scholarly journals Pharmacological Studies Pertaining to Smooth Muscle Relaxant, Platelet Aggregation Inhibitory and Hypotensive Effects of Ailanthus altissima

2019 ◽  
Vol 2019 ◽  
pp. 1-14 ◽  
Author(s):  
Hafiz Muhammad Abdur Rahman ◽  
Muhammad Fawad Rasool ◽  
Imran Imran
Keyword(s):  
Smooth Muscle ◽  
Platelet Aggregation ◽  
Castor Oil ◽  
Ailanthus Altissima ◽  
Sd Rats ◽  
High K ◽  
Rabbit Jejunum ◽  
Smooth Muscle Relaxant

Objective. This in vitro and in vivo study was conducted to rationalize some of traditional medicinal uses of Ailanthus altissima in gastrointestinal, respiratory, and cardiovascular systems. Materials. Crude extract of Ailanthus altissima (Aa.Cr) and its fractions were prepared and utilized in in vitro and in vivo studies. For in vitro studies, Aa.Cr was investigated on isolated rabbit jejunum, isolated tracheal strip, and isolated aorta of rat suspended in tissue organ bath. Platelet rich and platelet poor plasma were used to study platelet aggregation inhibitory activity. In vivo antidiarrheal effect of Aa.Cr was investigated on balb/c mice pretreated with castor oil to induce diarrhea and SD rats were used to study hypotensive activity. Results. Concentration dependent spasmolytic effects of Aa.Cr and its DCM fraction (Aa.DCM) were observed on spontaneous and spasmogen induced contractions in jejunum isolated from rabbit, but effect against high potassium (high-K+) induced contractions was more potent. Moreover Aa.Cr showed parallel shifting of calcium response curve to the right side. While its aqueous fraction (Aa.aq) caused spasmogenesis of isolated rabbit jejunum, this effect was blocked partially with prior administration of atropine (1μM). Concentration dependent protection against castor oil induced diarrhea was also observed. Relaxant effect was observed by the application of Aa.Cr and Aa.DCM against high-K+ and carbachol (CCh) induced contractions in tracheal strips isolated from SD rats, while Aa.Aq caused partial relaxation of high-K+ induced contractions, but no effect was observed against CCh induced contractions. Relaxation of rat aorta by the application of Aa.Cr and its fractions was also observed. Inhibition of force of contraction in rabbit atrium was also observed. Inhibition of platelet aggregation was observed against epinephrine and ADP induced aggregation. Conclusion. Keeping in view the observed results, it is concluded that smooth muscle relaxant, platelet aggregation inhibitory and hypotensive effect may be due to the blockage of calcium channels.

scholarly journals Pharmacological Modulation of Smooth Muscles and Platelet Aggregation by Psidium cattleyanum

2020 ◽  
Vol 2020 ◽  
pp. 1-14
Author(s):  
Hafiz Muhammad Abdur Rahman ◽  
Khaled Ahmed Saghir ◽  
Muhammad Sajjad Haider ◽  
Usman Javaid ◽  
Muhammad Fawad Rasool ◽  
...  
Keyword(s):  
Platelet Aggregation ◽  
Castor Oil ◽  
Platelet Rich Plasma ◽  
Research Work ◽  
Smooth Muscles ◽  
Bioactive Molecules ◽  
High K ◽  
Tracheal Tissue

Traditionally, in the Southern Asian countries, Psidium cattleyanum is a widely used plant for the management of various ailments such as gastrointestinal, respiratory, and cardiac disorders, but it lacks proof on a scientific basis, and therefore, this is the major emphasis of the current research work. Crude extract of Psidium cattleyanum (Pc.Cr) was preliminary analyzed for the presence of different classes of bioactive molecules. The aqueous and dichloromethane fractions of Pc.Cr were subjected to in vitro and in vivo studies. It was applied at variable concentrations (0.1–10 mg/ml) to isolated rabbit jejunum to investigate spasmolytic effect. Concentration dependent curves of calcium were constructed to check the calcium channel antagonistic activity. For the evaluation of tracheorelaxant activity, isolated tracheal tissue was treated with High-K+ (80 mM) and carbachol (CCh) and then challenged cumulatively with Pc.Cr. To study the antidiarrheal effect of the plant extract, castor oil-induced diarrhea model was adopted. For evaluation of the hypotensive effect of Pc.Cr, it was given intravenously to preanesthetized normotensive rats, and the response was recorded using pressure transducer. Platelet rich plasma was used for the assessment of the antiplatelet activity when challenged with purinergic and adrenergic agonists. Concentration-dependent inhibition of spontaneous and High-K+ mediated contractions in isolated jejunum was observed by the application of Pc.Cr. Contractions induced in isolated tracheal tissue by High-K+ and CCh were inhibited by application of Pc.Cr to these tissues. Similarly, application of Pc.Cr to High-K+ and phenylephrine (PE) treated aortic strips resulted in vasodilation. Platelet aggregation inhibition was shown by Pc.Cr against adenosine diphosphate (ADP) only. The antidiarrheal effect was observed as a reduction in the total number of feces in Pc.Cr-treated mice when given castor oil. Dose-dependent hypotension was seen in normotensive rats when treated with Pc.Cr intravenously. This study showed the spasmolytic, tracheorelaxant, vasodilator, platelet aggregation inhibitory, antidiarrheal, and hypotensive activities of P. cattleyanum which may be due to the blockage of calcium channels, but the involvement of any other pathway cannot be ignored.

