Effect ofLuteolinon 11Beta-Hydroxysteroid Dehydrogenase in Rat Liver and Kidney

Abstract

11Beta-hydroxysteroid dehydrogenase (11β-HSD) enzymes control the glucocorticoid (GC) signaling, which is essential in regulating homeostasis. Our previous study revealed thatEclipta prostrata(EP) affected the activity and expression of 11β-HSD enzymes which might improve the efficacy and reduce the adverse drug effects of glucocorticoid in patients undergoing combinational therapy. However, it is still unclear which composition of EP plays a major role and how it works. In this paper, we choseLuteolinwhich is one of the main ingredients of EP and evaluated its effect and metabolism in combination with prednisone. The effects of different concentrations ofLuteolinextract on prednisone/prednisolone metabolism indicated the enzyme activity of 11β-HSD, so the production rate (pmol/min per mg protein) of metabolites was used to indicate enzyme activity. Furthermore, we explored the influence ofLuteolinon gene and protein expressions of 11β-HSD I/II in rat liver and kidney tissue. Our results showed that oral administration ofLuteolinsignificantly increased the gene and protein expressions of hepatic 11β-HSD I and renal 11β-HSD II, which may improve the efficacy and reduce the adverse drug effect of glucocorticoid in clinical application. A potential clinical value ofLuteolinwould also be indicated in combination therapy with prednisone for the treatment of nephrotic syndrome.