Long-term combination therapy of ezetimibe and acarbose for non-alcoholic fatty liver disease

J Hepatol. 2009 Sep;51(3):548-56. doi: 10.1016/j.jhep.2009.05.017. Epub 2009 Jun 6.

Abstract

Background/aims: Non-alcoholic fatty liver disease (NAFLD) is a hepatic manifestation of metabolic syndrome that is closely associated with multiple factors such as obesity, hyperlipidemia, type 2 diabetes mellitus and hypertension, making it difficult to treat NAFLD effectively using any monotherapy available to date. In this study, we propose a novel combination therapy for NAFLD comprising ezetimibe (EZ), a cholesterol absorption inhibitor, and acarbose (AC), an alpha-glucosidase inhibitor.

Methods: C57BL/6J mice were divided into five treatment groups as follows: basal diet (BD), high-fat diet (HFD) only, HFD with EZ (5mg/kg/day), HFD with AC (100mg/kg/day), and HFD with both EZ and AC for 24 weeks.

Results: Long-term combination therapy with EZ and AC significantly reduced steatosis, inflammation and fibrosis in the liver, compared with long-term monotherapy with either drug, in an HFD-induced NAFLD mouse model; the combination therapy also significantly increased the expression of microsomal triglyceride transfer protein (MTP) and peroxisome proliferators-activated receptor-alpha1 (PPAR-alpha1) in the liver, compared with either monotherapy, which may have led to the improvement in lipid metabolic disorder seen in this model.

Conclusions: Combination therapy with EZ and AC for 24 weeks improved the histopathological findings in a mouse model of NAFLD.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acarbose / pharmacology
  • Acarbose / therapeutic use*
  • Animals
  • Anticholesteremic Agents / pharmacology
  • Anticholesteremic Agents / therapeutic use*
  • Azetidines / pharmacology
  • Azetidines / therapeutic use*
  • Carrier Proteins / metabolism
  • Cholesterol / metabolism
  • Dietary Fats / adverse effects
  • Disease Models, Animal
  • Drug Therapy, Combination
  • Enzyme Inhibitors / pharmacology
  • Enzyme Inhibitors / therapeutic use*
  • Ezetimibe
  • Fatty Liver / drug therapy*
  • Fatty Liver / etiology
  • Fatty Liver / metabolism
  • Liver / drug effects
  • Liver / metabolism
  • Liver / pathology
  • Liver Cirrhosis / drug therapy
  • Liver Cirrhosis / metabolism
  • Liver Cirrhosis / pathology
  • Male
  • Mice
  • Mice, Inbred C57BL
  • PPAR alpha / metabolism
  • Receptors, LDL / metabolism
  • Sterol Regulatory Element Binding Protein 1 / metabolism
  • Triglycerides / metabolism

Substances

  • Anticholesteremic Agents
  • Azetidines
  • Carrier Proteins
  • Dietary Fats
  • Enzyme Inhibitors
  • PPAR alpha
  • Receptors, LDL
  • Srebf1 protein, mouse
  • Sterol Regulatory Element Binding Protein 1
  • Triglycerides
  • microsomal triglyceride transfer protein
  • Cholesterol
  • Ezetimibe
  • Acarbose