scholarly journals Effect of Furostanol Saponins from Allium Macrostemon Bunge Bulbs on Platelet Aggregation Rate and PI3K/Akt Pathway in the Rat Model of Coronary Heart Disease

2019 ◽  
Vol 2019 ◽  
pp. 1-7
Author(s):  
Hui Feng ◽  
Zhipeng Wang ◽  
Changsong Wang ◽  
Xinyi Zhu ◽  
Zhigang Liu ◽  
...  
Keyword(s):  
Coronary Heart Disease ◽  
Heart Disease ◽  
Platelet Aggregation ◽  
Akt Phosphorylation ◽  
Aggregation Rate ◽  
Furostanol Saponins ◽  
Sd Rats ◽  
Allium Macrostemon

Aim. To investigate the effect of Furostanol Saponins from Allium Macrostemon Bunge Bulbs (FSAMB) on platelet aggregation rate of rats with coronary heart disease and discuss the mechanism of FSAMB affecting the platelet aggregation rate through PI3K/Akt pathway. We established the rat models with coronary heart disease (CHD) and prepared the platelet-rich plasma. The effect of different concentrations of FSAMB on platelet aggregation in SD rats induced by ADP was observed in vitro and in vivo. And Lactate Dehydrogenase (LDH), Creatine Kinase-MB Form (CK-MB), and Cardiac Troponin I (cTnI) are detected in the blood to know the level of damage to heart cells. The expansion of platelets in the immobilized fibrinogen in different concentrations of FSAMB was observed. Western blot was conducted to detect the phosphorylation level of protein kinase B (also known as Akt) and the expression level of phosphoinositide 3-kinase (PI3K). We found that FSAMB had a significant inhibitory effect on the ADP-induced platelet aggregation in vitro. Intragastric administration of FSAMB also inhibited platelet aggregation induced by ADP in rats. LDH, CK-MB, and cTnI levels in serum of rats in FSAMB (672 mg/kg) group were lower than those in the model control group after the intervention (P<0.01 or P<0.05). FSAMB inhibited the expansion of platelets on immobilized fibrinogen. Also, FSAMB inhibited ADP-induced platelet PI3K expression and Akt phosphorylation. The inhibition of Akt phosphorylation by FSAMB was more obvious after the inhibition of the expression of PI3K. This study demonstrated that FSAMB can reduce the degree of myocardial cell damage and inhibit ADP-induced platelet aggregation in SD rats, possibly by inhibiting platelet PI3K/Akt signaling pathway in vitro and in vivo.

Effect of Propofol on Norepinephrine-induced Increases in [Ca2+](i) and Force in Smooth Muscle of the Rabbit Mesenteric Resistance Artery 

1998 ◽  
Vol 88 (6) ◽  
pp. 1566-1578 ◽  
Author(s):  
Nami Imura ◽  
Yoshihisa Shiraishi ◽  
Hirotada Katsuya ◽  
Takeo Itoh
Keyword(s):  
Smooth Muscle ◽  
Isometric Force ◽  
Resistance Artery ◽  
Resistance Arteries ◽  
High K ◽  
Small Resistance ◽  
Vasodilating Activity ◽  
Mesenteric Resistance Artery

