A new fluorene compound disrupts amyloid formation

Wednesday 02 May 2012

Researchers at the University of California (UC) have shown that small molecules called spin-labelled fluorene compounds can be used to detect amyloid in imaging studies, to disrupt the formation of amyloid and to reduce inflammation.

Fluorene compounds are small, three-ringed molecules that were originally developed as imaging agents to detect amyloid with PET imaging. In the current study, researchers "labelled" the fluorine compounds by adding a nitroxide molecule. This allows the activity of the compound to be visible using electron paramagnetic resonance (EPR) spectroscopy.

The group found that spin-labeled compounds disrupted Aβ peptide formation more effectively than did non-labeled fluorenes. In addition, the antioxidant properties of the nitroxide molecule contributed to the protective effects on neurons. Another benefit is that the compounds can easily pass through the blood-brain barrier.

"We have found these small molecules to have significant beneficial effects on cultured neurons, from protecting against toxic compounds that form in neurons to reducing inflammatory factors," said John C. Voss, Professor of Biochemistry and Molecular Medicine at the UC Davis School of Medicine and the principal investigator of the study. "As a result, they have great potential as a therapeutic agent to prevent or delay injury in individuals in the earliest stages of Alzheimer's disease, before significant damage to the brain occurs."

www.plosone.org/article/info%3Adoi%2F10.1371%2Fjournal.pone.0035443