<p>Quercetin (QCT), a potent flavonoid with recognized antioxidant and anticancer properties, faces limitations due to its poor water solubility, low stability, and limited bioavailability. Here, we introduce a novel, cost-effective, and rapid one-step oxidative self-polymerization approach using manganese dioxide (MnO₂) nanosheets to synthesize monodispersed polyquercetin (PQCT) nanoparticles under neutral pH conditions. The resulting PQCT nanoparticles (&lt; 50&#xa0;nm) exhibited high aqueous solubility, long-term thermal and colloidal stability, and uniform morphology, as confirmed by UV-Vis, TGA, FESEM, and DLS analyses. Despite a moderate decrease in antioxidant activity compared to free QCT, PQCT demonstrated significantly improved anticancer efficacy against HCT116 colon cancer cells, with a 2-fold lower IC50 (21.98 ± 0.97&#xa0;µg/mL) than QCT. Flow cytometry and RT-qPCR analyses further revealed that PQCT enhances apoptosis via upregulation of proapoptotic Bax and suppression of antiapoptotic Bcl2 and Survivin genes. PQCT also displayed high biocompatibility in normal HFF cells up to 80&#xa0;µg/mL. These findings position MnO₂-derived PQCT nanoparticles as promising multifunctional agents for nutraceutical and oncological applications, offering improved physicochemical properties and therapeutic potential over native quercetin.</p>

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Polyquercetin nanoparticles: enhanced anticancer activity with improved solubility and stability for biomedical and food applications

  • Hajar Jaberie,
  • Safieh Momeni,
  • Alireza Khosravani

摘要

Quercetin (QCT), a potent flavonoid with recognized antioxidant and anticancer properties, faces limitations due to its poor water solubility, low stability, and limited bioavailability. Here, we introduce a novel, cost-effective, and rapid one-step oxidative self-polymerization approach using manganese dioxide (MnO₂) nanosheets to synthesize monodispersed polyquercetin (PQCT) nanoparticles under neutral pH conditions. The resulting PQCT nanoparticles (< 50 nm) exhibited high aqueous solubility, long-term thermal and colloidal stability, and uniform morphology, as confirmed by UV-Vis, TGA, FESEM, and DLS analyses. Despite a moderate decrease in antioxidant activity compared to free QCT, PQCT demonstrated significantly improved anticancer efficacy against HCT116 colon cancer cells, with a 2-fold lower IC50 (21.98 ± 0.97 µg/mL) than QCT. Flow cytometry and RT-qPCR analyses further revealed that PQCT enhances apoptosis via upregulation of proapoptotic Bax and suppression of antiapoptotic Bcl2 and Survivin genes. PQCT also displayed high biocompatibility in normal HFF cells up to 80 µg/mL. These findings position MnO₂-derived PQCT nanoparticles as promising multifunctional agents for nutraceutical and oncological applications, offering improved physicochemical properties and therapeutic potential over native quercetin.