AJP - Gastrointestinal and Liver Physiology, Vol 248, Issue 3 320-G325, Copyright © 1985 by American Physiological Society
Structure-activity relation among macrolide antibiotics in initiation of interdigestive migrating contractions in the canine gastrointestinal tract
Z. Itoh, T. Suzuki, M. Nakaya, M. Inoue, H. Arai and K. Wakabayashi
The relation between the chemical structure of commercially available
macrolide antibiotics and their activity in inducing interdigestive
migrating contractions (IMC) was studied in conscious dogs. It was found
that the 14-membered macrolides erythromycin and oleandomycin are active in
inducing IMC in the stomach in association with the endogenous release of
motilin. These erythromycin- and oleandomycin-induced contractions in the
stomach migrated through the small intestine in a caudad direction.
Conversely, 16-membered macrolide antibiotics such as leucomycin,
acetylspiramycin, and tylosin do not induce any contractions in the stomach
or stimulate endogenous release of motilin. These findings suggest that the
IMC-inducing activity in macrolides seems to be closely related to their
chemical configuration, i.e., the structure of 14-membered macrolides with
dimethylaminosugar (desosamine) bound at C-5 and neutralsugar at C-3 in
glycosidic linkage in parallel is likely to be necessary for IMC-inducing
activity. The mechanisms by which erythromycin and oleandomycin stimulate
endogenous motilin release are not known.
