Isolated Rabbit Jejunum Preparations Research Articles

Antidiarrheal and Antioxidant Activities of the Aerial Parts of Caralluma dalzielii N. E. Brown

Pharmacognosy Research,2022,14,1,82-88.DOI:10.5530/pres.14.1.12Published:December 2021Type:Original ArticleAuthors:Chinenye J. Ugwah-Oguejiofor, Halilu E. Mshelia, Junaidu Bello, Isah Inuwa, and Abdullahi Sulaiman Author(s) affiliations:Chinenye J. Ugwah- Oguejiofor1,*, Halilu E. Mshelia2,3, Junaidu Bello1, Isah Inuwa1, Abdullahi Sulaiman1 1Department of Pharmacology and Toxicology, Faculty of Pharmaceutical Sciences Usmanu Danfodiyo University Sokoto, Sokoto, NIGERIA. 2Department of Faculty of Pharmacy, Cyprus International University, Nicosia, Mersin 10, TURKEY. 3Department of Pharmacognosy and Ethnopharmacy, Faculty of Pharmaceutical Sciences, Usmanu Danfodiyo University, P.M.B. 2346 Sokoto, NIGERIA. Abstract:Background: Caralluma dalzielii N.E. Brown is commonly referred to as “Karan massalanci” in the Northwest Nigeria where it is used in treating several ailments including pain, diarrhea and stomach issues. Objectives: This study was aimed to investigate the antidiarrheal and antioxidant activities of aqueous aerial parts extract of Caralluma dalzielii. Materials and Methods: The aqueous aerial parts extract of Caralluma dalzielii (CDE) (100, 200 and 400 mg/kg) was evaluated for antidiarrheal properties against gastrointestinal motility, castor oil-induced and prostaglandin-E2 (PGE2) enteropooling models in Wistar rats. Its antioxidant properties were studied by determining the total phenolic content (TPC) using Folin-Ciocalteu reagent, its free radical scavenging activity using 1, 1-Diphenyl-2-Picrylhydrazyl (DPPH) and its ferric reducing antioxidant power (FRAP) assays using potassium ferrocyanide ferric chloride methods. Ascorbic acid was used as the reference. Spasmolytic effect was studied in isolated rabbit jejunum preparations in an organ bath experiment using acetylcholine (ACh). Results: CDE significantly (p<0.05) reduced gastrointestinal transit of charcoal meal and the total number of diarrheal feces in the animals. The total phenolic content was determined to be 36.67±3.33 mg GAE/g. IC50 value of 63.44 mg/mL was calculated in DPPH assay. The FRAP value was found to increase as the concentration of the extract increased. CDE inhibited acetylcholine-induced contraction of the rabbit jejunum in a concentration dependent manner with complete inhibition at 20.48 mg/mL of the extract. Conclusion: The extract of Caralluma dalzielii possesses antidiarrheal activities which may be related to its antimotility, antioxidant and antispasmodic properties. Keywords:Antioxidant, Antispasmodic, Caralluma dalzielii, Gastrointestinal motility, Rabbit jejunum.View:PDF (543.04 KB) Full Text

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

BackgroundFicus 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.MethodsIn-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.ResultsFicus 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.ConclusionThis 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.

English

Many patients in Africa often utilize herbal medicine for the management of hyperactive gut disorders such as diarrhea and abdominal colic. There is therefore a need to scientifically evaluate efficacy of this herbal remedies. This study investigated the myorelaxant effect of Carissa edulis (Forssk.) Vahl and its possible mechanism of action using isolated rabbit jejunum preparations. Pieces of jejunum were isolated from adult New Zealand white rabbits. They were then mounted in an organ bath containing Tyrode’s solution. The rate and force of jejunal contraction were recorded and analyzed using a Powerlab that was coupled to Chart5 software for windows. The effects of the extract (0.1-10.0 mg/ml) on spontaneous contraction were investigated. Its effect (3.0 mg/ml) was also studied in the presence of LG-NAME (nitric oxide synthase inhibitor), methylene blue (soluble guanylyl cyclase inhibitor) and propranolol (non-selective β adrenergic receptors antagonist). The extract dose-dependent significantly decreased the force but not the rate of spontaneous rabbit jejunal contraction. Among the blockers used, only LG -NAME significantly blocked the effect of the extract. Aqueous root bark extracts of C. edulis possess significant myorelaxant effect on isolated rabbit jejunum. This appears to be mediated through stimulation of nitric oxide release by nitric oxide synthase. Key words: Carissa edulis, diarrhea, jejunum, motility, myorelaxant.

