BACKGROUND: Quercetin is one of the most potent antioxidants showing anti-inflammatory, antiproliferative and antitumoral effects; however its short half-life in buffered solution (e.g. body fluids) has so far hampered its introduction into clinical practice. Aim: To overcome this inconvenience, quercetin was covalently conjugated into a polymethacrylic acid backbone and the conjugate was tested on HeLa cancer cells. MATERIALS AND METHODS: FT-IR, UV-Vis, Gel Permeation Chromatography analyses and the Folin-Ciocalteu test were performed to characterize the conjugate. Antioxidant properties were assessed by the DPPH test and the viability experiments by trypan blue exclusion assay. RESULTS: The conjugate showed a functionalization degree of 2.01 mg of Q per g, an IC(50) of 2.62 mg ml(-1) in the DPPH assay and was able to induce a 90% cell death after one day treatment, while the value for free Quercetin was 40% after three days. CONCLUSION: Polymer conjugation significantly increases quercetin stability, leading to a sustained activity of the flavonoid.

Anticancer Activity of a Quercetin-based Polymer Towards HeLa Cancer Cells

PUOCI, Francesco;Morelli C;Cirillo G;Curcio M;SISCI, Diego;PICCI, Nevio
2012

Abstract

BACKGROUND: Quercetin is one of the most potent antioxidants showing anti-inflammatory, antiproliferative and antitumoral effects; however its short half-life in buffered solution (e.g. body fluids) has so far hampered its introduction into clinical practice. Aim: To overcome this inconvenience, quercetin was covalently conjugated into a polymethacrylic acid backbone and the conjugate was tested on HeLa cancer cells. MATERIALS AND METHODS: FT-IR, UV-Vis, Gel Permeation Chromatography analyses and the Folin-Ciocalteu test were performed to characterize the conjugate. Antioxidant properties were assessed by the DPPH test and the viability experiments by trypan blue exclusion assay. RESULTS: The conjugate showed a functionalization degree of 2.01 mg of Q per g, an IC(50) of 2.62 mg ml(-1) in the DPPH assay and was able to induce a 90% cell death after one day treatment, while the value for free Quercetin was 40% after three days. CONCLUSION: Polymer conjugation significantly increases quercetin stability, leading to a sustained activity of the flavonoid.
Quercitin; Polymer conjugation
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/20.500.11770/141666
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