Contractions Of Rabbit Jejunum Research Articles

Spasmolytic Effect of Grewia asiatica Fruit Extract on Isolated Smooth Muscles is Mediated via Multiple Pathways.

BackgroundGrewia asiatica Linn, or phalsa, is a commonly consumed fruit in Pakistan. The fruit is employed in the traditional medicine practice of Pakistan as a smooth muscle relaxant in different gastrointestinal (GI) and cardiovascular diseases. In this investigation, we show the antispasmodic and vasorelaxant actions of Grewia asiatica fruit extract. Methods A 70% methanolic crude extract of the plant material was prepared (Ga.Cr). Different isolated GI tissue preparations and endothelium-intact aortas from rats were utilized to observe the pharmacological actions of the extract. Results Ga.Cr, in increasing concentrations, inhibited the spontaneously contracting rabbit jejunum. In an effort to determine the mechanism of this relaxant action, contractions were induced in jejunum and ileum tissues with K+ (80 mM). Ga.Cr was able to only partially inhibit these induced contractions indicating that the mechanism might not be completely through a blockade of Ca2+ channels (CCB). When tested on low K+-(25 mM) sustained contractions, Ga.Cr cumulatively suppressed these contractions (0.1–10 mg/ml), indicating an opening of K+ channels (KCO) as the mechanism. Cromakalim, a standard KCO, was also more specific in blocking low K+-induced contractions. For the effect in aorta tissues, Ga.Cr suppressed the agonist-induced contractions from 0.3 mg/ml to 10 mg/ml. Upon challenge with L-NAME, a nitric oxide (NO) blocker, the extract response curve shifted right, indicating vasodilation was mediated via endothelial NO. Conclusion This study shows that GI antispasmodic and vasodilator activities of Ga.Cr may be mediated via a KCO mechanism in the GI tract and through the release of NO from vascular endothelium.

Gastroprotective effects of polyphenol rich extract of <i>Anacardium occidentale</i> L. leaf

The leaves of Anacardium occidentale are used in folkloric medicine for the management of gastrointestinal disorders. This study evaluated the gastroprotective properties of methanol extract of A. occidentale leaf against ethanol- and indomethacin-induced gastric ulcers. Cold maceration method was used in the preparation of methanol extract of A. occidentale leaf. The extract was concentrated under reduced pressure using a rotary evaporator. The gastroprotective effects of the methanol extract of A. occidentale was tested at 100, 200 and 400 mg/kg against ethanol and indomethacin-induced gastric ulcer. Omeprazole and misoprostol were used as the positive controls for the ethanol and indomethacin-induced gastric ulcer models respectively while distilled water was used as the negative control. The effects of the extract on histamine receptor were also evaluated on isolated rabbit jejunum. The extract significantly (p < 0.05) reduced ulcer index in the treated rats relative to the negative control. The effects of the extract were comparable with the effects of the reference drugs. The extract relaxed spontaneously contracting rabbit jejunum and inhibited histamine induced contraction of rabbit jejunum. This study suggests a pharmacological basis for the folkloric use of Anacardium occidentale in the management of gastric ulcer.Keywords: Anacardium occidentale; ulcer; ethanol; indomethacin; misoprotol; omeprazole

Validation of ethnopharmacological uses of Heliotropium strigosum Willd. as spasmolytic, bronchodilator and vasorelaxant remedy.

BackgroundHeliotropium strigosum is used in traditional medicine to manage gastrointestinal pain, respiratory distress and vascular disorders. The present study was undertaken to provide scientific evidences for these folkloric uses by in vitro experimental settings.MethodsA crude methanol extract of the Heliotropium strigosum (Hs.Cr) was tested in vitro on isolated rabbit jejunum preparations to detect the possible presence of spasmolytic activity. Moreover, isolated rabbit tracheal and aorta preparations were used to ascertain the relaxant effects of the extract.ResultsThe Hs.Cr exhibited relaxant effects in rabbit jejunum in a concentration dependent manner (0.01-3.0 mg/ml). The Hs.Cr also relaxed K+ (80 mM)-induced spastic contractions in rabbit jejunum and shifted the Ca2+ concentration response curves towards right. The extract relaxed carbachol (1 μM)- as well as K+ (80 mM)-induced contractions in rabbit trachea at concentrations ranging from 0.01 to 10 mg/ml. Moreover, Hs.Cr. also relaxed (0.01-3.0 mg/ml) the phenylephrine (1 μM)- and K+ (80 mM)-induced contractions in isolated rabbit aorta.ConclusionsThe Hs.Cr was found to exhibit spasmolytic, bronchodilator and vasorelaxant activities on isolated rabbit jejunum, trachea and aorta preparations, likely mediated through Ca2+ channel blockade. This finding may provide a scientific basis for the folkloric uses of the plant.

