Uses
Lucanthone is an endonuclease inhibitor of Apurinic endonuclease-1 (APE-1).
Definition
ChEBI: Lucanthone is a thioxanthen-9-one compound having a methyl substituent at the 1-position and a 2-[(diethylamino)ethyl]amino substituent at the 4-position. Formerly used for the treatment of schistosomiasis. It is a prodrug, being metabolised to hycanthone. It has a role as a schistosomicide drug, an antineoplastic agent, a photosensitizing agent, an EC 5.99.1.2 (DNA topoisomerase) inhibitor, an EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor, a prodrug, an adjuvant and a mutagen.
Safety Profile
Poison by intravenous
route. Human mutation data reported.
When heated to decomposition it emits very
toxic fumes of NOx and SOx.
References
[1] Chowdhury SM, et al. Graphene nanoribbons as a drug delivery agent for lucanthone mediated therapy of glioblastoma multiforme. Nanomedicine. 2015 Jan;11(1):109-18. DOI:
10.1016/j.nano.2014.08.001[2] Carew JS, et al. Lucanthone is a novel inhibitor of autophagy that induces cathepsin D-mediated apoptosis. J Biol Chem. 2011 Feb 25;286(8):6602-13. DOI:
10.1074/jbc.M110.151324
