Hageman Ida, Buschard Karsten
Bartholin Institute, Kommunehospitalet, Copenhagen, Denmark.
Pharmacol Toxicol. 2002 Sep;91(3):123-8. doi: 10.1034/j.1600-0773.2002.910306.x.
Fusidic acid and its sodium salt (fusidin) are widely used antistaphylococcal drugs which possesses immunomodulatory properties. This prompted us to investigate whether high concentrations of fusidin could lower the diabetes incidence in diabetes-prone BB (BioBreeding) rats. As fusidin has previously been claimed to be poorly absorbed in rats after oral administration we wanted to measure the activity of the drug in various organs. Three groups of BB rats were used: 63 rats received fusidin dissolved in drinking water; 65 rats received chow containing fusidin; and 72 rats served as controls. The content of fusidin in the organs were examined microbiologically. The incidence of diabetes was significantly lower in the two fusidin-treated groups compared to the control group. The incidence was lower for male than for female rats in both experimental groups while no gender difference was seen in the control group. The female rats had a substantially higher content of fusidin in their organs than the males regardless of the administration way and regardless of diabetes outbreak or not. Interestingly, the fusidin treated non-diabetic rats displayed a lower random blood glucose level than the controls. In conclusion, fusidin is well absorbed after oral administration and it significantly reduces the diabetes incidence in BB rats. Fusidin accumulates substantially more in female rats which may be due to the steroid structure of fusidin. Whether the same phenomenon takes place in human beings is not known.
夫西地酸及其钠盐（夫西地素）是广泛使用的具有免疫调节特性的抗葡萄球菌药物。这促使我们研究高浓度的夫西地素是否能降低糖尿病易感性BB（BioBreeding）大鼠的糖尿病发病率。由于此前有人称夫西地素口服给药后在大鼠体内吸收不佳，我们想测量该药物在各个器官中的活性。使用了三组BB大鼠：63只大鼠饮用溶解有夫西地素的水；65只大鼠食用含有夫西地素的食物；72只大鼠作为对照。通过微生物学方法检测各器官中夫西地素的含量。与对照组相比，两个接受夫西地素治疗的组的糖尿病发病率显著降低。在两个实验组中，雄性大鼠的发病率低于雌性大鼠，而在对照组中未观察到性别差异。无论给药方式如何，无论是否发生糖尿病，雌性大鼠器官中夫西地素的含量都明显高于雄性大鼠。有趣的是，接受夫西地素治疗的非糖尿病大鼠的随机血糖水平低于对照组。总之，夫西地素口服给药后吸收良好，且能显著降低BB大鼠的糖尿病发病率。夫西地素在雌性大鼠体内的蓄积量明显更多，这可能是由于夫西地素的类固醇结构所致。尚不清楚人类是否会出现同样的现象。
