Stereoselective Characteristics and Mechanisms of Epidermal Carboxylesterase Metabolism Observed in HaCaT Keratinocytes
| Autor: | Quangang Zhu, Jin-Hong Hu, Ji-Yong Liu, Song-Wei Lu, Yan Xia Liu, Jin Wang |
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| Rok vydání: | 2007 |
| Předmět: |
Keratinocytes
Ketoprofen Stereochemistry Pharmaceutical Science Gene Expression Regulation Enzymologic Carboxylesterase Cell Line Substrate Specificity Hydrolysis medicine Humans Prodrugs RNA Messenger Chromatography High Pressure Liquid Pharmacology integumentary system Reverse Transcriptase Polymerase Chain Reaction Chemistry Stereoisomerism General Medicine Metabolism Prodrug stomatognathic diseases HaCaT Biochemistry Percutaneous absorption Hepatocytes Stereoselectivity sense organs Epidermis Carboxylic Ester Hydrolases medicine.drug |
| Zdroj: | Biological and Pharmaceutical Bulletin. 30:532-536 |
| ISSN: | 1347-5215 0918-6158 |
| DOI: | 10.1248/bpb.30.532 |
| Popis: | There is increasing evidence that epidermal carboxylesterase may be involved in the stereoselective hydrolysis of prodrugs in percutaneous absorption. The present study was designed to evaluate the stereoselective characteristics and mechanisms of ketoprofen ethyl ester hydrolysis by epidermal carboxylesterase expressed in HaCaT keratinocytes. Ketoprofen ethyl ester was mainly hydrolyzed to R-ketoprofen by carboxylesterase of human HaCaT keratinocytes. Human carboxylesterase-1 (hCE-1) and human carboxylesterase-2 (hCE-2) were intensively detected in L02 hepatocytes, hCE-2 was also intensively detected in HaCaT keratinocytes, but hCE-1 was not detected in HaCaT keratinocytes. hCE-2 is thus an abundant carboxylesterase in HaCaT keratinocytes which may be responsible for stereoselective hydrolysis of ketoprofen ethyl ester. |
| Databáze: | OpenAIRE |
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