| Full text | |
| Author(s): |
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
|
| Affiliation: | [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 |
| Abstract | |
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 Opportunities: | 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 Opportunities: | 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 Opportunities: | Scholarships in Brazil - Master |