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Effect of Luteolin on 11Beta-Hydroxysteroid Dehydrogenase in Rat Liver and Kidney.

Tang L, Deng B, Shi L, Wei B, Ren B, Fu X - Evid Based Complement Alternat Med (2015)

Bottom Line: In this paper, we chose Luteolin which is one of the main ingredients of EP and evaluated its effect and metabolism in combination with prednisone.Our results showed that oral administration of Luteolin significantly 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 of Luteolin would also be indicated in combination therapy with prednisone for the treatment of nephrotic syndrome.

View Article: PubMed Central - PubMed

Affiliation: Department of Pharmacy, The First Affiliated Hospital, Sun Yat-Sen University, 58 Zhongshan No. 2 Road, Guangzhou, Guangdong 510080, China.

ABSTRACT
11Beta-hydroxysteroid dehydrogenase (11β-HSD) enzymes control the glucocorticoid (GC) signaling, which is essential in regulating homeostasis. Our previous study revealed that Eclipta 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 chose Luteolin which is one of the main ingredients of EP and evaluated its effect and metabolism in combination with prednisone. The effects of different concentrations of Luteolin extract 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 of Luteolin on gene and protein expressions of 11β-HSD I/II in rat liver and kidney tissue. Our results showed that oral administration of Luteolin significantly 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 of Luteolin would also be indicated in combination therapy with prednisone for the treatment of nephrotic syndrome.

No MeSH data available.


Related in: MedlinePlus

Effects of Luteolin on the enzyme activity of 11β-HSD I in liver (a) and 11β-HSD II in kidney (b). Rats were orally administrated with vehicle (CMC-Na) or Luteolin (5 mg/kg, 10 mg/kg, 20 mg/kg) for 14 days. Liver and kidney microsomes were isolated and then 11β-HSD I and 11β-HSD II enzyme activities were analyzed. ∗P < 0.05 compared with the control group, ∗∗P < 0.01 compared with the control group (mean ± SD, n = 6).
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fig1: Effects of Luteolin on the enzyme activity of 11β-HSD I in liver (a) and 11β-HSD II in kidney (b). Rats were orally administrated with vehicle (CMC-Na) or Luteolin (5 mg/kg, 10 mg/kg, 20 mg/kg) for 14 days. Liver and kidney microsomes were isolated and then 11β-HSD I and 11β-HSD II enzyme activities were analyzed. ∗P < 0.05 compared with the control group, ∗∗P < 0.01 compared with the control group (mean ± SD, n = 6).

Mentions: Effects of Luteolin on enzyme activity of 11β-HSD I/II in rat liver and kidney were shown in Figure 1. Compared with the negative control group, the 11β-HSD I activities from all orally administrated Luteolin groups were increased with the medium and high dose groups exhibiting significantly statistical differences (P < 0.05). The activities of renal 11β-HSD II from all treatment groups were significantly increased compared to the negative control group. The relative 11β-HSD II activities of low, medium, and high dose groups were 153.9 ± 33.3%, 155.9 ± 33.9%, and 164.5 ± 10.9%, respectively. There were significant differences (P < 0.05) between treatment groups and the negative control group. Therefore, Luteolin could significantly induce the activity of hepatic 11β-HSD I and renal 11β-HSD II, and the effects were positively related to concentration of Luteolin. The effects of Luteolin on rat liver/kidney 11β-HSD indicated that Luteolin could affect the metabolism of prednisone/prednisolone and regulate the local tissue concentrations by 11β-HSD modulation.


Effect of Luteolin on 11Beta-Hydroxysteroid Dehydrogenase in Rat Liver and Kidney.

Tang L, Deng B, Shi L, Wei B, Ren B, Fu X - Evid Based Complement Alternat Med (2015)

Effects of Luteolin on the enzyme activity of 11β-HSD I in liver (a) and 11β-HSD II in kidney (b). Rats were orally administrated with vehicle (CMC-Na) or Luteolin (5 mg/kg, 10 mg/kg, 20 mg/kg) for 14 days. Liver and kidney microsomes were isolated and then 11β-HSD I and 11β-HSD II enzyme activities were analyzed. ∗P < 0.05 compared with the control group, ∗∗P < 0.01 compared with the control group (mean ± SD, n = 6).
© Copyright Policy - open-access
Related In: Results  -  Collection

Show All Figures
getmorefigures.php?uid=PMC4496493&req=5

fig1: Effects of Luteolin on the enzyme activity of 11β-HSD I in liver (a) and 11β-HSD II in kidney (b). Rats were orally administrated with vehicle (CMC-Na) or Luteolin (5 mg/kg, 10 mg/kg, 20 mg/kg) for 14 days. Liver and kidney microsomes were isolated and then 11β-HSD I and 11β-HSD II enzyme activities were analyzed. ∗P < 0.05 compared with the control group, ∗∗P < 0.01 compared with the control group (mean ± SD, n = 6).
Mentions: Effects of Luteolin on enzyme activity of 11β-HSD I/II in rat liver and kidney were shown in Figure 1. Compared with the negative control group, the 11β-HSD I activities from all orally administrated Luteolin groups were increased with the medium and high dose groups exhibiting significantly statistical differences (P < 0.05). The activities of renal 11β-HSD II from all treatment groups were significantly increased compared to the negative control group. The relative 11β-HSD II activities of low, medium, and high dose groups were 153.9 ± 33.3%, 155.9 ± 33.9%, and 164.5 ± 10.9%, respectively. There were significant differences (P < 0.05) between treatment groups and the negative control group. Therefore, Luteolin could significantly induce the activity of hepatic 11β-HSD I and renal 11β-HSD II, and the effects were positively related to concentration of Luteolin. The effects of Luteolin on rat liver/kidney 11β-HSD indicated that Luteolin could affect the metabolism of prednisone/prednisolone and regulate the local tissue concentrations by 11β-HSD modulation.

Bottom Line: In this paper, we chose Luteolin which is one of the main ingredients of EP and evaluated its effect and metabolism in combination with prednisone.Our results showed that oral administration of Luteolin significantly 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 of Luteolin would also be indicated in combination therapy with prednisone for the treatment of nephrotic syndrome.

View Article: PubMed Central - PubMed

Affiliation: Department of Pharmacy, The First Affiliated Hospital, Sun Yat-Sen University, 58 Zhongshan No. 2 Road, Guangzhou, Guangdong 510080, China.

ABSTRACT
11Beta-hydroxysteroid dehydrogenase (11β-HSD) enzymes control the glucocorticoid (GC) signaling, which is essential in regulating homeostasis. Our previous study revealed that Eclipta 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 chose Luteolin which is one of the main ingredients of EP and evaluated its effect and metabolism in combination with prednisone. The effects of different concentrations of Luteolin extract 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 of Luteolin on gene and protein expressions of 11β-HSD I/II in rat liver and kidney tissue. Our results showed that oral administration of Luteolin significantly 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 of Luteolin would also be indicated in combination therapy with prednisone for the treatment of nephrotic syndrome.

No MeSH data available.


Related in: MedlinePlus