Dual effectiveness of Flaxseed in constipation and diarrhea: Possible mechanism

Ethnopharmacological relevanceThis study was planned to assess pharmacological basis for the medicinal use of Flaxseed in constipation and diarrhea. Materials and methodsThe oil and mucilage of Flaxseeds were studied for their laxative, and antidiarrheal activities in mice. The mechanisms of laxative and antidiarrheal activities were further studied using the isolated tissue preparations (rabbit jejunum and guinea-pig ileum) immersed in Tyrode׳s solution maintained at 37°C and aerated with carbogen gas. Isotonic responses were measured on spontaneously contracting isolated jejunum and guinea-pig ileum preparations. ResultsOral administration of Flaxseed oil (30 and 70mg/kg, orally) and mucilage (1 and 2.5g/kg, orally) caused dose-dependent increase in wet feces in mice. The spasmogenic effect of Flaxseed oil was partially blocked by pyrilamine (p<0.05) and atropine (p<0.01) in isolated rabbit jejunum whereas atropine completely blocked the effect of Flaxseed mucilage on isolated guinea-pig ileum. When studied for its antidiarrheal effect, Flaxseed oil reduced the castor oil-induced diarrheal score by 49.35% and 84.41% and intestinal secretions by 19% and 33.62% at the oral doses of 100 and 300mg/kg respectively. In isolated rabbit jejunum preparations, Flaxseed oil produced a dose-dependent inhibition of both spontaneous and low K+ (25mM) -induced contractions in rabbit jejunum. The inhibitory effect against low K+ was most sensitive to tetra-ethylammonium chloride, a non-specific K+ channel blocker, followed by glibenclamide, a partial ATP-dependent K+ channels blocker and 4-Aminopyridine, a voltage gated K+-channel blocker. ConclusionsOur results indicate that Flaxseed oil and mucilage exhibit laxative activity, mediated primarily through cholinergic pathway with weak histaminergic effect component evident in Flaxseed oil, which also showed antidiarrheal activity, mediated possibly through K+ channels activation. Thus this study rationalizes the medicinal use of Flaxseed in both the constipation and diarrhea with sound mechanistic basis.

Pharmacological evaluation of &lt;i&gt;Dactyloctenium aegyptium&lt;/i&gt;: An indigenous plant used to manage gastrointestinal ailments

&lt;p&gt;Crude extract of &lt;em&gt;Dactylotenium aegyptium&lt;/em&gt; 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, &lt;em&gt;D. aegyptium&lt;/em&gt; (1.0 mg/mL) caused relaxation of K&lt;sup&gt;+ &lt;/sup&gt;(80 mM)-induced spastic contractions in isolated rabbit jejunum preparations and there was non-parallel shift in Ca&lt;sup&gt;++&lt;/sup&gt; dose response curves towards right (0.1-0.3 mg/mL). These findings were found to be comparable with verapamil, a standard Ca&lt;sup&gt;++&lt;/sup&gt; 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&lt;sup&gt;++&lt;/sup&gt; channel blocking activity in ethanolic extract of &lt;em&gt;D. aegyptium&lt;/em&gt; thus providing scientific basis for its folkloric use in constipation and diarrhea.&lt;/p&gt;&lt;p&gt; &lt;/p&gt;&lt;p&gt; &lt;/p&gt;

Effects of aqueous and ethanol extracts of the stem bark of &lt;i&gt;Zizyphus spina-christi&lt;/i&gt; L. on isolated rabbit jejunum

