NDLI: Species Differences in Stereoselective Hydrolase Activity in Intestinal Mucosa

Content Provider	Springer Nature Link
Author	Yoshigae, Yasushi Imai, Teruko Horita, Akira Matsukane, Hidebu Otagiri, Masaki
Copyright Year	1998
Abstract	Purpose. The aim of this study is to investigate species differences in the stereoselective hydrolysis for propranolol ester prodrugs in mammalian intestinal mucosa and Caco-2 cells. Methods. Hydrolase activities for propranolol prodrugs and p-nitro-phenylacetate in man (age: 51−71 years), the beagle dog (age: 4 years) and Wistar rat (age: 8 weeks) intestinal mucosa, and also in Caco-2 cells (passage between 60−70) were estimated by determining the rate of production of propranolol and p-nitrophenol, respectively. Results. The hydrolase activities for both propranolol prodrugs and p-nitrophenylacetate were in the order of man > rat >> Caco-2 cells > dog for intestinal microsomes, and rat > Caco-2 cells = man > dog for intestinal cytosol. Dog microsomes showed stereoselective hydrolysis for propranolol prodrugs, but not those from human or rat. Interestingly, both subcellular fractions of Caco-2 cells showed remarkable R-enantioselectivity except acetyl propranolol. Enzyme kinetic experiments for each enantiomer of butyryl propranolol in microsomes revealed that dog possesses both low and high affinity hydrolases. Both Km and Vmax values in rat were largest among examined microsomes, while Vmax/Km was largest in man. Finally, it was shown that the carboxylesterases might contribute to the hydrolysis of propranolol prodrug in all species by inhibition experiments. Conclusions. The hydrolase activities for propranolol prodrugs and p-nitrophenylacetate in intestinal mucosa showed great species differences and those in human intestine were closer to those of rat intestine than dog intestine or Caco-2 cells.
Starting Page	626
Ending Page	631
Page Count	6
File Format	PDF
ISSN	07248741
Journal	Pharmaceutical Research
Volume Number	15
Issue Number	4
e-ISSN	1573904X
Language	English
Publisher	Kluwer Academic Publishers-Plenum Publishers
Publisher Date	1998-01-01
Publisher Place	New York
Access Restriction	One Nation One Subscription (ONOS)
Subject Keyword	Pharmacology/Toxicology Pharmacy Biochemistry Medical Law Biomedical Engineering
Content Type	Text
Resource Type	Article
Subject	Organic Chemistry Pharmacology Molecular Medicine Pharmacology (medical) Biotechnology Pharmaceutical Science

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