Chymase inhibitor prevents the development and progression of non-alcoholic steatohepatitis in rats fed a high-fat and high-cholesterol diet

J Pharmacol Sci. 2017 Jul;134(3):139-146. doi: 10.1016/j.jphs.2017.04.005. Epub 2017 Jun 20.

Abstract

The effect of the chymase inhibitor TY-51469 on the development and progression of non-alcoholic steatohepatitis (NASH) was evaluated in rats fed a high-fat and high-cholesterol (HFC) diet. To evaluate the preventive effect of TY-51469 on the development of NASH, stroke-prone spontaneously hypertensive rat 5 (SHRSP5)/Dmcr rats were fed either a normal or HFC diet for 8 weeks, and concurrently administered either placebo or TY-51469 (1 mg/kg per day). To evaluate the effect of TY-51469 on the survival rate, TY-51469 was administered either concurrently with HFC diet (pretreated group) or 8 weeks after HFC diet at which point NASH had developed (posttreated group). Eight weeks after HFC diet, significant increases of steatosis, fibrosis and chymase-positive cells were observed in liver from the placebo-treated rats. Significant increases of myeloperoxidase, transforming growth factor-β, matrix metalloproteinase-9, and collagen I mRNA levels were also observed. However, all parameters were significantly attenuated in the TY-51469-treated group. A survival rate of the placebo-treated group fed the HFC diet was 0% at 14 weeks. In comparison, the rates of TY-51469-pretreated and TY-51469-posttreated groups were 100% and 50% at 14 weeks, respectively. Chymase inhibitor may be applicable to preventing the development and progression of NASH.

Keywords: Chymase; Inhibitor; Liver failure; Non-alcoholic steatohepatitis; Rat.

MeSH terms

  • Animals
  • Cholesterol, Dietary / administration & dosage*
  • Cholesterol, Dietary / adverse effects*
  • Chymases / antagonists & inhibitors*
  • Diet, High-Fat / adverse effects*
  • Disease Models, Animal
  • Disease Progression
  • Enzyme Inhibitors / administration & dosage*
  • Male
  • Non-alcoholic Fatty Liver Disease / etiology*
  • Non-alcoholic Fatty Liver Disease / prevention & control*
  • Rats, Inbred SHR
  • Sulfonamides / administration & dosage*
  • Thiophenes / administration & dosage*

Substances

  • Cholesterol, Dietary
  • Enzyme Inhibitors
  • Sulfonamides
  • TY 51469
  • Thiophenes
  • Chymases