Table I.
Compound | Promastigote Killing (IC50) |
Amastigote Killing** (IC50) |
Macrophage cytotoxicity§ (CC50) |
In vitro Therapeutic Index§§ |
---|---|---|---|---|
SSG | 306.8 + 5.06 | 13.32 + 5.14 | 53.4 + 1 | 4 |
TR 001 | 5.4 + 2.4Π | 0.069 + 0.02Π | 46.5 + 2 | 659 |
TR 002 | 7.04 + 0.15Π | 0.26 + 0.18Π | 49.2 + 2.7 | 189.2 |
IC50 is the concentration of drug (µM) to achieve 50% killing of parasites per 106 axenic promastigotes or 2.5 × 106 amastigotes inside of 0.5 × 106 BMDM after 48 h of culture.
Drug concentration (µM) per 0.5 × 106 BMDM to achieve 50% killing of macrophages.
Therapeutic index = CC50/IC50**.
significantly different (p<0.05) as compared to SSG.