Evaluation of Hepatoprotective Effects of Piperlongumine Derivative PL 1-3-Loaded Albumin Nanoparticles on Lipopolysaccharide/d-Galactosamine-Induced Acute Liver Injury in Mice

Mol Pharm. 2022 Dec 5;19(12):4576-4587. doi: 10.1021/acs.molpharmaceut.2c00215. Epub 2022 Aug 16.

Abstract

In recent years, piperlongumine (PL) having specific cytotoxicity has attracted considerable attention for anticancer activity. Through structural modification, the active derivative PL 1-3 shows potential anti-inflammatory activity and low cytotoxicity, but its water solubility is low. Here, PL 1-3-loaded bovine serum albumin nanoparticles (1-3 NPs) were prepared and characterized, which can improve the dissolution. 1-3 NPs exhibited effective hepatoprotective effects on lipopolysaccharide/d-galactosamine-induced acute liver injury of mice, which was similar to liver injury in clinical settings. 1-3 NPs treatment can inhibit inflammation, oxidative stress, and apoptosis via the downregulation of NF-κB signaling pathways, the activation of Nrf2/HO-1 signaling pathways, and the inhibition of expression of Bax and caspase 3 proteins. The above results demonstrated that PL 1-3-loaded bovine serum albumin nanoparticles possessed potential value in intervention of inflammation-based liver injury.

Keywords: acute liver injury; apoptosis; bovine serum albumin nanoparticles; inflammation; oxidative stress; piperlongumine derivative.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Chemical and Drug Induced Liver Injury* / drug therapy
  • Chemical and Drug Induced Liver Injury* / metabolism
  • Galactosamine / pharmacology
  • Inflammation / metabolism
  • Lipopolysaccharides / pharmacology
  • Liver / metabolism
  • Mice
  • NF-E2-Related Factor 2 / metabolism
  • NF-kappa B / metabolism
  • Nanoparticles*
  • Serum Albumin, Bovine / metabolism

Substances

  • Galactosamine
  • Lipopolysaccharides
  • piperlongumine
  • Serum Albumin, Bovine
  • NF-E2-Related Factor 2
  • NF-kappa B