Effects of Heliotropium strigosum and Trapa bicornis in hyperactive gut disorders

The current study was aimed to investigate the extracts from Heliotropium strigosum and Trapa bicornis phytochemically for various constituents and pharmacologically for gastro-intestinal disorders. Phytochemical analysis indicated the presence of alkaloids, flavonoids, glycosides and tannins in both the extracts. In castor oil-induced diarrhea, H. strigosum and T. bicornis, at 100-1000 mg/kg dose provided protection of 10-83% and 14-76% respectively. In isolated rabbit jejunum preparations, T. bicornis (0.01-5 mg/mL) relaxed the spontaneous and K+ (80 mM)-induced contractions with EC&lt;sub&gt;50&lt;/sub&gt; values of 1.2 mg/mL and 2.6 mg/mL respectively, suggesting that spasmolytic effect was possibly mediated through calcium channel blockade. This was further authenticated when pretreatment of tissues with T. bicornis (1-5 mg/mL) caused rightward shift of Ca++ concentration–response curves, similar to verapamil. In acute toxicity test, both extracts were safe up to 10 g/kg dose. These results indicated the usefulness of H. strigosum and T. bicornis in the treatment of hyperactive gut disorders.

Gut modulatory and butyrylcholinesterase inhibitory activities of Gaultheria trichophylla

Context: Gaultheria trichophylla Royle (Ericaceae) and related species have been used in the traditional system of medicine for the treatment of diarrhoea, pain and inflammation.Objective: The present investigation explores G. trichophylla for its potential activity in hyperactive gut disorders.Materials and methods: Antidiarrheal activity was evaluated on castor oil induced diarrhoea in mice with reference to standard drug verapamil. Gut modulatory activity was performed on isolated jejunum tissue preparations on spontaneous and high potassium induced contractions. Butyrylcholinesterase (BChE) inhibitory activity was performed with an in vitro study. Extract was tested for toxicity in mice.Results: In the in vivo studies, the methanol extract of G. trichophylla and verapamil significantly (p < 0.05, 0.01, 0.001) inhibited the frequency of defecation as well as wetting of faeces when compared with the negative control. The methanol (Gt. MeOH) extract of G. trichophylla caused a dose-dependent inhibitory effect on spontaneous contractions in isolated rabbit jejunum preparations and exhibited a partial inhibitory effect against high K+ (80 mM) induced precontractions. Gt. MeOH shifted the Ca2+ concentration–response curves (CRCs) to the right, suggesting calcium channel blocking like constituents. In an in vitro assay Gt. MeOH inhibited BChE enzyme with an IC50 values of 35.52 ± 1.17 μg/mL. The extract showed no toxicity in mice at the dose of 3 g/kg.Discussion and conclusion: This study provides evidence that G. trichophylla possesses combinations of inhibitory and stimulatory effects mediated through possible cholinergic and less potent calcium blocking constituents, respectively. The latter may be responsible for the antidiarrheal effect.

Calcium entry blocking activity of the &lt;i&gt;Elaeagnus umbellata&lt;/i&gt; fruit extract explains its use in diarrhea and gut spasm

