Improvement bioavailability of silymarin ameliorates severe dyslipidemia associated with metabolic syndrome

Xenobiotica. 2015;45(9):751-6. doi: 10.3109/00498254.2015.1010633. Epub 2015 Jul 16.

Abstract

1. To compare the effectiveness of different drug forms of silymarin: standardized extract of silymarin (SS), micronized silymarin (MS) and silymarin in the form of phytosome (PS) on dyslipidemia and liver fat accumulation in a model of metabolic syndrome, in non-obese hereditary hypertriglyceridemic rats. The second aim of this study was to slightly uncover the silymarin action on enzymes and proteins involved in cholesterol metabolism and excretion. 2. Silymarin administered to hereditary hypertriglyceridemic rats as dietary supplements (1%) for 4 weeks significantly lowered the plasma levels of triglycerides, total cholesterol and markedly increased HDL cholesterol level. Western blot analyses showed significant increase in the protein expression of CYP7A1 and CYP4A and increase in protein expression of selected ABC transporters. Silymarin in the form of phytosome and micronized silymarin were more effective forms of silymarin. 3. These findings suggest that silymarin may favorably affect the metabolism of cholesterol and triglycerides in rats with metabolic syndrome. Raising HDL levels suggests potentially important anti-atherogenic effect of silymarin. The changes in expression of cytochromes P450 and ABC transporters involved in cholesterol metabolism and excretion could be partially responsible for the hypolipidemic effect of silymarin.

Keywords: ABC transporters; CYP4A; CYP7A1; HDL-cholesterol.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • ATP-Binding Cassette Transporters / metabolism
  • Animals
  • Biological Availability
  • Blotting, Western
  • Cholesterol 7-alpha-Hydroxylase / metabolism
  • Cytochrome P-450 CYP4A / metabolism
  • Dyslipidemias / blood
  • Dyslipidemias / complications*
  • Dyslipidemias / drug therapy*
  • Lipids / blood
  • Liver / drug effects
  • Liver / enzymology
  • Metabolic Syndrome / blood
  • Metabolic Syndrome / complications*
  • Metabolic Syndrome / drug therapy*
  • Rats, Wistar
  • Silymarin / pharmacology
  • Silymarin / therapeutic use*

Substances

  • ATP-Binding Cassette Transporters
  • Lipids
  • Silymarin
  • CYP7A1 protein, rat
  • Cholesterol 7-alpha-Hydroxylase
  • Cytochrome P-450 CYP4A