Detalle de: 11C-Labeling of a Flavanone Extracted from a South American Native Species for Evaluation of Its Interaction with GSK-3β
| Title | 11C-Labeling of a Flavanone Extracted from a South American Native Species for Evaluation of Its Interaction with GSK-3β |
| 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. |
| Apa Reference | Zeni, M., Santi, M. D., Arredondo, F., Reyes, L., Bentura, M., Carvalho, D., Peralta, M., Ortega, M. G., Abin-Carriquiry, J. A., Martínez-Gonzalez, L., Gambini, J. P., Duarte, P., Martinez, A., Rey, A., & Giglio, J. (2025). 11C-Labeling of a Flavanone Extracted from a South American Native Species for Evaluation of Its Interaction with GSK-3β. Molecules, 30(4), 874. 10.3390/molecules30040874 |
| Doi | 10.3390/molecules30040874 |
| Publication Date | 14 Feb 2025 |
| Publication Type | Article |
| Researcher | Ana Martínez |
| Ontology | Computational models and simulations, Drug Discovery and design |
| Research Groups | Translational Medicinal and Biological Chemistry |
| Tools |