&lt;p class="Abstract"&gt;This study was aimed to explore the pharmacological basis of potential medicinal use of &lt;em&gt;Elaeagnus umbellata&lt;/em&gt; in gut disorders. Crude extract of &lt;em&gt;E. umbellata&lt;/em&gt;, 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&lt;sup&gt;+&lt;/sup&gt;-induced contractions, with respective EC&lt;sub&gt;50&lt;/sub&gt; values of 0.3 (0.1-0.5) and 0.5 mg/mL, suggesting Ca&lt;sup&gt;++&lt;/sup&gt; channel blockade (CCB). Pretreatment of tissue with crude extract (0.1–1 mg/mL) caused a rightward shift in Ca&lt;sup&gt;++&lt;/sup&gt; concentration-response curves. With the exception of aqueous fraction, &lt;em&gt;n&lt;/em&gt;-hexane, chloroform and ethyl acetate inhibited spontaneous and high K&lt;sup&gt;+&lt;/sup&gt;-induced contractions and displaced rightward Ca&lt;sup&gt;++&lt;/sup&gt; 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 &lt;em&gt;E. umbellate&lt;/em&gt; is due to CCB-mediated spasmolytic effect, concentrated in the ethyl acetate fraction and suggests its medicinal importance in diarrhea and spasm.&lt;/p&gt;&lt;p&gt;&lt;strong&gt;Video Clip&lt;/strong&gt;&lt;/p&gt;&lt;p&gt;&lt;a href="https://youtube.com/v/Qo_y3ULC4E0"&gt;Isolation of rat jejunum&lt;/a&gt;: 2 min 32 sec &lt;/p&gt;

Antispasmodic activity of &lt;i&gt;Symplocos paniculata&lt;/i&gt; is mediated through opening of ATP-dependent K+ channel

&lt;p class="Abstract"&gt;&lt;em&gt;Symplocos paniculata&lt;/em&gt; is a medicinal plant used by native healers to manage gastrointestinal ailments. The crude methanolic extract of &lt;em&gt;S. paniculata&lt;/em&gt; was screened pharmacologically both in vitro and in vivo for the validation of its therapeutic potential. It suppressed the spontaneous activity of isolated rabbit jejunum preparations and also caused inhibition of the low K&lt;sup&gt;+ &lt;/sup&gt;(20 mM)- induced spastic contractions in isolated rabbit jejunum preparations in a manner comparable to cromakalim. The relaxant effect was found to be blocked following glibenclamide exposure of the isolated tissue preparations similar to cromakalim, suggesting that observed response was likely to be mediated through opening of ATP dependent K&lt;sup&gt;+ &lt;/sup&gt;channels. Following oral administration to mice provided protection against castor oil-induced diarrhea in a manner similar to loperamide. The plant material was found safe in toxicity study up to oral dose of 8 g/kg in mice. Hence, present study provides a scientific basis for the vernacular use of &lt;em&gt;S. paniculata&lt;/em&gt; in gastro-intestinal system.&lt;/p&gt;&lt;p&gt; &lt;/p&gt;

Rationalizing ethnopharmacological uses of Alternanthera sessilis: A folk medicinal plant of Pakistan to manage diarrhea, asthma and hypertension

Ethnopharmacological relevanceTribal herbal practitioners of Pakistan use Alternanthera sessilis (Amaranthaceae) to treat diarrhea, asthma and hypertension. ObjectiveThe current study was conducted to provide mechanistic basis for anti-spasmodic, anti- asthmatic and anti-hypertensive use of Alternanthera sessilis. Materials and methodsThe crude ethanolic extract of Alternanthera sessilis (As.Cr) and its fractions were tested in- vitro on isolated rabbit tissue preparations (i.e., jejunum, trachea, and aorta) and in-vivo in ketamin-diazepam anaesthetized normotensive rats.The responses were recorded using isotonic and isometric transducers coupled with Power Lab data acquisition system. ResultsOn isolated rabbit jejunum preparations, As.Cr exerted concentration-dependent (0.01–1.0mg/ml) spasmolytic effect and caused relaxation of K+(80mM)-induced spastic contractions. Furthermore, there was non-parallel shift in Ca++concentration response curves (CRCs) towards right at tissue bath concentrations of 0.1 and 0.3mg/ml. On isolated rabbit trachea, it relaxed carbachol (1μM)- and K+(80mM)-induced contractions at respective tissue bath concentrations of 5.0 and 1.0mg/ml. On isolated rabbit aorta, it also demonstrated relaxant effect on phenylephrine (1μM)- and K+(80mM)-induced contractions at tissue bath concentrations of 5.0 and 3.0mg/ml respectively. These findings were found to be comparable with verapamil, a reference Ca++channel blocker (CCB). The solvent-solvents fractionation revealed domination of spasmolytic effects in dichloromethane fraction as compared to aqueous fraction. Intravenous administration of As.Cr decreased mean arterial blood pressure, systolic blood pressure and diastolic blood pressure of ketamine-diazepam anaesthetized normotensive albino rats dose-dependently, at dose range of 1–10mg/kg. ConclusionOur results reflected presence of Ca++ channel blocking (CCB) activity in As.Cr, thus rationalizing medicinal use of Alternanthera sessilis in diarrhea, asthma and hypertension.

