Cantharidin: natural bioactive molecule with a long history

Abstract

sociální fakulta, katedra radiologie, toxikologie a ochrany obyvatelstva 2 Fakultní nemocnice v Hradci Králové, Centrum biomedicínského výzkumu 3 Univerzita obrany v Hradci Králové, Fakulta vojenského zdravotnictví, Centrum pokročilých studií summary Cantharidin, a vesicant produced by insects in the order Coleoptera, has a long history both in folk and traditional medicine. Cantharidin, terpenoid of 7-oxabicyclo-[2.2.1]-heptane type, is a poisonous chemical compound secreted by many species of blister beetle (Meloidae), and most notably by the Spanish fly, Lytta vesicatoria. In dermatology, diluted solutions of cantharidin can be used as a topical medication for the treatment of benign epithelial growths: to remove warts and to treat the small papules of Molluscum contagiosum. The potential of cantharidin for adverse effects has led to its inclusion in a list of hazardous drugs. The extreme risk in acute toxicity of cantharidin makes any use as an aphrodisiac. It is highly dangerous because it can easily cause death. As a result, it is illegal to use cantharidin for this purpose in many countries. Nevertheless, according to new clinical results, cantharidin is a safe and valuable medication and should be readded to the dermatologic therapeutic armamentarium. In addition to topical medical applications, cantharidin, as well as its some analogues (mainly norcantharidin), show potential anticancer activities. Laboratory studies with cultured tumor cell lines suggest that this activity may relate to inhibition of protein phosphatase 2A, a specific serine/threonine phosphatase that can dephosphorylate multiple kinases. It is generally considered to be a cancer suppressor and its inhibition can induce phosphorylation and activation of substrate kinases that mainly accelerate growth. Cantharidin has shown potent anticancer activities on human cancer cells. It induces cell cycle arrest and apoptosis in many types of cancer cells.