Search Results (81)

Background: Cardiovascular diseases, particularly hypertension, and gastrointestinal disorders represent major public health concerns in Mexico. Although a range of pharmacological treatments exists, their use is associated with adverse effects, highlighting the need for safer therapeutic alternatives. Species of the Ipomoea genus are widely employed in Mexican traditional medicine (MTM) for their purgative, anti-inflammatory, analgesic, and sedative properties. Particularly, Ipomoea purpurea is traditionally used as a diuretic and purgative; its leaves and stems are applied topically for their anti-inflammatory and soothing effects. This study aimed to determine their phytochemical composition and to evaluate the associated vasodilatory activity, modulatory effects on intestinal smooth-muscle motility, and toxicological effects of the methanolic (ME-Ip) and dichloromethane (DE-Ip) extracts obtained from the aerial parts of I. purpurea. Methods: The phytochemical composition of the ME-Ip and DE-Ip extracts of I. purpurea was assessed using UPLC-QTOF-MS and GC-MS, respectively. For both extracts, the vasodilatory activity and effects on intestinal smooth muscle were investigated using ex vivo models incorporating isolated rat aorta and ileum, respectively, whereas acute toxicity was evaluated in vivo. Results: Phytochemical analysis revealed, for the first time, the presence of two glycosylated flavonoids within the Ipomoea genus; likewise, constituents with potential anti-inflammatory activity were detected. The identified compounds in I. purpurea extracts may contribute to the vasodilatory, biphasic, and purgative effects observed in this species. The EC₅₀ values for the vasodilatory effects of the methanolic (ME-Ip) and dichloromethane (DE-Ip) extracts were 0.80 and 0.72 mg/mL, respectively. In the initial phase of the experiments on isolated ileal tissues, both extracts induced a spasmodic (contractile) effect on basal motility, with ME-Ip exhibiting higher potency (EC₅₀ = 27.11 μg/mL) compared to DE-Ip (EC₅₀ = 1765 μg/mL). In contrast, during the final phase of the experiments, both extracts demonstrated a spasmolytic effect, with EC₅₀ values of 0.43 mg/mL for ME-Ip and 0.34 mg/mL for DE-Ip. In addition, both extracts exhibited low levels of acute toxicity. Conclusions: The phytochemical profile and the vasodilatory and biphasic effects of the I. purpurea extracts explain, in part, the use of I. purpurea in MTM. The absence of acute toxic effects constitutes a preliminary step in the toxicological safety assessment of I. purpurea extracts and demonstrates their potential for the development of phytopharmaceutic agents as adjuvants for the treatment of cardiovascular and gastrointestinal disorders. Full article

Decoctions of stem barks from Aucoumea klaineana, Canarium schweinfurthii, Pentadesma butyracea and Scorodophloeus zenkeri are used against affections of irritable bowel syndrome in Gabonese traditional medicine. In the present study, we aim to determine whether the bark polysaccharides may contribute to the activity of these plants against the symptoms of gastrointestinal disorders. To this end, we investigated the structure and the pharmacological activity of polysaccharides extracted from their stem barks. The pectic and hemicellulose polysaccharides were isolated, and their sugar compositions were determined by gas chromatography. In addition, analysis by MALDI-TOF mass spectrometry of oligosaccharides released after digestion with an endo-xylanase indicated that glucuronoarabinoxylans are the main hemicellulose of stem barks. We then evaluated the influence of the polysaccharide fractions on the spontaneous contractile activity of rat ileal smooth muscle and the cholinergic system. Spasmolytic activity of pectic fractions from all stem barks, as well as lemon polygalacturonic acid, were observed, indicating that these extracts exhibit a myorelaxant activity. In contrast, the bark hemicellulose fractions, as well as commercially available beechwood glucuronoxylan and wheat arabinoxylan, were demonstrated to be able to increase the basal contractile activity of smooth muscle. These data show that, beyond physicochemical effects affecting the bowel water content, plant polysaccharides have also an impact on the spontaneous smooth muscle contractility, the main mechanism involved in the pathophysiology of gastrointestinal disorders. Full article