Gut modulator effect of methanolic extract of &lt;i&gt;Solanum surattense&lt;/i&gt; explains its traditional use in constipation and diarrhea

&lt;p class="Abstract"&gt;Current research was conducted to find out the pharmacological basis of the methanolic extract of &lt;em&gt;Solanum surattense&lt;/em&gt; for its traditional uses in constipation and diarrhea. In isolated rabbit jejunum preparations, &lt;em&gt;S. surattense&lt;/em&gt; 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&lt;sub&gt;50 &lt;/sub&gt;value of3.17 mg/mL. &lt;em&gt;S. surattense&lt;/em&gt; and verapamil (standard Ca&lt;sup&gt;2+&lt;/sup&gt; channel blocker) caused an inhibition of K&lt;sup&gt;+ &lt;/sup&gt;(80 mM)-induced contractions with EC&lt;sub&gt;50 &lt;/sub&gt;value of0.85 and 0.15 mg/mL respectively, suggesting Ca&lt;sup&gt;2+ &lt;/sup&gt;channels block-ade.Extract caused the rightward shift in Ca&lt;sup&gt;2+ &lt;/sup&gt;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 &lt;em&gt;S. surattense&lt;/em&gt; contains spasmogenic and spasmolytic constituents, which explains its traditional uses in constipation and diarrhea.&lt;/p&gt;&lt;p&gt; &lt;/p&gt;

Folkloric uses of &lt;i&gt;Jatropha gossypifolia&lt;/i&gt; in emesis and gut motility disorders: Pharmacological validation

&lt;p class="Abstract"&gt;&lt;em&gt;Jatropha gossypifolia&lt;/em&gt; 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 &lt;em&gt;in vivo&lt;/em&gt; and &lt;em&gt;in vitro&lt;/em&gt; experimental setting. Ethanolic extract of &lt;em&gt;J. gossypifolia&lt;/em&gt; showed the significant antiemetic potential (p&amp;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.&lt;em&gt; J. gossypifolia&lt;/em&gt; caused relaxation of high K&lt;sup&gt;+ &lt;/sup&gt;(80 mM)-induced contraction and shifted the Ca&lt;sup&gt;2+ &lt;/sup&gt;concentration-response curve to the right in a manner similar to verapamil, thus conforming its Ca&lt;sup&gt;2+&lt;/sup&gt;-channel blocking activity. These findings provide pharmacological validation for the presence of antiemetic and gut modulator (spasmogenic and spasmolytic) activates, validating its folkloric uses.&lt;/p&gt;&lt;p&gt; &lt;/p&gt;

Pharmacological basis for the medicinal use of &lt;i&gt;Viola odorata&lt;/i&gt; in diarrhea, bronchial asthma and hypertension

&lt;p class="Abstract"&gt;&lt;em&gt;Viola odorata&lt;/em&gt; 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 &lt;em&gt;V. odorata&lt;/em&gt; 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&lt;sup&gt;+ &lt;/sup&gt;(80 mM)-induced contractions and shifted the Ca&lt;sup&gt;2+ &lt;/sup&gt;concentration response curves toward right in isolated jejunum similar to verapamil (standard Ca&lt;sup&gt;2+ &lt;/sup&gt;channel blocker), confirming Ca&lt;sup&gt;2+ &lt;/sup&gt;channel blocking activity. &lt;em&gt;V. odorata&lt;/em&gt; also caused relaxation of carbachol (1 µM)- and K&lt;sup&gt;+ &lt;/sup&gt;(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&lt;sup&gt;2+ &lt;/sup&gt;channel blocking activities. It also exerted relaxant effect on phenylephrine (1 µM)- and K&lt;sup&gt;+ &lt;/sup&gt;(80 mM)-induced contractions in isolated rabbit aortic preparations thus providing rationale for its folkloric uses to treat diarrhea, asthma and hypertension.&lt;/p&gt;

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.

