Search Results (46)

Acute diarrhea is a frequent problem worldwide, mostly due to gastrointestinal infections or food poisoning. Boswellia serrata could be active in the treatment of acute diarrhea due to its anti-inflammatory, antispasmodic, and antimicrobial activity. In this randomized, double-blind, placebo-controlled clinical study, 49 adults with acute diarrhea were randomly allocated to receive 250 mg of a lecithin-based delivery form of Boswellia serrata (CASP) or placebo for 5 days. The time it took to become healthy with stoppage of diarrhea (primary end point) was significantly shorter in the intervention group (3.08 vs. 4.44 days: p-value < 0.0001). The probability of subjects treated with CASP to recover sooner was equal to 80.2%. A significantly lower number of stools was observed in the CASP group over time (β = −0.17, p-value < 0.0001). A significant difference was observed between the two groups for abdominal pain, nausea, and GAE (global assessment of efficacy). In conclusion, the lecithin-based delivery form of Boswellia serrata extract could be a useful addition to the treatment of acute diarrhea in adults. CASP is safe and reduces the time it takes to become healthy, the frequency of stools, the abdominal pain and nausea of subjects with acute diarrhea. Further studies are needed to confirm these promising results. Full article

The present study attempted to evaluate and rationalize the medicinal use of the methanolic extract of the fruits of Balanites aegyptiaca (B. aegyptiaca) in the treatment of hyperactive gut disorders. The in vivo, castor oil-induced diarrhea model in mice was followed to test its antidiarrheal effect. To test the antispasmodic effect and to explore its pharmacodynamic details, isolated small intestines (ileum) obtained from rats were selected to provide physiological conditions for the ex vivo assays. In the in vivo assays, the orally administered extract of B. aegyptiaca protected mice from diarrheal drops with resultant percent inhibitions of 40% and 80% at the respective doses of 200 mg/kg and 400 mg/kg, while the highest protection (100%) was observed with a positive control drug, loperamide, at 10 mg/kg. In the ileum, B. aegyptiaca produced an antispasmodic effect in a concentration-dependent manner by inhibiting the carbachol (CCh; 1 µM) and high K⁺ (80 mM)-evoked spasms with resultant EC₅₀ values of 1.44 mg/mL (1.08–1.78) and 1.27 mg/mL (0.98–1.66), respectively. Papaverine, a known phosphodiesterase enzyme (PDE) inhibitor and blocker of Ca⁺⁺ channels (CCB), also inhibited both CCh and high K⁺ induced contractions at comparable EC₅₀ values of 8.72 µM (7.92–9.24) and 8.14 µM (7.62–8.84), respectively. Contrary to the extract and papaverine, verapamil showed distinctly higher potency in regard to inhibiting high K⁺, compared to CCh-evoked spasms that had EC₅₀ values of 0.16 µM (0.13–0.261) and 2.54 µM (2.28–2.92), respectively. The inhibitory effects of B. aegyptiaca on PDE were further confirmed when the pre-incubated extract shifted the isoprenaline-mediated relaxation curves (CRCs) towards the left, similar to papaverine, whereas the CCB-like effect was confirmed when the pre-incubated tissues with B. aegyptiaca caused deflection in the Ca⁺⁺ CRCs towards the right, constructed in Ca⁺⁺ free medium with suppression of the maximum response. Thus, this study provides detailed, mechanistic support for the medicinal use of B. aegyptiaca in the treatment of hyperactive gut disorders. Full article

Preclinical data indicate that bergamot essential oil (BEO) can modulate the synaptic functions within the central nervous system (CNS). Particularly, several data shows that essential oil is endowed with reproducible analgesic and anxiolytic effects that may derived from the ability to modulate the excitatory and inhibitory neurotransmission in the CNS. Although there are differences in the functional complexity of the enteric nervous system (ENS), it is likely that the phytocomplex has biological properties in gut superimposable to those showed in the CNS. Accordingly, the aim of this study was to investigate ex-vivo the effect of bergamot essential oil and its main constituents on the contractile activity of rat isolated colon, jejunum and ileum induced by different muscle stimulants such as acetylcholine (10⁻⁶ M) and potassium chloride (80 mM). Our present data demonstrate that BEO inhibits cholinergically- and non cholinergically-mediated contractions in rat isolated gut and that linalool is the most active component. These results suggest that the phytocomplex might be useful in the treatment of spastic disorders in ENS mainly characterized by the presence of pain; incidentally, irritable bowel syndrome (IBS) is a painful condition in which a role for neurotransmitter dysfunction has been envisaged. More investigation is required for clinical translation of the present data. Full article

