Table 6.
Pharmacokinetic properties of standard and lead compounds.
| Curcumin (standard) | Augustamine | Camptothecin | |
|---|---|---|---|
| Water solubility (log mol/L) | -4.01 | -2.426 | -4.688 |
| Caco2 permeability (log Papp in 10–6 cm/s) | -0.093 | 1.429 | 0.125 |
| Human Intestinal absorption (% Absorbed) | 82.19 | 97.237 | 92.007 |
| Skin Permeability (log Kp) | -2.764 | -3.508 | -3.275 |
| P-glycoprotein substrate (Yes/No) | Yes | No | Yes |
| P-glycoprotein I inhibitor (Yes/No) | Yes | No | No |
| P-glycoprotein II inhibitor (Yes/No) | Yes | No | No |
| VDss (human) (log L/kg) | -0.215 | 0.8 | 0.028 |
| Fraction unbound (human) (Fu) | 0 | 0.332 | 0.502 |
| BBB permeability (log BB) | -0.562 | 0.288 | -0.451 |
| CNS permeability (log PS) | -2.99 | -2.579 | -3.017 |
| CYP2D6 substrate (Yes/No) | No | No | No |
| CYP3A4 substrate (Yes/No) | Yes | Yes | Yes |
| CYP1A2 inhibitor (Yes/No) | Yes | No | No |
| CYP2C19 inhibitor (Yes/No) | Yes | No | No |
| CYP2C9 inhibitor (Yes/No) | Yes | No | No |
| CYP2D6 inhibitor (Yes/No) | No | No | No |
| CYP3A4 inhibitor (Yes/No) | Yes | No | No |
| Total Clearance (log ml/min/kg) | -0.002 | 1.21 | 1.237 |
| Renal OCT2 substrate (Yes/No) | No | No | No |
| AMES toxicity (Yes/No) | No | No | No |
| Max. Tolerated dose (human) (log mg/kg/day) | 0.081 | -0.221 | -0.581 |
| hERG I inhibitor (Yes/No) | No | No | No |
| hERG II inhibitor (Yes/No) | No | No | No |
| Oral Rat Acute Toxicity (LD50) (mol/kg) | 1.833 | 2.986 | 2.865 |
| Oral Rat Chronic Toxicity (log mg/kg_bw/day) | 2.228 | 1.532 | 1.047 |
| Hepatotoxicity (Yes/No) | No | No | Yes |
| Skin Sensitization (Yes/No) | No | No | No |
| T. Pyriformis toxicity (log ug/L) | 0.494 | 0.355 | 0.482 |
| Minnow toxicity (log mM) | -0.081 | 1.323 | 2.272 |