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Antileishmanial Activity and Immunomodulatory Effects of Tricin Isolated from Leaves of Casearia arborea (Salicaceae) |
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| Authors: | Augusto L Santos Eduardo S Yamamoto Luiz Felipe D Passero Márcia D Laurenti Ligia F Martins Marta L Lima Miriam Uemi Marisi G Soares João Henrique G Lago Andre G Tempone Patricia Sartorelli |
| Institution: | 1. Institute of Environmental, Chemical and Pharmaceutical Sciences, Federal University of S?o Paulo, Rua Prof. Artur Riedel, n° 275 ‐ Jd. Eldorado, CEP 09972‐270, Diadema, S?o Paulo, Brazil;2. Laboratory of Pathology of Infectious Diseases, Medical School, University of S?o Paulo, Av. Dr. Arnaldo, 455 ‐ Cerqueira César, CEP 01246‐903, S?o Paulo, SP, Brazil;3. Institute of Biosciences, S?o Paulo State University (UNESP), Pra?a Infante Dom Henrique, s/n ‐ Parque Bitaru, CEP 11330‐900, S?o Vicente, SP, Brazil;4. Center of Parasitology and Mycology, Adolfo Lutz Institute, Av. Dr. Arnaldo, 355 ‐ Cerqueira César, CEP 01246‐000, S?o Paulo, SP, Brazil;5. S?o Paulo Tropical Medicine Institute, University of S?o Paulo, Avenida Dr. Enéas Carvalho de Aguiar, 470, CEP 05403‐000, S?o Paulo, SP, Brazil;6. Chemistry Institute, Federal University of Alfenas, Rua Gabriel Monteiro da Silva, 700 Centro, CEP 37130‐001, Alfenas, MG, Brazil;7. Center of Natural Sciences and Humanities, Federal University of ABC, Avenida dos Estados, 5001, Bairro Santa Terezinha, CEP 09210‐580, Santo Andre, SP, Brazil |
| Abstract: | Bioactivity‐guided fractionation of antileishmanial active extract from leaves of Casearia arborea led to isolation of three metabolites: tricin ( 1 ), 1′,6′‐di‐O‐β‐d ‐vanilloyl glucopyranoside ( 2 ) and vanillic acid ( 3 ). Compound 1 demonstrated the highest activity against the intracellular amastigotes of Leishmania infantum, with an IC50 value of 56 μm . Tricin ( 1 ) demonstrated selectivity in mammalian cells (SI > 7) and elicited immunomodulatory effect on host cells. The present work suggests that tricin modulated the respiratory burst of macrophages to a leishmanicidal state, contributing to the parasite elimination. Therefore, the natural compound tricin could be further explored in drug design studies for leishmaniasis treatment. |
| Keywords: | Casearia arborea Salicaceae Tricin Divanilloyl glucopyranoside Vanillic acid Leishmania Immunomodulation |