11C-Labeling of a Flavanone Extracted from a South American Native Species for Evaluation of Its Interaction with GSK-3β

对从南美本土物种中提取的黄烷酮进行 11C 标记,以评估其与 GSK-3β 的相互作用

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作者:Maia Zeni, Maria Daniela Santi, Florencia Arredondo, Laura Reyes, Manuela Bentura, Diego Carvalho, Mariana Peralta, Maria Gabriela Ortega, Juan A Abin-Carriquiry, Loreto Martínez-Gonzalez, Juan Pablo Gambini, Pablo Duarte, Ana Martinez, Ana Rey, Javier Giglio

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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