CantharidinÂ was first isolated in 1810 by Pierre Robiquet, a French chemist then living in Paris, fromÂ Lytta vesicatoria. Secreted by many species of blister beetle, most notably by the 'Spanish fly' (Lytta vesicatoria),Â cantharidin inhibits protein phosphatases 1 and 2AÂ (PP1, PP2A). Blister beetle has been used in Asian traditional medicine to treatMolluscum contagiosumÂ 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 ofÂ cantharidin can be used as a topical medicationÂ to remove warts and tattoos and to treat the small papules ofÂ Molluscum contagiosum.Â CantharidinÂ 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 toÂ cantharidin.Â CantharidinÂ 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 ofÂ cantharidinÂ by inducing DNA strand breaks which may be subject to base excision repair and induce apoptosis in a p53- and Bcl2-dependent manner.Â Cantharidin has been used as an anticancer agentÂ 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.
AlthoughÂ 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 modifiedÂ cantharidin analogues are synthesized chemically in order to achieve a comparable anti tumor propertyÂ 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.