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A subset of NSAIDs lower amyloidogenic Abeta42 independently of cyclooxygenase activity

Bibliographic

Year of Publication:
2001
Contact PI Name:
Edward H. Koo
Contact PI Affiliation:
Department of Neurosciences, University of California San Diego, La Jolla, California, USA
Co-Authors:
Sascha Weggen, Jason L. Eriksen, Pritam Das, Sarah A. Sagi, Rong Wang, Claus U. Pietrzik, Kirk A. Findlay, Twanya Smith, Michael P. Murphy, Thomas Butler, David E. Kang, Numa Marquez-Sterling, Todd E.Golde
Primary Reference (PubMED ID):
Funding Source:
National Institutes of Health (NIH)
Ellison Medical Foundation
John Douglas French Foundation
Emmy Noether Fellowship
Paul B. Beeson Emerging Leaders Career Development Award in Aging
Study Goal and Principal Findings:

The recognition that a robust inflammatory response is a component of the Alzheimer’s disease process led to the discovery that long-term treatment with non-steroidal anti-inflammatory drugs (NSAIDs) dramatically reduced the risk for Alzheimer’s disease, and delayed disease onset.  The mechanisms by which NSAIDs act to reduce AD risk are controversial. Some investigators have proposed NSAIDs reduce AD risk by dampening down inflammation in the brain via inhibition of cyclooxygenases (COX) 1 and 2;others have proposed  that some NSAIDs reduce the risk for AD by selectively lowering the production of Abeta42.The overarching goal of this study was to examine whether treatment of cells and transgenic mice with non-steroidal anti-inflammatory drugs (NSAIDs) alters APP processing and generation of Abeta, particularly the Abeta 42 species. The study reports that the NSAIDs ibuprofen, indomethacin and sulindac sulphide preferentially decrease the highly amyloidogenic Abeta 42 peptide produced from a variety of cultured cells by as much as 80%. This effect was not seen in all NSAIDs and seemed not to be mediated by inhibition of COX activity. These data suggest that alternative targets of NSAID action have to be considered.The short-term administration of ibuprofen to  transgenic mice that produce mutant APP lowered their brain levels of Abeta 42. In cultured cells, the decrease in Abeta 42 secretion was accompanied by an increase in the Abeta(1±38) isoform, indicating that NSAIDs target gamma-secretase activity without significantly perturbing other APP processing pathways or Notch cleavage.These findings suggest that NSAIDs directly affect beta -amyloid pathology in the brain by reducing Abeta 42 peptide levels by altering gamma secretase activity on APP, and that this Abeta 42-lowering activity could be optimized to selectively target the pathogenic Abeta 42 species.

Therapeutic Agent

Therapeutic Information:
Therapy Type:
Small Molecule
Therapeutic Agent:
Ibuprofen
Therapeutic Target:
Cyclooxygenase 1 (COX 1)
Therapeutic Target:
Cyclooxygenase 2 (COX 2)
Therapy Type:
Small Molecule
Therapeutic Agent:
Indomethacin
Therapeutic Target:
Cyclooxygenase 1 (COX 1)
Therapeutic Target:
Cyclooxygenase 2 (COX 2)
Therapy Type:
Small Molecule
Therapeutic Agent:
Sulindac Sulfide/Sulphide
Therapeutic Target:
Cyclooxygenase 1 (COX 1)
Therapeutic Target:
Cyclooxygenase 2 (COX 2)
Therapy Type:
Small Molecule
Therapeutic Agent:
Celecoxib
Therapeutic Target:
Cyclooxygenase 2 (COX 2)

Animal Model

Model Information:
Species:
Mouse
Model Type:
APP
Strain/Genetic Background:
Not Reported

Experimental Design

Is the following information reported in the study?:
Power/Sample Size Calculation
Randomized into Groups
Blinded for Treatment
Blinded for Outcome Measures
Pharmacokinetic Measures
Pharmacodynamic Measures
Toxicology Measures
ADME Measures
Biomarkers
Dose
Formulation
Route of Delivery
Duration of Treatment
Frequency of Administration
Age of Animal at the Beginning of Treatment
Age of Animal at the End of Treatment
Sex as a Biological Variable
Study Balanced for Sex as a Biological Variable
Number of Premature Deaths
Number of Excluded Animals
Statistical Plan
Genetic Background
Inclusion/Exclusion Criteria Included
Conflict of Interest

Outcomes

Outcome Measured
Outcome Parameters
Biochemical
Brain-beta Amyloid Peptide 42
Brain-beta Amyloid Peptide 40
Brain-beta Amyloid Peptide 39
Brain-beta Amyloid Peptide 38
Brain-beta Amyloid Peptide 37
Notch Cleavage
beta Amyloid Turnover