Triterpenoids as inhibitors of erythrocytic and liver stages of Plasmodium infections

In vivo evaluation of isolated triterpenes and semi-synthetic derivatives as antimalarial agents

“…While isolated compounds from Momordica balsamina were active, semi-synthetic derivative karavoate B (3) exhibited the strongest effects including a concentrationdependent decrease in the in vitro P. berghei infection rate [23,25]. Even at the lowest concentration tested (1 µM) this diester exhibited significant liver stage antiplasmodial activity [25].…”

“…Fractionation of the methanol extract led to the isolation of several triterpenoids with the cucurbitane skeleton, namely balsaminoside B (1) and karavilagenin C (2) [20,23]. …”

“…Briefly, the residue of the methanol extract (45 g), after removing the waxy material, was chromatographed over silica gel to obtain six crude fractions (Fr 1−6). Karavilagenin C (2) and balsaminoside B (1) were obtained from the crude fractions Fr 2 (n-hexane/ethyl acetate, 11:9 to 9:11), and Fr 6 (ethyl acetate/methanol, 93:7 to 9:1), respectively [20,23].…”

“…Using criteria for in vitro antimalarial activity adopted by Batista et al [24], most of these compounds and semi-synthetic derivatives exhibited excellent/good inhibitory effects (IC50 ≤ 1 µM/IC50 = 1 -20 µM) against blood schizonts of chloroquine-sensitive and resistant strains of P. falciparum [21][22][23]. Some of these terpenoids exhibited promising in vitro activity against liver stages of P. berghei Vincke and Lips infections, emphasizing their dual-stage antimalarial activity [23,25].…”

“…balsamina led to the isolation of several cucurbitane triterpenoids [19][20][21][22][23]. Using criteria for in vitro antimalarial activity adopted by Batista et al [24], most of these compounds and semi-synthetic derivatives exhibited excellent/good inhibitory effects (IC50 ≤ 1 µM/IC50 = 1 -20 µM) against blood schizonts of chloroquine-sensitive and resistant strains of P. falciparum [21][22][23].…”