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

• Published in: Molecular pharmaceutics Vol. 19; no. 12; pp. 4576 - 4587
• Main Authors: Li, Pengxiao, Guo, Xiaoyuan, Liu, Ting, Liu, Qing, Yang, Jie, Liu, Guoyun
• Format: Journal Article
• Language: English
• Published: United States American Chemical Society 05.12.2022
• Subjects: 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; Nanoparticles; NF-E2-Related Factor 2 - metabolism; NF-kappa B - metabolism; Serum Albumin, Bovine - metabolism; bovine serum albumin nanoparticles; apoptosis; piperlongumine derivative; inflammation; oxidative stress; acute liver injury
• ISSN: 1543-8384; 1543-8392
• DOI: 10.1021/acs.molpharmaceut.2c00215

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.