A STUDY OF ESTERASE-ITS APPLICATION TO BIOTRANSFORMATION OF MIDECAMYCIN DERIVATIVES
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- MORIKAWA MASAKO
- Department of Pharmacology, Tokyo College of Pharmacy
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- INOUE MICHIKO
- Department of Pharmacology, Tokyo College of Pharmacy
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- TSUBOI MINORU
- Department of Pharmacology, Tokyo College of Pharmacy
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- SHOMURA TOMOKO
- Central Research Laboratories, Meiji Seika Kaisha, Ltd.
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- SOMEYA SAWAKO
- Central Research Laboratories, Meiji Seika Kaisha, Ltd.
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- MURATA SHINJIRO
- Central Research Laboratories, Meiji Seika Kaisha, Ltd.
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- UMEMURA KOSHIRO
- Central Research Laboratories, Meiji Seika Kaisha, Ltd.
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- SUGIURA MAMORU
- Department of Pharmacy, Gifu College of Pharmacy
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Abstract
Esterases of intestinal mucosa and liver from human and rat were used to study the biotransformation of midecamycin 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 (Ml) 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 Ml, 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. These results suggest that the experiment with the use of these esterases is useful to estimate the biotransformation of midecamycin derivatives.
Journal
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- Journal of pharmacobio-dynamics
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Journal of pharmacobio-dynamics 5 (5), 314-318, 1982-05
The Pharmaceutical Society of Japan
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Keywords
Details 詳細情報について
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- CRID
- 1572543027231751808
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- NII Article ID
- 110003636346
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- NII Book ID
- AA00704585
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- ISSN
- 0386846X
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- Text Lang
- en
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- Data Source
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- CiNii Articles