Table 4.
Compounds | IC50 (µM) Erythrocytes in vitro assay P. falciparum strain | % parasitaemia inhibition Hepatic cells in vitro assay | % parasitaemia inhibition In vivo assay Oral administration | ||||
---|---|---|---|---|---|---|---|
3D7 | Dd2 | 15 µM | 5 µM | 1 µM | 50* | 25* | |
Balsaminol F (6) | 18.0 | 20.0 | 97 | 31.4 | 14.7 | – | – |
Triacetylbalsaminol F (7) | 0.8 | 0.4 | 98.0 | 93.4 | 48.1 | – | – |
Tribenzoylbalsaminol F (8) | 57.3 | 68.4 | 27.0 | 18.5 | – | – | |
Balsaminoside A (10) | 4.6 | 4.0 | 99.0 | 44.0 | 26.6 | – | – |
Balsaminoside B (11) | 2.9 | 6.3 | 98.0 | 95.0 | 35.4 | 33.1 | 22.1 |
Balsaminoside C (12) | 3.4 | 7.2 | 51.0 | 12.3 | 7.4 | – | – |
Kuguaglycoside A (13) | 3.9 | 4.7 | – | – | – | – | – |
Karavilagenin C (17) | 10.4 | 11.2 | 96 | 71.8 | 25.8 | 33.1 | 22.1 |
Karavoate A (18) | 6.7 | 3.5 | 97 | 92.5 | 28.2 | – | – |
Karavoate B (19) | 0.5 | 0.5 | 99.0 | 96.1 | 59 | 58.1 | 41.8 |
Karavoate C (20) | 5.1 | 22.0 | 98.0 | 59.9 | 11.5 | – | – |
Karavoate D (21) | 1.5 | 0.4 | 93.4 | 82.5 | 34.4 | 45.5 | 12.3 |
Karavoate M (30) | 1.3 | 0.6 | 97 | 87.4 | 13.6 | – | – |
Karavoate N (31) | 2.4 | 47.9 | 0 | 0 | 0 | – | – |
Karavilagenin E (36) | 7.4 | 8.2 | – | – | – | – | – |
*mg kg−1 day−1