A study of esterase-its application to biotransformation of midecamycin derivatives.

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Abstract
Esterases of intestinal mucosa and liver from human and rat were used to study the biotransformation of midecamycin [an antibacterial agent] derivatives. In the in vitro experiment with rat esterases, the 4''''-acyl derivatives were more easily hydrolyzed than the 9-acyl derivatives. Among the 9-acyl esters, the highest hydrolytic activity was observed with butyrate. In the in vivo experiment, when the rats were administered with the derivatives of 4''''-depropionylmidecamycin (MI) orally, comparatively more 9-acyl metabolites were excreted in the urine, but the amount of the 4''''-acyl metabolites was very small. In the in vitro experiment with human esterases, the 9-acyl esters were hydrolyzed more easily than the 4''''-acyl esters. Among the 9-acyl esters of MI, the highest hydrolytic activity was observed with butyrate. When the 9-acyl esters were administered to humans, the n-butyl ester was hydrolyzed faster than the acetyl ester. When the 9,4''''-diacetyl ester was administered to humans, comparatively more 4''''-acyl metabolites were excreted in the urine.