Matricaria chamomilla L. is a famous medicinal plant distributed worldwide. It is widely used in traditional medicine to treat all kinds of diseases, including infections, neuropsychiatric, respiratory, gastrointestinal, and liver disorders. It is also used as a sedative, antispasmodic, antiseptic, and antiemetic. In this review, reports on M. chamomilla taxonomy, botanical and ecology description, ethnomedicinal uses, phytochemistry, biological and pharmacological properties, possible application in different industries, and encapsulation were critically gathered and summarized. Scientific search engines such as Web of Science, PubMed, Wiley Online, SpringerLink, ScienceDirect, Scopus, and Google Scholar were used to gather data on M. chamomilla. The phytochemistry composition of essential oils and extracts of M. chamomilla has been widely analyzed, showing that the plant contains over 120 constituents. Essential oils are generally composed of terpenoids, such as α-bisabolol and its oxides A and B, bisabolone oxide A, chamazulene, and β-farnesene, among other compounds. On the other hand, M. chamomilla extracts were dominated by phenolic compounds, including phenolic acids, flavonoids, and coumarins. In addition, M. chamomilla demonstrated several biological properties such as antioxidant, antibacterial, antifungal, anti-parasitic, insecticidal, anti-diabetic, anti-cancer, and anti-inflammatory effects. These activities allow the application of M. chamomilla in the medicinal and veterinary field, food preservation, phytosanitary control, and as a surfactant and anti-corrosive agent. Finally, the encapsulation of M. chamomilla essential oils or extracts allows the enhancement of its biological activities and improvement of its applications. According to the findings, the pharmacological activities of M. chamomilla confirm its traditional uses. Indeed, M. chamomilla essential oils and extracts showed interesting antioxidant, antibacterial, antifungal, anticancer, antidiabetic, antiparasitic, anti-inflammatory, anti-depressant, anti-pyretic, anti-allergic, and analgesic activities. Moreover, the most important application of M. chamomilla was in the medicinal field on animals and humans. Full article

This present study evaluated and rationalized the medicinal use of the fruit part of Acacia nilotica methanolic extract. The phytochemicals were detected using gas chromatography–mass spectrometry (GC–MS) while the in vivo antidiarrheal test was done using Swiss albino mice. To determine the details of the mechanism(s) involved in the antispasmodic effect, isolated rat ileum was chosen using different ex vivo assays by maintaining a physiological environment. GC–MS results showed that A. nilotica contained pyrogallol as the major polyphenol present (64.04%) in addition to polysaccharides, polyphenol, amino acid, steroids, fatty acid esters, and triterpenoids. In the antidiarrheal experiment, A. nilotica inhibited diarrheal episodes in mice significantly (p < 0.05) by 40% protection of mice at 200 mg/kg, while 80% protection was observed at 400 mg/kg by the orally administered extract. The highest antidiarrheal effect was observed with loperamide (p < 0.01), used as a control drug. In the ex vivo experiments, A. nilotica inhibited completely in increasing concentrations (0.3 to 10 mg/mL) the carbachol (CCh; 1 µM) and high K⁺ (80 mM)-evoked spasms in ileum tissues at equal potencies (p > 0.05), similar to papaverine, a dual inhibitor of the phosphodiesterase enzyme (PDE) and Ca⁺⁺ channels. The dual inhibitory-like effects of A. nilotica on PDE and Ca⁺⁺ were further validated when A. nilotica extract (1 and 3 mg/mL)-pre-incubated ileum tissues potentiated and shifted isoprenaline relaxation curves towards lower doses (leftward), similar to papaverine, thus confirming the PDE inhibitory-like mechanism whereas its CCB-like effect of the extract was confirmed at 3 and 5 mg/mL by non-specific inhibition of CaCl₂-mediated concentration response curves towards the right with suppression of the maximum peaks, similar to verapamil, used as standard CCB. Thus, this study characterized the chemical composition and provides mechanistic support for medicinal use of A. nilotica in diarrheal and hyperactive gut motility disorders. Full article

