Effect of the anti-microtubule compound tubulozole on Leishmania protozoan parasites in vitro.
For the cis and trans stereoisomers of the synthetic anti-microtubule compound tubulozole, at micromolar concentrations, tubulozole-C is cytotoxic to mammalian cells whereas tubulozole-T is not. The effect of tubulozoles on the parasitic protozoan Leishmania was tested. For the promastigote stage of L. mexicana amazonensis, both isomers inhibited parasite growth. For the amastigote stage of L. mexicana amazonensis and L. major, within murine J774 macrophage line as host cells in vitro, tubulozole-T reduced the infective index. Despite the observation of macrophage cytotoxicity of tubulozole-T, this compound may be a potentially useful and novel anti-leishmanial drug.
Fong
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Department of Biological Sciences, Rutgers, State University of New Jersey, Piscataway 08855-1059.
D000818:Animals; D000981:Antiprotozoal Agents / Q000737:chemistry / Q000494:pharmacology*; D004148:Dioxolanes / Q000737:chemistry / Q000494:pharmacology*; D007894:Leishmania mexicana / Q000187:drug effects* / Q000254:growth & development / Q000648:ultrastructure; D007895:Leishmania tropica / Q000187:drug effects* / Q000254:growth & development / Q000648:ultrastructure; D008264:Macrophages / Q000187:drug effects / Q000469:parasitology; D051379:Mice; D008870:Microtubules / Q000187:drug effects*; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
D000981:Antiprotozoal Agents; D004148:Dioxolanes; C040422:tubulazole