Academic Journal
Enhanced brain delivery and antiproliferative activity of resveratrol using milk-derived exosomes
| العنوان: | Enhanced brain delivery and antiproliferative activity of resveratrol using milk-derived exosomes |
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| المؤلفون: | María Ángeles Ávila-Gálvez, Beatriz Garay-Mayol, Juan Antonio Giménez-Bastida, María del Carmen López de las Hazas, Carmen Mazarío-Gárgoles, Maria Alexandra Brito, Alberto Dávalos, Juan Carlos Espín, Antonio González-Sarrías |
| المصدر: | Journal of Agriculture and Food Research, Vol 18, Iss , Pp 101370- (2024) |
| بيانات النشر: | Elsevier, 2024. |
| سنة النشر: | 2024 |
| المجموعة: | LCC:Agriculture (General) LCC:Nutrition. Foods and food supply |
| مصطلحات موضوعية: | Exosome, Nanocarrier, Polyphenol, Resveratrol, Brain cancer, Blood-brain barrier, Agriculture (General), S1-972, Nutrition. Foods and food supply, TX341-641 |
| الوصف: | The polyphenol resveratrol (RSV) undergoes extensive phase II metabolism, which limits its bioavailability and bioactivity, including anticancer effects. Growing preclinical evidence reinforces milk-derived exosomes (EXOs) as promising nanocarrier drugs and bioactives delivery systems. Herein, to overcome the mentioned RSV's drawbacks, EXOs were loaded with RSV (EXO-RSV) to evaluate its brain delivery in Sprague-Dawley rats and its in vitro antiproliferative effects against human neuroblastoma SH-SY5Y and glioblastoma U-87MG cancer cells compared with non-encapsulated RSV. Pharmacokinetic analyses in perfused brains showed RSV detection only after EXO-RSV administration, not after non-encapsulated RSV administration. Encapsulation also resulted in lower concentrations of phase II-derived RSV metabolites in circulation. Additionally, blood-brain barrier (BBB) transport assays using human brain microvascular endothelial cells (HBMECs) corroborated that encapsulation enhanced RSV transport efficiency and protected it from cellular metabolism. In vitro and in silico analyses of phase-II conjugates, primarily RSV 3-glucuronide, showed lower capacity than RSV to cross the BBB. Finally, EXO-RSV (47−750 nM) showed an increased dose-dependent antiproliferative efficacy on both cancer cell lines compared with the non-encapsulated RSV (10 μM), which was ineffective after 72 h of treatment. Our findings suggest that EXOs protect RSV from phase II metabolism and enhance its brain delivery and antiproliferative activity. |
| نوع الوثيقة: | article |
| وصف الملف: | electronic resource |
| اللغة: | English |
| تدمد: | 2666-1543 36967157 |
| Relation: | http://www.sciencedirect.com/science/article/pii/S2666154324004071; https://doaj.org/toc/2666-1543 |
| DOI: | 10.1016/j.jafr.2024.101370 |
| URL الوصول: | https://doaj.org/article/369671571ba04b79a3dfb9c8c8e5ccd2 |
| رقم الانضمام: | edsdoj.369671571ba04b79a3dfb9c8c8e5ccd2 |
| قاعدة البيانات: | Directory of Open Access Journals |
Full Text Finder | تدمد: | 26661543 36967157 |
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| DOI: | 10.1016/j.jafr.2024.101370 |