Anticancer activity of a quercetin-based polymer towards HeLa cancer cells.

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.
To overcome this inconvenience, quercetin was covalently conjugated into a polymethacrylic acid backbone and the conjugate was tested on HeLa cancer cells.
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.
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.
Polymer conjugation significantly increases quercetin stability, leading to a sustained activity of the flavonoid.
AuthorsFrancesco Puoci, Catia Morelli, Giuseppe Cirillo, Manuela Curcio, Ortensia Ilaria Parisi, Pamela Maris, Diego Sisci, Nevio Picci
JournalAnticancer research (Anticancer Res) Vol. 32 Issue 7 Pg. 2843-7 (Jul 2012) ISSN: 1791-7530 [Electronic] Greece
PMID22753746 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
Chemical References
  • Antineoplastic Agents
  • Antioxidants
  • Polymethacrylic Acids
  • Quercetin
  • Antineoplastic Agents (chemical synthesis, chemistry, pharmacology)
  • Antioxidants (chemical synthesis, chemistry, pharmacology)
  • Chromatography, Gel
  • Drug Screening Assays, Antitumor
  • Drug Stability
  • HeLa Cells
  • Humans
  • Polymethacrylic Acids (chemical synthesis, chemistry, pharmacology)
  • Quercetin (analogs & derivatives, chemical synthesis, chemistry, pharmacology)
  • Spectrophotometry, Ultraviolet
  • Spectroscopy, Fourier Transform Infrared

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