Human pathogenic fungi are the source of various illnesses, including invasive, cutaneous, and mucosal infections. One promising solution is using nanoparticles (NPs) as an antifungal agent. The current study aims to assess the antimicrobial and antifungal effects of drug-loaded silver nanoparticles (AgNPs) with previously reported mebeverine analogue (MA) as a potential drug candidate targeting gut microbiota and inflammation in the gastrointestinal tract. Density Functional Theory (DFT) calculations were conducted to identify possible mechanisms by which AgNPs could prevent microorganisms from growing. In vitro and ex vivo anti-inflammatory, in vitro antimicrobial, ex vivo spasmolytic activities, and in vitro hepatic cell morphology and proliferation of drug-loaded AgNPs were assessed. The drug-loaded AgNPs were considered to have promising antifungal activity against all tested fungal strains, Aspergillus niger, Penicillium chrysogenum, and Fusarium moniliforme, and yeasts, Candida albicans, Saccharomyces cerevisiae, and good antimicrobial activity against Gram-positive and Gram-negative bacterial strains. The results of in vitro and ex vivo determination of anti-inflammatory activity indicated that the drug-loaded AgNPs preserved MA’s anti-inflammatory activity and decreased inflammation. A similar effect was observed in spasmolytic activity measurements. Drug-loaded AgNPs also influenced the morphology and proliferation of hepatic cells, indicating a potential for improved gut and liver therapeutic efficacy. Each test was performed in triplicate, and the results were reported as mean values. Based on the results, drug-loaded AgNPs might be a promising antimicrobial agent, maintaining the MA’s potential as a spasmolytic and anti-inflammatory agent. Future in vivo and preclinical experiments will contribute to establishing the in vivo properties of drug-loaded AgNPs. Full article

Background/Objectives: Haloxylon griffithii is a medicinal plant possessing therapeutic effects in disorders associated with the gastrointestinal (GIT) system. This research aims to study the pharmacological activity of Haloxylon griffithii in a multidimensional manner, involving phytochemistry screening and in vitro and in vivo experiments. Methods: The whole dried plant was extracted with 80% methanol and further fractionation using solvents of increasing polarity. GC-MS analysis was performed on the crude extract to discover volatile compounds. The spasmolytic/spasmogenic effect was assessed in isolated rabbit jejunum using spontaneous and K⁺-induced contractions, as well as contractions induced by increasing concentrations of calcium ions in depolarized tissue. Antidiarrheal activity was evaluated in Swiss albino rats/mice (n = 6/group) using castor oil-induced diarrhea and peristaltic index models. In silico ADMET screening was conducted via SwissADME and pkCSM. Results: The GC-MS profiling of H. griffithii revealed the presence of 59 phytochemicals and a rare azulene derivative and constituents, including α-santonin and hexadecanoic acid esters, with favorable pharmacokinetic profiles, as predicted using SwissADME and pkCSM computational tools. The in vitro and in vivo experiments revealed the significant calcium channel blocking activity in non-polar fractions (n-hexane and ethyl acetate), while the polar extracts (ethanolic, aqueous) exhibited cholinergic effects, indicating a dual mode of action. Conclusions: This was a first-time demonstration of both antidiarrheal and smooth muscle-relaxant activity in H. griffithii, supported by GC-MS profiling and pharmacological assay. The findings lend scientific credibility to the traditional use of the plant in community healthcare, while also reinforcing the need for further pharmacological and clinical studies to explore its potential in drug development. Full article

Background/Objectives: This study is the first report on isolating a natural benzyl benzoate (nBB) from Acridocarpus smeathmannii (DC.) Guill. & Perr roots. Methods: The structure was verified using GC-MS, HPLC-UV-VIS, and two-dimensional NMR. Since it is known for its vasodilatory and anti-spasmolytic actions, we investigated the biological effects of nBB on human prostate smooth tissue (rPx) obtained from a radical prostatectomy. For this purpose, rPx was incubated with nBB (0.05, 0.25, or 0.5 µM) in an organ bath, and then cumulative concentration–response curves were constructed for adrenergic agonists and electrical field stimulation (EFS). Results: Adding the various concentrations, nBB showed potential inhibition during agonist-induced contractions (0.1–100 µM). Also, neurogenic contractions of rPx by EFS (2–32 Hz) were reduced by up to 57%. Conclusions: Overall, this study reports on an efficient protocol of nBB isolation from A. smeathmannii and its contractility effects on human prostate smooth muscle. Potentially, this could contribute to the natural production of BB from A. smeathmannii species while giving it evolutionary recognition. However, since BB influences prostate smooth muscle contractility, caution in patients taking herbal supplements containing nBB is essential, as this may play a role in contributing to the symptoms of urinary tract conditions. Full article

The flowers of Santolina chamaecyparissus have a distinct aroma and taste, with a wide range of applications in medicine, food, and packaging. Its essential oil offers numerous health benefits, including antioxidant, hepatoprotective, anticancer, antidiabetic, spasmolytic, anti-inflammatory, immunomodulatory, antimicrobial, and antiparasitic properties. Additionally, it is used as a flavoring agent in food and beverages and as a natural preservative in edible coatings for food packaging. This study investigates the chemical composition and sensory properties of the S. chamaecyparissus essential oil from Serbia, obtained via hydrodistillation, and includes a literature-based analysis of the existing profiles. Gas Chromatography–Mass Spectrometry (GC–MS) was employed for identifying the essential oil composition, while chemometric techniques like the genetic algorithm (GA), quantitative structure–retention relationship (QSRR) analysis, artificial neural network (ANN), and molecular descriptors were applied to ensure accurate and reliable results for authenticating the oil. Among the 47 identified compounds, oxygenated monoterpenes, especially artemisia ketone (36.11%), and oxygenated sesquiterpenes, notably vulgarone B (22.13%), were the primary constituents. Chemometric analysis proved effective in predicting the oil’s composition, and sensory evaluation revealed a herbal aroma with earthy, woody, and camphoraceous notes. A literature review highlighted the variability in oil composition due to geographical, environmental, and extraction factors, underscoring its chemical diversity, bioactivity, and potential applications. Full article

