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(Reference retrieved automatically from Web of Science through information on FAPESP grant and its corresponding number as mentioned in the publication by the authors.)

Immunomodulatory and Antileishmanial Activity of Phenylpropanoid Dimers Isolated from Nectandra leucantha

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da Costa-Silva, Thais Alves [1] ; Grecco, Simone S. [2] ; de Sousa, Fernanda S. [3] ; Lago, Joao Henrique G. [3] ; Martins, Euder G. A. [4] ; Terrazas, Cesar A. [5, 6] ; Varikuti, Sanjay [5, 6] ; Owens, Katherine L. [7] ; Beverley, Stephen M. [7] ; Satoskar, Abhay R. [5, 6] ; Tempone, Andre G. [1]
Total Authors: 11
[1] Adolfo Lutz Inst, Ctr Parasitol & Mycol, Sao Paulo - Brazil
[2] Fed Univ ABC, Ctr Nat Sci & Humanities, Sao Paulo - Brazil
[3] Univ Fed Sao Paulo, Inst Environm Chem & Pharmaceut Sci, Sao Paulo - Brazil
[4] Univ Sao Paulo, Dept Bot, Inst Biosci, Sao Paulo - Brazil
[5] Ohio State Univ, Dept Microbiol, Columbus, OH 43210 - USA
[6] Ohio State Univ, Dept Pathol, Columbus, OH 43210 - USA
[7] Washington Univ, Sch Med, Dept Mol Microbiol, St Louis, MO 63110 - USA
Total Affiliations: 7
Document type: Journal article
Source: Journal of Natural Products; v. 78, n. 4, p. 653-657, APR 2015.
Web of Science Citations: 23

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 mu M, 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 mu M, whereas compound 2 demonstrated a CC50 value of 111.2 mu M. 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. (AU)

FAPESP's process: 13/50318-7 - Natural product-based drug design: novel compounds against Leishmania (L.) infantum
Grantee:André Gustavo Tempone Cardoso
Support type: Regular Research Grants
FAPESP's process: 12/18756-1 - Evaluation of novel alternative therapies with synthetic drugs using in vitro and experimental models of Leishmania (L.) infantum chagasi
Grantee:André Gustavo Tempone Cardoso
Support type: Regular Research Grants
FAPESP's process: 13/07275-5 - In vitro study of cellular immune response against synthetic drugs with antileishmanial activities
Grantee:Thaís Alves da Costa Silva
Support type: Scholarships in Brazil - Post-Doctorate