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  • Effects of flavonoids on cell proliferation and caspase activation in a human colonic cell line HT29: an SAR study.

Effects of flavonoids on cell proliferation and caspase activation in a human colonic cell line HT29: an SAR study.

Journal of medicinal chemistry (2005-04-15)
Jean-Baptiste Daskiewicz, Flore Depeint, Lionel Viornery, Christine Bayet, Geraldine Comte-Sarrazin, Gilles Comte, Jennifer M Gee, Ian T Johnson, Karine Ndjoko, Kurt Hostettmann, Denis Barron
ABSTRACT

A library of 42 natural and synthetic flavonoids has been screened for their effect on cell proliferation and apoptosis in a human colonic cell line (HT-29). Examples of different classes of flavonoids have been screened, and the effects of hydroxylation, methoxylation and/or C-alkylation at various positions in the A- and B-rings have been assessed. Flavones and flavonols possess greater antiproliferative activity than chalcones and flavanones. With respect to structural modification of flavonoids, C-isoprenylation was by far the most effective, with substitution at the 8-position and longer chains, such as geranyl giving the best results. Finally, most compounds that significantly reduced cell survival also increased caspase activity, suggesting that at least part of their antiproliferative activity might be attributable to an apoptotic response.

MATERIALS
Product Number
Brand
Product Description

Sigma-Aldrich
Kaempferol, ≥97.0% (HPLC)
Sigma-Aldrich
Kaempferol, ≥90% (HPLC), powder
Sigma-Aldrich
Chrysin, 97%

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