Table 1.
The cytotoxicity of artesunic acid (ARTA) derivatives and doxorubicin. CCRF-CEM and P-glycoprotein-expressing CEM/ADR5000 cells were incubated for 72 h with artemisinin-, egonol-, and thymoquinone-based hybrids. Resazurin assays were performed to determine dose–response curves and IC50 measurements were calculated (mean ± SD). Experiments were repeated at least twice. Resistance indices were obtained by dividing the IC50 values on the resistant cell line through that of the sensitive cell line.
| Compound | IC50 (µM) ± SD | Degree of Resistance | |
|---|---|---|---|
| CCRF-CEM | CEM/ADR5000 | ||
| Doxorubicin | 0.0033 ± 0.00065 | 1.613 ± 0.166 | 488.79 |
| Artesunic acid | 0.069 ± 0.03 | 0.189 ± 0.003 | 2.739 |
| DHA | 0.085 ± 0.003 | 0.265 ± 0.008 | 3.118 |
| REI213 | 0.568 ± 0.215 | 0.582 ±0.224 | 1.025 |
| REI220+26 | 43.685 ± 4.385 | 17.450 ± 1.010 | 0.399 |
| REI230 | 2.748 ± 0.021 | 2.789 ± 0.018 | 1.015 |
| REI234 | 0.0018 ± 0.0001 | 0.0068 ± 0.0006 | 3.778 |
| REI235 | 0.092 ± 0.006 | 0.199 ± 0.023 | 2.163 |
| REI259 | 0.876 ± 0.192 | 3.852 ± 1.021 | 4.397 |
| TF19 | 6.071 ± 0.247 | 5.663 ± 0.190 | 0.933 |
| TF26 | 0.0027 ± 0.001 | 7.872 ± 0.594 | 2915.556 |
| TF27 | 0.0024 ± 0.0001 | 0.196 ± 0.008 | 81.667 |
| TF29 | 0.0021 ± 0.0003 | 0.485 ± 0.210 | 230.952 |
| HH3 | 7.343 ± 0.911 | 7.071 ± 1.408 | 0.963 |
| VK3 | 0.134 ± 0.140 | 5.210 ± 0.153 | 38.881 |