Two phenylpropanoid conjugated iridoids, deglucosyl gaertneroside (1) and morindoidin (2), were isolated from the leaves of Morinda morindoides (Rubiaceae) by activity-guided fractionation using an anti-malarial activity assay. The known related iridoids molucidin (3) and prismatomerin (4), two lignans, abscisic acid, two megastigmanes, and two avonol glycosides were also identi ed. The structures of isolated compounds were elucidated using spectroscopic analysis. The isolated compounds were evaluated for anti-malarial activity against the chloroquine/me oquine-sensitive strains of Plasmodium falciparum together with cytotoxicity against adult mouse brain cells. Potent anti-malarial activity of and 4 (IC 50 of 0.96 and 0.80 µM, respectively) was shown, while new iridoids 1 and 2 and pinoresinol (5) displayed moderate activity (IC 50 of 40.9, 20.6, and 24.2 µM, respectively). These results indicate that 1-5 may be promising lead compounds for anti-malarial drugs and that extracts of M. morindoides leaves could be effective remedies for malaria infection.