| Literature DB >> 25835647 |
Thais Alves da Costa-Silva1, Simone S Grecco2, Fernanda S de Sousa3, João Henrique G Lago3, Euder G A Martins4, César A Terrazas5, Sanjay Varikuti5, Katherine L Owens6, Stephen M Beverley6, Abhay R Satoskar5, Andre G Tempone1.
Abstract
Three phenylpropanoid dimers (1-3) including two new metabolites were isolated from the extract of the twigs of Nectandra leucantha using antileishmanial bioassay-guided fractionation. The in vitro antiparasitic activity of the isolated compounds against Leishmania donovani parasites and mammalian cytotoxicity and immunomodulatory effects were evaluated. Compounds 1-3 were effective against the intracellular amastigotes within macrophages, with IC50 values of 26.7, 17.8, and 101.9 μM, respectively. The mammalian cytotoxicity, given by the 50% cytotoxic concentration (CC50), was evaluated against peritoneal macrophages. Compounds 1 and 3 were not toxic up to 290 μM, whereas compound 2 demonstrated a CC50 value of 111.2 μM. Compounds 1-3 also suppressed production of disease exacerbatory cytokines IL-6 and IL-10 but had minimal effect on nitric oxide production in L. donovani-infected macrophages, indicating that antileishmanial activity of these compounds is mediated via an NO-independent mechanism. Therefore, these new natural products could represent promising scaffolds for drug design studies for leishmaniasis.Entities:
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Year: 2015 PMID： 25835647 PMCID： PMC4730870 DOI： 10.1021/np500809a
Source DB: PubMed Journal: J Nat Prod ISSN： 0163-3864 Impact factor: 4.050