title: In vitro effects of artemisinin ether, cycloguanil hydrochloride (alone and in combination with sulfadiazine), quinine sulfate, mefloquine, primaquine phosphate, trifluoperazine hydrochloride, and verapamil on Toxoplasma gondii.
abstract: The in vitro effect of the following antimicrobial agents on Toxoplasma gondii tachyzoites were studied: artemisinin ether (arteether), cycloguanil hydrochloride (cycloguanil), mefloquine, primaquine phosphate, and quinine sulfate, as well as the calcium channel blocker verapamil and the calmodulin inhibitor trifluoperazine hydrochloride. Arteether at > or = 0.5 micrograms/ml and cycloguanil at > or = 1.0 micrograms/ml inhibited T. gondii in vitro. Cycloguanil (2.5 micrograms/ml) combined with a noninhibitory concentration of sulfadiazine (25 micrograms/ml) inhibited T. gondii more than cycloguanil alone. Neither primaquine phosphate, mefloquine, nor quinine sulfate had an inhibitory effect on intracellular T. gondii. Verapamil and trifluoperazine hydrochloride were not inhibitor at lower physiologic concentrations, but higher physiologic concentrations were toxic to cell cultures in vitro and therefore our assay could not be used to assess their effects.
authors.affiliation: Department of Medicine, Michael Reese Hospital, Chicago, Illinois 60616.
authors.forename: E
authors.initials: E
authors.lastname: Holfels
authors.forename: J
authors.initials: J
authors.lastname: McAuley
authors.forename: D
authors.initials: D
authors.lastname: Mack
authors.forename: W K
authors.initials: WK
authors.lastname: Milhous
authors.forename: R
authors.initials: R
authors.lastname: McLeod
mesh_terms: D000818:Animals; D037621:Artemisinins; D005260:Female; D015767:Mefloquine / Q000494:pharmacology; D051379:Mice; D011319:Primaquine / Q000494:pharmacology; D002727:Proguanil; D011803:Quinine / Q000494:pharmacology; D012717:Sesquiterpenes / Q000494:pharmacology; D013411:Sulfadiazine / Q000494:pharmacology; D014122:Toxoplasma / Q000187:drug effects* / Q000378:metabolism; D014227:Triazines / Q000494:pharmacology; D014268:Trifluoperazine / Q000494:pharmacology; D014498:Uracil / Q000378:metabolism; D014700:Verapamil / Q000494:pharmacology
chemical_list: D037621:Artemisinins; D012717:Sesquiterpenes; D014227:Triazines; D013411:Sulfadiazine; D014268:Trifluoperazine; C026009:cycloguanil; D014498:Uracil; C031327:artemisinin; D011803:Quinine; D014700:Verapamil; D011319:Primaquine; D002727:Proguanil; D015767:Mefloquine