Urolithiasis (UL) involves the formation of stones in different parts of the urinary tract. UL is a health problem, and its prevalence has increased considerably in developing countries. Several regions use plants in traditional medicine as an alternative in the treatment or prevention of UL. Mexico has known about the role of traditional medicine in the management of urinary stones. Mexican traditional medicine uses plants such as Argemone mexicana L., Berberis trifoliata Hartw. ex Lindl., Costus mexicanus Liebm, Chenopodium album L., Ammi visnaga (L.) Lam., Eysenhardtia polystachya (Ortega) Sarg., Selaginella lepidophylla (Hook. & Grev.) Spring, and Taraxacum officinale L. These plants contain different bioactive compounds, including polyphenols, flavonoids, phytosterols, saponins, furanochromones, alkaloids, and terpenoids, which could be effective in preventing the process of stone formation. Evidence suggests that their beneficial effects might be associated with litholytic, antispasmodic, and diuretic activities, as well as an inhibitory effect on crystallization, nucleation, and aggregation of crystals. The molecular mechanisms involving these effects could be related to antioxidant, anti-inflammatory, and antimicrobial properties. Thus, the review aims to summarize the preclinical evidence, bioactive compounds, and molecular mechanisms of the plants used in Mexican traditional medicine for the management of UL. Full article

Background: Irritable bowel syndrome (IBS) is a common gastrointestinal tract disorder, affecting 10–20% of adults worldwide. Mebeverine is an antispasmodic agent indicated for the symptomatic treatment of abdominal pain caused by intestinal smooth muscle spasms and intestinal functional disorders in the course of IBS. The aim of this article was to perform a systematic literature review and update previous overviews of the efficacy and safety of mebeverine treatment in IBS. Methods: Major electronic medical databases, PubMed, EMBASE and Cochrane, were systematically searched from January 1965 to January 2021. Results: Twenty-two studies met our inclusion criteria, including 19 randomised trials, two observational retrospective studies, and one non-randomised, single-blinded study. Six studies reported a significant decrease in abdominal pain after mebeverine treatment (p-values ranging from <0.05 to <0.001). Only three studies showed no improvement after mebeverine treatment in terms of the severity of abdominal pain or discomfort. Some of the included studies also showed significant improvements in abnormal bowel habits, abdominal distension, as well as stool frequency and consistency. Adverse events were rare and associated mainly with IBS symptoms. Conclusions: Mebeverine is an effective treatment option in IBS, with a good safety profile and low frequency of adverse effects. Full article

Formulations with two or more active pharmaceutical ingredients (APIs) are a researched trend due to their convenient use compared with multiple medications. Moreover, drug-drug combinations may have a synergistic effect. Drotaverine hydrochloride (D-HCl) is commonly used for its antispasmodic action. The combination of a spasmolytic and an analgesic drug such as ibuprofen (Ibu) or ketoprofen (Ket) could become the answer for the treatment of localized pain. D-HCl:Ibu and D-HCl:Ket drug-drug interactions leading to the formation of eutectic compositions with increased bioavailability, obtained by mechanosynthesis, a green, solvent-free method was explored for the first time. The compatibility of Ibuprofen, Ketoprofen, and Drotaverine Hydrochloride was investigated using differential scanning calorimetry (DSC), X-ray diffraction (XRD), and Fourier-Transform Infrared spectroscopy (FTIR). Solid-liquid equilibrium (SLE) phase diagrams for the binary systems of active pharmaceutical ingredients were developed and the Tammann diagrams were designed to determine the eutectic compositions. The excess thermodynamic functions G^E for the pre-, post-, and eutectic compositions were obtained using the computed activity coefficients data. Results show that drotaverine-based pharmaceutical forms for pain treatment may be obtained at 0.9 respectively 0.8 molar fractions of ibuprofen and ketoprofen which is advantageous because the maximum allowed daily dose of Ibu is about 6 times higher than those of D-HCl and Ket. The obtained eutectics may be a viable option for the treatment of pain associated with cancer therapy. Full article

German chamomile (M. chamomilla) is recognized as a star herb due to its medicinal and aromatic properties. This plant is found across a wide range of climatic and soil conditions. Both the flower heads and blue essential oils of German chamomile possess several pharmacological properties of an anti-inflammatory, antimicrobial, antiseptic, antispasmodic and sedative, etc., nature, which makes it a highly sought after herb for use in many pharma and aroma industries. Chamomile tea, prepared from its flower heads, is also a well-known herbal tea for mind and body relaxation. Though it is a high-demand herb, farmers have not adopted this plant for large scale cultivation as a crop, which could improve their livelihood, due to the high cost in flower heads harvesting, loss in over mature and immature flower heads picking during harvesting, unavailability of varieties and agrotechnologies for machine harvesting, a lack of efficient process development of oil extraction and in the lack of improved stable varieties. There are many studies that have reported on the phytochemistry and pharmacological uses of chamomile, which further explore its importance in the medicine industry. Several studies are also present in the literature on its cultivation practices and plant ecology. However, studies on breeding behavior, genetic improvement, varietal development and mechanical harvesting are scarce in German chamomile. Hence, keeping in mind various aspects of farmers’ and researchers’ interest, earlier reports on taxonomy, floral biology, processing of oil extraction, active constituents, uses, agronomy, breeding challenges and opportunities in German chamomile are summarized in this review. Full article

