scholarly journals Pharmacological Effects ofLactuca serriolaL. in Experimental Model of Gastrointestinal, Respiratory, and Vascular Ailments

2013 ◽  
Vol 2013 ◽  
pp. 1-9 ◽  
Author(s):  
Khalid Hussain Janbaz ◽  
Muhammad Farhaj Latif ◽  
Fatima Saqib ◽  
Imran Imran ◽  
M. Zia-Ul-Haq ◽  
...  
Keyword(s):  
Muscarinic Receptors ◽  
Channel Blocker ◽  
Methanol Extract ◽  
Contractile Response ◽  
Rabbit Aorta ◽  
Pharmacological Effects ◽  
Response Curves ◽  
Lactuca Serriola ◽  
Rabbit Jejunum ◽  
Isolated Rabbit Aorta

Lactuca serriolaL. has traditionally been used in folkloric medicine to manage respiratory, gastrointestinal, and multiple other ailments. The present study was undertaken to explore the effect of methanol extract ofL. serriolaon isolated rabbit tissue preparations, that is, jejunum, trachea, and aorta in an attempt to validate its folkloric use in traditional medicine for gastrointestinal, respiratory, and vascular ailments. The application of the methanol extract to isolated rabbit jejunum preparations exhibited concentration-dependent spasmogenic effect (0.03 to 3.0 mg/mL), but interestingly further increase in concentration (5.0 mg/mL) resulted in complete spasmolytic effect. The pretreatment of the tissue preparations with atropine (0.1 μM) caused the suppression of the contractile response. Moreover, the same extract also caused relaxation of K+-(80 mM) induced spastic contractions of isolated rabbit jejunum preparations (5.0 mg/mL) and shifted the Ca++dose response curves towards right at concentration range of 0.3–1.0 mg/mL. Similarly, the extract application to isolated rabbit tracheal preparations relaxed the carbachol-(1 μM) induced (0.3–1.0 mg/mL) as well as K+-(80 mM) induced contractions (3.0 mg/mL). Furthermore, it relaxed the phenylephrine (1 μM)-induced contractions in isolated rabbit aorta preparations (3.0 mg/mL) and K+(80 mM)-induced contractions (1.0 mg/mL). These effects were found comparable to that of dicyclomine, as an antagonist of muscarinic receptors as well as a possible Ca++channel blocker. The previously mentioned findings may partially justify the folkloric use ofLactuca serriolain the management of conditions pertaining to spasm of intestine, bronchioles, and vasculature.

Studies on antihypertensive and antispasmodic activities of Andropogon muricatus Retz.This article is one of a selection of papers published in this special issue (part 1 of 2) on the Safety and Efficacy of Natural Health Products.

2007 ◽  
Vol 85 (9) ◽  
pp. 911-917 ◽  
Author(s):  
Anwar H. Gilani ◽  
Abdul J. Shah ◽  
Khalid H. Janbaz ◽  
Shahida P. Ahmed ◽  
Muhammad N. Ghayur
Keyword(s):  
Calcium Channel ◽  
Rabbit Aorta ◽  
Natural Health Products ◽  
Response Curves ◽  
Medicinal Uses ◽  
Health Products ◽  
Rabbit Jejunum ◽  
The Right

The aqueous-methanolic crude extract of Andropogon muricatus (Am.Cr) was investigated pharmacologically to determine some of its medicinal uses in cardiovascular and gastrointestinal disorders. A series of in vivo and in vitro studies were conducted to evaluate dose-dependent effects of Am.Cr on mean arterial pressure (MAP), cardiac and vascular contractions, and to further investigate the potential mechanism of action. Intravenous administration of Am.Cr (10–50 mg/kg) caused a fall (18%–56%) in MAP in normotensive rats under anesthesia. When tested in isolated guinea pig atria, Am.Cr (0.03–5.0 mg/mL) exhibited a cardiodepressant effect on the rate and force of spontaneous contractions. In isolated rabbit aorta, Am.Cr caused inhibition of K+ (80 mmol/L)-induced contractions at a lower concentration than of phenylephrine. In isolated rabbit jejunum preparations, Am.Cr (0.01–0.10 mg/mL) caused relaxation of spontaneous and high K+ (80 mmol/L)-induced contractions, suggesting that the spasmolytic effect is mediated possibly through calcium channel blockade (CCB). The CCB activity was confirmed when pretreatment of the tissue with Am.Cr (0.03–0.1 mg/mL) shifted the Ca2+ dose–response curves to the right, similar to that caused by verapamil. These data indicate that the blood pressure-lowering and spasmolytic effects of Am.Cr are mediated possibly through a calcium channel blocking activity. Phytochemical screening of Am.Cr revealed the presence of phenols, saponins, tannins, and terpenes, which may be responsible for the observed vasodilator, cardiodepressant, and antispasmodic activities. This study shows potential with respect to its medicinal use in cardiovascular and gut disorders.