Background Propofol (2,6-diisopropylphenol) possesses vasodilating activity in vivo and in vitro. The propofol-induced relaxation of agonist-induced contractions in small resistance arteries has not been clarified. Methods The effect of propofol was examined on the contractions induced by norepinephrine and high K+ in endothelium-denuded rabbit mesenteric resistance artery in vitro. The effects of propofol on the [Ca2+]i mobilization induced by norepinephrine and high K+ were studied by simultaneous measurement of [Ca2+]i using Fura 2 and isometric force in ryanodine-treated strips. Results Propofol attenuated the contractions induced by high K+ and norepinephrine, the effect being greater on the high K+-induced contraction than on the norepinephrine-induced contraction. In Ca2+-free solution, norepinephrine produced a transient contraction resulting from the release of Ca2+ from storage sites that propofol attenuated. In ryanodine-treated strips, propofol increased the resting [Ca2+]i but attenuated the increases in [Ca2+]i and force induced by both high K+ and norepinephrine. In the presence of nicardipine, propofol had no inhibitory action on the residual norepinephrine-induced [Ca2+]i increase, whereas it still modestly increased resting [Ca2+]i, as in the absence of nicardipine. Conclusions In smooth muscle of the rabbit mesenteric resistance artery, propofol attenuates norepinephrine-induced contractions due to an inhibition both of Ca2+ release and of Ca2+ influx through L-type Ca2+ channels. Propofol also increased resting [Ca2+]i, possibly as a result of an inhibition of [Ca2+]i removal mechanisms. These results may explain in part the variety of actions seen with propofol in various types of vascular smooth muscle.

scholarly journals Antidiarrheal and antispasmodic activities of Polygonum bistorta rhizomes are mediated predominantly through K+ channels activation

2015 ◽  
Vol 10 (3) ◽  
pp. 627 ◽  
Author(s):  
Muhammad Zeeshan Ali ◽  
Khalid Hussain Janbaz ◽  
Malik Hassan Mehmood ◽  
Anwar Hassan Gilani
Keyword(s):  
Tetraethylammonium Chloride ◽  
Relaxant Effect ◽  
Complete Relaxation ◽  
High K ◽  
Rabbit Jejunum ◽  
Low K ◽  
Dose Dependent ◽  
Antagonist Effect

<p class="Abstract"><em>Polygonum bistorta</em> is a popular medicinal herb used to treat diarrhea. This study provides pharmacological basis to its folk use in diarrhea using <em>in vivo</em> and <em>in vitro</em> assays. Administration of<em> P. bistorta</em>  rhizomes extract to mice offered protection against castor oil-induced diarrhea at 300-1,000 mg/kg and was found safe up to the dose of 5 g/kg. In isolated rabbit jejunum, the extract caused a dose-dependent relaxation of spontaneous and low K<sup>+</sup> (25 mM)-induced contractions with weak effect against high K<sup>+ </sup>(80 mM). In tissues pretreated with glibenclamide or tetraethylammonium chloride (TEA), the relaxant effect of the extract was markedly inhibited by TEA only. While verapamil showed complete relaxation of spontaneous, low K<sup>+</sup>, low K<sup>+</sup> with TEA and high K<sup>+</sup>-induced contractions. In guinea-pig ileum, mild atropine-sensitive effect was observed. This study indicates that <em>P. bistorta</em> possesses anti-diarrheal and antispasmodic activities mediated predominantly through K<sup>+</sup>-channels activation along with weak Ca<sup>++</sup> antagonist effect.</p><p> </p>

scholarly journals Antidiarrheal activity of methanolic leaf extract of Rumex vesicarius

2016 ◽  
Vol 11 (1) ◽  
pp. 175 ◽  
Author(s):  
Imran Ahmad Khan ◽  
Khalid Hussain Janbaz ◽  
Fatima Saqib
Keyword(s):  
Castor Oil ◽  
Gastrointestinal Transit ◽  
Intestinal Content ◽  
Positive Control ◽  
Tissue Preparation ◽  
Rabbit Jejunum ◽  
Antidiarrheal Activity ◽  
Spontaneous Contractions

<p>This study evaluates the antidiarrheal activity of <em>Rumex vesicarius</em> (leaf) by using in vitro and in vivo assays. Antidiarrheal effect of <em>R. vesicarius</em> was  evaluated using castor oil-induced diarrhea model in rat. Weight and  volume of the intestinal content were assessed using the enteropooling method. Atropine (3 mg/kg, i.p) was used as positive control. <em>R. Vesicarius</em> at the  doses of 200 and 400 mg/kg p.o. significantly retarded castor oil-induced  enteropooling and intestinal transit. The gastrointestinal transit rate was  studied and <em>R. vesicarius</em> at the doses of 200 and 400 mg/kg significantly inhibited (p&lt;0.001) weight and volume of intestinal content. <em>R. vesicarius</em> caused concentration-dependent (0.01–1 mg/mL) relaxation of spontaneous contractions in isolated rabbit jejunum tissue preparation and inhibited K<sup>+</sup>-80 induced contractions (0.01-5 mg/mL), similar to verapamil, suggestive of calcium channel blockade. Results obtained herein indicate that <em>R. vesicarius</em> may contain effective compounds which can be used as an antidiarrheal agent.</p>

scholarly journals Pharmacological and computational evaluation of fig for therapeutic potential in hyperactive gastrointestinal disorders

