Effect of 18alpha-glycyrrhizic acid and 18beta-glycyrrhizic acid on P-gp function and expression in Caco-2 cells / 中国中药杂志
China Journal of Chinese Materia Medica
;
(24): 99-103, 2012.
Artigo
em Chinês
| WPRIM
| ID: wpr-356113
ABSTRACT
<p><b>OBJECTIVE</b>The aim of the present study was to evaluate the modulating effect of glycyrrhizic acid C-18 epimers, 18alpha-glycyrrhizic acid (alpha-GL) and 18beta-glycyrrhizic acid (beta-GL) on both P-glycoprotein (P-gp) activity and expression in Caco-2 cell.</p><p><b>METHOD</b>The effects of P-gp activity were analyzed by rhodamine (Rhd 123) accumulation test, and those of P-gp expression were analyzed by flow cytometry and real-time PCR.</p><p><b>RESULT</b>At middle and high concentrations (10, 60 micromol x L(-1)), alpha-GL inhibited the function of P-gp and with on dose dependent while beta-GL induced the function of P-gp at three test concentrations with no dose dependent too. At middle and high concentrations (10, 60 micromol x L(-1)), alpha-GL down-regulated the expression of MDR1 mRNA. At high concentrations (60 micromol x L(-1)), beta-GL up-regulated the expression of MDR1 mRNA; At high concentrations (60 micromol x L(-1)), beta-GL induced the expression of P-gp protein while alpha-GL has no effect on the expression of P-gp protein at three test concentrations.</p><p><b>CONCLUSION</b>The effects of alpha-GL and beta-GL on the expression of MDR1 mRNA and CYP3A mRNA showed the same trend. The character that epimers of GL act on CYP3A and P-gp show similar stereo selectivity whether relate to PXR need further study.</p>
Texto completo:
DisponíveL
Índice:
WPRIM (Pacífico Ocidental)
Assunto principal:
Farmacologia
/
Medicamentos de Ervas Chinesas
/
Regulação para Baixo
/
Expressão Gênica
/
Química
/
Células CACO-2
/
Ácido Glicirrízico
/
Subfamília B de Transportador de Cassetes de Ligação de ATP
/
Genética
/
Metabolismo
Limite:
Humanos
Idioma:
Chinês
Revista:
China Journal of Chinese Materia Medica
Ano de publicação:
2012
Tipo de documento:
Artigo
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