TY - JOUR
T1 - Antihypertensive properties of a novel morphologic derivative (4-Tert-buthyl-2,6-bis (thiomorpholine-4-ilmethyl)phenol)
AU - Martínez-Aguilar, Luisa
AU - Lezama-Martínez, Diego
AU - Orozco-Cortés, Nancy V.
AU - González-Espinosa, Claudia
AU - Flores-Monroy, Jazmin
AU - Valencia-Hernández, Ignacio
N1 - Publisher Copyright:
Copyright © 2015 Wolters Kluwer Health, Inc. All rights reserved.
PY - 2016/3
Y1 - 2016/3
N2 - We evaluated the antihypertensive properties of 4-Tertbuthyl-2,6-bis(thiomorpholine-4-ilmethyl)phenol (TBTIF). Spontaneously hypertensive rats were treated with TBTIF or captopril (both at 1 mgkg-1d-1 intramuscularly for 4 days), and their blood pressure (BP) was assessed. In some experiments, concentration response curves to angiotensin I or angiotensin II were generated in rat aortic rings and in the absence or presence of Ang-(1-7), NG-monomethyl L-Arginine, or both; additionally, the angiotensin-converting enzyme (ACE) and ACE2 mRNA levels were quantified in the aortic rings using reverse transcription- polymerase chain reaction. TBTIF diminished BP and reduced angiotensin I-or angiotensin II-induced vasoconstriction. The presence of Ang-(1-7) induced a greater reduction in vasoconstriction, and this effect was reversed by L-NG-monomethyl arginine. Moreover, TBTIF decreased the mRNA of ACE and increased the mRNA of ACE2. In conclusion, TBTIF diminished rat BP through nitric oxide-dependent and nitric oxide-independent mechanisms. In contrast to captopril, TBTIF exhibits better antihypertensive properties through mechanisms that involve ACE2.
AB - We evaluated the antihypertensive properties of 4-Tertbuthyl-2,6-bis(thiomorpholine-4-ilmethyl)phenol (TBTIF). Spontaneously hypertensive rats were treated with TBTIF or captopril (both at 1 mgkg-1d-1 intramuscularly for 4 days), and their blood pressure (BP) was assessed. In some experiments, concentration response curves to angiotensin I or angiotensin II were generated in rat aortic rings and in the absence or presence of Ang-(1-7), NG-monomethyl L-Arginine, or both; additionally, the angiotensin-converting enzyme (ACE) and ACE2 mRNA levels were quantified in the aortic rings using reverse transcription- polymerase chain reaction. TBTIF diminished BP and reduced angiotensin I-or angiotensin II-induced vasoconstriction. The presence of Ang-(1-7) induced a greater reduction in vasoconstriction, and this effect was reversed by L-NG-monomethyl arginine. Moreover, TBTIF decreased the mRNA of ACE and increased the mRNA of ACE2. In conclusion, TBTIF diminished rat BP through nitric oxide-dependent and nitric oxide-independent mechanisms. In contrast to captopril, TBTIF exhibits better antihypertensive properties through mechanisms that involve ACE2.
KW - Ace
KW - Angiotensin (1-7)
KW - Angiotensin I
KW - Angiotensin II
KW - Hypertension
KW - Thiomorpholin
UR - http://www.scopus.com/inward/record.url?scp=84962539356&partnerID=8YFLogxK
U2 - 10.1097/FJC.0000000000000340
DO - 10.1097/FJC.0000000000000340
M3 - Artículo
C2 - 26566152
SN - 0160-2446
VL - 67
SP - 246
EP - 251
JO - Journal of Cardiovascular Pharmacology
JF - Journal of Cardiovascular Pharmacology
IS - 3
ER -