Effective oral countermeasures against ionizing radiation-induced damagewithout hindering cancer radiotherapy

High-dose ionizing radiation induces severe multi-organ injury, yet no broadly effective, orally available countermeasure has been validated. Here we describe a fully oral, multi-component formulation comprising bioavailable polyphenol derivatives (pterostilbene cocrystals and silybin-phosphatidylch...

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Bibliographic Details
Authors: López-Blanch, Rafael, Oriol-Caballo, María, Salvador-Palmer, Rosario, Moreno-Murciano, Paz, Benlloch, María, Villaescusa, Juan I., Montoro, Alegría, Prohens López, Rafael, Albertí, Joan, Estrela, José M., Obrador, Elena
Format: article
Status:Published version
Publication Date:2026
Country:España
Institution:Varias* (Consorci de Biblioteques Universitáries de Catalunya, Centre de Serveis Científics i Acadèmics de Catalunya)
Repository:Recercat. Dipósit de la Recerca de Catalunya
OAI Identifier:oai:dnet:recercat____::71839b0c195d0be72386e68c0ff1a80c
Online Access:https://hdl.handle.net/2445/229185
Access Level:Open access
Keyword:Radioteràpia
Radiació ionitzant
Polifenols
Radiotherapy
Ionizing radiation
Polyphenols
Description
Summary:High-dose ionizing radiation induces severe multi-organ injury, yet no broadly effective, orally available countermeasure has been validated. Here we describe a fully oral, multi-component formulation comprising bioavailable polyphenol derivatives (pterostilbene cocrystals and silybin-phosphatidylcholine), the NAD⁺ precursor nicotinamide riboside, and captopril, an angiotensin-converting enzyme inhibitor with established radiomitigative activity that synergizes with the polyphenols. This combination provides robust systemic radioprotection, enabling long-term survival in 90% of mice exposed to a lethal (LD50/30) dose of X-rays. Mechanistically, the formulation mitigates hematopoietic, intestinal, and neuromotor injury while enhancing DNA repair, suppressing oxidative stress, preserving NAD⁺ homeostasis, and activating autophagy. In intestinal epithelial cells, it markedly reduces radiation-induced apoptosis, inflammatory signaling, and mitochondrial dysfunction through coordinated modulation of Nrf2, NF-κB, and sirtuin-regulated stress responses. Critically, normal tissue protection does not compromise tumor control. In triple-negative breast cancer models, irradiation-induced tumor regression is preserved, whereas in glioblastoma (a typically radioresistant malignancy) tumor radiosensitivity is significantly enhanced via sustained oxidative stress, reduced PARP1 expression, and inhibition of HIF-1α and VEGF signaling. Collectively, these findings define an orally deployable, mechanistically integrated strategy that protects normal tissues while preserving or augmenting tumor radiosensitivity, supporting its translational potential as a practical and effective countermeasure against ionizing radiation exposure.