Zizyphus spina-christi commonly known as Kurna has often been prescribed by traditional medicine practitioners in Borno State for the control of gastro intestinal disorders. The study focused on investigating the curative potentials of the plant material on gastro intestinal motility. Fresh samples of the stem bark were collected and used for this study. The plant material were air-dried for two weeks and pulverized. Six hundred gram of the powdered plant was placed in a thimble and extracted with 2 liters of 95% ethanol (60-80oC). Also, Six hundred gram of the powdered sample was extracted using 2 liters distilled water. The extract concentrates were subjected to preliminary phytochemical screening and then tested on rabbit jejunum. The stem bark extract of Zizyphus spina-christi demonstrated antagonism to acetylcholine induced contraction of rabbit jejunum. The effect was similar to atropine which is a known intestinal smooth muscle relaxant. The effect of acetylcholine on rabbit jejunum showed a dose dependent depolarization response between 10 ƒEg/ml-160 ƒEg/ml. Atropine was able to antagonize the effect of acetylcholine competitively at 10 ƒEg/ml. At lower doses of acetylcholine, the stem bark water extract showed more antagonist effect. However, as the doses increased similar antagonism was observed for both extracts. The result obtained therefore justifies the traditional use of the plant in controlling abnormal intestinal motility. Keywords : Zizyphus spina-christi; Aqueous extract; Ethanol extract; Rabbit jejunum; Intestinal motility

Ethnopharmacological studies on &lt;i&gt;Chrozophora prostrata&lt;/i&gt; in perspective of its folkloric reputation as purgative

This study was undertaken to validate the medicinal use of Chrozophora prostrata in constipation. The crude extract of C prostrata produced laxative effect in mice at 100 and 300 mg/kg, similar to carbachol and castor oil. In spontaneously contracting rabbit jejunum tissues, C. prostrata (0.01-3 mg/mL) exhibited atropine-sensitive spasmogenic effect, which was reproducible in guinea-pig ileum. Interestingly, at high concentrations, C. prostrata showed concentration-dependent inhibitory effect on rabbit jejunum, suggesting the presence of accompanied spasmolytic activity. When tested on induced contractions, C. prostrata completely relaxed low K+-induced contraction, while partially inhibited high K+, similar to cromakalim. Tetraethylammonium pretreatment abolished the relaxant effect of C. prostrata on low K+-induced contractions while glibenclamide caused partial inhibition, suggesting the involvement of some non-specific and ATP-dependent K+ channels. These data show that C. prostrata possesses laxative effect at low doses mediated through cholinergic action followed by the spasmolytic activity at high doses mediated possibly through K+ channel activation.

Evaluation of gut modulatory and bronchodilator activities of Amaranthus spinosus Linn.

BackgroundThe aqueous-methanolic extract of Amaranthus spinosus (A. spinosus Linn.,) whole plant, was studied for its laxative, spasmolytic and bronchodilator activities to validate some of its medicinal uses.MethodsThe crude extract of A. spinosus was studied in-vivo for bronchodilator and laxative activities and in-vitro using isolated tissue preparations which were mounted in tissue baths assembly containing physiological salt solutions, maintained at 37°C and aerated with carbogen, to assess the spasmolytic effect and to find out the possible underlying mechanisms.ResultsIn the in-vivo experiments in mice, the administration of A. spinosus increased fecal output at doses of 100 and 300 mg/kg showing laxative activity. It also inhibited carbachol-induced bronchospasm in anesthetized rats at 1, 3, 10 and 30 mg/kg indicative of bronchodilator activity. When tested on isolated gut preparations, the plant extract showed a concentration-dependent (0.01-10.0 mg/ml) spasmogenic effect in spontaneously contracting rabbit jejunum and guinea-pig ileum. The spasmogenic effect was partially blocked in tissues pretreated with atropine (0.1 μM). When tested on K+ (80 mM)-induced sustained contractions in isolated rabbit jejunum, the plant extract caused complete relaxation and also produced a shift in the Ca++ concentration-response curves (CRCs) towards right, similar to diltiazem. In rabbit trachea, the plant extract completely inhibited K+ (80 mM) and carbachol (CCh, 1 μM)-induced contractions at 1 mg/ml but pretreatment of tissue with propranolol (1 μM), caused around 10 fold shift in the inhibitory CRCs of the plant extract constructed against CCh-induced contraction. The plant extract (up to 0.3 mg/ml) also increased both force and rate of spontaneous contractions of isolated guinea-pig atria, followed by relaxation at higher concentration (1.0-5.0 mg/ml). The cardio-stimulant effect was abolished in the presence of propranolol, similar to that of isoprenaline. Activity-directed fractionation revealed that the spasmolytic component(s) was separated in the organic fraction, whereas the spasmogenic component was concentrated in the aqueous fraction.ConclusionThese results indicate that A. spinosus possesses laxative activity partially mediated through cholinergic action. The spasmolytic effect was mediated through calcium channel blocking (CCB), while bronchodilator activity through a combination of β-adrenergic and CCB pathways, which may explain the traditional uses of A. spinosus in gut and airways disorders.

