Investigation of the laxative, spasmolytic and prokinetic properties of aqueous methanol extract of Buxus sempervirens Linn (Buxaceae)

Purpose: To investigate the spasmolytic and laxative properties of Buxus sempervirens Linn (Buxaceae) in rabbits and mice.Methods: Aqueous methanol extract (AqMeBS) as well as the dichloromethane (DCMF) and aqueous (AqF) fractions of Buxus sempervirens were investigated on isolated rabbit jejunum to explore its antispasmodic effect, relative to the standard drug, verapamil. Laxative and prokinetic potentials of 250 and 500 mg/kg doses of AqMeBS extract were evaluated in mice and compared to that of negative (normal saline) and positive (carbachol) control groups. The effects of AqMeBS and carbachol were also tested in mice pretreated with atropine (10 mg/kg). Single dose, acute oral toxicity study on AqMeBS was also executed in mice at 4000, 8000 and 12000 mg/kg doses.Results: AqMeBS, DCMF and AqF significantly inhibited the rhythmic contractility of jejunum with 0.961, 0.0327 and 0.242 mg/mL, respectively, as median effective concentrations (EC50). In addition, AqMeBS, DCMF and AqF significantly relaxed the contractions due to K+, with EC50 of 1.85, 0.05 and 1.07 mg/mL, respectively. Ca2+ concentration response curves (CCRCs) were shifted to the right by AqMeBS and DCMF, in the same manner as verapamil. In the in vivo experiments, AqMeBS produced significant (p < 0.0001) laxative and prokinetic effects at 250 and 500 mg/kg doses and was comparable to that of carbachol. The acute toxicity study showed that AqMeBS was associated with one mortality at the highest tested dose (12000 mg/kg).Conclusion: These results provide the pharmacological basis for the traditional use of B. sempervirens Linn as a laxative and prokinetic remedy in the management of constipation.Keywords: Buxus sempervirens, Calcium channel blocker, Prokinetic, Laxative, Spasmolyti

Pharmacological evaluation and validation for the folkloric use of Oligochaeta ramosa in constipation and diarrhea

Crude extract of Oligochaeta ramosa and its fractions were studied to rationalize its traditional use in GIT disturbance. In spontaneous contracting jejunum preparation, O. ramosa (0.01-1.0 mg/mL) caused a transient spasmogenic effect followed by the spasmolytic effect at higher doses (3.0-10.0 mg/mL). In atropinized jejunum preparation, O. ramosa inhibit the spontaneous and K+ (80 mM)-induced contraction at the similar doses (0.01-1.0 mg/mL), suggesting calcium channel blocking effect. The calcium channel blocking effect was confirmed when pretreatment of tissue with O. ramosa produced a dose-dependent shift in Ca+2 dose- response curve to the right, similar to that produced by the verapamil. Activity-directed fractionation revealed that the spasmolytic effect is concentrated in the dichloromethane fraction while, aqueous fraction contains both spasmogenic and spasmolytic constituents. This study validate the presence of both spasmogenic and spasmolytic components mediated through muscarinic receptor activation and calcium channel blockade respectively, which may explain its traditional uses in constipation and diarrhea

Antidiarrheal and antispasmodic activities of adiantum capillus-veneris are predominantly mediated through ATP-dependent K+ channels activation

The study was tempted to explore the scientific basis for the medicinal use of Adiantum capillus-veneris L. in diarrhea using the in vivo and in vitro assays. The crude extract of dried leaves of A. capillus-veneris exhibited antidiarrheal effect against castor oil-induced diarrhea in mice at 300 and 500 mg/kg, similar to the effect loperamide. It was also found safe up to administered dose of 7 g/kg in mice. In isolated rabbit jejunum, extract of A. capillus-veneris showed a concentration-dependent relaxation of spontaneous and low K+ (25 mM)-induced contractions and had weak inhibitory effect on high K+ (80 mM), similar to the activity pattern of cromakalim, an ATP-dependent K+ channel opener. Interestingly, its inhibitory effect on spontaneous contractions was potentiated in the presence of atropine. These data demonstrates that A. capillus-veneris possesses antidiarrheal and antispasmodic properties mediated possibly through ATP-dependent K+ channels activation, thus providing scientific basis to its folk use in abdominal colic and diarrhea

Pharmacological basis for the medicinal use of Rhus coriaria in hyperactive gut disorders

This study was aimed at providing the pharmacological basis for the medicinal use of Rhus coriaria in diarrhea. In mice, the crude of R. coriaria demonstrated antisecretory and antidiarrheal effects against castor oil-induced fluid accumulation and diarrhea at at 100 and 300 mg/kg, respectively, and was found safe up to tested dose of 5 g/kg. In isolated rabbit jejunum, R. coriaria exhibited concentration-dependent (0.01-3.0 mg/mL) relaxation of spontaneous and high K+ (80 mM)-induced contractions, similar to verapamil. The Ca++ antagonist activity was confirmed when pretreatment of R. coriaria shifted Ca++ concentration-response curves to the right with suppression of maximal response, similar to verapamil. R. coriaria also suppressed the high K+-evoked transient contractile peaks similar to the effect of cyclopiazonic acid and verapamil. This study indicates that R. coriaria possesses antisecretory, antidiarrheal and antispasmodic properties mediated possibly through Ca++ antagonist pathway, thus providing evidence to its medicinal use in diarrhea and abdominal spasm

