Conophylline inhibits non-alcoholic steatohepatitis in mice

PLoS One. 2017 Jun 8;12(6):e0178436. doi: 10.1371/journal.pone.0178436. eCollection 2017.

Abstract

Conophylline (CnP), a vinca alkaloid extracted from the leaves of the tropical plant Ervatamia microphylla, attenuates hepatic fibrosis in mice. However, little is known about whether CnP inhibits steatosis, inflammation, and fibrosis in non-alcoholic steatohepatitis (NASH) in mice. A methionine-choline-deficient (MCD) diet was administered to male db/db mice as a NASH model, and CnP (1 μg/kg/d) was co-administered. Eight weeks after the commencement of the MCD diet, hepatic steatosis, inflammation, and fibrosis, and hepatic fat metabolism-, inflammation-, and fibrosis-related markers were examined. Feeding on an MCD for 8 weeks induced hepatic steatosis, inflammation, and fibrosis. CnP significantly attenuated the MCD-induced increases in hepatic steatosis, as well as hepatic inflammation and fibrosis. The MCD diet increased hepatic transforming growth factor-β (TGF-β) mRNA levels, which are correlated with hepatic steatosis, inflammation, and fibrosis. The diet also attenuated acyl-coenzyme A oxidase 1 (ACOX1) and carnitine palmitoyltransferase 1 (CPT1) mRNA levels, which are involved in β-oxidation. The putative mechanism of the CnP effect involves reduced hepatic TGF-β mRNA levels, and increased mRNA levels of hepatic peroxisome proliferator-activated receptor (PPAR) α and its target genes ACOX1 and CPT1. The results of this study indicate that CnP inhibits steatohepatitis, possibly through the inhibition of hepatic TGF-β mRNA levels, and induces an increase in PPARα mRNA levels, resulting in the attenuation of hepatic steatosis, inflammation, and fibrosis in mice. CnP might accordingly be a suitable therapeutic option for NASH.

MeSH terms

  • Alanine Transaminase / blood
  • Animals
  • Fatty Acids, Nonesterified / blood
  • Fatty Liver / blood
  • Fatty Liver / drug therapy
  • Fatty Liver / metabolism
  • Immunohistochemistry
  • Inflammation / blood
  • Inflammation / drug therapy
  • Inflammation / metabolism
  • Lipid Metabolism / physiology
  • Liver / drug effects
  • Liver / metabolism
  • Male
  • Malondialdehyde / blood
  • Mice
  • Non-alcoholic Fatty Liver Disease / blood
  • Non-alcoholic Fatty Liver Disease / drug therapy*
  • Non-alcoholic Fatty Liver Disease / metabolism
  • RNA / genetics
  • Real-Time Polymerase Chain Reaction
  • Triglycerides / blood
  • Vinca Alkaloids / therapeutic use*

Substances

  • Fatty Acids, Nonesterified
  • Triglycerides
  • Vinca Alkaloids
  • conophylline
  • Malondialdehyde
  • RNA
  • Alanine Transaminase

Grants and funding

This work was supported in part by the Program for the Strategic Research Foundation at Private Universities 2011-2015 (S1101027) from the Ministry of Education, Culture, Sports, Science, and Technology in Japan (MEXT) (http://www.mext.go.jp/a_menu/koutou/shinkou/07021403/002/002/1218299.htm).