Table 3.
Antimalarial activity of selected diarylpentanoid analogues and derivatives against P. falciparum CQ-sensitive (3D7), P. falciparum CQ-resistant (Gombak A) and P. knowlesi A1H1.
Compound | P. falciparum 3D7 (CQ-sensitive) EC50 (μM) ± SD | P. falciparum Gombak A (CQ-resistant) EC50 (μM) ± SD | P. knowlesi PKA1H1 EC50 (μM) ± SD | Vero cell (Normal cell) CC50 (μM) ± SD | Selectivity Index (SI) |
Resistance Index (RI) on P. falciparum strains |
||
---|---|---|---|---|---|---|---|---|
P. falciparum 3D7 (CQ-sensitive) | P. falciparum Gombak A (CQ-resistant | P. knowlesi PKA1H1 | P. falciparum 3D7 (CQ-sensitive) | |||||
MAAC1 | 12.0 ± 0.7 | >200 | 17.4 ± 0.8 | 157.0 ± 0.9 | 13.1 | NC | 9.0 | NC |
MAAC2 | 39.3 ± 5.1 | >200 | 13.4 ± 0.7 | NDa | NDa | NDa | NDa | NDa |
MS33A | 3.1 ± 0.2 | 87.5 ± 0.9 | 3.6 ± 0.2 | 82.6 ± 1.7 | 26.6 | 1.0 | 22.9 | 28.2 |
MS33C | 2.5 ± 0.4 | 56.2 ± 1.3 | 5.1 ± 0.2 | 163.1 ± 1.8 | 65.2 | 2.9 | 32.0 | 22.5 |
MS33D | 21.7 ± 0.8 | 74.4 ± 2.4 | 23.7 ± 2.6 | 225.3 ± 3.0 | 10.4 | 3.0 | 9.5 | 3.4 |
MS34C | 1.6 ± 0.2 | 8.8 ± 0.9 | 11.8 ± 1.1 | 134.4 ± 3.2 | 84.0 | 15.4 | 11.4 | 5.5 |
MS40B | 13.7 ± 0.8 | 45.6 ± 1.3 | 16.6 ± 0.5 | 164.0 ± 2.1 | 12.0 | 3.6 | 9.9 | 3.3 |
MS47 | 16.1 ± 0.5 | 51.4 ± 2.7 | 21.7 ± 1.2 | 170.6 ± 1.7 | 10.6 | 3.3 | 7.9 | 3.2 |
MS69 | 785.8 ± 4.2 | 28.7 ± 2.0 | 324.1 ± 5.9 | ND | ND | ND | ND | ND |
MS72A | 530.0 ± 3.6 | >200 | 507.5 ± 1.3 | ND | ND | ND | ND | ND |
MS72C | 515.1 ± 4.9 | >200 | 430.1 ± 2.3 | ND | ND | ND | ND | ND |
MS78 | 689.1 ± 4.2 | >200 | 354.8 ± 7.1 | ND | ND | ND | ND | ND |
MS79 | 329.3 ± 2.6 | >200 | 194.6 ± 2.7 | ND | ND | ND | ND | ND |
MS87 | 10.8 ± 1.3 | 1.85 ± 2.8 | 11.4 ± 0.9 | 564.1 ± 0.4 | 52.2 | 304.9 | 49.5 | 0.17 |
CQ | 0.0017 ± 0.2 | 5.56 ± 3.2 | 0.0018 ± 0.1 | 491.7 ± 2.4 | >2000 | 89.0 | >2000 | >2000 |
ND = Not determine (EC50 > 200 μM).
NDa = Not determine due to limited sample.
NC = Not calculated.
SI > 10 (Acceptable value); SI > 50 (Ideal value) RI < 100 (High resistance); RI < 10 (Intermediate resistance); RI < 1 (Low resistance).