W2) | |
24
| β-haematin | Rhenium bioorganometalics, Aminoquinoline | 0.048 μM (3D7) | |
25
| β-haematin | Aminoquinolines, thiazolidinone | 0.25 μM (3D7) | |
26
| β-haematin | E-2-quinolinylbenzo-cycloalcanones | 90%3 | |
27
| β-haematin | Quinolone, 6-thiopurine | inactive | |
28
| β-haematin | 4-aminoquinolines, platinum (II) complexes | 84 %4 | |
29
| β-haematin | 4-aminoquinolines | 1.39 μg/mL (W2) | |
30
| β-haematin | Quinoline | Active | |
31
| Cysteine protease falcipain | Quinolinyl chalcones | 19 μM (FcB1) | |
32
| β-haematin | Chloroquinolines | 94.93%3 | |
33
| β-haematin | Gold-chloroquine complexes | −5 | |
34
| Cysteine protease β-haematin | Phenylurenyl chalcones | 1.76 μM | |
35
| - | Naphthoquinones, Phenazines | 1.67 μM (W2) | |
36
| - | 3-alkylpyridines alkaloids | <3.38 μM (W2) | |
37
| β-haematin | Bisquinoline | 56.76 %2 |