TABLE 2.
In vitro activity of PS glycoside analogues against P. falciparum 3D7-C3PS3 and 3D7-C3 parasites
| Compound | PS present | Structural featurea
|
IC50 (μM)b
|
Ric | P valued | ||||
|---|---|---|---|---|---|---|---|---|---|
| Sugar | R | Y | X | 3D7-C3 | 3D7-C3PS3 | ||||
| PS-3 | Yes | Glucose | Ac | I | S | 1.25 (±0.64) | 10.41 (±1.38) | 8.3 | 0.0006 |
| PS-3′ | No | Glucose | Ac | I | S | 6.42 (±1.43) | 38.73 (±2.40) | 6.0 | 0.0003 |
| PS-7 | Yes | Glucose | Ac | I | SO2 | 9.08 (±2.70) | 65.53 (±4.90) | 7.2 | 0.0351 |
| PS-10 | Yes | Glucose | Ac | I | O | 5.15 (±1.42) | 31.56 (±18.53) | 6.1 | 0.1420 |
| PS-11 | Yes | Gal | Ac | I | S | 5.03 (±2.50) | 22.40 (±7.90) | 4.5 | 0.0219 |
| PS-12 | Yes | GlcOMe | Ac | I | S | 4.13 (±2.36) | 19.62 (±6.95) | 4.8 | 0.0217 |
| PS-15 | Yes | Mal | Ac | I | S | 3.14 (±0.97) | 7.83 (±0.85) | 2.5 | 0.0032 |
| PS-1 | Yes | Glucose | Ac | H | S | 43.19 (±9.04) | >100.00 | >2.3 | ND |
a
Gal, galactose; GlcOMe, glucuronic acid; Mal, maltose; Ac, acetate; H, hydrogen; I, iodine; S, sulfur; SO2, sulfur dioxide; O, oxygen.
b
Mean IC50 ± SD for three independent experiments each in triplicate wells.
c
Ri, resistance index: IC50 resistant line (3D7-C3PS3)/IC50 wild-type line (3D7-C3). The higher the Ri, the higher the level of resistance.
d
Statistical difference between IC50s was determined using an unpaired t test with GraphPad Prism data analysis software.