Pharmacological justification of use of Solena heterophylla Lour. in gastrointestinal, respiratory and vascular disorders.

BackgroundSolena heterophylla Lour. has traditionally been used in the management of diseases pertaining to gastrointestinal, respiratory and vascular system and present study was undertaken to validate its traditional uses.MethodsThe aqueous ethanolic extract of Solena heterophylla Lour (Sh.Cr) was tested in-vitro on isolated rabbit jejunum, tracheal and aorta preparations. The responses of tissues were recorded using isotonic transducers coupled with PowerLab data acquisition system.ResultsThe aqueous ethanolic extract of Solena heterophylla Lour (Sh.Cr) (0.03-1.0 mg/ml) on application to spontaneous contractions in isolated rabbit jejunum preparation exerted relaxant effect through decrease in magnitude and frequency of contractions, caused relaxation of K+(80 mM)-induced contractions and shifted the Ca2+ concentration response curves toward right in isolated rabbit jejunum preparations in a manner similar to verapamil (a standard Ca2+ channel blocker), thus confirming its Ca2+ channel blocking activity. The Sh.Cr also caused relaxation of carbachol (1 μM)- and K+(80 mM)-induced contractions in isolated rabbit tracheal preparations in a manner comparable to dicyclomine.ConclusionsThe observed relaxant effect may be outcome of anti-muscarinic and Ca2+ channel blocking activities. The Sh.Cr (0.03-1.0 mg/ml) against phenyephrine (1 μM)- and K+(80 mM)-induced contractions in isolated rabbit aortic preparations exerted a relaxant effect, possibly through Ca2+ channel blocking activity. These findings provide a rationale for the folkloric uses of the plant in the management of ailments pertaining to gastrointestinal, respiratory and vascular system.

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;

Scientific basis for use of Pyrus pashia Buch.-Ham. ex D. Don. fruit in gastrointestinal, respiratory and cardiovascular ailments.

Background Pyrus pashia Buch.-Ham. ex D. Don. has been used conventionally by many communities in the Himalayan region for the management of gastrointestinal, respiratory, and vascular complications. Set against this background, this study was carried out to justify the scientific basis to validate folkloric uses of fruits of Pyrus pashia Buch.-Ham. ex D. Don. (Pp.Cr) in traditional systems of medicine.MethodsThe crude ethanol extract of fruits of Pyrus pashia Buch.-Ham. ex D. Don. (Pp.Cr) was tested in vitro on isolated rabbit jejunum, tracheal, and aorta preparations. The responses of tissues were recorded using isotonic transducers coupled with a PowerLab data acquisition system.ResultsThe Pp.Cr on application (0.01–5.0 mg/ml) to isolated rabbit jejunum preparation exhibited relaxation through decrease in magnitude and frequency of spontaneous contractions. The Pp.Cr also exerted a relaxant (0.01–5.0 mg/ml) effect on K+(80 mM) induced contractions in isolated rabbit jejunum preparations and caused shifting of the Ca2+ curves (1.0–3.0 mg/ml) toward right in a manner similar to that of verapamil (3μM), possibly suggesting presence of Ca2+ channel blocking activity. Subsequently, Pp.Cr in a concentration-dependent fashion (0.01–10.0 mg/ml) caused relaxation of CCh (1μM) and K+ (80 mM) induced contractions in isolated rabbit tracheal preparations in a manner comparable to that of dicyclomine, suggesting that the observed relaxant effect is likely to be mediated through antimuscarinic and/or Ca2+ channel blocking activities. Moreover, when evaluated against isolated rabbit aortic preparations, the Pp.Cr in concentrations up to 10 mg/ml exhibited a contractile response that was found to be abolished subsequent to pretreatment of isolated tissue preparation with cyproheptadine (1μM), phentolamine (1μM), and losartan (1μM), suggesting that Pp.Cr may have some α-adrenergic, muscarinic, serotonergic, and angiotensin II activities.ConclusionsThe aqueous ethanolic extract of Pyrus pashia (Pp.Cr) exhibited spasmolytic, bronchodilator, and vaso-constrictive activities possibly through different mechanisms. The spasmolytic and bronchodilator activities are likely to be mediated through blockade of Ca2+ channels, while vasoconstrictive activity may be due to presence of a α-adrenergic, muscarinic, serotonergic, and angiotensin II agonistic component.

