TY  - JOUR
AU  - Ramalhete, C.
AU  - Da Cruz, F.P.
AU  - Mulhovo, S.
AU  - Sousa, I.J.
AU  - Fernandes, M.X.
AU  - Prudêncio, M.
AU  - Ferreira, M.-J.U.
T1  - Dual-stage triterpenoids from an African medicinal plant targeting the malaria parasite
LA  - eng
PY  - 2014
SP  - 3887
EP  - 3890
T2  - Bioorganic and Medicinal Chemistry
SN  - 1464-3391
VL  - 22
IS  - 15
PB  - Elsevier Ltd
AB  - Sixteen triterpenoids (1-16), previously isolated from the aerial parts of the African medicinal plant Momordica balsamina or obtained by derivatization, were evaluated for their activity against liver stages of Plasmodium berghei, measuring the luminescence intensity in Huh-7 cells infected with a firefly luciferase-expressing P. berghei line, PbGFP-Luccon. Toxicity of compounds (1-16) was assessed on the same cell line through the fluorescence measurement of cell confluency. The highest activity was displayed by a derivative bearing two acetyl residues, karavoate B (7), which led to a dose-dependent decrease in the P. berghei infection rate, exhibiting a very significant activity at the lowest concentration employed (1 μM) and no toxicity towards the Huh-7 cells. It is noteworthy that, in previous studies, this compound was found to be a strong inhibitor of blood-stages of Plasmodium falciparum, thus displaying a dual-stage antimalarial activity. © 2014 Elsevier Ltd. All rights reserved.
DO  - 10.1016/J.BMC.2014.06.019
UR  - https://portalciencia.ull.es/documentos/5e3c394629995246bbf5f260
DP  - Dialnet - Portal de la Investigación
ER  -