- Effects of (+)-, (-)- and (±)-indenestrols A and B on microtubule polymerization
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Indenestrol A (IA) is a metabolite of diethylstilbestrol (DES), and indenestrol B (IB) is an analog of IA. IA was simply obtained from E,E-dienestrol in the presence of dilute sulfuric acid, and a mixture of IA and IB was formed by thermal cyclization of
- Oda,Sakakibara,Sato,Hanzawa,Hata
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p. 588 - 592
(2007/10/02)
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- NON-ESTROGENIC METABOLITES OF DIETHYLSTILBESTROL PRODUCED BY PROSTAGLANDIN SYNTHASE MEDIATED METABOLISM
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Incubation of trans-diethylstilbestrol (E-DES) with prostaglandin synthase (PGS) in vitro leads to the formation of the metabolites cis,cis-dienestrol (Z,Z-DIES) and cis-diethylstilbestrol (Z-DES) which have considerably decreased estrogenic activity compared to their parent compound.Incubations of (14C)-E-DES with PGS in the presence of arachidonic acid (AA) predominantly catalyze formation of the oxidative metabolite Z,Z-DIES, accompanied by the formation of protein bound radioactivity.Inhibition of peroxidative metabolism through addition of indomethacin or absence of AA favors isomerization of E-DES to Z-DES without concomitant formation of protein bound radioactivity.Isomerization is inhibited by phenidone (1-phenyl-3-pyrazolidone).Since PGS activity is present in uterine tissue, these pathways may play a role in the metabolism of DES in its target tissue.
- Degen, Gisela H.,McLachlan, John A.
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p. 253 - 266
(2007/10/02)
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