Stereoselectivity of skin carboxylesterase metabolism / 药学学报
Acta Pharmaceutica Sinica
;
(12): 322-326, 2005.
Artigo
em Chinês
| 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>
Texto completo:
DisponíveL
Índice:
WPRIM (Pacífico Ocidental)
Assunto principal:
Pele
/
Estereoisomerismo
/
RNA Mensageiro
/
Pró-Fármacos
/
Linhagem Celular
/
Células Cultivadas
/
Cetoprofeno
/
Biologia Celular
/
Carboxilesterase
/
Genética
Limite:
Adulto
/
Humanos
Idioma:
Chinês
Revista:
Acta Pharmaceutica Sinica
Ano de publicação:
2005
Tipo de documento:
Artigo
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