2019 ◽  
Vol 19 (1) ◽  
Author(s):  
Muhammad Bilal Riaz ◽  
Arif-ullah Khan ◽  
Neelam Gul Qazi
Keyword(s):  
Castor Oil ◽  
Therapeutic Potential ◽  
Gastrointestinal Transit ◽  
Gastric Ulcers ◽  
Binding Affinities ◽  
Computational Evaluation ◽  
Rabbit Jejunum ◽  
Ficus Palmata

Abstract Background Ficus palmata (Fig), are distributed in different parts of the world, and are used in traditional medicine to treat various ailments including inflammation, tumor, epilepsy, jaundice, influenza and bacillary dysentery. The present study aimed to evaluate the antidiarrheal, antisecretary, antispasmodic, antiulcer and anti motility properties of Ficus palmata. Methods In-vivo, in-vitro and in-silico techniques were used to investigate various gastrointestinal effects of Ficus palmata. Antidiarrheal, antisecretary, antispasmodic, antiulcer, anti motility and molecular docking were performed using castor oil induced diarrhea and fluid accumulation, isolated tissue preparations, ethanol-HCl induced ulcer assay, charcoal meal transit time and Auto Doc Vina. Results Ficus palmata crude extract (Fp.Cr) exhibited protection against castor oil-induced diarrhea in mice and dose-dependently inhibited intestinal fluid secretions. Fp.Cr caused relaxation of spontaneous and K+ (80 Mm)-induced contractions in isolated rabbit jejunum preparations. It showed protective effect against gastric ulcers induced by ethanol-hydrochloric acid in rats. Fp.Cr reduced distance travelled by charcoal meal in the gastrointestinal transit model in mice. The plant constituents: psoralenoside and bergapten showed high binding affinities (E-value ≥ − 6.5 Kcal/mol) against histaminergic H1, calmodulin and voltage gated L-type calcium channels, while showed moderate affinities (E-value ≥7 Kcal/mol) against dopaminergic D2, adrenergic α1, muscranic M3, mu-opioid, whereas revealed lower affinities (E-value ≥9.5 Kcal/mol) vs. muscranic M1, histaminergic H2 and H+/K+ ATPase pump. Germanicol acetate and psoralene exhibited weak affinities against aforementioned targets. Conclusion This study reveals that Ficus palmata possesses anti-diarrheal, anti-secretory, anti-spasmodic, anti-motility and anti-ulcer activities. The various constituents reveal different binding affinities against target proteins, which mediate the gastrointestinal functions.

Effects of adlay hull extracts on uterine contraction and Ca2+ mobilization in the rat

2008 ◽  
Vol 295 (3) ◽  
pp. E719-E726 ◽  
Author(s):  
Shih-Min Hsia ◽  
Yueh-Hsiung Kuo ◽  
Wenchang Chiang ◽  
Paulus S. Wang
Keyword(s):  
Smooth Muscle ◽  
Muscle Contraction ◽  
Uterine Contraction ◽  
Smooth Muscle Contraction ◽  
Uterine Contractions ◽  
High K ◽  
Intracellular Ca ◽  
Feasible Alternative

Dysmenorrhea is directly related to elevated PGF2α levels. It is treated with nonsteroid antiinflammatory drugs (NSAIDs) in Western medicine. Since NSAIDs produce many side effects, Chinese medicinal therapy is considered as a feasible alternative medicine. Adlay ( Coix lachryma-jobi L. var. ma-yuen Stapf.) has been used as a traditional Chinese medicine for treating dysmenorrhea. However, the relationship between smooth muscle contraction and adlay extracts remains veiled. Therefore, we investigated this relationship in the rat uterus by measuring uterine contraction activity and recording the intrauterine pressure. We studied the in vivo and in vitro effects of the methanolic extracts of adlay hull (AHM) on uterine smooth muscle contraction. The extracts were fractionated using four different solvents: water, 1-butanol, ethyl acetate, and n-hexane; the four respective fractions were AHM-Wa, AHM-Bu, AHM-EA, and AHM-Hex. AHM-EA and its subfractions (175 μg/ml) inhibited uterine contractions induced by PGF2α, the Ca2+ channel activator Bay K 8644, and high K+ in a concentration-dependent manner in vitro. AHM-EA also inhibited PGF2α-induced uterine contractions in vivo; furthermore, 375 μg/ml of AHM-EA inhibited the Ca2+-dependent uterine contractions. Thus 375 μg/ml of AHM-EA consistently suppressed the increases in intracellular Ca2+ concentrations induced by PGF2α and high K+. We also demonstrated that naringenin and quercetin are the major pure chemical components of AHM-EA that inhibit PGF2α-induced uterine contractions. Thus AHM-EA probably inhibited uterine contraction by blocking external Ca2+ influx, leading to a decrease in intracellular Ca2+ concentration. Thus adlay hull may be considered as a feasible alternative therapeutic agent for dysmenorrhea.

