title: In vitro antileishmanial activity of trans-stilbene and terphenyl compounds.
abstract: Leishmaniasis are globally widespread parasitic diseases which often leads to death if left untreated. Currently available drugs present different drawbacks, so there is an urgent need to develop new, safe and cost-effective drugs against leishmaniasis. In this study we tested a small library of trans-stilbene and terphenyl derivatives against promastigote, amastigotes and intramacrophage amastigote forms of Leishmania infantum. Two compounds of the series, the trans-stilbene 3 and the terphenyl 11, presented the best activity and safety profiles. Terphenyl 11 showed a leshmanicidal activity higher than pentostam and the ability to induce apoptosis selectively in Leishmania infantum while saving macrophages and primary epithelial cells. Our data indicate that terphenyl compounds, as well as stilbenes, are endowed with leishmanicidal activity, showing potential for further studies in the context of leishmanial therapy.
authors.affiliation: National Reference Center for Leishmaniasis (C.Re.Na.L.), Istituto Zooprofilattico Sperimentale della Sicilia, Via Gino Marinuzzi 3, 90129, Palermo, Italy.
authors.forename: Germano
authors.initials: G
authors.lastname: Castelli
authors.affiliation: National Reference Center for Leishmaniasis (C.Re.Na.L.), Istituto Zooprofilattico Sperimentale della Sicilia, Via Gino Marinuzzi 3, 90129, Palermo, Italy.
authors.forename: Federica
authors.initials: F
authors.lastname: Bruno
authors.affiliation: National Reference Center for Leishmaniasis (C.Re.Na.L.), Istituto Zooprofilattico Sperimentale della Sicilia, Via Gino Marinuzzi 3, 90129, Palermo, Italy.
authors.forename: Fabrizio
authors.initials: F
authors.lastname: Vitale
authors.affiliation: Department of Pharmacy and Biotechnology, University of Bologna, Via Belmeloro 6, 40126, Bologna, Italy.
authors.forename: Marinella
authors.initials: M
authors.lastname: Roberti
authors.affiliation: Department of Health Promotion Sciences, Section of Infectious Diseases, University of Palermo, Via del Vespro 129, 90127, Palermo, Italy.
authors.forename: Claudia
authors.initials: C
authors.lastname: Colomba
authors.affiliation: D3 Compunet, Istituto Italiano di Tecnologia, Via Morego 30, I-16163, Genova, Italy.
authors.forename: Elisa
authors.initials: E
authors.lastname: Giacomini
authors.affiliation: Department of Pharmacy and Biotechnology, University of Bologna, Via Belmeloro 6, 40126, Bologna, Italy.
authors.forename: Laura
authors.initials: L
authors.lastname: Guidotti
authors.affiliation: Department of Health Promotion Sciences, Section of Infectious Diseases, University of Palermo, Via del Vespro 129, 90127, Palermo, Italy.
authors.forename: Antonio
authors.initials: A
authors.lastname: Cascio
authors.affiliation: Department of Health Promotion Sciences, Section of Infectious Diseases, University of Palermo, Via del Vespro 129, 90127, Palermo, Italy. Electronic address: mtolomeo@hotmail.com.
authors.forename: Manlio
authors.initials: M
authors.lastname: Tolomeo
mesh_terms: D000818:Animals; D000981:Antiprotozoal Agents / Q000737:chemistry / Q000494:pharmacology*; D017209:Apoptosis; D002453:Cell Cycle / Q000187:drug effects; D002521:Cercopithecus; D004847:Epithelial Cells / Q000187:drug effects; D005434:Flow Cytometry; D006801:Humans; D020128:Inhibitory Concentration 50; D018314:Leishmania infantum / Q000166:cytology / Q000187:drug effects* / Q000254:growth & development; D008264:Macrophages / Q000187:drug effects / Q000469:parasitology; D008856:Microscopy, Fluorescence; D013267:Stilbenes / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D013730:Terphenyl Compounds / Q000737:chemistry / Q000494:pharmacology*; D020298:U937 Cells
chemical_list: D000981:Antiprotozoal Agents; D013267:Stilbenes; D013730:Terphenyl Compounds
keywords: Leishmaniasis; Programmed cell death; Stilbenes; Terphenyls