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Molecules (Basel, Switzerland) Jun 2016The Chrysactinia mexicana A. Gray (C. mexicana) plant is used in folk medicine to treat fever and rheumatism; it is used as a diuretic, antispasmodic; and it is used for...
The Chrysactinia mexicana A. Gray (C. mexicana) plant is used in folk medicine to treat fever and rheumatism; it is used as a diuretic, antispasmodic; and it is used for its aphrodisiac properties. This study investigates the effects of the essential oil of C. mexicana (EOCM) on the contractility of rabbit ileum and the mechanisms of action involved. Muscle contractility studies in vitro in an organ bath to evaluate the response to EOCM were performed in the rabbit ileum. EOCM (1-100 µg·mL(-1)) reduced the amplitude and area under the curve of spontaneous contractions of the ileum. The contractions induced by carbachol 1 µM, potassium chloride (KCl) 60 mM or Bay K8644 1 µM were reduced by EOCM (30 µg·mL(-1)). Apamin 1 µM and charybdotoxin 0.01 µM decreased the inhibition induced by EOCM. The d-cAMP 1 µM decreased the inhibition induced by EOCM. l-NNA 10 µM, Rp-8-Br-PET-cGMPS 1 µM, d,l-propargylglycine 2 mM, or aminooxyacetic acid hemihydrochloride 2 mM did not modify the EOCM effect. In conclusion, EOCM induces an antispasmodic effect and could be used in the treatment of intestinal spasms or diarrhea processes. This effect would be mediated by Ca(2+), Ca(2+)-activated K⁺ channels and cAMP.
Topics: Animals; Apamin; Asteraceae; Calcium; Humans; Ileum; Muscle Contraction; Muscle, Smooth; Oils, Volatile; Parasympatholytics; Plant Oils; Potassium Chloride; Rabbits
PubMed: 27322223
DOI: 10.3390/molecules21060783 -
Acta Pharmaceutica (Zagreb, Croatia) Jun 2011A series of 1-substituted imidazoles 1a-d and 2a-d were synthesized and screened for antispasmodic and antidiarrheal activities. Antispasmodic activity was tested at... (Comparative Study)
Comparative Study
A series of 1-substituted imidazoles 1a-d and 2a-d were synthesized and screened for antispasmodic and antidiarrheal activities. Antispasmodic activity was tested at various concentrations on isolated tissue preparations; concentration-response curves were plotted and compared with atropine. All compounds were found to inhibit contraction of the guinea pig ileum. Castor oil-induced diarrhea model in rats was used for evaluation of antidiarrheal activity. Parameters such as intestinal transit and volume of intestinal fluid were measured for antidiarrheal activity at 40 mg kg-1 dose and compared with the standard drug loperamide at 6 mg kg-1 dose. Defecation frequency in the test group was found to be significantly lower (p < 0.01) compared to the control group and comparable with that of the standard. The present study reveals that the compounds exert antidiarrheal activity through possible inhibition of intestinal movement and reduction of capillary permeability in the abdominal cavity.
Topics: Animals; Antidiarrheals; Cholinergic Antagonists; Diarrhea; Drug Design; Guinea Pigs; Ileum; Imidazoles; Magnetic Resonance Spectroscopy; Male; Molecular Structure; Muscle Relaxation; Parasympatholytics; Random Allocation; Rats; Rats, Wistar; Spectroscopy, Fourier Transform Infrared; Structure-Activity Relationship; Transition Temperature
PubMed: 21684849
DOI: 10.2478/v10007-011-0014-6 -
Planta Medica Jan 2015Myrrh is the oleo-gum resin of mainly Commiphora molmol and as a powdered substance, one compound in the traditional medicinal product Myrrhinil-Intest®, which has been...
