title: Transmission blocking effects of neem (Azadirachta indica) seed kernel limonoids on Plasmodium berghei early sporogonic development.
abstract: Azadirachta indica, known as neem tree and traditionally called "nature's drug store" makes part of several African pharmacopeias and is widely used for the preparation of homemade remedies and commercial preparations against various illnesses, including malaria. Employing a bio-guided fractionation approach, molecules obtained from A. indica ripe and green fruit kernels were tested for activity against early sporogonic stages of Plasmodium berghei, the parasite stages that develop in the mosquito mid gut after an infective blood meal. The limonoid deacetylnimbin (3) was identified as one the most active compounds of the extract, with a considerably higher activity compared to that of the close analogue nimbin (2). Pure deacetylnimbin (3) appeared to interfere with transmissible Plasmodium stages at a similar potency as azadirachtin A. Considering its higher thermal and chemical stability, deacetylnimbin could represent a suitable alternative to azadirachtin A for the preparation of transmission blocking antimalarials.
authors.affiliation: School of Pharmacy, University of Camerino, Piazza dei Costanti, 62032 Camerino, MC, Italy.
authors.forename: Sofia
authors.initials: S
authors.lastname: Tapanelli
authors.affiliation: Department of Pharmacy, University of Naples Federico II, Via Montesano 49, 80131 Naples, Italy.
authors.forename: Giuseppina
authors.initials: G
authors.lastname: Chianese
authors.affiliation: Discovery Biology, Eskitis Institute for Drug Discovery, Griffith University, Nathan, 4111, Queensland, Australia.
authors.forename: Leonardo
authors.initials: L
authors.lastname: Lucantoni
authors.affiliation: Institut de Recherche en Sciences de la Santé, 01BP545 Bobo Dioulasso, Burkina Faso.
authors.forename: Rakiswendé Serge
authors.initials: RS
authors.lastname: Yerbanga
authors.affiliation: School of Pharmacy, University of Camerino, Piazza dei Costanti, 62032 Camerino, MC, Italy. Electronic address: annette.habluetzel@unicam.it.
authors.forename: Annette
authors.initials: A
authors.lastname: Habluetzel
authors.affiliation: Department of Pharmacy, University of Naples Federico II, Via Montesano 49, 80131 Naples, Italy. Electronic address: scatagli@unina.it.
authors.forename: Orazio
authors.initials: O
authors.lastname: Taglialatela-Scafati
mesh_terms: D000818:Animals; D000962:Antimalarials / Q000302:isolation & purification / Q000494:pharmacology*; D031601:Azadirachta / Q000737:chemistry*; D005260:Female; D036701:Limonins / Q000302:isolation & purification / Q000494:pharmacology*; D008807:Mice, Inbred BALB C; D015394:Molecular Structure; D010962:Plasmodium berghei / Q000187:drug effects*; D012639:Seeds / Q000737:chemistry*
chemical_list: D000962:Antimalarials; D036701:Limonins; C000613549:deacetylnimbin; C008621:nimbin; C010329:azadirachtin
keywords: Azadirachta indica; Deacetylnimbin; Malaria; Neem; Transmission blocking