scholarly journals Folkloric uses of Jatropha gossypifolia in emesis and gut motility disorders: Pharmacological validation

2015 ◽  
Vol 10 (4) ◽  
pp. 864 ◽  
Author(s):  
Musaddique Hussain ◽  
Shahid Masood Raza ◽  
Abdul Majeed
Keyword(s):  
Ethanolic Extract ◽  
Receptor Activation ◽  
Motility Disorders ◽  
High K ◽  
Jatropha Gossypifolia ◽  
Channel Blocking ◽  
Rabbit Jejunum ◽  
The Right

<p class="Abstract"><em>Jatropha gossypifolia</em> is used in folkloric system to manage emesis and gastrointestinal motility disorders such as constipation and diarrhea. The present study was undertaken to provide pharmacological evidences for these folkloric uses by <em>in vivo</em> and <em>in vitro</em> experimental setting. Ethanolic extract of <em>J. gossypifolia</em> showed the significant antiemetic potential (p&lt;0.05) against different emetogenic stimuli, when compared with chlorpromazine. The extract (0.01-1.0 mg/mL) on application to isolated rabbit jejunum preparation exerted spasmogenic effect, followed by the spasmolytic effect (3-10 mg/mL). In the presence of atropine, spasmogenic effect was blocked while spasmolytic effect was emerged, suggesting the involvement of muscarinic receptor activation.<em> J. gossypifolia</em> caused relaxation of high K<sup>+ </sup>(80 mM)-induced contraction and shifted the Ca<sup>2+ </sup>concentration-response curve to the right in a manner similar to verapamil, thus conforming its Ca<sup>2+</sup>-channel blocking activity. These findings provide pharmacological validation for the presence of antiemetic and gut modulator (spasmogenic and spasmolytic) activates, validating its folkloric uses.</p><p> </p>

Enhancement of ADP-induced Platelet Aggregation by Adrenaline in Vivo and Its Prevention

1973 ◽  
Vol 29 (02) ◽  
pp. 490-498 ◽  
Author(s):  
Hiroh Yamazaki ◽  
Itsuro Kobayashi ◽  
Tadahiro Sano ◽  
Takio Shimamoto
Keyword(s):  
Platelet Count ◽  
Platelet Aggregation ◽  
Platelet Rich Plasma ◽  
The Other ◽  
Endothelial Surface ◽  
Important Interaction ◽  
Blood Coagulability ◽  
The Difference

SummaryThe authors previously reported a transient decrease in adhesive platelet count and an enhancement of blood coagulability after administration of a small amount of adrenaline (0.1-1 µg per Kg, i. v.) in man and rabbit. In such circumstances, the sensitivity of platelets to aggregation induced by ADP was studied by an optical density method. Five minutes after i. v. injection of 1 µg per Kg of adrenaline in 10 rabbits, intensity of platelet aggregation increased to 115.1 ± 4.9% (mean ± S. E.) by 10∼5 molar, 121.8 ± 7.8% by 3 × 10-6 molar and 129.4 ± 12.8% of the value before the injection by 10”6 molar ADP. The difference was statistically significant (P<0.01-0.05). The above change was not observed in each group of rabbits injected with saline, 1 µg per Kg of 1-noradrenaline or 0.1 and 10 µg per Kg of adrenaline. Also, it was prevented by oral administration of 10 mg per Kg of phenoxybenzamine or propranolol or aspirin or pyridinolcarbamate 3 hours before the challenge. On the other hand, the enhancement of ADP-induced platelet aggregation was not observed in vitro, when 10-5 or 3 × 10-6 molar and 129.4 ± 12.8% of the value before 10∼6 molar ADP was added to citrated platelet rich plasma (CPRP) of rabbit after incubation at 37°C for 30 second with 0.01, 0.1, 1, 10 or 100 µg per ml of adrenaline or noradrenaline. These results suggest an important interaction between endothelial surface and platelets in connection with the enhancement of ADP-induced platelet aggregation by adrenaline in vivo.

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