Targeting FoxO1-STX17-mediated autophagic flux: Quercetin's therapeutic mechanism in diabetic nephropathy

Eur J Pharmacol. 2025 Dec 5:1008:178309. doi: 10.1016/j.ejphar.2025.178309. Epub 2025 Nov 7.

Abstract

Background: Diabetic nephropathy (DN) involves autophagic stress from defective lysosomal clearance. Quercetin, a flavonol, shows therapeutic potential but its mechanism remains unclear.

Objective: Investigate quercetin's role in DN via FoxO1-STX17-mediated autophagosome-lysosome fusion.

Methods: DN was induced in C57BL/6J mice (uninephrectomy + streptozotocin [50 mg/kg]). Quercetin (150 mg/kg/day) or valsartan (40 mg/kg/day) was administered for 12 weeks. Renal function, histopathology, and autophagy markers (p62, LC3-II, STX17) were evaluated. Quercetin metabolites were identified via UPLC-HRMS. Network pharmacology, molecular docking, dynamics (MD), and biolayer interferometry (BLI) validated targets. Advanced glycation end products (AGE) (100 μg/mL)-stimulated podocytes, Bafilomycin (Baf)-A1-treated and FoxO1-silenced podocytes were used for mechanistic validation.

Results: In vivo, quercetin ameliorated renal injury and restored autophagic flux without affecting upstream autophagy initiation. Ten quercetin-derived metabolites were identified in serum. Bioinformatics analysis nominated FoxO1 as a key regulator of quercetin-modulated autophagy. In vitro, quercetin protected podocytes and promoted autophagosome-lysosome fusion, effects that were reversed by Baf-A1 and replicated in FoxO1-silenced cells.

Conclusion: Quercetin alleviates DN by targeting FoxO1 to restore STX17-dependent autophagosome-lysosome fusion, thereby resolving autophagic stress. These findings support quercetin as a promising therapeutic candidate for DN.

Keywords: Autophagic stress; Autophagosome-lysosome fusion; Diabetic nephropathy; FoxO1; Quercetin.

MeSH terms

  • Animals
  • Autophagosomes / drug effects
  • Autophagosomes / metabolism
  • Autophagy* / drug effects
  • Diabetes Mellitus, Experimental / complications
  • Diabetes Mellitus, Experimental / drug therapy
  • Diabetes Mellitus, Experimental / metabolism
  • Diabetic Nephropathies* / drug therapy
  • Diabetic Nephropathies* / metabolism
  • Diabetic Nephropathies* / pathology
  • Forkhead Box Protein O1* / genetics
  • Forkhead Box Protein O1* / metabolism
  • Kidney / drug effects
  • Kidney / metabolism
  • Kidney / pathology
  • Lysosomes / drug effects
  • Lysosomes / metabolism
  • Male
  • Mice
  • Mice, Inbred C57BL
  • Molecular Docking Simulation
  • Podocytes / drug effects
  • Podocytes / metabolism
  • Podocytes / pathology
  • Quercetin* / metabolism
  • Quercetin* / pharmacology
  • Quercetin* / therapeutic use

Substances

  • Quercetin
  • Forkhead Box Protein O1
  • Foxo1 protein, mouse