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Updated: Jun 1, 2026

Biosynthesis of a Flavonol from a Flavanone by Establishing a One-pot Bienzymatic Cascade
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Biosynthesis of a Flavonol from a Flavanone by Establishing a One-pot Bienzymatic Cascade

Published on: August 14, 2019

In vitro activity of dietary flavonol congeners against human cancer cell lines

Chrisiida Tsimplouli1, Costas Demetzos, Margarita Hadzopoulou-Cladaras

  • 1Division of Pharmacology-Pharmacotechnology, Biomedical Research Foundation, Academy of Athens, Athens, Greece.

European Journal of Nutrition
|May 21, 2011
PubMed
Abstract

Insights

Dietary flavonols show weak anticancer activity, but modifying their sugar components, like in peracetylated tiliroside, significantly enhances their antiproliferative and cytotoxic effects against human solid tumors.

Area of Science:

  • Natural Products Chemistry
  • Pharmacology
  • Cancer Biology

Background:

  • Flavonoids possess diverse pharmacological properties, including potential anticancer activity.
  • Structure-activity relationships of flavonoids against cancer remain largely undefined.
  • Investigating dietary flavonols offers insights into novel anticancer agents.

Purpose of the Study:

  • To evaluate the anticancer potential of dietary flavonol congeners against human solid tumor cell lines.
  • To determine if specific structural features correlate with observed in vitro anticancer activity.
  • To elucidate the role of chemical modifications in enhancing flavonol efficacy.

Main Methods:

  • Assessed antiproliferative and cytotoxic effects using the sulforhodamine B (SRB) assay against eight human cancer cell lines.
  • Analyzed cell cycle perturbations via flow cytometry with propidium iodide staining.
  • Monitored induction of apoptosis in treated cancer cells.

Main Results:

  • Most tested flavonols exhibited limited antiproliferative and cytotoxic effects.
  • Peracetylated tiliroside demonstrated significant antiproliferative and cytotoxic activity.
  • Peracetylated tiliroside uniquely induced apoptosis, unlike other tested flavonols.

Conclusions:

  • Hydroxyl groups on aromatic ring B are not critical for cytotoxic or antiproliferative activity.
  • Peracetylation of glycosides offers a moderate improvement in activity.
  • Acetylation of the sugar moiety in tiliroside, specifically with coumaric acid, substantially enhances anticancer efficacy.
  • Substituents on the sugar moiety play a crucial role in the anticancer activity of flavonols.

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