Table 1. MeOX enhances the lethality of ß-lap in an NQO1-dependent manner in a broad range of human cancer cells.
| Cell line | Cancer Type | No Addition | MeOX (12 mM) | Dicoumarol (50 μM) | DER at LD50 |
|---|---|---|---|---|---|
| 231-NQO1(−) | Breast | >10 | >10 | >10 | NA |
| 231-NQO1(+) | Breast | 1.8 ± 0.2 | 0.85 ± 0.09** | >10 | 2.12 |
| UM-SCC-104-NQO1(−) | Head and Neck | >10 | >10 | >10 | NA |
| SqCC/Y1-NQO1(+) | Head and Neck | 2.0 ± 0.15 | 1.2 ± 0.07*** | >10 | 1.67 |
| H596-NQO1(−) | NSCLC | >10 | >10 | >10 | NA |
| H596-NQO1(+) | NSCLC | 3 ± 0.3 | 1.7 ± 0.2* | >10 | 1.76 |
Values represent ß-lap LD50 in μM concentration. Genetically matched NQO1-overexpressing (NQO1+) versus NQO1-deficient (NQO1−) cancer cells were screened for sensitivity to ß-lap alone, MeOX alone or the ß-lap + MeOX combination. Breast cancer: MDA-MB-231 NQO1 proficient = 231-NQO1(+); MDA-MB-231 NQO1 deficient = 231-NQO1(−). NSCLC: H596; Head and Neck cancer: UM-SCC104 and SqCC/Y1. DER = dose enhancement ratio; DER = LD50 +MeOX / LD50 No addition. All results were compared using Student’s t-tests (+/−SD). *p < 0.05; **p < 0.01; ***p < 0.001.