Carboxylesterase in the Liver and Small Intestine of Experimental Animals and Human.
From: Graduate School of Pharmaceutical Sciences, Kumamoto University, 5-1 Oe-honmachi, Kumamoto, 862-0973, Japan.
Life sciences
- Publish Date: Aug 2007
- ISSN: 0024-3205
- Volume: 81
- Issue: 11
- Pages: 924-32
- Medium: Print
- Language: English
- Citation (JAMA): Taketani Megumi, Shii Mayumi, Ohura Kayoko, et al. Carboxylesterase in the Liver and Small Intestine of Experimental Animals and Human.. Life Sci. Aug 2007;81:924-32
Abstract
Native polyacrylamide gel electrophoresis showed carboxylesterase (CES) to be the most abundant hydrolase in the liver and small intestine of humans, monkeys, dogs, rabbits and rats. The liver contains both CES1 and CES2 enzymes in all these species. The small intestine contains only enzymes from the CES2 family in humans and rats, while in rabbits and monkeys, enzymes from both CES1 and CES2 families are present. Interestingly, no hydrolase activity at all was found in dog small intestine. Flurbiprofen derivatives were R-preferentially hydrolyzed in the liver microsomes of all species, but hardly hydrolyzed in the small intestine microsomes of any species except rabbit. Propranolol derivatives were hydrolyzed in the small intestine and liver microsomes of all species except dog small intestine. Monkeys and rabbits showed R-preferential and non-enantio-selective hydrolysis, respectively, for propranolol derivatives in both organs. Human and rat liver showed R- and S-preferential hydrolysis, respectively, in spite of non-enantio-selective hydrolysis in their small intestines. The proximal-to-distal gradient of CES activity in human small intestine (1.1-1.5) was less steep than that of CYP 3A4 and 2C9 activity (three-fold difference). These findings indicate that human small intestine and liver show extensive hydrolase activity attributed to CES, which is different from that in species commonly used as experimental animals.
Mesh Headings (Keywords): Adult, Animals, Carboxylic Ester Hydrolases, Dogs, Female, Haplorhini, Humans, Hydrolysis, Intestine, Small, Liver, Male, Rabbits, Rats, Rats, Wistar, Species Specificity
Check for Full Text / PubMed Unique Identifier (PMID): 17764701
This abstract is part of PubMed, a service of the U.S. National Library of Medicine. PubMed includes more than 17 million citations from MEDLINE and other life science journals for biomedical articles. See Copyright and Disclaimers.
Linked medical terms appearing on this page are added by Healia to help readers find more information and are not part of the original PubMed document.
The data herein was last updated on July 8th, 2008 and may not reflect the most current and accurate data available from NLM.