Cantharidin was first isolated in 1810 by Pierre Robiquet, a French chemist then living in Paris, from Lytta vesicatoria. Secreted by many species of blister beetle, most notably by the 'Spanish fly' (Lytta vesicatoria), cantharidin inhibits protein phosphatases 1 and 2A (PP1, PP2A). Blister beetle has been used in Asian traditional medicine to treatMolluscum contagiosum virus (MCV) infections and associated warts, and is now also used for cancer treatment. It is an odorless and colorless solid at room temperature. Diluted solutions of cantharidin can be used as a topical medication to remove warts and tattoos and to treat the small papules of Molluscum contagiosum. Cantharidin has also shown potent anticancer activities on many types of human cancer cells.
combination of both genomic and postgenomic techniques was used in our studies to identify candidate genes affecting sensitivity or resistance to cantharidin. Cantharidin was not found to be related to multidrug resistance phenotype, suggesting its potential usefulness for the treatment of refractory tumors. Oxidative stress response genes diminish the activity of cantharidin by inducing DNA strand breaks which may be subject to base excision repair and induce apoptosis in a p53- and Bcl2-dependent manner. Cantharidin has been used as an anticancer agent by the Chinese for the treatment of hepatoma and oesophageal carcinoma for a long time. Combined methods of pharmaceutical biology and molecular biology can help elucidate modes of action of these natural products.
Although cantharidin is a natural toxin that possesses potent anti-tumor properties, its clinical application is limited due to severe side-effects and highly toxic nature. Therefore, some modified cantharidin analogues are synthesized chemically in order to achieve a comparable anti tumor property to the mother compound but simultaneously produce a less toxic effect on non-cancer cells.
Sources: Rauh R, Kahl S, Boechzelt H, Bauer R, Kaina B, Efferth T.