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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.)

Antileishmanial activity and ultrastructural changes of sesquiterpene lactones isolated from Calea pinnatifida (Asteraceae)

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Caldas, Lhais Araujo [1] ; Yoshinaga, Meire L. [1] ; Ferreira, Marcelo J. P. [2] ; Lago, Joao H. G. [3] ; de Souza, Adriana B. [4] ; Laurenti, Marcia D. [4] ; Passero, Luiz Felipe D. [5, 6] ; Sartorelli, Patricia [1]
Total Authors: 8
[1] Univ Fed Sao Paulo, Inst Ciencias Ambientais Quim & Farmaceut, BR-09972270 Diadema, SP - Brazil
[2] Univ Sao Paulo, Inst Biociencias, Dept Bot, BR-05508090 Sao Paulo, SP - Brazil
[3] Univ Fed ABC, Ctr Ciencias Nat & Humans, BR-09210180 Santo Andre, SP - Brazil
[4] Univ Sao Paulo, Dept Patol, Lab Patol Molestias Infecciosas LIM50, Fac Med, Sao Paulo, SP - Brazil
[5] Sao Paulo State Univ UNESP, Inst Biosci, Praca Infante Dom Henrique S-N, BR-11330900 Sao Vicente, SP - Brazil
[6] Sao Paulo State Univ UNESP, Inst Adv Studies Ocean, Sao Vicente Av Joao Francisco Bensdorp 1178, BR-11350011 Sao Vicente, SP - Brazil
Total Affiliations: 6
Document type: Journal article
Source: BIOORGANIC CHEMISTRY; v. 83, p. 348-353, MAR 2019.
Web of Science Citations: 1

Bioactivity-guided fractionation of antileishmanial active CH2Cl2 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 EC50 of 1.7 and 4.6 mu g mL(-1), respectively. Compound 2 presented low cytotoxicity for J774 macrophages and displayed activity against amastigote forms of L. amazonensis similar to miltefosine with CC50 values of 31.73 and 27.18 mu g 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. (AU)

FAPESP's process: 16/00468-0 - Use of drug repurposing and natural product bioprospection to characterize compounds with in vitro and in vivo leishmanicidal action
Grantee:Luiz Felipe Domingues Passero
Support type: Regular Research Grants
FAPESP's process: 16/24985-4 - Study the chemical composition of fungi and plants of the Atlantic Forest aimed at antitumor, antiparasitic and antimicrobial potential
Grantee:Patricia Sartorelli
Support type: Regular Research Grants