TY - JOUR
T1 - Synthesis and evaluation of biological activity from two steroid-diazacyclododecin derivatives on left ventricular pressure
AU - Marcela, Rosas Nexticapa
AU - Lauro, Figueroa Valverde
AU - Francisco, Diaz Cedillo
AU - Virginia, Mateu Armand
AU - Maria, Lopez Ramos
AU - Elodia, García Cervera
AU - Eduardo, Pool Gómez
AU - Rolando, García Martínez
AU - Perla, Parra Galindo
AU - Regina, Cauich Carrillo
AU - Alondra, Alfonso Jimenez
AU - Jhai, Cabrera Tuz
N1 - Publisher Copyright:
© 2018 by the authors.
PY - 2018/6/15
Y1 - 2018/6/15
N2 - There are several studies which indicate that some cardiovascular diseases are relationship with biological activity of estrogens through of its receptors activation. The objective of this work was synthesizing two new steroid-diazacyclododecin derivatives (compounds 11 or 12) to evaluate their effect on left ventricular pressure in Langendorff model using as control to 17 β -estradiol. In addition, a theoretical study was carried out to evaluate the interaction of compound 11 or 12 with the estrogen receptor (3os8 protein) using a docking model. The experimental results showed that only the compound 12 decreased left ventricular pressure in a similar form to 17 β -estradiol. In addition, other experimental data showed that effect exerted by 17β-estradiol was inhibited in presence of 12. Finally, theoretical results indicated that interaction of 12 with 3os8 protein involved some aminoacid residues such as Pro224, Leu319, Leu320, Leu327, Asp321, Ala322, Glu323, Pro324, Pro325, Ile326 and Leu327. All these data suggest that compound 12 may act as a selective agonist of estrogen receptor which translated as changes on left ventricular pressure.
AB - There are several studies which indicate that some cardiovascular diseases are relationship with biological activity of estrogens through of its receptors activation. The objective of this work was synthesizing two new steroid-diazacyclododecin derivatives (compounds 11 or 12) to evaluate their effect on left ventricular pressure in Langendorff model using as control to 17 β -estradiol. In addition, a theoretical study was carried out to evaluate the interaction of compound 11 or 12 with the estrogen receptor (3os8 protein) using a docking model. The experimental results showed that only the compound 12 decreased left ventricular pressure in a similar form to 17 β -estradiol. In addition, other experimental data showed that effect exerted by 17β-estradiol was inhibited in presence of 12. Finally, theoretical results indicated that interaction of 12 with 3os8 protein involved some aminoacid residues such as Pro224, Leu319, Leu320, Leu327, Asp321, Ala322, Glu323, Pro324, Pro325, Ile326 and Leu327. All these data suggest that compound 12 may act as a selective agonist of estrogen receptor which translated as changes on left ventricular pressure.
KW - 17 β–estradiol
KW - Derivatives
KW - Docking
KW - Left ventricular pressure
KW - Steroid-diazacyclododeci
UR - http://www.scopus.com/inward/record.url?scp=85052217013&partnerID=8YFLogxK
M3 - Artículo
SN - 2069-5837
VL - 8
SP - 3306
EP - 3313
JO - Biointerface Research in Applied Chemistry
JF - Biointerface Research in Applied Chemistry
IS - 3
ER -
