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One monoterpene indole alkaloid, atheruramine ( 1 ) bearing an ether bridge linking, one hydrobenzoin derivative, tricalydioloside ( 2 ) and two ursane-type triterpenes, atherurosides (A and B) ( 3  and  4 ) were isolated from the leaves of  Tricalysia atherura , together with eight known compounds. The structures of these new compounds were elucidated on the basis of the results of spectroscopic analysis, and the relative configurations of compounds  1–3  were established by NOE difference. Four of the metabolites were screened  in vitro  against both chloroquine (CQ)-sensitive (3D7) and -resistant (Dd2) strains of  Plasmodium falciparum ; they were found to exhibit moderate activity against chloroquine-resistant (Dd2) (IC 50  64.99–92.29 μg/mL). Meanwhile, crude extract possesses high antiplasmodial activity against both 3D7 and Dd2 strains of  P. falciparum  (IC 50  4.39–7.54 μg/mL) and high selectivity indices values (SI &gt; 10) and was found to be safe.

Secondary metabolites of the leaves of Tricalysia atherura N. Hallé (Rubiaceae) and their potential antiplasmodial activity