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  • Phytoestrogens as inhibitors of fungal 17ß-hydroxysteroid dehydrogenase
    Kristan, Katja, 1975- ...
    Different phytoestrogens were tested as inhibitors of 17B-hydroxysteroid dehydrogenase from the fungus Cochliobolus lunatus (17BHSDcI), a member of theshort-chain dehydrogenase/reductase superfamily. ... Phytoestrogens inhibited the oxidation of 100 uM 17B-hydroxyestra-4-en-3-one and the reduction of 100 uM estra-4-en-3,17-dione, the best substrate pair known. The best inhibitors of oxidation, with IC50 below 1 uM, were flavones hydroxylated at positions 3,5 and 7: 3-hydroxyflavone, 3,7-dihydroxyftavone, 5,7-dihydroxyftavone (chrysin) and 5-hydroxyflavone, together with 5-methoxyflavone. The best inhibitors of reduction were less potent; 3-hydroxyflavone, 5-methoxyflavone, coumestrol, 3,5,7,4'-tetrahydroxyflavone (kaempferol) and 5-hydroxyflavone, all had IC50 values between 1 and 5 uM. Docking the representative inhibitors chrysin and kaempferol into the active site of 17B-HSDcI revealed the possiblebinding mode, in which they are sandwiched between the nicotinamide moiety and Tyr212. The structural features of phytoestrogens, inhibitors of both oxidation and reduction catalyzed by the fungal 17B-HSD, are similar to the reported structural features of phytoestrogen inhibitors of human 17B-HSD types 1 and 2.
    Vir: Steroids. - ISSN 0039-128X (no. 9, Vol. 70, 2005, str. 626-635)
    Vrsta gradiva - članek, sestavni del
    Leto - 2005
    Jezik - angleški
    COBISS.SI-ID - 19811033
vir: Steroids. - ISSN 0039-128X (no. 9, Vol. 70, 2005, str. 626-635)
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