Myrrh is the oleo-gum resin of mainly Commiphora molmol and as a powdered substance, one compound in the traditional medicinal product Myrrhinil-Intest®, which has been used for the treatment of unspecific, inflammatory intestinal disorders. The aim of the present study was to evaluate the antispasmodic effect of myrrh under healthy and inflamed conditions, and to evaluate a calcium-antagonistic effect as a possible mode of action. Therefore, an ethanolic myrrh extract was tested for its effects on muscle tone and acetylcholine-induced contractions in untreated and inflamed rat ileum/jejunum preparations. Inflammation was experimentally induced by 2,4,6-trinitrobenzene sulfonic acid (10 mM, 30 min). Additionally, the effect of the calcium channel agonist Bay K8644 in the presence of varying myrrh extract concentrations was examined. Myrrh extract (0.99 mg/mL) suppressed the acetylcholine-induced contraction down to 25.8 % in untreated and 15.2 % in inflamed preparations. Myrrh extract (0.15; 0.25 and 0.35 mg/mL) induced a concentration-dependent rightward shift of the Bay K8644 concentration-response curve in untreated and inflamed preparations with a significant EC50 shift. Schild analysis resulted in a pA2 value of 0.93 for untreated preparations. Increasing myrrh extract concentrations induced a concentration-dependent decrease of the agonistic maximum effect in untreated and inflamed preparations down to 15.8 % and 25.8 %, respectively, for the highest concentration leading to a pD2 value of 0.58. Myrrh extract reduced intestinal muscle tone and acetylcholine-induced contraction of untreated and inflamed ileum/jejunum preparations based on dual calcium antagonism characterized by a right shift of the agonistic dose-response curve and a depression of the maximum effect. The resulting reduction of intestinal motility and spasmolytic effects provide a rationale for the symptom treatment of intestinal disorders such as irritable bowel syndrome.
Topics: Acetylcholine; Animals; Calcium; Calcium Channel Blockers; Commiphora; Disease Models, Animal; Enteritis; Female; Gastrointestinal Motility; Ileum; Jejunum; Male; Parasympatholytics; Plant Extracts; Rats; Rats, Wistar; Terpenes; Trinitrobenzenes
PubMed: 25590370
DOI: 10.1055/s-0034-1383391 -
Planta Medica Apr 1983
Topics: Animals; Guinea Pigs; In Vitro Techniques; Parasympatholytics; Plant Extracts
PubMed: 6867167
DOI: 10.1055/s-2007-969997 -
Planta Medica Apr 1980
Topics: Animals; Duodenum; Guinea Pigs; Humans; Ileum; Muscle Contraction; Muscle, Smooth; Parasympatholytics; Plants, Medicinal; Rats; Terpenes; Thymol
PubMed: 6445067
DOI: 10.1055/s-2008-1074884 -
Toxicology and Applied Pharmacology Mar 1959
Topics: Hydroxyzine; Parasympatholytics; Spasm; Tranquilizing Agents
PubMed: 13635686
DOI: 10.1016/0041-008x(59)90137-1 -
Journal of Natural Products Aug 2009Marrubium globosum ssp. libanoticum is a medicinal plant used in Lebanon to reduce pain and smooth muscle spasms. A chloroform extract obtained from M. globosum aerial...
Marrubium globosum ssp. libanoticum is a medicinal plant used in Lebanon to reduce pain and smooth muscle spasms. A chloroform extract obtained from M. globosum aerial parts reduced acetylcholine-induced contractions in the isolated mouse ileum. The purification of this extract identified, among 12 isolated labdane diterpenoids, four new compounds, named 13-epicyllenin A (4), 13,15-diepicyllenin A (5), marrulibacetal (9), and marrulactone (11). Their structures were determined by spectroscopic methods. Compound 9, which exerted antispasmodic activity, is likely the active ingredient of the extract. Preliminary structure-activity relationships for this class of compounds are suggested.
Topics: Acetylcholine; Animals; Diterpenes; Ileum; Lebanon; Male; Marrubium; Mice; Molecular Structure; Muscle, Smooth; Parasympatholytics; Plant Extracts; Plants, Medicinal; Structure-Activity Relationship
PubMed: 19650652
DOI: 10.1021/np9002756 -
Journal of Ethnopharmacology Jul 2000Satureja hortensis L. (Lamiaceae) is an annual herb that is used in the traditional medicine of Iran for treating stomach and intestinal disorders. The antispasmodic...
Satureja hortensis L. (Lamiaceae) is an annual herb that is used in the traditional medicine of Iran for treating stomach and intestinal disorders. The antispasmodic activity of S. hortensis essential oil (SHEO) was assessed on contractions of isolated ileum, induced by KCl and acetylcholine, and compared with the effect of atropine and dicyclomine. SHEO inhibited the response to 80 mM KCl in a concentration-dependent manner (pD(2)=1.55+/-0.09 microg/ml; this is negative log concentration of SHEO causing 50% of maximum inhibition) and attenuating the maximum inducible response of acetylcholine concentration-response curve. Effect of SHEO on KCl was similar to that of dicyclomine. Dicyclomine (3.46 and 34.6 ng/ml) also reduced the response to acetylcholine on rat isolated ileum without altering the maximum response and shifted the acetylcholine concentration-response curve to the right by 16-fold at 34.6 ng/ml (100 nM) bath concentration, while atropine only inhibited the response to acetylcholine. This study shows that SHEO is a relaxant of rat isolated ileum. In addition to antispasmodic activity in vitro, essential oil of this plant at a dose of 0.1 ml/100 g inhibited castor oil induced diarrhoea in mice. As the inhibition of contractile overactivity of the ileum is the base of the treatment of some gastrointestinal disorders such as colic, SHEO may have clinical benefits for treatment of these conditions.
