Green Extraction and Molecular Docking-Guided Discovery of Asiaticoside as a Multi-Target Modulator of the SIRT1/HMGB1/p53-p21 Axis in H2O2-Induced Senescent Endothelial Cells
Endothelial cell senescence is a key contributor to vascular ageing and cardiovascular diseases. Asiaticoside, a pentacyclic triterpenoid saponin from Centella asiatica, exhibits anti-inflammatory and antioxidant activities, yet its potential to modulate endothelial senescence remains unexplored. Herein, we report the molecular docking-guided discovery of asiaticoside as a multi-target modulator of the SIRT1/HMGB1/p53–p21 senescence regulatory axis. Asiaticoside was isolated via a green acid-hydrolysis strategy using dilute HCl as the extraction solvent, followed by polyamide enrichment and C18 reversed-phase purification (purity > 98%). Molecular docking revealed that asiaticoside binds favourably to SIRT1 (−8.1 kcal mol−1), the HMGB1–DNA complex (−10.7 kcal mol−1), and several senescence-associated secretory phenotype (SASP)-related inflammatory cytokines. In H2O2-induced senescent human umbilical vein endothelial cells (HUVECs), asiaticoside at 100 μM significantly reduced senescence-associated β-galactosidase activity and alleviated G0/G1 cell cycle arrest without cytotoxicity. Mechanistically, asiaticoside restored SIRT1 expression, suppressed the secretion of IL-1β, IL-6, IL-8, TNF-α, and HMGB1, downregulated p21 at both mRNA and protein levels, reduced p53 protein expression, and suppressed p16 mRNA expression. These findings demonstrate that asiaticoside attenuates endothelial senescence and SASP-driven inflammation, an effect associated with restoration of SIRT1 expression and suppression of the HMGB1/p53–p21 pathway.
Authors
- Junjie Wang (ORCID: https://orcid.org/0000-0003-4164-9458)
- 刘思妤
- Fei Zeng (ORCID: https://orcid.org/0000-0002-1555-1812)
- Xiong Liu (ORCID: https://orcid.org/0000-0002-7113-2313)
- Jianhua Huang
- Yuping Wang
- Wenkai Li
Institutions
- Xiangnan University (CN)
Publication Details
- Journal
- Molecules
- Published
- 2026-09-28
- DOI
- https://doi.org/10.3390/molecules31193451
- Primary Topic
- Medicinal Plants and Neuroprotection
- Type
- article
- Field-Weighted Citation Impact
- 0.00