Chemical Composition and Vasorelaxant and Antispasmodic Effects of Essential Oil from Rosa indica L. Petals.

Rosa indica L. belongs to the family Rosaceae and is locally known as gulaab. It has different traditional uses in cardiovascular and gastrointestinal disorders but there is no scientific data available in this regard. Therefore, the basic aim of this study was to explore the chemical composition and gastrointestinal and cardiovascular effects of the essential oil obtained from R. indica. The chemical composition of the essential oil was investigated using gas chromatography-mass spectrometry (GC-MS) technique. The cardiovascular and gastrointestinal effects were investigated using electrophysiological measurements. The GC-MS analysis of the essential oil showed various chemical components including acetic acid, mercaptohexyl ester, butanoic acid, 2-methyl-5-oxo-1-cyclopentene-1-yl ester, artemiseole, methyl santonilate, isosteviol, caryophyllene oxide, pentyl phenyl acetate, dihydromyrcene, 1,5-octadecadien, octadecanoic acid, ethyl ester, palmitic acid (2-phenyl-1,3-dioxolan-4-yl methyl ester), santolina epoxide, and 9-farnesene. The electrophysiological measurements revealed that essential oil was more potent against K+ (80 mM) than phenylephrine precontractions using isolated rabbit aorta preparations. In isolated rabbit jejunum preparations, it showed more potency against high K+ induced contractions than spontaneous contractions. Considering these evidences, it can be concluded that R. indica essential oil may work as a complementary and alternative medicine in gastrointestinal and cardiovascular diseases.

Studies on antidiarrhoeal, antispasmodic and bronchodilator activities of Operculina turpethum Linn.

BackgroundTraditionally, Operculina turpethum has been used in a wide range of ailments such as, gastrointestinal disturbances and asthma. It is found in China, South Asia, Pacific Islands, and Australia. This study was aimed to provide a possible pharmacological basis for the medicinal use of O. turpethum in gut and airways disorders.MethodsCastor oil-induced diarrhoeal mice model and isolated tissue preparations such as, rabbit jejunum and guinea-pig tracheal preparations were used to test the antidiarrhoeal, antispasmodic and bronchodilator effects and the possible mode of action(s) of the 70% aqueous-ethanolic extract of O. turpethum black variety (OTB).ResultsIn the castor oil-induced diarrhoea in mice, the crude extract of OTB caused a dose-dependent (300–1000 mg/kg) protection from diarrhoea, similar to that of loperamide. In isolated rabbit jejunum preparations, OTB produced a dose-dependent inhibition of spontaneous and high K+(80 mM)-induced contractions with resultant median effective concentrations (EC50 with 95% confidence interval) of 1.04 mg/ml (0.59-1.54) and 0.12 mg/ml (0.10-0.15; n = 4) respectively, thus showing more potency against K+. Pretreatment of the tissue with OTB (0.01 and 0.03 mg/ml) caused a rightward shift in the concentration response curves of Ca++, similar to that of verapamil. In isolated guinea-pig tracheal preparations, OTB caused inhibition of carbachol and high K+-induced constriction at similar concentrations with respective EC50 value of 0.66 mg/ml (0.53-0.82) and 0.59 mg/ml (0.45-0.62). Activity-directed fractionation revealed that the ethyl acetate fraction was more potent than the parent crude extract and hexane fraction.ConclusionThese results suggest that the crude extract of O. turpethum possesses antidiarrhoeal, antispasmodic and bronchodilator activities, mediated possibly through the presence of Ca++ antagonist like constituent(s), though additional mechanism(s) cannot be ruled out. Thus, this study provides the evidence for the medicinal use of plant in diarrhoea and asthma.

