Synthesis and evaluation of biological activity from two steroid-diazacyclododecin derivatives on left ventricular pressure

Rosas Nexticapa Marcela, Figueroa Valverde Lauro, Diaz Cedillo Francisco, Mateu Armand Virginia, Lopez Ramos Maria, García Cervera Elodia, Pool Gómez Eduardo, García Martínez Rolando, Parra Galindo Perla, Cauich Carrillo Regina, Alfonso Jimenez Alondra, Cabrera Tuz Jhai

Research output: Contribution to journalArticle

Abstract

© 2018 by the authors. 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.
Original languageAmerican English
Pages (from-to)3306-3313
Number of pages2974
JournalBiointerface Research in Applied Chemistry
StatePublished - 15 Jun 2018

Fingerprint

Ventricular Pressure
Bioactivity
Estradiol
Steroids
Derivatives
Estrogens
Proteins
Theoretical Models
Cardiovascular Diseases
Chemical activation

Cite this

Marcela, Rosas Nexticapa ; Lauro, Figueroa Valverde ; Francisco, Diaz Cedillo ; Virginia, Mateu Armand ; Maria, Lopez Ramos ; Elodia, García Cervera ; Eduardo, Pool Gómez ; Rolando, García Martínez ; Perla, Parra Galindo ; Regina, Cauich Carrillo ; Alondra, Alfonso Jimenez ; Jhai, Cabrera Tuz. / Synthesis and evaluation of biological activity from two steroid-diazacyclododecin derivatives on left ventricular pressure. In: Biointerface Research in Applied Chemistry. 2018 ; pp. 3306-3313.
@article{66c736ea878a4ae292947bba6913e72e,
title = "Synthesis and evaluation of biological activity from two steroid-diazacyclododecin derivatives on left ventricular pressure",
abstract = "{\circledC} 2018 by the authors. 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.",
author = "Marcela, {Rosas Nexticapa} and Lauro, {Figueroa Valverde} and Francisco, {Diaz Cedillo} and Virginia, {Mateu Armand} and Maria, {Lopez Ramos} and Elodia, {Garc{\'i}a Cervera} and Eduardo, {Pool G{\'o}mez} and Rolando, {Garc{\'i}a Mart{\'i}nez} and Perla, {Parra Galindo} and Regina, {Cauich Carrillo} and Alondra, {Alfonso Jimenez} and Jhai, {Cabrera Tuz}",
year = "2018",
month = "6",
day = "15",
language = "American English",
pages = "3306--3313",
journal = "Biointerface Research in Applied Chemistry",
issn = "2069-5837",
publisher = "AMG Transcend Association",

}

Marcela, RN, Lauro, FV, Francisco, DC, Virginia, MA, Maria, LR, Elodia, GC, Eduardo, PG, Rolando, GM, Perla, PG, Regina, CC, Alondra, AJ & Jhai, CT 2018, 'Synthesis and evaluation of biological activity from two steroid-diazacyclododecin derivatives on left ventricular pressure', Biointerface Research in Applied Chemistry, pp. 3306-3313.

Synthesis and evaluation of biological activity from two steroid-diazacyclododecin derivatives on left ventricular pressure. / Marcela, Rosas Nexticapa; Lauro, Figueroa Valverde; Francisco, Diaz Cedillo; Virginia, Mateu Armand; Maria, Lopez Ramos; Elodia, García Cervera; Eduardo, Pool Gómez; Rolando, García Martínez; Perla, Parra Galindo; Regina, Cauich Carrillo; Alondra, Alfonso Jimenez; Jhai, Cabrera Tuz.

In: Biointerface Research in Applied Chemistry, 15.06.2018, p. 3306-3313.

Research output: Contribution to journalArticle

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

PY - 2018/6/15

Y1 - 2018/6/15

N2 - © 2018 by the authors. 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 - © 2018 by the authors. 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.

UR - https://www.scopus.com/inward/record.uri?partnerID=HzOxMe3b&scp=85052217013&origin=inward

UR - https://www.scopus.com/inward/citedby.uri?partnerID=HzOxMe3b&scp=85052217013&origin=inward

M3 - Article

SP - 3306

EP - 3313

JO - Biointerface Research in Applied Chemistry

JF - Biointerface Research in Applied Chemistry

SN - 2069-5837

ER -