Author(s): Caldas, Lhaís Araújo ; Yoshinaga, Meire L. ; Ferreira, Marcelo J.P. ; Lago, João H.G. ; de Souza, Adriana B. ; Laurenti, Márcia D. ; Passero, Luiz Felipe. D. [UNESP] ; Sartorelli, Patricia
Date: 2019
Persistent ID: http://hdl.handle.net/11449/188306
Origin: Oasisbr
Subject(s): Antileishmanial activity; Calea pinnatifida; Mitochondrial membrane potential; Sesquiterpene lactones; Ultrastructural changes
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Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)
Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)
Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)
Laboratórios de Investigação Médica - Hospital das Clínicas da Faculdade de Medicina da Universidade de São Paulo
Bioactivity-guided fractionation of antileishmanial active CH 2 Cl 2 phase of MeOH extract from leaves of Calea pinnatifida led to isolation of two sesquiterpene lactones calein C (1) and calealactone C (2), which structures were stablished on the basis of spectroscopic analysis. Compounds 1 and 2 displayed potent activity against Leishmania amazonensis promastigotes with EC 50 of 1.7 and 4.6 µg mL −1 , respectively. Compound 2 presented low cytotoxicity for J774 macrophages and displayed activity against amastigote forms of L. amazonensis similar to miltefosine with CC 50 values of 31.73 and 27.18 µg mL −1 , respectively. Additionally, compounds 1 and 2 caused ultrastructural changes in promastigotes leading to a loss of their classical structural morphology, as evidenced by electron microscopy. Also compound 2 decreased the mitochondria membrane potential. To the best of our knowledge, this is the first occurrence of 1 and 2 in C. pinnatifida. The results obtained highlighted the importance of studying sesquiterpene lactones isolated from Calea pinnatifida in terms of antileishmanial activity, in order to understand the mechanism of action of the isolated compounds in promastigotes forms of L. amazonensis.
Instituto de Ciências Ambientais Químicas e Farmacêuticas Universidade Federal de São Paulo
Departamento de Botânica Instituto de Biociências Universidade de São Paulo
Centro de Ciências Naturais e Humanas Universidade Federal do ABC, 09210-180 Santo André
Laboratório de Patologia de Moléstias Infecciosas (LIM50) Departamento de Patologia Faculdade de Medicina da Universidade de São Paulo
São Paulo State University (UNESP) Institute of Biosciences, São Vicente. Praça Infante Dom Henrique, s/n, 11330-900 São Vicente
São Paulo State University (UNESP) Institute for Advanced Studies of Ocean, São Vicente. Av. João Francisco Bensdorp, 1178, 11350-011 São Vicente
São Paulo State University (UNESP) Institute of Biosciences, São Vicente. Praça Infante Dom Henrique, s/n, 11330-900 São Vicente
São Paulo State University (UNESP) Institute for Advanced Studies of Ocean, São Vicente. Av. João Francisco Bensdorp, 1178, 11350-011 São Vicente
FAPESP: 2016/00468-0
FAPESP: 2016/24985-4
CNPq: 470853/2012-3
