Isobavachin Ameliorates Acetaminophen‐Induced Liver Injury Through Modulation of CYP2E1‐Mediated Bioactivation and NRF2/PI3K/AKT Cytoprotective Pathways
Acetaminophen (APAP)-induced liver injury (AILI) remains a critical clinical challenge with limited therapeutic options. This research elucidates the mechanisms through which the natural flavonoid isobavachin (ISO) confers protection against APAP-induced liver injury. In vivo experiments demonstrated that ISO treatment significantly attenuated histopathological parameters, oxidative stress and inflammation, as indicated by serum ALT/AST, MDA, SOD/GSH, TNF-α/IL-1β levels. Mechanistically, ISO inhibited CYP2E1 expression and promoted NRF2 activation. Furthermore, integrated network pharmacology, transcriptomics, and molecular docking simulations revealed the PI3K/AKT signaling pathway as a potential targets of ISO, demonstrating high-affinity confirmed between ISO and PI3K (-8.6 kcal/mol) or AKT (-6.4 kcal/mol) respectively. western blotting assay confirmed that ISO activated PI3K/AKT signaling and upregulated downstream anti-apoptotic- protein BCL2. These findings collectively suggest that ISO alleviates AILI through multi-mechanisms: inhibiting CYP2E1-mediated APAP bioactivation, modulating of the NRF2/PI3K/AKT signaling, ISO attenuates oxidative damage, suppresses inflammatory activation, and inhibits apoptosis. The results suggest that ISO represents a potential therapeutic agent for managing APAP-induced hepatotoxicity.
Authors
- Yuexin Xu (ORCID: https://orcid.org/0000-0002-7140-6505)
- Shuaishuai Zhang (ORCID: https://orcid.org/0000-0002-1441-4840)
- X. Liu
- Xuhong Huang
- Wenjie Ye
- Ting Wu
- Youxi Zhou (ORCID: https://orcid.org/0009-0009-2180-9195)
- Mengting Li
- Zhenkun Wu
Institutions
- Guangdong Pharmaceutical University (CN)
- Ministry of Education (RW)
Publication Details
- Journal
- Journal of Biochemical and Molecular Toxicology
- Published
- 2026-01-01
- DOI
- https://doi.org/10.1002/jbt.70682
- Primary Topic
- Drug-Induced Hepatotoxicity and Protection
- Type
- article
- Field-Weighted Citation Impact
- 0.00