Effects of flavonoids on cell proliferation and caspase activation in a human colonic cell line HT29: an SAR study
| Autor: | Karine Ndjoko, Denis Barron, Christine Bayet, Flore Depeint, Jennifer M. Gee, Kurt Hostettmann, Ian T. Johnson, Jean-Baptiste Daskiewicz, Lionel Viornery, Geraldine Comte-Sarrazin, Gilles Comte |
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| Rok vydání: | 2005 |
| Předmět: |
Alkylation
INDUCE APOPTOSIS Flavonoid Enzyme Activators CARCINOMA-CELLS Antineoplastic Agents Apoptosis ANTIPROLIFERATIVE ACTIVITIES Hydroxylation Flavones Structure-Activity Relationship Flavonols Chalcone Cell Line Tumor Drug Discovery Humans MULTIDRUG-RESISTANCE Cytotoxicity DIET-RELATED APOPTOSIS Caspase Cell Proliferation chemistry.chemical_classification Flavonoids STRUCTURAL REQUIREMENTS biology Cell growth CITRUS FLAVONOIDS MYELOID-LEUKEMIA CELLS Biochemistry chemistry Cell culture Caspases Colonic Neoplasms HUMAN CANCER-CELLS biology.protein Molecular Medicine CARBOXYLIC-ACID ANHYDRIDES |
| Zdroj: | Journal of Medicinal Chemistry, Vol. 48, No 8 (2005) pp. 2790-2804 |
| ISSN: | 0022-2623 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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