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Specificity of procaine and ester hydrolysis by human, minipig, and rat skin and liver

Lookup NU author(s): Dr Christopher Jewell, Professor Faith Williams


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The capacity of human, minipig, and rat skin and liver subcellular fractions to hydrolyze the anesthetic ester procaine was compared with carboxylesterase substrates 4-methylumbelliferyl-acetate, phenylvalerate, and para-nitrophenylacetate and the arylesterase substrate phenylacetate. Rates of procaine hydrolysis by minipig and human skin microsomal and cytosolic fractions were similar, with rat displaying higher activity. Loperamide inhibited procaine hydrolysis by human skin, suggesting involvement of human carboxylesterase hCE2. The esterase activity and inhibition profiles in the skin were similar for minipig and human, whereas rat had a higher capacity to metabolize esters and a different inhibition profile. Minipig and human liver and skin esterase activity was inhibited principally by paraoxon and bis-nitrophenyl phosphate, classical carboxylesterase inhibitors. Rat skin and liver esterase activity was inhibited additionally by phenylmethylsulfonyl fluoride and the arylesterase inhibitor mercuric chloride, indicating a different esterase profile. These results have highlighted the potential of skin to hydrolyze procaine following topical application, which possibly limits its pharmacological effect. Skin from minipig used as an animal model for assessing transdermal drug preparations had similar capacity to hydrolyze esters to human skin. Copyright © 2007 by The American Society for Pharmacology and Experimental Therapeutics.

Publication metadata

Author(s): Jewell C, Ackermann C, Payne NA, Fate G, Voorman R, Williams FM

Publication type: Article

Publication status: Published

Journal: Drug Metabolism and Disposition

Year: 2007

Volume: 35

Issue: 11

Pages: 2015-2022

ISSN (print): 0090-9556

ISSN (electronic): 1521-009X

Publisher: American Society for Pharmacology and Experimental Therapeutics


DOI: 10.1124/dmd.107.015727

PubMed id: 17664252


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