Studies on Prokinetic, Laxative and Spasmodic Activities of Phyllanthus emblica in Experimental Animals

This study was aimed to provide pharmacological basis for the medicinal use of Phyllanthus emblica fruit in indigestion and constipation using the in-vivo and in-vitro assays. The crude extract of the dried fruits of Phyllanthus emblica (Pe.Cr) and its fractions were tested positive for alkaloids, saponins, tannins, terpenes, flavonoids, sterols and coumarins. Pe.Cr at the doses of 100 and 300 mg/kg exhibited the prokinetic and laxative activities in mice, which were found partially sensitive to atropine. In isolated guinea-pig ileum and rabbit jejunum, the crude extract and its aqueous fraction (Pe.Aq) caused concentration-dependent and partially atropine-sensitive stimulatory effects followed by relaxation at higher tested concentrations, being more efficacious in guinea pig, while more potent in rabbit tissues. The petroleum fraction (0.003-0.1 mg/mL) exhibited fully atropine-sensitive contractions in both guinea-pig and rabbit tissues. However, the ethyl acetate and chloroform fractions (0.003-1.0 mg/mL) showed only spasmolytic activity when studied in spontaneously contracting rabbit jejunum. This study showed that the Phyllanthus emblica possesses prokinetic and laxative activities in mice along with spasmodic effect in the isolated tissues of guinea pig and rabbit, mediated partially through activation of muscarinic receptors; thus, this study provides a rationale for the medicinal use of Phyllanthus emblica fruits in indigestion and constipation.

Intestinal, Airway, and Cardiovascular Relaxant Activities of Thymoquinone

Thymoquinone (TQ) is a bioactive component found in many medicinal herbs. In this study, we report the smooth and cardiac muscle relaxant activities of this compound. TQ concentration dependently suppressed spontaneously contracting rabbit jejunum while also relaxed high K+-(80 mM) induced contractions in jejunum and guinea-pig ileum, indicating activity at voltage-operated Ca++ channels (VOCC). Further, TQ displaced Ca++ concentration-response curves, obtained in a Ca++-free environment, to the right, showing blockade of VOCC. Similar activity was observed with verapamil, a standard VOCC blocker. TQ also exhibited nonadrenergic relaxation of agonist-induced contractions in guinea-pig trachea. When tested in fluo-4-loaded mouse lung slices, TQ inhibited ACh-induced airway narrowing and Ca++ signalling in airway smooth muscle cells. In endothelium-intact and endothelium-denuded rat aorta, TQ inhibited high K+-induced contractions at significantly lower concentrations than phenylephrine-(PE-) (1 microM) induced contractions. Relaxation of PE-induced contractions was resistant to blockade by L-NAME and atropine. In guinea-pig atria, TQ showed noncholinergic relaxation of atrial force and rate of contractions. These data suggest smooth and cardiac muscle relaxant activity of TQ possibly mediated, in part, via blockade of VOCC. The results also justify the use of TQ containing plants in related health disorders like colic, diarrhoea, cough, and asthma.

Antioxidant activity and bioactive compounds in Alhagi maurorum

drugs, we considered the response of guinea pig's ileum or rabbit's jejunum to 1 μg/ml of acetylcholine as 100% response. Results: Statistical analysis was performed using one way ANOVA and Tukey's Post Hoc test (SPSS 17), with p<0.05 considered to be significant. Aqueous fractions of Rosa damascena caused increase on the basal contraction of rabbit's jejunum and guinea pig's ileum contractions, dose dependently (p<0.001). The response of ileum and jejunum to aqueous fraction was decreased after antagonizing the cholinergic receptors.

