title: In vitro antileishmanial and antimalarial activities of tetrahydrofuran lignans isolated from Nectandra megapotamica (Lauraceae).
abstract: Seven tetrahydrofuran lignans, isolated from Nectandra megapotamica (Lauraceae), were evaluated for their in vitro antileishmanial and antimalarial activities. Among the evaluated compounds, machilin-G (1a) and veraguensin (2a) showed the highest antileishmanial activities, displaying for both compounds an IC(50) value of 18 microg/mL and an IC(90) value of 36 microg/mL, while galgravin (1b), nectandrin-A (1c), nectandrin-B (1d), calopeptin (2b) and ganshisandrine (3) were inactive against Leishmania donovani. In the antimalarial assay against Plasmodium falciparum, it was observed that calopeptin (2b) displayed moderate activity, with IC(50) values of 3800 ng/mL (D6 clone) and 3900 ng/mL (W2 clone), while the lignans 1a-1d, 2a and 3 were inactive. In order to compare the effect on the parasites with toxicity to mammalian cells, the cytotoxic activity of the isolated compounds were evaluated against the Vero cells, showing that all evaluated tetrahydrofuran lignans exhibited no cytotoxicity at the maximum dose tested.
authors.affiliation: Laboratório de Produtos Naturais, Núcleo de Pesquisa em Ciências Exatas e Tecnológicas, Universidade de Franca, Franca, SP 14404-600, Brazil. ademar@unifran.br
authors.forename: Ademar A
authors.initials: AA
authors.lastname: da Silva Filho
authors.forename: Eveline S
authors.initials: ES
authors.lastname: Costa
authors.forename: Wilson R
authors.initials: WR
authors.lastname: Cunha
authors.forename: Márcio L A
authors.initials: ML
authors.lastname: e Silva
authors.forename: N P Dhammika
authors.initials: NP
authors.lastname: Nanayakkara
authors.forename: Jairo K
authors.initials: JK
authors.lastname: Bastos
mesh_terms: D000818:Animals; D000962:Antimalarials / Q000737:chemistry / Q000494:pharmacology*; D000981:Antiprotozoal Agents / Q000737:chemistry / Q000494:pharmacology*; D002522:Chlorocebus aethiops; D005663:Furans / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology; D019770:Lauraceae / Q000737:chemistry*; D007893:Leishmania donovani / Q000187:drug effects*; D017705:Lignans / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology; D009682:Magnetic Resonance Spectroscopy; D010963:Plasmodium falciparum / Q000187:drug effects; D014709:Vero Cells
chemical_list: D000962:Antimalarials; D000981:Antiprotozoal Agents; D005663:Furans; D017705:Lignans