TY - JOUR
T1 - Pharmacological basis for the medicinal use of polyherbal formulation and its ingredients in cardiovascular disorders using rodents
AU - Malik, Abdul
AU - Mehmood, Malik Hassan
AU - Channa, Hajra
AU - Akhtar, Muhammad Shoaib
AU - Gilani, Anwarul Hassan
N1 - Publisher Copyright:
© 2017 The Author(s).
PY - 2017/3/7
Y1 - 2017/3/7
N2 - Background: A compound herbal formulation (POL4) has been used in the indigenous system of medicine to treat cardiometabolic disorders like diabetes and associated hypertension. POL4 and most of its constituents have not been studied widely for its therapeutic use in hypertension. This study is aimed to determine the efficacy and possible insight into mechanism(s) for the medicinal use of POL4 and its ingredients in hypertension. Methods: The aqueous methanolic extracts of POL4 (POL4.Cr) and its components [Cichorium intybus (Ci.Cr), Gymnema sylvestre (Gs.Cr), Nigella sativa (Ns.Cr) and Trigonella foenum graecum (Tfg.Cr)] were tested for blood pressure lowering activity in anaesthetized Sprague-Dawley rats. To assess the vasomodulatory effect, isolated tissue experiments were performed on rat aortic strips using isometric force transducer coupled with PowerLab data acquisition system. Results: Administration of POL4 to rats caused a dose-dependent (1-100 mg/kg) fall in mean arterial pressure (MAP) with maximum effect of 85.33 ± 1.76% at 100 mg/kg, similar to the effect of verapamil. All ingredients of POL4 also decreased blood pressure with varying efficacy in following order Ns.Cr Ci.Cr > Tfg.Cr > Gs.Cr. In rat aortic preparations, POL4 and its ingredients inhibited K+ (80 mM)-induced contractions, Ci.Cr was the most potent followed by Ns.Cr > Tfg.Cr > Gs.Cr POL4. Against phenylephrine (P.E) contractions, Ci.Cr and Tfg.Cr exhibited complete relaxation, while POL4.Cr, Gs.Cr and Ns.Cr showed vasomodulatory effect. The Ca++ antagonist activity was confirmed when POL4 and its ingredients shifted Ca++ concentrations-response curves to the right in a manner similar to that of verapamil. On baseline of rat aorta, the parent formulation and its ingredients (except Tfg.Cr) exhibited partially phentolamine (1 μM)-sensitive vasoconstriction. Conclusion: These data show that POL4 and its constituents possess blood pressure lowering activity mediated through inhibition of Ca++ influx via membranous Ca++ channels and receptor (α-adrenergic) operated pathways. Thus, this study provides a rationale to the medicinal use of POL4 and its constituents in hypertension.
AB - Background: A compound herbal formulation (POL4) has been used in the indigenous system of medicine to treat cardiometabolic disorders like diabetes and associated hypertension. POL4 and most of its constituents have not been studied widely for its therapeutic use in hypertension. This study is aimed to determine the efficacy and possible insight into mechanism(s) for the medicinal use of POL4 and its ingredients in hypertension. Methods: The aqueous methanolic extracts of POL4 (POL4.Cr) and its components [Cichorium intybus (Ci.Cr), Gymnema sylvestre (Gs.Cr), Nigella sativa (Ns.Cr) and Trigonella foenum graecum (Tfg.Cr)] were tested for blood pressure lowering activity in anaesthetized Sprague-Dawley rats. To assess the vasomodulatory effect, isolated tissue experiments were performed on rat aortic strips using isometric force transducer coupled with PowerLab data acquisition system. Results: Administration of POL4 to rats caused a dose-dependent (1-100 mg/kg) fall in mean arterial pressure (MAP) with maximum effect of 85.33 ± 1.76% at 100 mg/kg, similar to the effect of verapamil. All ingredients of POL4 also decreased blood pressure with varying efficacy in following order Ns.Cr Ci.Cr > Tfg.Cr > Gs.Cr. In rat aortic preparations, POL4 and its ingredients inhibited K+ (80 mM)-induced contractions, Ci.Cr was the most potent followed by Ns.Cr > Tfg.Cr > Gs.Cr POL4. Against phenylephrine (P.E) contractions, Ci.Cr and Tfg.Cr exhibited complete relaxation, while POL4.Cr, Gs.Cr and Ns.Cr showed vasomodulatory effect. The Ca++ antagonist activity was confirmed when POL4 and its ingredients shifted Ca++ concentrations-response curves to the right in a manner similar to that of verapamil. On baseline of rat aorta, the parent formulation and its ingredients (except Tfg.Cr) exhibited partially phentolamine (1 μM)-sensitive vasoconstriction. Conclusion: These data show that POL4 and its constituents possess blood pressure lowering activity mediated through inhibition of Ca++ influx via membranous Ca++ channels and receptor (α-adrenergic) operated pathways. Thus, this study provides a rationale to the medicinal use of POL4 and its constituents in hypertension.
KW - Antihypertensive
KW - Ca antagonist
KW - POL
KW - Vasomodulatory
KW - α-adrenergic antagonist
UR - http://www.scopus.com/inward/record.url?scp=85014704336&partnerID=8YFLogxK
U2 - 10.1186/s12906-017-1644-0
DO - 10.1186/s12906-017-1644-0
M3 - Article
C2 - 28270141
AN - SCOPUS:85014704336
SN - 1472-6882
VL - 17
JO - BMC Complementary and Alternative Medicine
JF - BMC Complementary and Alternative Medicine
IS - 1
M1 - 142
ER -