Mead J R, You X, Pharr J E, Belenkaya Y, Arrowood M J, Fallon M T, Schinazi R F
Department of Pediatrics, Emory University, Atlanta, Georgia 30022, USA.
Antimicrob Agents Chemother. 1995 Apr;39(4):854-8. doi: 10.1128/AAC.39.4.854.
Two polyether ionophores, maduramicin and alborixin, were evaluated for anticryptosporidial activity in a severe combined immune deficient (SCID) mouse model of cryptosporidiosis. Groups of SCID mice were inoculated with 10(6) oocysts of bovine origin by oral gavage. Maduramicin or alborixin was administered beginning 4 weeks postinfection at 3 mg/kg of body weight per day. Maduramicin treatment resulted in a 96% reduction in fecal parasite load over the 3-week treatment period (P < 0.003). This reduction correlated with decreases in tissue parasite loads observed in histological sections of the small intestine (P < 0.000002) and the colon (P < 0.000006). A significant decrease in oocyst shedding was also observed after a 3-week treatment with alborixin (71% reduction, P < 0.01). Maduramicin was also evaluated in a relapsing model of cryptosporidiosis in which the infection was observed to recur after treatments were discontinued. Some toxicity, as demonstrated by weight loss, was observed with both maduramicin and alborixin. Both drugs exhibited significant anticryptosporidial activities with concomitant moderate toxicity. These polyether ionophores should be valuable as positive controls in compound evaluation studies and as lead compounds for chemical optimization (modification).
在严重联合免疫缺陷(SCID)小鼠隐孢子虫病模型中,对两种聚醚离子载体马杜霉素和白硼菌素的抗隐孢子虫活性进行了评估。将SCID小鼠分组,通过口服灌胃接种10⁶个牛源卵囊。感染后4周开始,每天按3mg/kg体重给予马杜霉素或白硼菌素。在为期3周的治疗期内,马杜霉素治疗使粪便寄生虫负荷降低了96%(P<0.003)。这种降低与在小肠组织切片(P<0.000002)和结肠组织切片(P<0.000006)中观察到的组织寄生虫负荷降低相关。用白硼菌素治疗3周后,卵囊排出量也显著减少(降低71%,P<0.01)。还在隐孢子虫病复发模型中对马杜霉素进行了评估,在该模型中观察到停药后感染复发。马杜霉素和白硼菌素均观察到一些毒性,表现为体重减轻。两种药物均表现出显著的抗隐孢子虫活性,同时伴有中度毒性。这些聚醚离子载体作为化合物评估研究中的阳性对照以及化学优化(修饰)的先导化合物应具有重要价值。