Beta-Lapachone

β-Lapachone is a naturally occurring quinone obtained from the bark of the lapacho tree (Tabebuia avellanedae) with cancer chemopreventive properties. A novel DNA topoisomerase I inhibitor which unlike camptothecin does not stabilize the cleavable complex indicating a novel mode of action (1). Induces apoptosis in a number of cancer cell lines (2). In cancer cells overexpressing NAD(P)H:quinone oxidoreductase, reduction of β-lapachone leads to futile cycling between quinone and hydroquinone forms (3) resulting in the production of reactive oxygen species (4). Suppresses radiation-induced activation of NFĸB (5). Attenuates cognitive impairment and inflammation in amyloid-induced mouse model.

1. CJ Li et al. J. Biol. Chem. 1993 268:22463 2. SM Wuerzberger et al. Cancer Res. 1998 58:1876 3. JJ Pink et al. J. Biol. Chem. 2000 275:5416 4. D Siegel et al. Biochem. Pharmacol. 2012 83:1033 5. GZ Dong et al. Exp. Mol. Med. 2010 42:327