Bioassay-Guided Isolation of Antimalarial Triterpenoid Acids from the Leaves ofMorinda lucida.

Abstract

The EtOH, CH₂Cl₂, and petroleum ether extracts from Morinda lucida. Benth. leaves have been shown to exhibit an in vitro. antiplasmodial activity against a chloroquine-sensitive Plasmodium falciparum. strain with IC₅₀ values 5.7 ± 1.3, 5.2 ± 0.8, and 3.9 ± 0.3 µg/mL, respectively. In vivo., at a daily oral dose of 200 mg/kg body weight, they produced at least 62.5%, 67.5%, and 72.2% reduction of parasitemia in mice infected with Plasmodium berghei berghei., respectively. A bioassay-guided fraction of the most active petroleum ether extract resulted in the isolation of two known triterpenic acids as ursolic acid 1 and oleanolic acid 2. In vitro., 1 and 2 exhibited an antiplasmodial activity with IC₅₀ values of 3.1 ± 1.3 and 15.2 ± 3.4 µg/mL, respectively. In vivo., at a daily dose of 200 mg/kg body weight, they produced 97.7% and 37.4% chemosuppression, respectively. However, all tested samples were inactive in vitro. against chloroquine-resistant Plasmodium falciparum. (K1) at the highest tested concentration of 25 µg/mL.