title: Different susceptibilities of Leishmania spp. promastigotes to the Annona muricata acetogenins annonacinone and corossolone, and the Platymiscium floribundum coumarin scoparone.
abstract: Leishmaniasis is a zoonotic disease that can manifest itself in visceral and cutaneous form. The aim of this study was to search for new leishmanicidal compounds. Preliminarily, Artemia salina assay was applied to compounds from two plants found in Northeastern Brazil, Platymiscium floribundum and Annona muricata. Then these compounds were tested against three Leishmania species (Leishmania donovani, Leishmania mexicana and Leishmania major). A screening assay using luciferase-expressing promastigote form were used to measure the viability of promastigote One coumarin, scoparone, isolated from P. floribundum and two acetogenins, annonacinone and corossolone isolated from A. muricata showed leishmanicidal activity in all species tested. Nevertheless, Leishmania species indicated different susceptibilities in relation to the tested compounds: L. mexicana was more sensitive to scoparone followed by L. major and L. donovani. The three species presented similar inhibition to corossolone and annonacinone. Acetogenin annonacinone (EC(50)=6.72-8.00 μg/mL) indicated high leishmanicidal activity; corossolone (EC(50)=16.14-18.73 μg/mL) and scoparone (EC(50)=9.11-27.51 μg/mL) moderate activity. A. saline larvae were less sensitive to the coumarin scoparone and acetogenin corossolone was the most toxic. In conclusion, the leishmanicidal activity demonstrated by the coumarin and acetogenins indicate these compounds for further studies aiming the development of new leishmanicidal agents.
authors.affiliation: Programa de Pós-Graduação em Ciências Veterinárias, Universidade Estadual do Ceará, Avenida Paranjana, 1700, Campus do Itaperi, 60740-000 Fortaleza, Ceará, Brazil.
authors.forename: Nadja Soares
authors.initials: NS
authors.lastname: Vila-Nova
authors.forename: Selene Maia
authors.initials: SM
authors.lastname: de Morais
authors.forename: Maria José Cajazeiras
authors.initials: MJ
authors.lastname: Falcão
authors.forename: Terezinha Thaize Negreiros
authors.initials: TT
authors.lastname: Alcantara
authors.forename: Pablito Augusto Travassos
authors.initials: PA
authors.lastname: Ferreira
authors.forename: Eveline Solon Barreira
authors.initials: ES
authors.lastname: Cavalcanti
authors.forename: Icaro Gusmão Pinto
authors.initials: IG
authors.lastname: Vieira
authors.forename: Cláudio Cabral
authors.initials: CC
authors.lastname: Campello
authors.forename: Mary
authors.initials: M
authors.lastname: Wilson
mesh_terms: D015107:4-Butyrolactone / Q000031:analogs & derivatives / Q000302:isolation & purification / Q000494:pharmacology / Q000633:toxicity; D000818:Animals; D031041:Annona / Q000737:chemistry*; D000981:Antiprotozoal Agents / Q000494:pharmacology* / Q000633:toxicity; D001156:Artemia / Q000187:drug effects; D001681:Biological Assay; D001938:Brazil; D002855:Chromatography, Thin Layer; D003374:Coumarins / Q000302:isolation & purification / Q000494:pharmacology / Q000633:toxicity; D004305:Dose-Response Relationship, Drug; D007887:Fabaceae / Q000737:chemistry*; D005663:Furans / Q000302:isolation & purification / Q000494:pharmacology / Q000633:toxicity; D007891:Leishmania / Q000187:drug effects*; D010936:Plant Extracts / Q000737:chemistry / Q000494:pharmacology* / Q000633:toxicity
chemical_list: D000981:Antiprotozoal Agents; D003374:Coumarins; D005663:Furans; D010936:Plant Extracts; C570175:annonacinone; C455172:corossolone; C018145:scoparone; D015107:4-Butyrolactone