Antidiarrheal and antispasmodic activities of polygonum bistorta rhizomes are mediated predominantly through K+ channels activation

Polygonum bistorta is a popular medicinal herb used to treat diarrhea. This study provides pharmacological basis to its folk use in diarrhea using in vivo and in vitro assays. Administration of P. bistorta 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+ (25 mM)-induced contractions with weak effect against high K+ (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+, low K+ with TEA and high K+-induced contractions. In guinea-pig ileum, mild atropine-sensitive effect was observed. This study indicates that P. bistorta possesses anti-diarrheal and antispasmodic activities mediated predominantly through K+-channels activation along with weak Ca++ antagonist effect

Ethnopharmacological studies on chrozophora prostrata 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

Antifungal and antispasmodic activities of the extracts of Euphorbia granulata

The dichloromethane and methanolic extracts of the plant Euphorbia granulata were investigated for their antifungal, antibacterial, phytotoxic, brine-shrimp cytotoxic, antioxidant, spasmolytic (antispasmodic) and acetylcholinestrase inhibitory activities. The dichloromethane extract showed strong inhibition against Microsporum canis (90%) and against Aspergillus flavus (50%). Both the extracts inhibited the spontaneous contractions in rabbit jejunum preparations with EC50 value of 0.17 and 1.3 mg/mL, respectively and also relaxed the K+-induced contractions with EC50 0.2 and 2.8 mg/mL, respectively, suggesting a calcium channel blocking activity. However, the extracts did not show antibacterial, phytotoxic, brine-shrimp cytotoxic, antioxidant and acetylcholinestrase inhibitory activities

Hepatoprotective potential of Convolvulus arvensis against paracetamol-induced hepatotoxicity

Convolvulus arvensis is traditionally used as laxative. Its decoction is used in cough, flu, jaundice and in skin diseases. It is also used to treat the painful joints, inflammation and swelling. The current study was conducted to determine its hepatoprotective activity. The results showed that extract of C. arvensis (200 mg/kg and 500 mg/kg) produced significant (p<0.05) decrease in paracetamol induced increased levels of liver enzymes and total bilirubin. Histopathological investigation and detection of active constituent, qurecetin by HPLC also supported the results. So the current study showed that ethanolic extract of C. arvensis possess hepatoprotective activity

Antispasmodic and bronchorelaxant activities of Salsola imbricata are mediated through dual Ca+2 antagonistic and β-adrenergic agonistic effects

Context: Salsola imbricata Forssk. (Chenopodiaceae) has folkloric repute for the treatment of various gastrointestinal and respiratory ailments. Objective: The present study investigates spasmolytic and bronchorelaxant effects of S. imbricata. Materials and methods: The crude aqueous-ethanol extract of the aerial parts of S. imbricata and its fractions, in cumulative concentrations (0.01–10 mg/mL), were tested on contractions of isolated rabbit jejunum and tracheal preparations. Furthermore, concentration response curves (CRCs) of Ca+2 and carbachol were constructed in the absence and presence of the extract. Standard organ bath methods were used. Results: The crude extract relaxed spontaneous, K+ (80 mM) and carbachol (1 μM)-induced contractions in jejunum preparations with respective EC50 values of 0.40 (0.35–0.46), 0.69 (0.60–0.79) and 0.66 (0.57–0.75) mg/mL. It shifted Ca+2 CRCs rightward in nonparallel manner. In isolated tracheal preparations, the crude extract caused relaxation of K+ (80 mM) and carbachol (1 μM)-induced contractions with EC50 values of 0.86 (0.75–0.98) and 0.74 (0.66–0.84) mg/mL, respectively. It displaced carbachol CRCs rightward with suppression of maximal response. In both tissues, pretreatment with propranolol (1 μM) caused rightward shift in inhibitory CRCs of the extract against carbachol-induced contractions. The ethyl acetate fraction was found more potent in relaxing smooth muscle contractions than the parent extract and its aqueous fraction. Discussion and conclusion: The results suggest that the spasmolytic and bronchorelaxant activities of S. imbricata are related to Ca+2 antagonistic and β-adrenergic agonistic effects, thus justifying some of the traditional uses of the plant

Ethnopharmacological basis for antispasmodic, antidiarrheal and antiemetic activities of Ceratonia siliqua pods

The study was conducted to provide the ethnopharmacological bases of the crude extract of seed pods of Ceratonia siliqua in the gastrointestinal spasm, diarrhea and emesis. In segregated rabbit jejunum, it showed dose-dependent (0.01-10 mg/mL) relaxation of spontaneous as well as carbachol (1 µM)-induced contraction. Pre-treatment of segregated rat ileum with C. siliqua, significantly (p<0.0001) suppressed the carbachol (1 µM)-induced contraction similar to atropine (1 µM). These results indicated that C. siliqua possesses spasmolytic activity through possible blockage of muscarinic receptor in jejunum preparations. Furthermore, the crude extract inhibited the castor oil-induced diarrhea, charcoal meal propulsion in mice and copper sulfate-induced retches in chicks in a dose-dependent manner (100, 200, 300 mg/kg). These in vitro and in vivo results indicate that C. siliqua possesses the spasmolytic and antidiarrheal activities mediated possibly through blockage of muscarinic receptors. Thus, this study provides a rationale for its folkloric use. Video Clip of Methodology: 12 min 42 sec   Full Screen   Alternat