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 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 Calcium entry blocking activity of the Elaeagnus umbellata fruit extract explains its use in diarrhea and gut spasm

2016 ◽  
Vol 11 (3) ◽  
pp. 585 ◽  
Author(s):  
Nayyab Rafique ◽  
Taous Khan ◽  
Abdul Jabbar Shah
Keyword(s):  
Ethyl Acetate ◽  
Crude Extract ◽  
Video Clip ◽  
Ethyl Acetate Fraction ◽  
Response Curves ◽  
Aqueous Fraction ◽  
Elaeagnus Umbellata ◽  
High K ◽  
Medicinal Use ◽  
Rabbit Jejunum

<p class="Abstract">This study was aimed to explore the pharmacological basis of potential medicinal use of <em>Elaeagnus umbellata</em> in gut disorders. Crude extract of <em>E. umbellata</em>, which was found positive for flavonoids, terpenoids and tannins, provided 9.9-71.9% protection in castor oil-induced diarrhea in mice, like verapamil. In isolated rabbit jejunum preparations, crude extract caused inhibition of spontaneous and high K<sup>+</sup>-induced contractions, with respective EC<sub>50</sub> values of  0.3 (0.1-0.5) and 0.5 mg/mL, suggesting Ca<sup>++</sup> channel blockade (CCB). Pretreatment of tissue with crude extract (0.1–1 mg/mL) caused a rightward shift in Ca<sup>++</sup> concentration-response curves. With the exception of aqueous fraction, <em>n</em>-hexane, chloroform and ethyl acetate inhibited spontaneous and high K<sup>+</sup>-induced contractions and displaced rightward Ca<sup>++</sup> concentration-response curves. Extract was found safe up to 10 mg/kg in mice. Our data shows that anti-diarrheal effect of crude extract of <em>E. umbellate</em> is due to CCB-mediated spasmolytic effect, concentrated in the ethyl acetate fraction and suggests its medicinal importance in diarrhea and spasm.</p><p><strong>Video Clip</strong></p><p><a href="https://youtube.com/v/Qo_y3ULC4E0">Isolation of rat jejunum</a>:  2 min 32 sec </p>

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>

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.

scholarly journals Chemical Analysis and Calcium Channel Blocking Activity of the Essential Oil of Perovskia abrotanoides

2013 ◽  
Vol 8 (11) ◽  
pp. 1934578X1300801 ◽  
Author(s):  
Abdul Jabbar Shah ◽  
Munawwer Rasheed ◽  
Qaiser Jabeen ◽  
Amir Ahmed ◽  
Rasool Bakhsh Tareen ◽  
...  
Keyword(s):  
Essential Oil ◽  
Calcium Channel ◽  
Response Curves ◽  
Spasmolytic Activity ◽  
Medicinal Use ◽  
Voltage Dependent ◽  
Rabbit Jejunum ◽  
Voltage Dependent Calcium Channels ◽  
Pre Treatment ◽  
Perovskia Abrotanoides

The aim of this study was to investigate the chemical composition and provide a pharmacological base for the medicinal use of the essential oil of Perovskia abrotanoides (Pa. Oil) in gastrointestinal disorders, such as colic. The chemical investigation resulted in the identification of 26 compounds, of which tricyclene, β- trans-ocimene, terpinene-4-acetate, terpinen-4-ol, caran-3β-ol, linalyl acetate, β-caryophyllene oxide and α-elemene had not previously been reported from P. abrotanoides. Major constituents were 1,8-cineol and δ–3-carene, which constituting 50% of the oil. In the isolated rabbit jejunum preparation Pa.Oil caused inhibition of spontaneous and high K+ (80 mM)-induced contractions, with respective EC50 values of 0.13 (0.08-0.20; n=4) and 0.90 mg/mL (0.50–1.60; n=5), thus showing that spasmolytic activity is mediated possibly through calcium channel blockade (CCB). The CCB activity was confirmed when pre-treatment of the tissue with Pa. Oil (0.03-0.1 mg/mL) caused a rightward shift in the Ca++ concentration-response curves, similar to that caused by verapamil, a standard calcium channel blocker. These data indicate that the essential oil of P. abrotanoides possesses spasmolytic activity mediated possibly through inhibition of voltage-dependent calcium channels, which may explain its medicinal use in colic and possibly diarrhea.

scholarly journals Pharmacological basis for medicinal use of Ziziphyus nummularia (Rhamnaceae) leaves in gastrointestinal disorders

2017 ◽  
Vol 16 (10) ◽  
pp. 2379-2385
Author(s):  
Sayed Muzahir Hussain ◽  
Aslam Khan ◽  
Arif-ullah Khan ◽  
Neelum Gul Qazi ◽  
Fawad Ali
Keyword(s):  
Castor Oil ◽  
Saline Group ◽  
Antagonistic Effect ◽  
Fluid Accumulation ◽  
Response Curves ◽  
Medicinal Use ◽  
Gastrointestinal Ulcer ◽  
Rabbit Jejunum ◽  
Ziziphus Nummularia ◽  
Pharmacological Basis

