Clarkson A B, Bacchi C J, Mellow G H, Nathan H C, McCann P P, Sjoerdsma A
Proc Natl Acad Sci U S A. 1983 Sep;80(18):5729-33. doi: 10.1073/pnas.80.18.5729.
DL-alpha-Difluoromethylornithine, a polyamine biosynthesis inhibitor, and bleomycin, a currently used antineoplastic agent, have each previously been shown to be curative for acute short-term infections of mice with Trypanosoma brucei brucei, an African trypanosome closely related to those that cause the human disease African sleeping sickness. These agents were tested singly and in combination in a previously described mouse model of sleeping sickness with demonstrable brain involvement. The original model is extended by using two additional strains of outbred mice and by demonstrating that melarsoprol, an arsenical and currently the only drug used for human African trypanosomiasis involving the brain, was also curative for these brain infections. Neither difluoromethylornithine nor bleomycin alone was curative for the brain infections; however, many combinations of the two drugs were found to be 100% curative with no evidence of immediate toxicity.
DL-α-二氟甲基鸟氨酸是一种多胺生物合成抑制剂,博来霉素是一种目前使用的抗肿瘤药物,先前已分别证明对感染布氏布氏锥虫的小鼠急性短期感染具有治愈作用,布氏布氏锥虫是一种与导致人类疾病非洲昏睡病的锥虫密切相关的非洲锥虫。在先前描述的具有明显脑部受累的昏睡病小鼠模型中,对这些药物进行了单独和联合测试。通过使用另外两种远交系小鼠品系,并证明美拉胂醇(一种砷剂,目前是用于治疗累及脑部的人类非洲锥虫病的唯一药物)对这些脑部感染也具有治愈作用,从而扩展了原始模型。单独使用二氟甲基鸟氨酸或博来霉素均不能治愈脑部感染;然而,发现这两种药物的许多组合具有100%的治愈率,且无立即毒性的证据。