Background/Objectives: Hyoscine butylbromide (HBB) is a spasmolytic drug classified as indispensable by the World Health Organization. While mostly used in adults, it is also approved for use in adolescents and children aged 6 years and older. We have comprehensively reviewed the efficacy and safety of HBB in approved and off-label childhood indications. Results: Childhood studies covered an age range starting as early as 2 days. A randomized controlled trial (RCT) found a similar efficacy compared to paracetamol in the approved indication of abdominal cramps and pain. Among off-label uses, several studies demonstrate efficacy in general anesthesia and various diagnostic procedures, but the largest body of evidence relates to use in childbirth/labor, including 17 RCTs. While these largely focused on efficacy outcomes on the mother, fetal safety outcomes were reported in 12 of these studies, mostly as effects on the APGAR score and/or heart rate. The overall evidence supports safety in infants and children including those younger than the approved use age of 6 years and older. Conclusions: While only limited pediatric efficacy data from RCTs are available in the approved indications, data from thousands of patients in RCTs, case series, and non-randomized trials do not raise concerns on the safety and tolerability of HBB in childhood. Additional dedicated childhood studies, particularly RCTs, on efficacy are recommended. Full article

Background/Objectives: Mebeverine hydrochloride (MBH) is an antispasmodic agent used to regulate bowel movements and relax intestinal smooth muscle, but its application is limited by specific side effects; therefore, this study investigates the effects of previously synthesized MBH-loaded silver nanoparticles (AgNPs) on smooth muscle contractile activity and their anti-inflammatory potential as an alternative delivery system. Methods: The interactions of AgNPs with cholinergic inhibitors, selective antagonists, Ca²⁺ blockers, and key neurotransmitters were analyzed. In vitro, albumin denaturation suppression and ex vivo assays evaluated the anti-inflammatory effects of AgNPs-MBH, validated using a DFT in silico approach. To comprehensively assess the systemic impact and IBS treatment potential of AgNPs-MBH, we also examined in vitro their antimicrobial activity and hepatic cell responses, as the liver is a key organ in evaluating the overall safety and efficacy of nanoparticles. Additionally, the drug-release capabilities of Ag NPs were established. Results: Our findings indicate that AgNPs with MBH do not affect blocked cholinergic receptors, but their effects are more pronounced and distinct in amplitude and character than MBH. MBH-loaded AgNPs showed a lower anti-inflammatory effect than MBH but were still better than diclofenac. They also affected hepatic cell morphology and proliferation, suggesting potential for enhanced therapeutic efficacy. Drug-loaded AgNPs are considered not bactericidal. Conclusions: Based on our results, drug-loaded AgNPs might be a promising medication delivery system for MBH and a useful treatment option for IBS. Future in vivo and preclinical experiments will contribute to the establishment of drug-loaded AgNPs in IBS treatment. Full article

Background: Moringa oleifera is one of the most famous plants used for medicinal purposes. Its leaf extracts have antimicrobial activity and antioxidant activities, and reduce swelling in ulcers. Objectives: The present article aimed to determine the metabolic profile of Moringa oleifera leaf extracts from two samples originating from India and to evaluate in vitro and ex vivo their biological activities. Methods: The antioxidant properties of Moringa oleifera leaf extracts (methanol, 50% ethanol, and 70% ethanol) were studied in vitro for antimicrobial, anti-inflammatory, and antioxidant activities. The ex vivo contractile effects of the extracts were determined by assaying circularly isolated smooth muscle (SM) strips from a rat’s stomach. Results: The obtained results indicated that one of the samples had amino acid and organic acid content approximately twice that of the second sample. In all the tests, the 50% ethanol extract of both samples showed better antioxidant activity (209 mM TE 100 g⁻¹ for the DPPH method). The 70% ethanolic extract of Sample 1 exhibited the strongest antimicrobial activity, inhibiting Gram-positive Bacillus cereus, Bacillus subtilis, and Staphylococcus aureus. The 50% ethanolic extract of both samples exhibited the highest anti-inflammatory activity, demonstrating a twice better effect than the reference drug diclofenac. Finally, the pre-incubation of SM preparations with both samples significantly enhanced the ACh-induced contractile response, increasing it by 134% and 111%, respectively. Conclusions: The findings suggested potential applications of Moringa oleifera as a suitable candidate for antimicrobial, antioxidant, anti-inflammatory, and antispasmodic supplementation for alternative pharmaceutical and nutraceutical products. Full article

