Deoxynyboquinone, an excellent NQO1 substrate, is a potent antineoplastic agent. Deoxynyboquinone induces Apoptosis in cancer cell lines. Deoxynyboquinone kills cancer cells through oxidative stress and reactive oxygen species (ROS) formation[1][2][3].
Deoxynyboquinone (DNQ; 72h) potently induces the death of cancer cells (SK-MEL-5, MCF-7, HL-60, HL-60/ADR) in culture, with IC50 values between 16 and 210 nM[2].
Deoxynyboquinone is still able to induce cancer cell death under hypoxic conditions (HeLa cell; IC50: 5.1 μM)[2].
Deoxynyboquinone (group B1; 0.5 μM; 3, 6, 24 hours) potently induces apoptosis in cancer cell lines (MCF-7, HL-60) through cytochrome c release[3].
Deoxynyboquinone (2.5, 5, and 10 mg/kg; every other day for 5 injections; i.v. for day 2-18) shows antitumor efficacy confirmed by overall survival (at 5 mg/kg), at a 6-fold lower dose than β-lapachone (30 mg/kg)[4].
[1]. Elizabeth I Parkinson, et al. Deoxynyboquinones as NQO1-Activated Cancer Therapeutics. Acc Chem Res. 2015 Oct 20;48(10):2715-23.
[2]. Joseph S Bair, et al. Chemistry and biology of deoxynyboquinone, a potent inducer of cancer cell death. J Am Chem Soc. 2010 Apr 21;132(15):5469-78.
[3]. Tudor G, et,al. Cytotoxicity and apoptosis of benzoquinones: redox cycling, cytochrome c release, and BAD protein expression. Biochem Pharmacol. 2003;65(7):1061-1075.
[4]. Huang X, et al. An NQO1 substrate with potent antitumor activity that selectively kills by PARP1-induced programmed necrosis. Cancer Res. 2012 Jun 15;72(12):3038-47.