- Myricitrin preparation method
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The invention belongs to the technical field of pharmaceutical chemical synthesis, in particular relates to a preparation method of the slots. The invention the equivalent preparation method is as follows: a, in order to 1 - 1 as shown in the compound as a raw material, with the methoxy second grade nitrile under acidic conditions in the acylation reaction to obtain 1 - 3 as shown in the; second, 1 - 3 is shown with the compound 3, 4, 5 - trimethoxy benzoic anhydride generating rearrangement reaction to 1 - 5 as shown in the; three, 1 - 5 shown BBr3 compound in the dichloromethane solution takes place in the demethylation reaction generating 3 - 1 compound of formula, is myricetin. The invention relates to a fully synthetic routes proceed from the phloroglucinol, by the three-step reaction, to 60% of the total yield has succeeded in synthesizing myricetin. With cheap raw material, mild reaction conditions, synthetic route is short, and the yield is high, the operation is simple, and little environmental pollution and the like.
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- Effects of flavonoids on cell proliferation and caspase activation in a human colonic cell line HT29: An SAR study
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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.
- Daskiewicz, Jean-Baptiste,Depeint, Flore,Viornery, Lionel,Bayet, Christine,Comte-Sarrazin, Geraldine,Comte, Gilles,Gee, Jennifer M.,Johnson, Ian T.,Ndjoko, Karine,Hostettmann, Kurt,Barron, Denis
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p. 2790 - 2804
(2007/10/03)
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