Possible antifibrotic effect of GDC-0449 (Vismodegib), a hedgehog-pathway inhibitor, in mice model of Schistosoma-induced liver fibrosis

Parasitol Int. 2017 Oct;66(5):545-554. doi: 10.1016/j.parint.2017.04.004. Epub 2017 Apr 10.

Abstract

Liver fibrosis is a pathological process complicating schistosomiasis. It is an active process of continuous extracellular matrix accumulation. In Egypt, schistosomiasis re-infection is a continuing problem especially in rural areas. In this study we examined the antifibrotic effect of GDC-0449 (Vismodegib), a hedgehog-pathway inhibitor as a new molecular target for Schistosoma-induced liver fibrosis, in addition to exploring its effect as antischistosomal drug. The effect of GDC-0449 alone or combined with Praziquantel was tried experimentally in infected mice with Schistosoma mansoni. Fifty CD-1 Swiss female albino mice were used, forty mice were infected with Schistosoma mansoni cercariae. Animals were grouped into five groups; uninfected control, infected untreated, infected treated with Praziquantel (500mg/kg/day) for two days, infected treated with GDC-0449 (40mg/kg/day) for seven days, and infected treated with combined Praziquantel and GDC-0449. Parasitological and chemical parameters, hydroxyproline level and liver granuloma were assessed. Liver fibrosis was reduced significantly evidenced by reduced hydroxyproline levels [P<0.01 for combined (Praziquantel/GDC-0449) treatment groups, P<0.001 for GDC-0449-treated group]. Also, histopathological examination of liver tissues revealed that the mean diameter of granulomas was statistically reduced (P=0.001) with a reduction rate of 24.4% on treatment with GDC-0449. In GDC-0449/Praziquantel combined treatment group, number and mean diameter of the granulomas were reduced significantly P<0.001, and P=0.001 respectively. No antischistosomal effect was recorded for GDC-0449 in this study.

Keywords: GDC-0449; Hedgehog pathway; Liver fibrosis; Schistosomiasis; Vismodegib.

MeSH terms

  • Anilides / administration & dosage
  • Anilides / therapeutic use*
  • Animals
  • Cercaria / drug effects
  • Disease Models, Animal
  • Drug Therapy, Combination
  • Egypt / epidemiology
  • Female
  • Hedgehog Proteins / antagonists & inhibitors
  • Hydroxyproline / blood
  • Liver / drug effects*
  • Liver / parasitology
  • Liver / pathology
  • Liver Cirrhosis / drug therapy*
  • Liver Cirrhosis / parasitology
  • Mice
  • Parasite Egg Count
  • Praziquantel / therapeutic use
  • Pyridines / administration & dosage
  • Pyridines / therapeutic use*
  • Schistosoma mansoni / drug effects*
  • Schistosomiasis mansoni / drug therapy*
  • Schistosomiasis mansoni / epidemiology

Substances

  • Anilides
  • Hedgehog Proteins
  • HhAntag691
  • Pyridines
  • Praziquantel
  • Hydroxyproline