Farthing M J, Inge P M
J Antimicrob Chemother. 1986 Feb;17(2):165-71. doi: 10.1093/jac/17.2.165.
Possible antigiardial activity of the bile salt-like antibiotic, sodium fusidate has been investigated during 24 h liquid culture of Giardia lamblia trophozoites and in 4 h microassays for parasite motility inhibition and viability. Sodium fusidate inhibited Giardia growth (ED50 0.2 mM; MIC 0.3 mM) but was considerably less potent than metronidazole (ED50 0.002 mM; MIC 0.05 mM). Sodium fusidate and metronidazole were active inhibitors of parasite motility (ED50 0.9 and 0.3 mM respectively) but were largely without effect in the 4 h viability assay. Sodium fusidate was active at concentrations well below its critical micellar concentration (2.7 mM) suggesting that its effect was not merely related to its membranolytic detergent properties. Its taurine and glycine conjugates were markedly less potent and paradoxically stimulated growth at low concentration. The studies suggest that sodium fusidate does have antigiardial activity and in view of its relative freedom from teratogenic and other toxic effects may be useful in pregnancy when other antigiardial agents are contra-indicated or as an adjunct in combination therapy when other single agents have failed to eradicate infection.
在蓝氏贾第鞭毛虫滋养体的24小时液体培养以及用于抑制寄生虫运动和活力的4小时微量测定中，研究了胆汁盐样抗生素夫西地酸钠可能的抗贾第虫活性。夫西地酸钠抑制贾第虫生长（半数有效浓度为0.2 mM；最低抑菌浓度为0.3 mM），但效力远低于甲硝唑（半数有效浓度为0.002 mM；最低抑菌浓度为0.05 mM）。夫西地酸钠和甲硝唑都是寄生虫运动的有效抑制剂（半数有效浓度分别为0.9和0.3 mM），但在4小时活力测定中基本无效。夫西地酸钠在远低于其临界胶束浓度（2.7 mM）的浓度下具有活性，这表明其作用不仅仅与其膜溶解洗涤剂特性有关。其牛磺酸和甘氨酸共轭物的效力明显较低，且在低浓度下反常地刺激生长。这些研究表明，夫西地酸钠确实具有抗贾第虫活性，鉴于其相对无致畸和其他毒性作用，在其他抗贾第虫药物禁忌时，可能对妊娠期有用，或者当其他单一药物未能根除感染时，可作为联合治疗的辅助药物。
