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A Potential Boron Neutron Capture Therapy Agent Selectively Suppresses High-Grade Glioma: In Vitro and in Vivo Exploration
10 October 2023
Glioblastoma (GBM), as the most central nervous system (CNS) intractable disease, has spoiled millions of lives due to its high mortality. Even though several efforts have been made, the existing treatments have had limited success. In this sense, we studied a lead compound, the boron-rich selective epidermal growth factor receptor (EGFR)-inhibitor hybrid 1, as a potential drug for GBM treatment.
For this end, we analyzed the in vitro activity of hybrid 1 in a glioma/primary astrocytes coculture, studying cellular death types triggered by treatment with this compound and its cellular localizations. Additionally, hybrid 1 concentrated boron in glioma cells selectively and more effectively than the boron neutron capture therapy (BNCT)-clinical agent 10B-l-boronophenylalanine and thus displayed a better in vitro-BNCT effect. This encouraged us to analyze hybrid 1 in vivo. Therefore, immunosuppressed mice bearing U87 MG human GBM were treated with both 1 and 1 encapsulated in a modified liposome (recognized by brain–blood barrier peptide transporters), and we observed a potent in vivo per se antitumor activity (tumor size decrease and animal survival increase). These data demonstrate that 1 could be a promising new targeted therapy for GBM.
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M4HTH Smart Nanomedicine

A Potential Boron Neutron Capture Therapy Agent Selectively Suppresses High-Grade Glioma: In Vitro and in Vivo Exploration


Catalina Alamón, Belén Dávila, María Fernanda García, Susana Nievas, María Alejandra Dagrosa, Silvia Thorp, Mariángeles Kovacs, Emiliano Trias, Ricardo Faccio, Martín Gabay, Nidal Zeineh, Abraham Weizman, Francesc Teixidor, Clara Viñas, Moshe Gavish*, Hugo Cerecetto*, and Marcos Couto*

Mol. Pharmaceutics 2023, 20, 5, 2702–2713
Publication DateApril 4, 2023
DOI: https://doi.org/10.1021/acs.molpharmaceut.3c00152