Dysphania ambrosioides (L.) Mosyakin and Clemants is an annual or ephemeral perennial herb used traditionally in the Mediterranean region in folk medicine to treat various illnesses, including those related to the digestive system. This study aims to assess the antispasmodic, myorelaxant, and antioxidant effects of D. ambrosioides flower hydroethanolic extract and its chloroform and ethyl acetate fractions in a comparative study to evaluate the result of the extraction type on the potential activity of the extract. Both rat and rabbit jejunum were used to evaluate the antispasmodic and myorelaxant effect, while the antioxidant effect was evaluated using DPPH, a ferric reducing power assay, and a beta-carotene bleaching test. LC/MS-MS analysis was carried out to reveal the composition of the different types of extract. Following the results, the hydroethanolic extract showed a significant myorelaxant effect (IC₅₀ = 0.39 ± 0.01 mg/mL). Moreover, it was shown that the hydroethanolic extract demonstrated the best antispasmodic activity (IC₅₀ = 0.51 ± 0.05 mg/mL), followed by the ethyl acetate (IC₅₀ = 4.05 ± 0.32 mg/mL) and chloroform (IC₅₀ = 4.34 ± 0.45 mg/mL) fractions. The antioxidant tests showed that the hydroethanolic extract demonstrated high antioxidant activity, followed by the ethyl acetate and chloroform fractions. The LC/MS-MS analysis indicates that the plant extract was rich in flavonoids, to which the extract activity has been attributed. This study supports the traditional use of this plant to treat digestive problems, especially those with spasms. Full article

Cancer is a complex ailment orchestrated by numerous intrinsic and extrinsic pathways. Recent research has displayed a deep interest in developing plant-based cancer therapeutics for better management of the disease and limited side effects. A wide range of plant-derived compounds have been reported for their anticancer potential in the quest of finding an effective therapeutic approach. Rutin (vitamin P) is a low-molecular weight flavonoid glycoside (polyphenolic compound), abundantly present in various vegetables, fruits (especially berries and citrus fruits), and medicinal herbs. Numerous studies have delineated several pharmacological properties of rutin such as its antiprotozoal, antibacterial, anti-inflammatory, antitumor, antiviral, antiallergic, vasoactive, cytoprotective, antispasmodic, hypolipidemic, antihypertensive, and antiplatelet properties. Specifically, rutin-mediated anticancerous activities have been reported in several cancerous cell lines, but the most common scientific evidence, encompassing several molecular processes and interactions, including apoptosis pathway regulation, aberrant cell signaling pathways, and oncogenic genes, has not been thoroughly studied. In this direction, we attempted to project rutin-mediated oncogenic pathway regulation in various carcinomas. Additionally, we also incorporated advanced research that has uncovered the notable potential of rutin in the modulation of several key cellular functions via interaction with mRNAs, with major emphasis on elucidating direct miRNA targets of rutin as well as the process needed to transform these approaches for developing novel therapeutic interventions for the treatment of several cancers. Full article

Functional gastrointestinal disorders (FGIDs) are characterized by abdominal pain, bloating and bowel disturbances. FGID therapy is primarily symptomatic, including treatment with herbal remedies. Flower extract of Tilia tomentosa Moench (TtM) is occasionally used as an anti-spasmodic in popular medicine. Since its effect on intestinal response is unknown, we evaluated the influence of TtM extract on small intestine contractility. Ileal preparations from C57BL/6J mice were mounted in organ baths to assess changes in muscle tension, following addition of TtM extract (0.5–36 μg/mL) or a vehicle (ethanol). Changes in contractile response to receptor- and non-receptor-mediated stimuli were assessed in ileal preparations pretreated with 12 μg/mL TtM. Alterations in the enteric nervous system neuroglial network were analyzed by confocal immunofluorescence. Increasing addition of TtM induced a marked relaxation in ileal specimens compared to the vehicle. Pretreatment with TtM affected cholinergic and tachykininergic neuromuscular contractions as well as K⁺-induced smooth muscle depolarization. Following incubation with TtM, a significant reduction in non-adrenergic non-cholinergic-mediated relaxation sensitive to Nω-Nitro-L-arginine methyl ester hydrochloride (pan-nitric oxide synthase inhibitor) was found. In vitro incubation of intestinal specimens with TtM did not affect the myenteric plexus neuroglial network. Our findings show that TtM-induced intestinal relaxation is mediated by nitric oxide pathways, providing a pharmacological basis for the use of TtM in FGIDs. Full article

