Nakayoshi T, Izumi M, Tatsuta K
Pharmaceutical Research Centre, Meiji Seika Kaisha, Ltd., Yokohama, Japan.
Drugs Exp Clin Res. 1992;18(4):103-9.
The effect of macrolide antibiotics on gastrointestinal motility was studied in unanaesthetized dogs by using strain-gauge transducers. Midecamycin acetate, leucomycin, josamycin and acetylspiramycin, which are 16-membered macrolides, did not affect the gastrointestinal motility and no symptoms of gastrointestinal disorder were observed. On the other hand, erythromycin, roxithromycin, clarithromycin and oleandomycin, which are 14-membered macrolides, caused giant contraction and disorder symptoms. Moreover, it was found that the glycosidic linkages of the lactone ring were necessary for a structure to exert strong contractile activity.
通过使用应变片式传感器，在未麻醉的犬身上研究了大环内酯类抗生素对胃肠动力的影响。作为16元大环内酯类抗生素的醋酸麦迪霉素、柱晶白霉素、交沙霉素和乙酰螺旋霉素，并未影响胃肠动力，也未观察到胃肠紊乱症状。另一方面，作为14元大环内酯类抗生素的红霉素、罗红霉素、克拉霉素和竹桃霉素，则引起了强烈收缩和紊乱症状。此外，还发现内酯环的糖苷键对于发挥强大收缩活性的结构是必需的。
