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11C-Labeling of a Flavanone Extracted from a South American Native Species for Evaluation of Its Interaction with
Maia Zeni1,2, Maria Daniela Santi2, Florencia Arredondo2
1Graduate Program in Chemistry, Facultad de Química, Universidad de la República, General Flores 2124, Montevideo 11800, Uruguay.
Abstract:
Natural products play a crucial role in drug discovery, primarily due to their structural complexity. The prenylated flavanone glabranin ((S)-5,7-dihydroxy-8-(3-methylbut-2-en-1-yl)-2-phenylchroman-4-one), isolated from the Dalea elegans plant species, has demonstrated neuroprotective effects, attributed to its inhibition of GSK-3β, as per our previous in silico studies. Given the enzyme's diverse functions and its potential as a target for neurodegenerative diseases, our group synthesized and evaluated an 11C-labeled derivative of glabranin. We present its in vitro biological activity, including IC50, neuronal uptake in Alzheimer's-affected brain regions, key physicochemical properties, and animal studies. This study confirms [11C]FLA's interaction with GSK-3β in vitro, highlighting the potential of radiotracers in bioactive compound research.
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