Pharmacological inhibition of plasminogen activator inhibitor-1 prevents memory deficits and reduces neuropathology in APP/PS1 mice

Psychopharmacology (Berl). 2023 Dec;240(12):2641-2655. doi: 10.1007/s00213-023-06459-8. Epub 2023 Sep 12.

Abstract

Rationale: Extracellular proteolytic activity plays an important role in memory formation and the preservation of cognitive function. Previous studies have shown increased levels of plasminogen activator inhibitor-1 (PAI-1) in the brain of mouse models of Alzheimer's disease (AD) and plasma of AD patients, associated with memory and cognitive decline; however, the exact function of PAI-1 in AD onset and progression is largely unclear.

Objective: In this study, we evaluated a novel PAI-1 inhibitor, TM5A15, on its ability to prevent or reverse memory deficits and decrease Aβ levels and plaque deposition in APP/PS1 mice.

Methods: We administered TM5A15 mixed in a chow diet to 3-month and 9-month-old APP/PS1 mice before and after neuropathological changes were distinguishable. We then evaluated the effects of TM5A15 on memory function and neuropathology at 9 months and 18 months of age.

Results: In the younger mice, 6 months of TM5A15 treatment protected against recognition and short-term working memory impairment. TM5A15 also decreased oligomer levels and amyloid plaques, and increased mBDNF expression in APP/PS1 mice at 9 months of age. In aged mice, 9 months of TM5A15 treatment did not significantly improve memory function nor decrease amyloid plaques. However, TM5A15 treatment showed a trend in decreasing oligomer levels in APP/PS1 mice at 18 months of age.

Conclusion: Our results suggest that PAI-1 inhibition could improve memory function and reduce the accumulation of amyloid levels in APP/PS1 mice. Such effects are more prominent when TM5A15 is administered before advanced AD pathology and memory deficits occur.

Keywords: Alzheimer’s disease; Brain aging; Plasmin system; Plasminogen activator inhibitor-1; TM5A15.

MeSH terms

  • Alzheimer Disease* / metabolism
  • Amyloid beta-Peptides* / metabolism
  • Amyloid beta-Protein Precursor / genetics
  • Amyloid beta-Protein Precursor / metabolism
  • Animals
  • Disease Models, Animal
  • Humans
  • Infant
  • Memory Disorders / complications
  • Memory Disorders / drug therapy
  • Memory Disorders / prevention & control
  • Mice
  • Mice, Transgenic
  • Plaque, Amyloid / metabolism
  • Plasminogen Activator Inhibitor 1 / metabolism
  • Plasminogen Activator Inhibitor 1 / therapeutic use
  • Presenilin-1 / genetics

Substances

  • Amyloid beta-Peptides
  • Plasminogen Activator Inhibitor 1
  • Amyloid beta-Protein Precursor
  • Presenilin-1