Gut modulatory effects of Daphne oleoides are mediated through cholinergic and Ca++ antagonist mechanisms

Context: The present study describes the spasmogenic and spasmolytic activities of Daphne oleoides Schreb. (Thymelaeaceae), exploring the possible underlying pharmacological mechanisms.Aim: Pharmacological investigation of Daphne oleoides to provide evidence for its therapeutic application in gastrointestinal motility disorders.Materials and methods: Methanol crude extract of Daphne oleoides (Do.Cr) was studied in gastrointestinal isolated tissues.Results: In spontaneously contracting rabbit jejunum preparations, Do.Cr at 0.3–3.0 mg/mL caused moderate stimulation, followed by relaxant effect at the next higher concentrations (5.0–10 mg/mL). In presence of atropine, spasmogenic effect was blocked and the relaxation was emerged, suggesting that the spasmogenic effect of Daphne oleoides is mediated through activation of muscarinic receptors. When tested against the high K+ (80 mM)-induced contractions, Do.Cr (0.3–5.0 mg/mL), like verapamil, inhibited the induced contractions, suggesting Ca++ channel blockade (CCB) effect. The CCB effect was further confirmed when pre-treatment of the tissue with Do.Cr shifted the Ca++ concentration-response curves to the right, similar to that caused by verapamil.Discussion and conclusion: These results indicate that Daphne oleoides exhibits gut excitatory and inhibitory effects, occurred via cholinergic and Ca++ antagonistic pathways, respectively.

Pharmacological basis for the medicinal use of Holarrhena antidysenterica in gut motility disorders

Context: Holarrhena antidysenterica Wall. (Apocynaceae) is widely used in traditional medical system for treatment of constipation, colic, and diarrhea.Aim: This study was carried out to provide pharmacological basis for medicinal use of Holarrhena antidysenterica in gastrointestinal disorders.Materials and methods: Hydro-ethanolic crude extract of Holarrhena antidysenterica (HaCE) and its fractions were studied in various gastrointestinal isolated tissue preparations.Results: In guinea pig ileum tissues, HaCE at 0.3-10 mg/mL caused pyrilamine-sensitive spasmogenic effect. When tested in spontaneously contracting rabbit jejunum preparations, HaCE (0.01-3.0 mg/mL) caused moderate stimulation, followed by a relaxant effect at next higher concentrations. In presence of pyrilamine, the contractile effect was blocked and the relaxation was observed at lower concentrations (0.01-0.3 mg/mL). HaCE inhibited the high K+ (80 mM)-induced contractions at concentration range of 0.01-1.0 mg/mL and shifted Ca++ concentration response curves to the right, like that caused by verapamil. Activity-directed fractionation revealed that the spasmogenic component was concentrated in the aqueous fraction, while the spasmolytic component was concentrated in the organic fraction.Discussion and conclusion: These results indicate that the gut stimulant and relaxant activities of Holarrhena antidysenterica are mediated possibly through activation of histamine receptors and Ca++ channel blockade, respectively and this study provides sound mechanistic background for its usefulness in gut motility disorders such as constipation, colic, and possibly diarrhea.

Preliminary evaluation of the antispasmodic and lipoxygenase inhibitory effects of some selected medicinal plants

The present study aimed to evaluate the possible antispasmodic and lipoxygenase inhibitory activity of some Pakistani medicinal plants. Extracts from Aconitum laeve Royle (Ranunculaceae), Trichodesma indicum Linn. (Boraginaceae), and Sauromatum guttatum Schott (Araceae) (corms) were tested on the isolated rabbit jejunum. All the extracts caused reduction in spontaneous and acetylcholine-induced contractions. A. laeve displayed excellent spasmolytic activity and almost (95%) diminished the normal contraction of rabbit jejunum at a concentration of 0.25 mg/mL of final bath. T. indicum inhibited the intestinal contractions by 78% at 5 mg/mL while S. guttatum (corms) caused 69% inhibition of spontaneous contractions at a concentration of 2 mg/mL. Extracts from A. laeve, T. indicum, S. guttatum (leaves and berries) and Paeonia emodi Wall. (Paeoniaceae) were screened in vitro for lipoxygenase inhibitory activity. All the extracts except A. laeve, showed good to excellent inhibition of the tested enzyme. P. emodi and S. guttatum (leaves) each inhibited the enzyme by 90% while T. indicum and S. guttatum (berries), respectively, showed 64.5% and 65% inhibitory activity against this enzyme.

