Preclinical studies with epiisopiloturine and epiisopilosine and their effect against other helminths

Abstract

Epiisopiloturine is an imidazole alkaloid extracted from Pilocarpus microphyllus Stapf ex Wardleworth, a Brazilian native plant, whose in vivo activity against Schistosoma mansoni led to parasite burden, to reduction in hepatosplenomegaly, the egg burden in faeces, and fell granuloma diameter. Epiisopilosine, another secondary metabolite from jaborandi, was tested in vitro (just accepted to publish) and at concentration of 3.125 ¼g/mL caused death of all adult worms after 96 hours incubation, besides prevent the mating and oviposition, reducing motor activity and altering the tegument of these worms. Previous biological assays showed the low toxicity of these alkaloids physicochemical and pharmacokinetic parameters point the anthelmintic activity. Once our main goal is get the knowledge of structure-activity relationship, preclinical studies will be conducted for the first time to check for structural changes generated by host metabolism. To verify the biological activity, they will be tested against a range of helminthiasis. (AU)