“…To evaluate ex vivo blood vessel function, rabbit aortic rings were prepared, and the effects of crude Anogeissus acuminata (Aa.Cr), its water fraction (Aa.Aq) and organic fraction (Aa.Dcm) were evaluated against phenylephrine (1 µM) and K + (80 mM) simulated contractions and compared with standard calcium channel blocker verapamil. K + (80 mM) is tissue organ bath concentration of 10-20 mL organ bath for isolated aorta, is being used in a series of already established experiments [32][33][34]. K + (80 mM) simulated contractions have the ability to depolarize the cell membrane for an enhanced period of time either via conductance of calcium ions toward the cell or increased intracellular calcium ions level culminating in strong contractile forces [32].…”
Section: Discussionmentioning
confidence: 99%
“…Standard calcium channel blocker Verapamil also completely relaxed both phenylephrine (1 µM) and K + (80 mM) simulated contractions. The most probable mechanism of relaxation by Aa.Cr, Aa.Aq and Aa.Dcm is calcium channel blocking activity [34]. The Ca ++ channel blocking activity is reported to have a curative effect not only by lowering the blood pressure elevation but also by decreasing the sympathetic activities of the heart in the left ventricular hypertrophy caused by hypertension [35].…”
Section: Discussionmentioning
confidence: 99%
“…Accomplishment of concentration dependent inhibitory response is dependent on applying test material in additive manner to sustained contractions. Percent (%) of control contraction response is used to show the relaxant effect of test material on simulated contractions [34].…”
Section: Mechanism Of Calcium Channel Blockadementioning
Anogeissus acuminata (Roxb. ex DC.) is a folkloric medicinal plant in Asia; including Pakistan; used as a traditional remedy for cardiovascular disorders. This study was planned to establish a pharmacological basis for the trivial uses of Anogeissus acuminata in certain medical conditions related to cardiovascular systems and to explore the underlying mechanisms. Mechanistic studies suggested that crude extract of Anogeissus acuminata (Aa.Cr) produced in vitro cardio-relaxant and vasorelaxant effects in isolated paired atria and aorta coupled with in vivo decrease in blood pressure by invasive method; using pressure and force transducers connected to Power Lab Data Acquisition System. Moreover; Aa.Cr showed positive effects in left ventricular hypertrophy in Sprague Dawley rats observed hemodynamically by a decrease in cardiac cell size and fibrosis; along with absence of inflammatory cells; coupled with reduced levels of angiotensin converting enzyme (ACE) and renin concentration along with increased concentrations of nitric oxide (NO) and cyclic guanosine monophosphate (cGMP). In Acute Myocardial Infarction (AMI) model; creatine kinase (CK), creatine kinase-MB (CK-MB) and lactic acid dehydrogenase (LDH levels) were found to be decreased; along with decreased necrosis; edema and recruitment of inflammatory cells histologically. In vivo and ex vivo studies of Anogeissus acuminata provided evidence of vasorelaxant; hypotensive and cardioprotective properties facilitated through blockage of voltage-gated Ca++ ion channel; validating its use in cardiovascular diseases
“…To evaluate ex vivo blood vessel function, rabbit aortic rings were prepared, and the effects of crude Anogeissus acuminata (Aa.Cr), its water fraction (Aa.Aq) and organic fraction (Aa.Dcm) were evaluated against phenylephrine (1 µM) and K + (80 mM) simulated contractions and compared with standard calcium channel blocker verapamil. K + (80 mM) is tissue organ bath concentration of 10-20 mL organ bath for isolated aorta, is being used in a series of already established experiments [32][33][34]. K + (80 mM) simulated contractions have the ability to depolarize the cell membrane for an enhanced period of time either via conductance of calcium ions toward the cell or increased intracellular calcium ions level culminating in strong contractile forces [32].…”
Section: Discussionmentioning
confidence: 99%
“…Standard calcium channel blocker Verapamil also completely relaxed both phenylephrine (1 µM) and K + (80 mM) simulated contractions. The most probable mechanism of relaxation by Aa.Cr, Aa.Aq and Aa.Dcm is calcium channel blocking activity [34]. The Ca ++ channel blocking activity is reported to have a curative effect not only by lowering the blood pressure elevation but also by decreasing the sympathetic activities of the heart in the left ventricular hypertrophy caused by hypertension [35].…”
Section: Discussionmentioning
confidence: 99%
“…Accomplishment of concentration dependent inhibitory response is dependent on applying test material in additive manner to sustained contractions. Percent (%) of control contraction response is used to show the relaxant effect of test material on simulated contractions [34].…”
Section: Mechanism Of Calcium Channel Blockadementioning
Anogeissus acuminata (Roxb. ex DC.) is a folkloric medicinal plant in Asia; including Pakistan; used as a traditional remedy for cardiovascular disorders. This study was planned to establish a pharmacological basis for the trivial uses of Anogeissus acuminata in certain medical conditions related to cardiovascular systems and to explore the underlying mechanisms. Mechanistic studies suggested that crude extract of Anogeissus acuminata (Aa.Cr) produced in vitro cardio-relaxant and vasorelaxant effects in isolated paired atria and aorta coupled with in vivo decrease in blood pressure by invasive method; using pressure and force transducers connected to Power Lab Data Acquisition System. Moreover; Aa.Cr showed positive effects in left ventricular hypertrophy in Sprague Dawley rats observed hemodynamically by a decrease in cardiac cell size and fibrosis; along with absence of inflammatory cells; coupled with reduced levels of angiotensin converting enzyme (ACE) and renin concentration along with increased concentrations of nitric oxide (NO) and cyclic guanosine monophosphate (cGMP). In Acute Myocardial Infarction (AMI) model; creatine kinase (CK), creatine kinase-MB (CK-MB) and lactic acid dehydrogenase (LDH levels) were found to be decreased; along with decreased necrosis; edema and recruitment of inflammatory cells histologically. In vivo and ex vivo studies of Anogeissus acuminata provided evidence of vasorelaxant; hypotensive and cardioprotective properties facilitated through blockage of voltage-gated Ca++ ion channel; validating its use in cardiovascular diseases
“…The K + (80 mM) was added to the tissue organ bath to induce the sustained contractions. The K + (80 mM)-induced contractions were relaxed by the testing substance to seek the possible activity of testing substance (Saqib et al, 2015;Saqib and Janbaz, 2016).…”
<p class="Abstract">The current study was conducted to screen the possible pharmacological activity of Cnicus arvensis on the gastrointestinal system. The methanolic extract exerted concentration-dependent (0.01–3.0 mg/mL) spasmolytic effect using isolated tissue preparations of rabbit jejunum and caused relaxation of K<sup>+</sup>(80 mM)-induced spastic contractions. There was non-parallel shift in Ca<sup>++ </sup>concentration response curves towards right at tissue bath concentrations of 0.3 and 1.0 mg/mL. The solvent-solvents fractionation revealed domination of spasmolytic effects in petroleum ether fraction as compared to aqueous fraction. The methanolic extract also found to reduce the retching in chicks at 150 mg/kg as compared to chlorpromazine. The methanolic crude extract also found to reduce the number of wet spots using castor oil-induced diarrhea in rat as compare to loperamide. Our results reflected the presence of Ca<sup>++</sup> channel blocking activity in methanolic extract, thus rationalizing the medicinal use of C. arvensis in diarrhea and vomiting.</p>
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