Serotonergic Properties of the Roots of Clerodendron capitatum

The aim of this study is to investigate the pharmacological effects of the methanolic extract of Clerodendron capitatum, CC, (family verbenaceae). These investigations were carried out on isolated frog rectus abdominus muscle and rabbit aortic strips and jejunum and non-pregnant rat uterus pretreated with oestradiol. Results showed that CC did not demonstrate any contracting, relaxant or blocking effects on frog rectus abdominus muscle and rat aortic strip preparations. The extract produced a concentration-dependent (p<0.05, t-test, n = 6) decrease of the normal rhythmic contraction of rabbit jejunum, however, this effect was reversed by prior addition of cyproheptadine (non-specific 5-HT antagonist). In addition, CC also produced a stimulant activity on rat uterus which was blocked by cyproheptadine. Future study is recommended to study the specificity of CC to different 5-HT receptors by using different isolated animal tissues and specific 5-HT antagonists.

Presence of cholinergic and calcium antagonist constituents in Saussurea lappa explains its use in constipation and spasm

This study was carried out to provide a scientific basis for the traditional use of Saussurea lappa, in constipation and spasms. Isolated tissue preparations were used to see if the aqueous-methanol crude extract of the S. lappa root (Sl.Cr) contains gut stimulatory and inhibitory constituents. In isolated guinea-pig ileum, a quiescent preparation, Sl.Cr caused a concentration-dependent (0.3-5.0 mg/mL) spasmogenic effect, with the maximum effect reaching 91% of the acetylcholine maximum. A further increase in concentration caused a declining effect, indicating the presence of spasmolytic constituent(s). The spasmolytic effect was more marked in the spontaneously contracting rabbit jejunum and in the atropinized preparations. The spasmolytic effect was mediated through calcium channel blocking (CCB) activity, as evident by its inhibitory effect against high K(+) (80 mm)-induced contraction and displacement of the Ca(++) concentration-response curves to the right. These data indicate that the crude extract of Sl.Cr contains gut stimulatory constituent(s) of cholinergic-type providing a scientific basis for its use in constipation. The presence of spasmolytic constituents of CCB-type more evident in the spontaneous contracting gut preparation may explain its use in spasms.

Presence of cholinergic and calcium channel blocking activities explains the traditional use of Hibiscus rosasinensis in constipation and diarrhoea

The aqueous-ethanolic extract of the aerial parts of Hibiscus rosasinensis Linn. (Malvaceae) was studied for the possible presence of spasmogenic and spasmolytic constituents to rationalize its traditional use in gastrointestinal disorders. The crude extract (Hr.Cr) caused a concentration-dependent (1–10 mg/mL) spasmogenic effect in isolated guinea-pig ileum, which was blocked in the presence of atropine (0.1 μM). In spontaneously contracting rabbit jejunum, the plant extract exhibited a weak stimulatory effect at lower doses (0.03–0.30 mg/mL) followed by an inhibitory effect at higher doses (1.0–3.0 mg/mL). Pretreatment of the tissues with atropine blocked the stimulatory effect resulting in the potentiation of the spasmolytic effect. Hr.Cr (0.03–1.0 mg/mL) also showed an inhibitory effect on K + (80 mM)-induced contractions. The calcium channel blocking activity was confirmed when Hr.Cr shifted the Ca 2+ concentration–response curves to the right, similar to verapamil. Activity-directed fractionation revealed that the spasmolytic component(s) was separated in the ethyl acetate, while the spasmogenic in the petroleum ether fraction. The aqueous fraction exhibited a combination of weak spasmogenic and spasmolytic effects. These data indicate that the crude extract contains spasmogenic and spasmolytic constituents mediating their effect through cholinergic receptors activation and blockade of Ca 2+ influx, respectively, which may explain its traditional use in constipation and diarrhoea.

