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Effects of flavonoids on cell proliferation and caspase activation in a human colonic cell line HT29: an SAR study.
J Med Chem. 2005 Apr 21; 48(8):2790-804.JM

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.

Authors+Show Affiliations

Laboratoire des Produits Naturels, CNRS-UMR 5013, UFR de Chimie-Biochimie, Université Claude Bernard Lyon 1, 43 Boulevard du 11 Novembre 1918, 69622 Villeurbanne, France.No affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

15828817

Citation

Daskiewicz, Jean-Baptiste, et al. "Effects of Flavonoids On Cell Proliferation and Caspase Activation in a Human Colonic Cell Line HT29: an SAR Study." Journal of Medicinal Chemistry, vol. 48, no. 8, 2005, pp. 2790-804.
Daskiewicz JB, Depeint F, Viornery L, et al. Effects of flavonoids on cell proliferation and caspase activation in a human colonic cell line HT29: an SAR study. J Med Chem. 2005;48(8):2790-804.
Daskiewicz, J. B., Depeint, F., Viornery, L., Bayet, C., Comte-Sarrazin, G., Comte, G., Gee, J. M., Johnson, I. T., Ndjoko, K., Hostettmann, K., & Barron, D. (2005). Effects of flavonoids on cell proliferation and caspase activation in a human colonic cell line HT29: an SAR study. Journal of Medicinal Chemistry, 48(8), 2790-804.
Daskiewicz JB, et al. Effects of Flavonoids On Cell Proliferation and Caspase Activation in a Human Colonic Cell Line HT29: an SAR Study. J Med Chem. 2005 Apr 21;48(8):2790-804. PubMed PMID: 15828817.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Effects of flavonoids on cell proliferation and caspase activation in a human colonic cell line HT29: an SAR study. AU - Daskiewicz,Jean-Baptiste, AU - Depeint,Flore, AU - Viornery,Lionel, AU - Bayet,Christine, AU - Comte-Sarrazin,Geraldine, AU - Comte,Gilles, AU - Gee,Jennifer M, AU - Johnson,Ian T, AU - Ndjoko,Karine, AU - Hostettmann,Kurt, AU - Barron,Denis, PY - 2005/4/15/pubmed PY - 2005/5/25/medline PY - 2005/4/15/entrez SP - 2790 EP - 804 JF - Journal of medicinal chemistry JO - J Med Chem VL - 48 IS - 8 N2 - 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. SN - 0022-2623 UR - https://www.unboundmedicine.com/medline/citation/15828817/Effects_of_flavonoids_on_cell_proliferation_and_caspase_activation_in_a_human_colonic_cell_line_HT29:_an_SAR_study_ DB - PRIME DP - Unbound Medicine ER -