Pharmacological basis for the medicinal use of Linum usitatissimum (Flaxseed) in infectious and non-infectious diarrhea

Ethnopharmacological relevanceLinum usitatissimum, commonly known as Flaxseed has traditionally been used for the management of diarrhea and gastrointestinal infections. This study was planned to assess pharmacological basis for the medicinal use of Flaxseed in infectious and non-infectious diarrhea. Materials and methodsThe crude aqueous-methanolic extract of Flaxseed was studied using the in vivo castor oil-induced diarrhea, gut motility and enteropooling assays. Mechanistic basis was further elucidated by testing the inhibitory effect on spontaneously contracting isolated rabbit jejunum preparations, suspended in a 10ml tissue bath containing Tyrode׳ solution, maintained at 37°C and aerated with carbogen. Antibacterial efficacy of the Flaxseed extract was tested against different enteric and non-enteric pathogenic bacteria using in vitro antibacterial assays. ResultsFlaxseed extract reduced the diarrheal score in mice, by 39%, 63.90% and 68.34% at the respective doses of 100, 300 and 500mg/kg. Intestinal secretions were reduced by 24.12%, 28.09% and 38.80%, whereas the intestinal motility was reduced by 31.66%, 46.98% and 56.20% at respective doses of 100, 300 and 500mg/kg. When tested on isolated rabbit jejunum preparations, Flaxseed extract produced a dose-dependent inhibition of both spontaneous and high K+ (80mM)-induced contractions, and shifted the concentration–response curves of Ca++ to the right with suppression of the maximum response, similar to that caused by verapamil. Flaxseed extract was found to possess bactericidal activity at the tested concentrations of 12.5mg/ml, against vancomycin-resistant Enterococcus faecalis (100%), Escherichia coli K1 (88.88%), methicillin-resistant Staphylococcus aureus (98.76%), Bacillus cereus (92.64%), Pseudomonas aeruginosa (76.83%) and Salmonella typhi (26.91±3.35%). The concentration of 10mg/ml showed bactericidal effects against all the aforementioned pathogens except Escherichia coli K1, whereas for Pseudomonas aeruginosa and Salmonella typhi, it was bacteriostatic at this concentration. ConclusionsOur results indicate that Linum usitatissimum (Flaxseed) extract exhibits antidiarrheal and antispasmodic activities by virtue of its antimotility and antisecretory effects which are mediated possibly through inhibition of Ca++ channels, though additional mechanism(s) cannot be ruled out. Flaxseed extract proved effective against both enteric and non-enteric pathogens causing diarrhea, thus ensuring wide coverage and rationalizing its medicinal use in both the infectious and non-infectious diarrhea.

Functional nature of the spasmolytic effect, phytochemical composition and acute toxicity studies on &lt;i&gt;Sauromatum guttatum&lt;/i&gt;

The aim of the present work was to study the functional nature of the potential spasmolytic effect of the crude extract of Sauromatum guttaum . It was found positive for the presence of alkaloid and tannins. In isolated rabbit jejunum preparation, S. guttaum caused inhibition of spontaneous and high K + (80 mM)-induced contractions, with respective EC 50 values (95% confidence intervals) of 1.50 mg/mL (0.69-3.02) and 1.17 mg/mL (0.81-1.61), similar to verapamil. Inhibition of high K + -induced contractions suggests Ca ++ antagonistic effect. The Ca ++ channel blocker activity of S. guttaum was confirmed when pre-treatment of the tissues with extract (0.3-3 mg/mL) caused a rightward displacement in the Ca ++ concentration-response curves. Moreover, in the acute toxicity test, S. guttaum was found safe up to the dose of 3 g/kg. The findings of the current study suggest that the S. guttaum exhibited spasmolytic activity, possibly mediated through inhibitory effect on Ca ++ entry and was found safe and this current study provides first evidence to the potential use of this plant as antispasmodic and can play a possible role as antidiarrheal.