Vouldoukis Ioannis, Rougier Sandrine, Dugas Bernard, Pino Paco, Mazier Dominique, Woehrlé Frédérique
INSERM U511, Immunobiologie Cellulaire et Moléculaire des Infections Parasitaires, Université Paris VI, CHU-Pitié Salpétrière, 75013 Paris, France.
Vet Parasitol. 2006 Jan 30;135(2):137-46. doi: 10.1016/j.vetpar.2005.09.003. Epub 2005 Oct 19.
The control of canine leishmaniasis largely depends on the success of treatment. Drugs currently available to treat this disease are toxic and partially effective. The curative effect of marbofloxacin, a third-generation fluoroquinolone developed for veterinarian individual treatment, was evaluated in vitro in the presence of Leishmania infantum promastigotes and dog-monocyte-derived macrophages; meglumine antimoniate and sodium stibogluconate were used as comparative treatments. We observed that the killing of Leishmania promastigotes and intracellular amastigotes by marbofloxacin was dose-dependent. We demonstrated that successful treatment of canine infected macrophages for 48 h was possible with 500 microg/ml of marbofloxacin. Leishmanicidal activity acted through a TNF-alpha and nitric oxide pathway and correlated with the generation of nitric oxide (NO(2)) production by monocytes derived macrophages from infected (23+/-5 microM) or healthy (21+/-6 microM) dogs, in comparison with NO(2) concentration in infected/non-treated macrophages (< 3 microM, P<0.01). This significant induced parasiticidal effect correlated with extensive elimination of amastigotes by macrophages derived from infected (11+/-5) and healthy dogs (6+/-2), when compared to infected/non-treated macrophages (530+/-105 and 472+/-86 amastigotes, respectively, P< 0.01). Marbofloxacin was shown to be non-toxic at 500 microg/ml in vitro and no cell apoptosis was observed. The molecule was able to induce a parasitic process after significant elimination of amastigotes in leishmania-infected dog macrophages. We propose that marbofloxacin, compared to standard chemotherapeutic agents (meglumine antimoniate and sodium stibogluconate), could be an effective and pragmatic oral route alternative to treat canine leishmaniasis.
犬利什曼病的控制在很大程度上取决于治疗的成效。目前可用于治疗该疾病的药物有毒且效果欠佳。对专为兽医个体治疗研发的第三代氟喹诺酮类药物马波沙星的疗效,在婴儿利什曼原虫前鞭毛体和犬单核细胞衍生巨噬细胞存在的情况下进行了体外评估;葡甲胺锑酸盐和葡萄糖酸锑钠用作对照治疗。我们观察到马波沙星对利什曼原虫前鞭毛体和细胞内无鞭毛体的杀伤作用呈剂量依赖性。我们证明,500微克/毫升的马波沙星能够成功治疗犬感染巨噬细胞48小时。杀利什曼活性通过肿瘤坏死因子-α和一氧化氮途径发挥作用,并且与感染犬(23±5微摩尔)或健康犬(21±6微摩尔)的单核细胞衍生巨噬细胞产生一氧化氮(NO₂)相关,相比之下,感染但未治疗的巨噬细胞中的NO₂浓度低于3微摩尔(P<0.01)。与感染但未治疗的巨噬细胞(分别为530±105和472±86个无鞭毛体,P<0.01)相比,这种显著的诱导杀寄生虫作用与感染犬(11±5)和健康犬(6±2)的巨噬细胞对无鞭毛体的广泛清除相关。在体外,500微克/毫升的马波沙星显示无毒,未观察到细胞凋亡。该分子在利什曼原虫感染的犬巨噬细胞中显著清除无鞭毛体后能够诱导一个寄生过程。我们提出,与标准化疗药物(葡甲胺锑酸盐和葡萄糖酸锑钠)相比,马波沙星可能是一种治疗犬利什曼病的有效且实用的口服替代药物。