Napisał
fallenursus
Inhibition of prostaglandin E2 production by flavone and its related compounds.
[link widoczny dla zalogowanych Użytkowników], [link widoczny dla zalogowanych Użytkowników], [link widoczny dla zalogowanych Użytkowników], [link widoczny dla zalogowanych Użytkowników], [link widoczny dla zalogowanych Użytkowników], [link widoczny dla zalogowanych Użytkowników], [link widoczny dla zalogowanych Użytkowników], [link widoczny dla zalogowanych Użytkowników].
Department of Oral and Maxillofacial Surgery, Tokyo Medical University, Shinjyuku-ku, Tokyo, Japan.
Abstract
We have previously reported that among 12 major ingredients of Sairei-to, Scutellariae radix inhibited prostaglandin E(2) (PGE(2)) production by lipopolysaccharide (LPS)-activated mouse macrophage-like RAW264.7 cells more efficiently than other ingredients, and wogonin, a major flavonoid from Scutellariae radix, showed greater inhibitory activity and membrane permeability than baicalein and baicalin. Here the effects of six other flavonoids, with similar structures, on membrane permeability and PGE(2) production were investigated. 7-Methoxyflavone inhibited the LPS-stimulated PGE(2) production to the greatest extent, followed by flavone>wogonin (5,7-dihydroxy-8-methoxyflavone)>> 7,8-dimethoxyflavone>chrysin (5,7-dihydroxyflavone)> baicalein (5,6,7-trihydroxyflavone)>>chromone. 7-Methoxyflavone also showed the highest membrane permeability, followed by flavone>chrysin>7,8-dimethoxy-flavone>wogonin>baicalein. When PGE(2) inhibitory activity was expressed per molecule incorporated into the cells, wogonin produced the greatest inhibition, further substantiating its anti-inflammatory potency.
dalej nie chce mi sie szukajc
ale tu udowodnili ze inhibituje estro.
[link widoczny dla zalogowanych Użytkowników] 2007 Oct;107(1-2):127-9. Epub 2007 Jun 6.
Aromatase inhibition by bioavailable methylated flavones.
[link widoczny dla zalogowanych Użytkowników], [link widoczny dla zalogowanych Użytkowników].
Department of Cell and Molecular Pharmacology & Experimental Therapeutics, Medical University of South Carolina, 173 Ashley Avenue, Charleston, SC 29425, USA.
Abstract
Previous studies have shown chrysin, 7-hydroxyflavone and 7,4'-dihydroxyflavone to be the most potent flavonoid inhibitors of aromatase. However, very poor oral bioavailability is a major limitation for the successful use of dietary flavonoids as chemopreventive agents. We have recently shown that methylated flavones, including 5,7-dimethoxyflavone, 7-methoxyflavone and 7,4'-dimethoxyflavone, are much more resistant to metabolism than their unmethylated analogs and have much higher intestinal absorption. In this study, we examined these fully methylated flavones as potential aromatase inhibitors for the prevention and/or treatment of hormone-dependent cancers. Whereas 5,7-dimethoxyflavone had poor effect compared to its unmethylated analog chrysin, 7-methoxyflavone and 7,4'-dimethoxyflavone were almost equipotent to their unmethylated analogs with IC(50) values of 2-9 microM. Thus, some fully methylated flavones appear to have great potential as cancer chemopreventive/chemotherapeutic agents
tu twierdza to samo, z ta roznica ze wchlanianie jest bardzo kiepskie.
Connect with Facebook
Nagrody:
Odpowiedź z Cytatem
