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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.)

Antitrypanosomal activity and evaluation of the mechanism of action of diterpenes from aerial parts of Baccharis retusa (Asteraceae)

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Ueno, Anderson K. [1] ; Barcellos, Aline F. [2] ; Costa-Silva, Thais A. [2] ; Mesquita, Juliana T. [3] ; Ferreira, Daiane D. [3] ; Tempone, Andre G. [3] ; Romoff, Paulete [4] ; Antar, Guilherme M. [5] ; Lago, Joao Henrique G. [2]
Total Authors: 9
[1] Univ Fed Sao Paulo, Inst Environm Chem & Pharmaceut Sci, BR-09972270 Sao Paulo - Brazil
[2] Fed Univ ABC, Ctr Nat Sci & Humanities, BR-09210580 Sao Paulo - Brazil
[3] Adolfo Lutz Inst, Ctr Parasitol & Mycol, BR-01246000 Sao Paulo - Brazil
[4] Univ Prebiteriana Mackenzie, Sch Engn, BR-01302907 Sao Paulo - Brazil
[5] Univ Sao Paulo, Inst Biosci, Dept Bot, BR-05508090 Sao Paulo - Brazil
Total Affiliations: 5
Document type: Journal article
Source: Fitoterapia; v. 125, p. 55-58, MAR 2018.
Web of Science Citations: 7

Baccharis retusa, a medicinal Brazilian plant from Asteraceae, has been used in Brazilian folk medicine to treatment of several illnesses, including parasitic diseases. Bioactivity-guided fractionation of the n-hexane extract from the aerial parts of B. retusa resulted in the isolation and characterization of three active related diterpenes: ent-15 beta-senecioyl-oxy-kaur-16-en-19-oic acid (1), ent-kaur-16-en-19-oic (2) and ent-16-oxo-17-nor-kauran-19-oic (3) acids. The structures of isolated compounds were defined by spectroscopic analysis, including NMR and HRESIMS. Antitrypanosomal activity of 1-3 was performed against cell-derived trypomastigotes using the colorimetric resazurin assay. The obtained results demonstrated that isolated compounds displayed a reduced toxicity against NCTC cells and were effective against the trypomastigote forms of T. cruzi with IC50 values of 3.8 mu M (1), 75.3 mu M (2) and 44.2 mu M (3). Additionally, compound 3 displayed activity against amastigote forms of T. cruzi with IC50 of 83.2 mu M. Compound 1 displayed the highest selectivity index (SI) when considered the trypomastigote forms, and its effect in the plasma membrane of parasite was evaluated using the fluorescent probe SYTOX Green. A considerable permeabilization (57%) in the membrane of the parasite was observed when compared to the untreated trypomastigotes. These data demonstrate, for the first time, the antitrypanosomal activity and mechanism of action of 1 and related compounds 2 and 3, obtained from aerial parts of B. retusa. (AU)

FAPESP's process: 15/23403-9 - Rational Pre-Clinical Study of New Drug Candidates Against Neglected Protozoan Diseases Using Pharmacokinetic Approaches
Grantee:André Gustavo Tempone Cardoso
Support type: Regular Research Grants
FAPESP's process: 15/11936-2 - Use of chemodiversity of plant species in remaining areas of Atlantic Forest from São Paulo State in the selection of biologically active prototypes
Grantee:João Henrique Ghilardi Lago
Support type: Regular Research Grants
FAPESP's process: 14/08961-2 - Chemical identification and evaluation of antitumoral potential of metabolites of Guarea macrophylla ssp. tuberculata (Meliaceae)
Grantee:Geanne Alexsandra Alves Conserva
Support type: Scholarships in Brazil - Master