Mechanisms Underlying the Relaxant Effect of Galetin 3,6- Dimethyl Ether, from Piptadenia stipulacea (Benth.) Ducke, on Guinea-Pig Trachea

2014 ◽  
Vol 69 (11-12) ◽  
pp. 434-442 ◽  
Author(s):  
Cibério Landim Macêdo ◽  
Luiz Henrique César Vasconcelos ◽  
Ana Carolina de Carvalho Correia ◽  
Italo Rossi Roseno Martins ◽  
Daysianne Pereira de Lira ◽  
...  
Keyword(s):  
Guinea Pig ◽  
Dimethyl Ether ◽  
Muscarinic Receptors ◽  
Channel Blocker ◽  
Response Curves ◽  
Relaxant Effect ◽  
Voltage Gated ◽  
Aerial Parts ◽  
Pka Pathway ◽  
Small Conductance

Abstract Galetin 3,6-dimethyl ether (FGAL), a flavonoid from the aerial parts of Piptadenia stipulacea (Benth.) Ducke, was found to exert a relaxant effect on carbachol (CCh)-pre-contracted guinea-pig trachea. Based on cumulative concentration-response curves to CCh, FGAL antagonized muscarinic receptors pseudo-irreversibly and noncompetitively, since it inhibited and shifted these curves towards higher concentrations in a nonparallel manner. In addition, FGAL was more potent in relaxing contractions induced by 18 mM as compared to 60 mM KCl (pD2 = 5:50 ±0:36 and 4.80 ±0.07, respectively), indicating the participation of K+ channels. In the presence of 10 mM tetraethylammonium (TEA+) chloride, a nonselective K+ channel blocker, the relaxant potency of FGAL was reduced (from pD2 = 5:12 ±0:07 to 4.87 ±0.02). Among several selective blockers of K+ channel subtypes, only apamin, an SKCa (small-conductance Ca2+-activated K+ channels) blocker, attenuated the relaxant potency of FGAL (pD2 = 4:85±0:06), suggesting SKCa activation. FGAL was equipotent in relaxing trachea contracted by 60 mM KCl (pD2 =4:80 ±0:07) or 10-6 M CCh (pD2 = 5:02 ±0:07), suggesting CaV (voltage-gated calcium channel), but not ROCs (receptor-operated calcium channels) participation. Furthermore, aminophylline-induced relaxation (pD2 = 4:12 ±0:06) was potentiated around 4-fold (pD2 = 4:80 ±0:44) in the presence of FGAL. Moreover, forskolininduced relaxation (pD2 = 6:51 ±0:06) was potentiated around 2.5-fold (pD2 = 6:90 ±0:05) by FGAL. Conversely, sodium nitroprusside-induced relaxation was unaffected, indicating that the AC/cAMP/PKA pathway, but not the NO pathway, may be modulated by the flavonoid. These results suggest that, in guinea-pig trachea, FGAL induces relaxation by pseudo-irreversible noncompetitive antagonism on muscarinic receptors, modulation of K+ and Ca2+ channels, as well as activation of the AC/cAMP/PKA pathway.

scholarly journals Pharmacological evaluation of Dactyloctenium aegyptium: An indigenous plant used to manage gastrointestinal ailments

2015 ◽  
Vol 10 (2) ◽  
pp. 295 ◽  
Author(s):  
Khalid Hussain Janbaz ◽  
Fatima Saqib
Keyword(s):  
Channel Blocker ◽  
Ethanolic Extract ◽  
Scientific Basis ◽  
Response Curves ◽  
Dactyloctenium Aegyptium ◽  
Channel Blocking ◽  
Blocking Activity ◽  
Rabbit Jejunum ◽  
Indigenous Plant ◽  
Higher Doses

