Fong D
Department of Biological Sciences, Rutgers, State University of New Jersey, Piscataway 08855-1059.
FEMS Microbiol Lett. 1993 Feb 15;107(1):95-9. doi: 10.1016/0378-1097(93)90360-e.
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.
对于合成抗微管化合物tubulozole的顺式和反式立体异构体，在微摩尔浓度下，tubulozole-C对哺乳动物细胞具有细胞毒性，而tubulozole-T则没有。测试了tubulozoles对寄生原生动物利什曼原虫的作用。对于亚马逊利什曼原虫的前鞭毛体阶段，两种异构体均抑制寄生虫生长。对于亚马逊利什曼原虫和硕大利什曼原虫的无鞭毛体阶段，在体外以鼠J774巨噬细胞系作为宿主细胞时，tubulozole-T降低了感染指数。尽管观察到tubulozole-T对巨噬细胞具有细胞毒性，但该化合物可能是一种潜在有用的新型抗利什曼原虫药物。
