Stereoselectivity of skin carboxylesterase metabolism / 药学学报
Acta Pharmaceutica Sinica
;
(12): 322-326, 2005.
Article
in Chinese
| WPRIM
| ID: wpr-353504
ABSTRACT
<p><b>AIM</b>To study the stereoselectivity of skin carboxylesterase metabolism and its molecular biological foundation for improving drug percutaneous absorption.</p><p><b>METHODS</b>Ketoprofen ethyl ester was used as a model drug, and skin homogenate was applied for studying the stereoselectivity of carboxylesterase metabolism. Human liver L02 cell was used as control of carboxylesterase expression, and RT-PCR was used for studying the expression of carboxylesterase.</p><p><b>RESULTS</b>The main metabolite of ketoprofen ethyl ester in human skin homogenate was R-ketoprofen. Human carboxylesterase-2 was highly expressed in skin and its cells. However, the expression of human carboxylesterase-1 was very weak or not detectable.</p><p><b>CONCLUSION</b>Human carboxylesterase-2 is the main hydrolytic enzyme of prodrugs in percutaneous absorption, and shows metabolic stereoselectivity to prodrugs with chiral esters.</p>
Full text:
Available
Index:
WPRIM (Western Pacific)
Main subject:
Skin
/
Stereoisomerism
/
RNA, Messenger
/
Prodrugs
/
Cell Line
/
Cells, Cultured
/
Ketoprofen
/
Cell Biology
/
Carboxylesterase
/
Genetics
Limits:
Adult
/
Humans
Language:
Chinese
Journal:
Acta Pharmaceutica Sinica
Year:
2005
Type:
Article
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