<p>Crude extract of <em>Dactylotenium aegyptium</em> and its fractions were evaluated to rationalize its folkloric use in gastrointestinal ailments. In spontaneous contracting rabbit jejunum preparation, D. aegyptium exert concentration-dependent spasmogenic effect (0.01-0.1 mg/mL) followed by spasmolytic effect at higher doses (0.3-3.0 mg/mL). Pretreatment of the tissue preparations with atropine resulted in suppression of the spasmogenic response. Furthermore, <em>D. aegyptium</em> (1.0 mg/mL) caused relaxation of K<sup>+ </sup>(80 mM)-induced spastic contractions in isolated rabbit jejunum preparations and there was non-parallel shift in Ca<sup>++</sup> dose response curves towards right (0.1-0.3 mg/mL). These findings were found to be comparable with verapamil, a standard Ca<sup>++</sup> channel blocker. The solvent-solvents fractionation reflected segregations of spasmogenic and spasmolytic effects in respective aqueous and dichloromethane fractions. The above-mentioned findings reflected, presence of cholinergic as well as Ca<sup>++</sup> channel blocking activity in ethanolic extract of <em>D. aegyptium</em> thus providing scientific basis for its folkloric use in constipation and diarrhea.</p><p> </p><p> </p>

Mechanism of activation of isolated rabbit aorta by PGH2 analogue U-44069

1981 ◽  
Vol 241 (5) ◽  
pp. C243-C249 ◽  
Author(s):  
R. Loutzenhiser ◽  
C. van Breemen
Keyword(s):  
Smooth Muscle ◽  
Contractile Response ◽  
Rabbit Aorta ◽  
Calcium Content ◽  
Prior Exposure ◽  
Maximal Tension ◽  
Isolated Rabbit Aorta ◽  
Free Media ◽  
45Ca Efflux ◽  
Stimulation Of

The effects of a stable analogue of PGH2 on 45Ca fluxes and tension were studied in the isolated rabbit aorta. U-44069 produced maximal tension responses at a concentration of 10(-7) M. The analogue increased smooth muscle Ca2+ content and increased the unidirectional 45Ca influx. U-44069 also induced contractions of reduced magnitude in the absence of external Ca2+ and caused a transient stimulation of 45Ca efflux, suggesting that the analogue releases intracellularly bound Ca2+. Both the contractile response in CA2+-free media and the stimulation of 45Ca efflux were greatly attenuated by prior exposure to norepinephrine. The analogue-induced contractions in Ca2+-free media were also prevented by prior exposure to histamine but not angiotensin II. D-600 completely blocked the U-44069-induced gain in calcium content (IC50 = 10(-6) M) but inhibited the contractile response by only 40%. It was concluded that the PGH2 analogue activates rabbit aorta by activating a CA2+ influx pathway and releasing a fraction of the intracellular Ca2+ pool that is sensitive to norepinephrine and other agonists.

scholarly journals Pharmacological basis for the medicinal use of Viola odorata in diarrhea, bronchial asthma and hypertension

2015 ◽  
Vol 10 (4) ◽  
pp. 836 ◽  
Author(s):  
Khalid Hussain Janbaz ◽  
Waseem Ullah Khan ◽  
Fatima Saqib ◽  
Mamoona Khalid
Keyword(s):  
Channel Blocker ◽  
Response Curves ◽  
Relaxant Effect ◽  
Viola Odorata ◽  
Medicinal Use ◽  
Channel Blocking ◽  
Blocking Activity ◽  
Rabbit Jejunum ◽  
Spontaneous Contractions ◽  
Pharmacological Basis

<p class="Abstract"><em>Viola odorata</em> is traditionally used in the management of gastrointestinal,  respiratory and vascular disorders. The present study was undertaken to validate its folkloric uses. The application of <em>V. odorata</em> to spontaneous contractions in isolated rabbit jejunum preparation exerted relaxant effect through decrease in magnitude and frequency of contractions. Moreover, it also caused relaxation of K<sup>+ </sup>(80 mM)-induced contractions and shifted the Ca<sup>2+ </sup>concentration response curves toward right in isolated jejunum similar to verapamil (standard Ca<sup>2+ </sup>channel blocker), confirming Ca<sup>2+ </sup>channel blocking activity. <em>V. odorata</em> also caused relaxation of carbachol (1 µM)- and K<sup>+ </sup>(80 mM)-induced contractions in isolated rabbit tracheal preparations comparable to verapamil, reflecting that observed relaxant effect may be the outcome of anti-muscarinic and/or Ca<sup>2+ </sup>channel blocking activities. It also exerted relaxant effect on phenylephrine (1 µM)- and K<sup>+ </sup>(80 mM)-induced contractions in isolated rabbit aortic preparations thus providing rationale for  its folkloric  uses to treat diarrhea, asthma and hypertension.</p>

scholarly journals Pharmacological Evaluation ofProsopis cineraria(L.) Druce in Gastrointestinal, Respiratory, and Vascular Disorders