Purpose: To explore the pharmacological basis for the folkloric use of Ziziphus nummularia for treating diarrhea and gastrointestinal spasm.Methods: Ziziphus nummularia crude extract (Zn.Cr) was investigated for  antidiarrheal activity (50, 100 and 300 mg/kg) in terms of reduction diarrhea  droppings as well as for antisecretory activity (300 and 1000 mg/kg) in castor-oil induced model in mice. The effect of the extract on potassium chloride (KCl, 80 mM)-induced contractions in isolated rabbit jejunum tissues were was also  examined. Furthermore, the antiulcer properties of the extract was assessed in an ethanol-induced gastrointestinal ulcer model.Results: Zn.Cr (50 – 1000 mg/kg) exhibited protective effect against castor  oil-induced diarrhea (p <0.05, p < 0.01 vs saline group) and intestinal fluid  accumulation (p < 0.001 vs. castor oil group) in mice. In isolated rabbit jejunum model, Zn.Cr concentration-dependently (0.01, 0.1, 0.3, 0.5, 1 and 3 mg/mL) caused relaxation of spontaneous and KCl-induced contractions, similar to  verapamil. Calcium antagonistic effect was indicated, as pretreatment of intestinal tissues with Zn.Cr (0.3, 0.5 and 1.0 mg/mL) produced a rightward shift in Ca2+ concentration-response curves, with suppression of maximum contraction. In ethanol-induced gastric ulceration assay, Zn.Cr (300 and 1000 mg/kg) caused52.5 and 93.6 % inhibition, respectively (p < 0.001 vs. saline group).Conclusion: These results reveal that Ziziphus nummularia possesses anti-diarrheal, anti-secretory, anti-spasmodic and anti-ulcer actions, mediated possibly through voltage-gated Ca2+channel blockade.Keywords: Ziziphus nummularia, Anti-diarrheal, Anti-secretory, Anti-spasmodic, Anti-ulcer

scholarly journals Gut modulator effect of methanolic extract of Solanum surattense explains its traditional use in constipation and diarrhea

2016 ◽  
Vol 11 (1) ◽  
pp. 159
Author(s):  
Shumaila Andleeb ◽  
Muhammad Masood Ahmed ◽  
Musaddique Hussain
Keyword(s):  
Response Curve ◽  
Channel Blocker ◽  
Methanolic Extract ◽  
Traditional Use ◽  
Aqueous Fraction ◽  
Solanum Surattense ◽  
Traditional Uses ◽  
Rabbit Jejunum ◽  
Concentration Response Curve ◽  
Pharmacological Basis

<p class="Abstract">Current research was conducted to find out the pharmacological basis of the methanolic extract of <em>Solanum surattense</em> for its traditional uses in constipation and diarrhea. In isolated rabbit jejunum preparations, <em>S. surattense</em> exhibited the spasmogenic effect at lower concentration (0.01-1.0 mg/mL) followed by the spasmolytic effect at next higher concentration (3-5 mg/mL) with EC<sub>50 </sub>value of3.17 mg/mL. <em>S. surattense</em> and verapamil (standard Ca<sup>2+</sup> channel blocker) caused an inhibition of K<sup>+ </sup>(80 mM)-induced contractions with EC<sub>50 </sub>value of0.85 and 0.15 mg/mL respectively, suggesting Ca<sup>2+ </sup>channels block-ade.Extract caused the rightward shift in Ca<sup>2+ </sup>concentration-response curve, similar to verapamil. Among the fractions, aqueous fraction showed the spasmogenic effect while dichloromethane fraction showed spasmolytic effect. It is concluded that methanolic extract of <em>S. surattense</em> contains spasmogenic and spasmolytic constituents, which explains its traditional uses in constipation and diarrhea.</p><p> </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.

Calcium channel blocking activity of Mentha longifolia L. explains its medicinal use in diarrhoea and gut spasm

2010 ◽  
Vol 24 (9) ◽  
pp. 1392-1397 ◽  
Author(s):  
Abdul Jabbar Shah ◽  
Nizar Noorali Bhulani ◽  
Sara Haroon Khan ◽  
Najeeb ur Rehman ◽  
Anwarul Hassan Gilani
Keyword(s):  
Calcium Channel ◽  
Medicinal Use ◽  
Channel Blocking ◽  
Blocking Activity ◽  
Mentha Longifolia

Voltage Gated Sodium Channel Blockers: Synthesis of Mexiletine Analogues and Homologues

2020 ◽  
Vol 27 ◽  
Author(s):  
Alessia Catalano ◽  
Carlo Franchini ◽  
Alessia Carocci
Keyword(s):  
Sodium Channel ◽  
Channel Blocker ◽  
Parent Compound ◽  
Channel Blockers ◽  
Sodium Channel Blocker ◽  
Starting Point ◽  
Channel Blocking ◽  
Blocking Activity ◽  
Synthetic Routes ◽  
Lateral Sclerosis

: Mexiletine is an antiarrhythmic drug belonging to IB class, acting as sodium channel blocker. Besides its well-known activity on arrhythmias, its usefulness in the treatment of myotonia, myotonic distrophy and amyotrophic lateral sclerosis is now widely recognized. Nevertheless, it has been retired from the market in several countries because of its undesired effects. Thus, several papers were reported in the last years about analogues and homologues of mexiletine being endowed with a wider therapeutic ratio and a more selectivity of action. Some of them showed sodium channel blocking activity higher than the parent compound. It is noteworthy that mexiletine is used in therapy as a racemate even though a difference in the activities of the two enantiomers were widely demonstrated, with (–)-(R)-enantiomer being more active: this finding led several research groups to study mexiletine and its analogues and homologues in their optically active forms. This review summarizes the different synthetic routes used to obtain these compounds. They could represent an interesting starting point to new mexiletine-like compounds without common side effects related to the use of mexiletine.

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