Article
Phenylpropanoids from Croton velutinus with cytotoxic, trypanocidal and anti-inflammatory activities
Registro en:
ABREU, Lucas Silva et al. Phenylpropanoids from Croton velutinus with cytotoxic, trypanocidal and anti-inflammatory activities. Fitoterapia, 2020.
0367-326X
Autor
Abreu, Lucas Silva
Nascimento, Yuri Mangueira do
Espirito-Santo, Renan Fernandes do
Meira, Cassio Santana
Santos, Ivanilson Pimenta
Brandao, Railda Batista
Souto, Augusto Lopes
Guedes, Maria Lenise Silva
Soares, Milena Botelho Pereira
Villarreal, Cristiane Flora
Veloz, Marcelo Sobral da Eudes da Silva
Tavares, Josean Fechine
Resumen
Coordenação de
Aperfeiçoamento de Pessoal de Nivel Superior - Brasil (CAPES) (Finance
Code 001) and Conselho Nacional de Desenvolvimento Cientifico e
Tecnologico (CNPq) for financial support and fellowships. We are also
thankful for Rede Norte-Nordeste de Fitoterapicos (INCT-RENNOFITO)
collaborations. This current study presents the phytochemical analysis of Croton velutinus, describing phenylpropanoids obtained
from this species. The fractionation of the roots hexane extract led to the isolation of four new phenylpropanoids
derivatives, velutines A—D (1-4) and three known (5-7). Their structures were established based on spectro-
scopic (1D-2D NAM; HRMS and IR) analysis. Cytotoxic, trypanocidal and anti-inflammatory activities of com-
pounds 1-7 were evaluated. Only compounds 2 and 5 showed cytotoxic activity against cancer cell lines
(016F10, HL-60, HCT116, MCF-7 and HepG2), with IC50 values ranging from 6.8 to 18.3 pM and 11.1 to
18.3 pM, respectively. Compounds 2 and 5 also showed trypanocidal activity against bloodstream trypomasti-
gotes with ECse values of 9.0 and 9.58 pM, respectively. Finally, the anti-inflammatory potential of these
compounds was evaluated on cultures of activated macrophages. All compounds exhibited concentration-de-
pendent suppressive activity on the production of nitrite and IL-1[i by macrophages stimulated with LPS and IFN-
y. These results indicate phenylpropanoids esters (2 and 5) from C. velutinus as promising cytotoxic, trypanocidal
and anti-inflammatory candidates that warrants further studies.