2012 ◽  
Vol 2012 ◽  
pp. 1-7 ◽  
Author(s):  
Khalid Hussain Janbaz ◽  
Sajjad Haider ◽  
Imran Imran ◽  
Muhammad Zia-Ul-Haq ◽  
Laura De Martino ◽  
...  
Keyword(s):  
Channel Blocker ◽  
Methanolic Extract ◽  
Biological Activities ◽  
Stem Bark ◽  
Response Curves ◽  
Traditional Use ◽  
Vascular Disorders ◽  
Relaxant Effect ◽  
Pharmacological Evaluation ◽  
Rabbit Jejunum

In this paper, a crude methanolic extract from the stem bark ofProsopis cineraria, a plant native of Pakistan, was tested for its possible presence of spasmolytic, bronchodilator, and vasodilator activities in an attempt to validate some of its folkloric uses. Moreover, attempts were made to provide plausible explanations of the observed biological activities. The extract caused relaxation of the spontaneous as well as K+(80 mM)-induced contractions at tissue bath concentrations of 3–10 mg/mL in isolated rabbit jejunum preparations, probably mediated through blockade of Ca+2channels. This finding was further confirmed by the shifting of the Ca+2concentration response curves to the rightward in a manner similar to verapamil used as a standard Ca+2channel blocker. The extract also exhibited nonspecific relaxant effect on carbachol (1 μM)- and K+(80 mM)-induced contractions in isolated rabbit tracheal preparations. The same effect was recorded for phenylephrine (11 μM) and K+(80 mM)-induced contractions in isolated rabbit aortic preparations in a manner similar to verapamil. These observations confirm that observed bronchodilator and vasodilator activities were possibly mediated through blockade of Ca+2channels. The above-mentioned observations validate the traditional use of the plant in the treatment of respiratory and gastrointestinal ailments.

scholarly journals Pharmacological effects of Cnicus arvensis on the gastrointestinal system

2018 ◽  
Vol 13 (1) ◽  
pp. 16
Author(s):  
Fatima Saqib ◽  
Sakeena Hassan ◽  
Imran Imran ◽  
Ambreen Aleem ◽  
Khalid Hussain Janbaz
Keyword(s):  
Methanolic Extract ◽  
Gastrointestinal System ◽  
Pharmacological Effects ◽  
Response Curves ◽  
Aqueous Fraction ◽  
Medicinal Use ◽  
Channel Blocking ◽  
Blocking Activity ◽  
Ether Fraction ◽  
Rabbit Jejunum

<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>

scholarly journals Pharmacologically mechanistic basis for the traditional uses of Rumex acetosa in gut motility disorders and emesis

2015 ◽  
Vol 10 (3) ◽  
pp. 548 ◽  
Author(s):  
Musaddique Hussain ◽  
Shahid Masood Raza ◽  
Khalid Hussain Janbaz
Keyword(s):  
Rumex Acetosa ◽  
Response Curves ◽  
Motility Disorders ◽  
Traditional Uses ◽  
Antiemetic Activity ◽  
Rabbit Jejunum ◽  
Mechanistic Basis ◽  
The Right

<p class="Abstract"><em>In vitro</em> and<em> in vivo</em> studies were undertaken to evaluate the pharmacologically mechanistic background to validate the traditional uses of <em>Rumex acetosa</em> in the treatment of emesis and gastrointestinal motility disorders such as constipation and diarrhea. In rabbit jejunum preparation, methanolic extract of <em>R. acetosa</em> (0.01-1.0 mg/mL) caused a transient spasmogenic effect, followed by the spasmolytic effect (3-10 mg/mL). In presence of atropine, spasmogenic effect was blocked while spasmolytic effect was emerged, suggesting that spasmogenic effect was mediated through activation of muscarinic receptors. Extract inhibited the K<sup>+ </sup>(80 mM)-induced contraction, suggesting Ca<sup>2+</sup>-cha-nnel blockade, which was further confirmed when pretreatment of tissue with extract shifted the Ca<sup>2+ </sup>concentration-response curves to the right, similarly as verapamil.<em> R. acetosa</em> also exhibited the significant antiemetic activity (p&lt;0.05) against different emetogenic stimuli, when compared with chlorpromazine. This study confirms the presence of gut modulator (spasmogenic and spasmolytic) and antiemetic activates, validating its traditional uses.</p><p> </p>

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