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Anticancer activity of a quercetin-based polymer towards HeLa cancer cells
Francesco Puoci1, Catia Morelli, Giuseppe Cirillo
1Department of Pharmaceutical Sciences, University of Calabria, Arcavacata di Rende (CS), 87036, Italy. francesco.puoci@unical.it
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.