Cholinomimetic and calcium channel blocking activities of Carthamus oxycantha

The crude extract of Carthamus oxycantha (Co.Cr) and its fractions were studied in vitro for their possible spasmogenic and spasmolytic activities. Co.Cr (0.03-10 mg/mL) caused an atropine sensitive spasmogenic effect in guinea-pig ileum. In spontaneously contracting rabbit jejunum preparations, Co.Cr caused a dose-dependent (0.03-3.0 mg/mL) spasmogenic effect, followed by relaxation at the next higher doses of 5.0-10.0 mg/mL. In the presence of atropine, the spasmogenic effect was blocked and the relaxant effect was observed at lower doses (0.1-5.0 mg/mL), shifting the inhibitory dose-response curves to the left. Co.Cr also inhibited K(+) (80 mm)-induced contractions in atropinized preparations at similar doses, suggesting calcium channel blockade (CCB) activity. The CCB effect was further confirmed when pretreatment of the tissue with Co.Cr produced a dose-dependent shift in the Ca(++) dose-response curves to the right, similar to that caused by verapamil. Activity-directed fractionation revealed that the spasmolytic effect was concentrated in organic fractions in the following order of potency: hexane > ethylacetate > chloroform, while the aqueous fraction exhibited spasmogenic and weak spasmolytic effects. These results indicate that Carthamus oxycantha contains a combination of spasmogenic (cholinergic) and spasmolytic (calcium antagonist) constituents.

Pharmacological basis for the use of Fumaria indica in constipation and diarrhea

The crude extract of Fumaria indica whole plant (Fi.Cr) and its fractions were studied in vitro for spasmogenic and spasmolytic effects to rationalize some of the traditional uses. Fi.Cr (1.0–5.0 mg/mL) caused a moderate degree of atropine-sensitive spasmogenic effect in guinea-pig ileum. In spontaneously contracting rabbit jejunum, Fi.Cr (0.03–0.3 mg/mL) caused a mild spasmogenicity followed by relaxation at the higher doses. In the atropinized preparations, Fi.Cr inhibited spontaneous and K +-induced contractions at the similar doses (0.1–1.0 mg/mL), which suggests calcium channel blockade (CCB). CCB effect was confirmed when pretreatment of the tissue with the Fi.Cr produced a dose-dependent shift in the Ca 2+ dose–response curves to the right, similar to that produced by verapamil. Activity-directed fractionation revealed that the spasmolytic effect is concentrated in the petroleum ether fraction, while dichloromethane fraction contains both spasmogenic and spasmolytic constituents. These data indicate that the presence of cholinergic and CCB constituents in Fi.Cr may explain the respective traditional use of Fumaria indica in constipation and diarrhoea.

ETHNOPHARMACOLOGICAL EVALUATION OF ANTISPLASMODIC ACTIVITY OF ESSENTIAL OILS FROM DIFFERENT PLANTS

Achillea santolina, Nepeta cataria and Salvia bucharica are mainly known to possess antispasmodic use in traditional medicine. The essential oils from these plants were screened for their possible pharmacological activity with possible mode of action explored. Volatile oil was extracted by steam distillation using standard procedure given in British Pharmacopoeia 2001. For pharmacological activity, rabbits were killed by cervical dislocation and jejunum was dissected out. About 2 cm pieces of rabbit jejunum were suspended separately in 10 ml isolated tissue baths containing Tyrode’s solution maintained at 37?C and aerated with carbogen. The responses were recorded on the Harvard Student Oscillograph. The oils, after solubilizing in different solvent systems according to their solubility, showed dose-dependent relaxation of spontaneous contractions of rabbit jejunum thus showing spasmolytic activity. The effect was dose-dependent, mediated at the dose range of 0.01-0.3 mg/ml. When tested on high K+ (80 mM)-induced contractions, the oils from all plants showed varying degree of relaxant effect observed at the dose range of 0.01-0.3 mg/ml. This study indicates that the spasmolytic effect is mediated through the presence of calcium channel blocking constituents in these plants, and thus provides sound scientific base for some of the traditional uses of the plants.