The structures and inhibitory effects of Buame [N-(3-hydroxy-1,3,5(10)-estratrien-17尾-yl)-butylamine] and Diebud [N,N鈥?bis-(3-hydroxy-1,3,5(10)-estratrien-17尾-yl)-1,4-butanediamine] on platelet aggregation

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• 作者：Mirthala Flores-Garcí ; a^a ; ^d ; Juan M. Ferná ; ndez-G^c ; ^{jmanuel@servidor.unam.mx} ; Mireille Le&oacute ; n-Martí ; nez^c ; Sim&oacute ; n Herná ; ndez-Ortega^c ; Oscar Pé ; rez-Mé ; ndez^a ; José ; Correa-Basurto^d ; Elizabeth Carre&oacute ; n-Torres^a ; Luis E. Tolentino-L&oacute ; pez^d ; Guillermo Manuel Ceballos-Reyes^d ; Aurora de la Peñ ; a-Dí ; az^a ; ^b ; ¹ ; ^{aurorade2002@yahoo.com}
• 关键词：Aminoestrogen ; Buame ; Diebud ; Platelet inhibition
• 刊名：Steroids
• 出版年：2012
• 期刊代码：142_0039128x
• 类别：bio
• 出版时间：April, 2012
• 卷：77
• 期：5
• 页码：512-520
• 文件大小：1122 K

摘要

Compounds with estrogenic effects that also inhibit platelet aggregation might be useful in reducing thrombotic events associated with estrogenic therapy. In this study, two aminoestrogens, Buame [N-(3-hydroxy-1,3,5(10)-estratrien-17尾-yl)-butylamine] and Diebud [N,N鈥?bis-(3-hydroxy-1,3,5(10)-estratrien-17尾-yl)-1,4-butanediamine], were synthesized and characterized using common analytical methods and spectrophotometric analyses. The location and orientation of these molecules on the estrogenic receptor 伪 (ER伪) were also evaluated. Platelet inhibitory effects were elucidated ADP-induced platelet aggregation and ADP- and collagen-induced ATP release. Molecular docking demonstrated that Buame can reach and bind to the ER伪 in the ligand binding domain (LBD) similar to 17尾-estradiol (co-crystallized ligand). On the other hand, Diebud binds only to the surface of ER伪 due to its high molecular volume compared to 17尾-estradiol and Buame.