Bouteille B, Darde M L, Pestre-Alexandre M
Service de Parasitologie-Mycologie, C. H. U. Dupuytren, Limoges.
Bull Soc Pathol Exot Filiales. 1988;81(3 Pt 2):533-42.
This study reports the action of ten drugs on two strains of Trypanosoma brucei brucei (Antat 1.9 virulent in mice and Antat 1.1E more chronic) in vitro in acellular semi defined medium and in vivo in Swiss mice. Minimum efficient concentration of drugs is evaluated by means of an in vitro assay: melarsoprol (1 microgram/ml); DFMO (cytostatic effect from 50 micrograms/ml); suramin (1 microgram/ml); 2 nitroimidazole derivative Ro 15-0216 (1 microgram/ml); triacetylbenzene trisguanylhydrazone (TBG) (between 1 and 10 mg/ml). Fluconazole is not efficient in vitro on T. b. brucei. In vivo: TBG is efficient at 3 mg/kg, DFMO given orally and intraperitoneally is not efficient at 4 g/kg, but surviving time of mice is increased. Suramin (20 mg/kg/d X 4) alone or associated with ornidazole (50 and 500 mg/kg/d X 4) is efficient on bloodstream trypanosomes but no efficacy is revealed on brain forms. Cyclosporin (30 mg/kg/d X 3) lightly increases surviving time of mice. Fluconazole, pefloxacin and acyclovir are not efficient in vivo.
本研究报告了十种药物对两株布氏布氏锥虫（Antat 1.9对小鼠有致病性，Antat 1.1E病程更长）在无细胞半限定培养基中的体外作用以及在瑞士小鼠体内的作用。通过体外试验评估药物的最低有效浓度：美拉胂醇（1微克/毫升）；二氟甲基鸟氨酸（DFMO，50微克/毫升起有细胞生长抑制作用）；苏拉明（1微克/毫升）；2-硝基咪唑衍生物Ro 15-0216（1微克/毫升）；三乙酰苯三胍腙（TBG）（1至10毫克/毫升）。氟康唑在体外对布氏布氏锥虫无效。体内试验：TBG在3毫克/千克时有疗效，口服和腹腔注射DFMO在4克/千克时无效，但可延长小鼠存活时间。苏拉明（20毫克/千克/天×4）单独使用或与奥硝唑（50和500毫克/千克/天×4）联合使用对血液中的锥虫有效，但对脑部的锥虫无效。环孢素（30毫克/千克/天×3）可轻度延长小鼠存活时间。氟康唑、培氟沙星和阿昔洛韦在体内无效。
