Artemisinin derivatives inhibit Toxoplasma gondii in vitro at multiple steps in the lytic cycle.

ABSTRACT:

Objectives

We sought to improve upon the usefulness of artemisinins as anti-Toxoplasma agents by synthesizing new unsaturated, carba derivatives and then testing them for in vitro efficacy against three steps of the lytic cycle of Toxoplasma gondii tachyzoites.

Methods

Novel derivatives of ART were synthesized and then tested for in vitro antiparasitic activity using T. gondii tachyzoites constitutively expressing beta-galactosidase and human fibroblast host cells. Compounds were evaluated for parasite growth inhibition and cytotoxicity, inhibition of replication and inhibition of parasite invasion of host cells.

Results

Five of the seven new derivatives, 3a-c, 3e and 3f, effectively inhibited T. gondii growth (IC50=1.0-4.4 microM); however, only three of these proved

SUBMITTER: D'Angelo JG 

PROVIDER: S-EPMC2639242 | biostudies-literature | 2009 Jan

REPOSITORIES: biostudies-literature