Antispasmodic agents are used for modulating gastrointestinal motility. Several compounds isolated from terrestrial plants have antispasmodic properties. This study aimed to explore the inhibitory effect of the pyrrolidine derivative, asperidine B, isolated from the soil-derived fungus Aspergillus sclerotiorum PSU-RSPG178, on spasmodic activity. Isolated rat ileum was set up in an organ bath. The contractile responses of asperidine B (0.3 to 30 µM) on potassium chloride and acetylcholine-induced contractions were recorded. To investigate its antispasmodic mechanism, CaCl₂, acetylcholine, Nω-nitro-l-arginine methyl ester (l-NAME), nifedipine, methylene blue and tetraethylammonium chloride (TEA) were tested in the absence or in the presence of asperidine B. Cumulative concentrations of asperidine B reduced the ileal contraction by ~37%. The calcium chloride and acetylcholine-induced ileal contraction was suppressed by asperidine B. The effects of asperidine B combined with nifedipine, atropine or TEA were similar to those treated with nifedipine, atropine or TEA, respectively. In contrast, in the presence of l-NAME and methylene blue, the antispasmodic effect of asperidine B was unaltered. These results suggest that the antispasmodic property of asperidine B is probably due to the blockage of the L-type Ca²⁺ channel and is associated with K⁺ channels and muscarinic receptor, possibly by affecting non-selective cation channels and/or releasing intracellular calcium. Full article

Transcutaneous spinal stimulation (TSS) and whole-body vibration (WBV) each have a robust ability to activate spinal afferents. Both forms of stimulation have been shown to influence spasticity in persons with spinal cord injury (SCI), and may be viable non-pharmacological approaches to spasticity management. In thirty-two individuals with motor-incomplete SCI, we used a randomized crossover design to compare single-session effects of TSS versus WBV on quadriceps spasticity, as measured by the pendulum test. TSS (50 Hz, 400 μs, 15 min) was delivered in supine through a cathode placed over the thoracic spine (T11-T12) and an anode over the abdomen. WBV (50 Hz; eight 45-s bouts) was delivered with the participants standing on a vibration platform. Pendulum test first swing excursion (FSE) was measured at baseline, immediately post-intervention, and 15 and 45 min post-intervention. In the whole-group analysis, there were no between- or within-group differences of TSS and WBV in the change from baseline FSE to any post-intervention timepoints. Significant correlations between baseline FSE and change in FSE were associated with TSS at all timepoints. In the subgroup analysis, participants with more pronounced spasticity showed significant decreases in spasticity immediately post-TSS and 45 min post-TSS. TSS and WBV are feasible physical therapeutic interventions for the reduction of spasticity, with persistent effects. Full article

A prospective study was conducted in patients with early-stage gastric cancer to determine the efficacy and safety of acupuncture stimulation as an antispasmodic compared with conventional medication during the procedure of endoscopic submucosal dissection (ESD) of the upper gastrointestinal tract. This study was a prospective single blinded quasi-randomized controlled trial. Seventy-three patients who were scheduled to undergo ESD for gastric cancer at Aizu Medical Center between 19 February 2016 and 30 June 2016 were assessed for eligibility for the study. Sixty out of 73 patients were included in the study and assigned into two intervention groups: medication group (MG) and acupuncture group (AG). Ease of the procedure was evaluated using modified NIWA classification (MNC) by endoscopist considering the frequency and amplitude of the upper gastrointestinal peristalsis. For the statistical analysis, Mann–Whitney test was used to compare the differences of MNC values (baseline and end of procedure) between two groups. The difference of MNC found in the AG (−2.00 (−3.0 to −2.0)) was significantly greater than that in the MG (−1.00 (−2.0 to −1.0), p < 0.0001, Mann–Whitney test). We consider that acupuncture to the abdomen could be an alternative antispasmodic method during upper gastrointestinal endoscopic procedure. Full article