Topics: Animals; Antidiarrheals; Castor Oil; Cathartics; Diarrhea; Female; Gas Chromatography-Mass Spectrometry; Ileum; In Vitro Techniques; Iran; Lamiaceae; Medicine, East Asian Traditional; Muscle Contraction; Muscle, Smooth; Oils, Volatile; Parasympatholytics; Phytotherapy; Plants, Medicinal; Rats; Rats, Wistar
PubMed: 10904162
DOI: 10.1016/s0378-8741(99)00209-3 -
Digestive Diseases (Basel, Switzerland) 2021Probiotics and antispasmodics have been tested extensively in the management of symptoms of irritable bowel syndrome (IBS), but they have rarely been evaluated in... (Randomized Controlled Trial)
Randomized Controlled Trial
BACKGROUND
Probiotics and antispasmodics have been tested extensively in the management of symptoms of irritable bowel syndrome (IBS), but they have rarely been evaluated in combination. The objective of this pilot study was to assess the efficacy of treatment with the probiotic formulation i3.1 (Lactobacillus plantarum CECT7484 and CECT7485 and Pediococcus acidilactici CECT7483), with or without the addition of the antispasmodic alverine/simethicone, in improving IBS-related quality of life (QoL) and reducing abdominal pain and diarrhea in patients with IBS.
METHODS
This was a randomized, placebo-controlled clinical trial with 3 parallel arms (probiotic, probiotic plus antispasmodic, and placebo). Patients with IBS (N = 55) were recruited at the Gastroenterology Department of the Juárez Hospital (México City). QoL was assessed with the IBS-QoL questionnaire, abdominal pain with a visual analog scale, and stool consistency with the Bristol scale.
RESULTS
The IBS-QoL rate of response (ITT analysis) was 50.0% for patients in the group with probiotic alone, 68.4% in the group with probiotic plus antispasmodic, and 16.7% in the group with placebo after 6 weeks of treatment (p = 0.005). Response to abdominal pain was reported by 38.9% of patients treated with probiotic, 57.9% with probiotic plus antispasmodic, and 16.7% with placebo (p = 0.035). Regarding stool consistency, a response to treatment was reported by 44.4% of patients treated with probiotic, 57.9% with probiotic plus antispasmodic, and 16.7% with placebo (p = 0.032).
CONCLUSION
The results are consistent with previous studies on the use of the i3.1 probiotic formulation for the management of symptoms in IBS patients, and the addition of an antispasmodic improves its observed effects.
Topics: Abdominal Pain; Adult; Double-Blind Method; Humans; Irritable Bowel Syndrome; Male; Middle Aged; Parasympatholytics; Pilot Projects; Probiotics; Quality of Life; Surveys and Questionnaires; Treatment Outcome
PubMed: 32810850
DOI: 10.1159/000510950 -
BioMed Research International 2018Natural products with antispasmodic activity have been used in traditional medicine to alleviate different illnesses since the remote past. We searched the literature... (Review)
Review
Natural products with antispasmodic activity have been used in traditional medicine to alleviate different illnesses since the remote past. We searched the literature and compiled the antispasmodic activity of 248 natural compounds isolated from terrestrial plants. In this review, we summarized all the natural products reported with antispasmodic activity until the end of 2017. We also provided chemical information about their extraction as well as the model used to test their activities. Results showed that members of the Lamiaceae and Asteraceae families had the highest number of isolated compounds with antispasmodic activity. Moreover, monoterpenoids, flavonoids, triterpenes, and alkaloids were the chemical groups with the highest number of antispasmodic compounds. Lastly, a structural comparison of natural versus synthetic compounds was discussed.
Topics: Animals; Asteraceae; Humans; Lamiaceae; Parasympatholytics; Structure-Activity Relationship
PubMed: 30402474
DOI: 10.1155/2018/3819714