The aim of this study was to evaluate extracts from two medicinal plants, Acanthospermum hispidum and Ficus thonningii, used in traditional medicine in Congo Brazzaville, for in vitro antiplasmodial activities against two laboratory strains of Plasmodium falciparum: the chloroquine sensitive 3D7 and the chloroquine resistant Dd2. ELISA HRP2 assay was used to evaluate the in vitro inhibitory act...

A rapid decrease in parasitaemia remains the major goal for new antimalarial drugs and thus, in vivo models must provide precise results concerning parasitaemia modulation. Hydroxyethylamine comprise an important group of alkanolamine compounds that exhibit pharmacological properties as proteases inhibitors that has already been proposed as a new class of antimalarial drugs. Herein, it was test...

A series of substituted 3-[(substituted-2-chloroquinolin-3-yl)methylene]-5-(substituted-phenyl)-furan-2(3H)-ones (4a-p) have been synthesized and evaluated for their in vitro antimalarial activity against P. falciparum. The title compounds were synthesized by condensing 3-(substituted-benzoyl)propionic acids (3a-d) with substituted 2-chloroquinoline-3-carbaldehydes (2a-d) following modified Per...

The present study was conducted to investigate the in vitro antimalarial activity of Flacourtia flavescens Willd. (Flacourtiaceae) and Rytigynia canthioides (Benth.) Robyns (Rubiaceae). These two plants are used in Benin folk medicine to treat malaria and fever. Antimalarial activity was assayed on fresh clinical isolates of chloroquine resistant Plasmodium falciparum using the in vitro semi-mi...

The stage-specific antimalarial activities of a panel of antiretroviral protease inhibitors (PIs), including two nonpeptidic PIs (tipranavir and darunavir), were tested in vitro against Plasmodium falciparum. While darunavir demonstrated limited antimalarial activity (effective concentration [EC(50)], >50 microM), tipranavir was active at clinically relevant concentrations (EC(50), 12 to 21 mic...

The aim of this study was to identify new active compounds against Plasmodium falciparum based on our previous research carried out on 3-phenylquinoxaline-2carbonitrile 1,4-di-N-oxide derivatives. Antimalarial activity was evaluated in vitro against Plasmodium falciparum (3D7 and K1 strains) by the incorporation of [H]hypoxanthine. Cytotoxicity was tested in KB cells by Alamar Blue assay. Twelv...

Human immunodeficiency virus type 1 protease inhibitors (HIVPIs) and pepstatin are aspartic protease inhibitors with antimalarial activity. In contrast to pepstatin, HIVPIs were not synergistic with a cysteine protease inhibitor or more active against parasites with the cysteine protease falcipain-2 knocked out than against wild-type parasites. As with pepstatin, HIVPIs were equally active agai...

ETHNOPHARMACOLOGICAL RELEVANCE Malaria continues to kill over a million people each year and in many populations affected by malaria, conventional drugs are often unaffordable or inaccessible. Historically, plants have been a prominent source of antimalarial drugs. Those plants currently used by indigenous people to treat malaria should be documented and investigated as potential sources of new...

C. Ichino, N. Soonthornchareonnon, W. Chuakul, H. Kiyohara, A. Ishiyama, H. Sekiguchi, M. Namatame, K. Otoguro, S. Omura and H. Yamada* The Kitasato Institute for Life Sciences, Kitasato University, Tokyo, Japan Faculty of Pharmacy, Mahidol University, Bangkok 10400, Thailand Oriental Medicine Research Center, The Kitasato Institute, Tokyo, Japan Research Center for Tropical Diseases, Institute...

The application of quinoline-based compounds for the treatment of malaria infections is hampered by drug resistance. Drug resistance has led to the combination of quinolines with other classes of antimalarials resulting in enhanced therapeutic outcomes. However, the combination of antimalarials is limited by drug-drug interactions. In order to overcome the aforementioned factors, several resear...