Navegando por Palavras-chave "Tricin"

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    Antileishmanial Activity and Immunomodulatory Effects of Tricin Isolated from Leaves of Casearia arborea (Salicaceae)
    (Wiley-V C H Verlag Gmbh, 2017) Santos, Augusto L. [UNIFESP]; Yamamoto, Eduardo S.; Passero, Luiz Felipe D.; Laurenti, Marcia D.; Martins, Ligia F.; Lima, Marta L.; Uemi, Miriam [UNIFESP]; Soares, Marisi G.; Lago, Joao Henrique G.; Tempone, Andre G.; Sartorelli, Patricia [UNIFESP]
    Bioactivity-guided fractionation of antileishmanial active extract from leaves of Casearia arborea led to isolation of three metabolites: tricin (1), 1,6 '-di-O-beta-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 mu m. 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.
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    Busca de substâncias antitumorais e antiparasitárias de Casearia arbórea RICH (Salicaceae)
    (Universidade Federal de São Paulo, 2015-09-10) Santos, Augusto Leonardo dos [UNIFESP]; Sartorelli, Patricia [UNIFESP]; Universidade Federal de São Paulo (UNIFESP)
    This presente work aimed the isolation of chemical constituintes accumulated on the leaves of Casearia arborea (Salicaceae) and evaluation of the cytotoxic activity, anti-proliferative ando anti-migratory against B16F10 cell line, evaluation of antiparasitic activity against Leishmania infantum and Trypanosoma cruzi. Melanoma skin cancer is amenable to be treated in the incial stages, but it?s the kind that causes most cases of death, growing each year, as well Visceral Leishmaniasis and Chagas Disease, parasitic diseases that occurs in less developed contries, without perspectives for new less aggressive therapies. So, Casearia arborea leaves was submitted to metanolic extraction, where the dichloromethane phase partition showed the higher activity in both cytotoxic and antileishmania assays, subjected to biomonitored fraction. After several cromatografic stages, aided by the biomonitoring process, was possible the purification of substances with antiparasitic and cytotoxic activity, analysed by nuclear magnetic ressonance spectroscopy of ¹H and ¹³C, DEPT, two-dimensional techiniques (HMBC, HMQC, COSY) and mass spectroscopy. Therefore, the flavone tricina was identified, presenting IC50 of 18,75 ?g/mL against amastigotes of L. infantum, CC50 > 300 ?g/mL e SI of 16, displaying promising results when compared to miltefosine (positive control), showing higher cytotoxic activity, less toxic to NCTC cells and more selective. Additionally was determined an antiproliferative potencial and antimigratory activity for the tricin against B16F10 cell line, which are directly to cancer metastasis stage, making the tricin a promising antiproliferative, antimetastatic. A divanilloylglucopiranoside was identified and determined as the 1?,6?-di-O-vanilloyl-?-D-glucopiranoside, showing antiparasitc activity against T. cruzi trypomastigotes with IC50 of 129,5 ?g/mL, CC50 > 200 ?g/mL e SI 1,5, that were more promising that benznidazol (positive control), proven to be so effective as the control, less toxic againg NCTC cells and more selective to the parasites.