The use of herbal medicines containing Petasites hybridus extracts has a long history in the treatment of various ailments. The observed effects are primarily due to pharmacologically active compounds such as petasin, isopetasin, and neopetasin. In evidence-based phytotherapy, extracts from leaves and rhizomes are applied for different indications. While leaf extracts are administered to treat allergic rhinitis symptoms, rhizome extracts are utilized among others in the management of gastrointestinal spasms and migraines. The quality and source of plants are critical for producing authorized herbal medicinal products. Although the preparation of P. hybridus leaf extracts from cultivated plant material is already established, the rhizomes used for preparing extracts are still derived from commercial wild collections. However, switching to cultivation is desirable to ensure consistent quality and availability. For regulatory purposes, comparative pharmacological studies are needed to assess the bioactivity of plant material from different sources. Therefore, this study analyzed rhizome extracts from wild harvesting and cultivation for their petasin composition (i.e., isopetasin, neopetasin, petasin) and spasmolytic effects on Ca²⁺-dependent precontracted guinea pig ileum ex vivo. The results confirm petasins as active compounds of P. hybridus rhizome extracts. Moreover, they demonstrate that the total content of petasins determines the spasmolytic effects, regardless of the individual composition of the different petasins. No significant differences in efficacy were found between cultivated and wild-collected rhizomes, demonstrating that cultivated material is a reliable, consistent, and sustainable alternative for P. hybridus rhizome extract production. Full article

Jasonia glutinosa (L.) DC., commonly known in Spain as “Rock Tea”, is a medicinal plant native to the Iberian Peninsula, southern France, and Morocco. It has traditionally been used as a digestive, analgesic, antimicrobial, antidepressant, or for respiratory diseases. This narrative review aims to scientifically validate the ethnopharmacological uses of J. glutinosa as a medicinal plant, emphasizing the relationship between its traditional applications, pharmacological activities, and mechanisms of action based on experimental evidence. A comprehensive search was conducted in various electronic databases to gather information on its traditional uses, phytochemical composition, and in vitro, ex vivo, and in vivo studies related to pharmacological properties. The literature review uncovered significant findings regarding the pharmacological and molecular mechanisms of this medicinal plant in various experimental models, particularly highlighting its spasmolytic, anti-inflammatory, and antioxidant properties. Full article

Background: Diagnostic angiography of coronary arteries is one of the most common procedures in invasive cardiology and is mainly performed via the radial artery. Rapid improvements in the quality of the equipment and operator’s experience have changed the landscape of this procedure. Methods: In this study, 284 patients were analyzed to determine whether heparin administration should be a necessity for all patients to prevent radial artery occlusion (RAO). Moreover, the possible influence of 51 other factors on RAO was analyzed. Results: This study revealed that heparin administration does not have a significant impact on RAO incidence (p = 0.131). However, it was found that a longer fluoroscopy time (p < 0.001) and smaller (5F) vascular sheath (p = 0.001) might serve as protective factors against RAO. On the other hand, a greater number of catheters (p < 0.001), greater compression time (p = 0.001), wider (6F) vascular sheath (p = 0.002), spasm occurrence (p = 0.001), spasmolytic administration (p < 0.001) and atherosclerotic changes in the radial artery (p = 0.005) were risk factors for RAO. Conclusions: This study demonstrates the need for a more personalized approach to the patient when analyzing the individual risk of RAO. In our opinion, it is possible to omit heparin in cases of patients with an initial low risk of RAO or possible adverse drug reactions during diagnostic angiography. Full article

Red currant (Ribes rubrum L.) berries are rich in bioactive compounds and exhibit nutritive and protective features. This research examined the content of secondary metabolites of the red currant variety Redpoll lyophilized juice and waste extract and their antioxidative and spasmolytic effects. The flavonol and anthocyanin contents of the samples were determined using high-performance liquid chromatography. The antispasmodic effects were assessed in in vitro conditions, and the potential impact of the samples and possible action mechanisms were revealed. The results showed the prevalence of cyanidin-3-O-glucoside as the dominant anthocyanin with higher content in the juice sample. Quercetin content, as the prevalent flavonol, was higher in the waste sample. The berry juice showed a greater ability for scavenging free radicals, whereas the waste better inhibited lipid peroxidation. The juice was a superior antispasmodic agent for spontaneous, KCl-, CaCl₂-, BaCl₂-, histamine-, and acetylcholine-induced ileal contractions. This first evaluation of the red currant variety Redpoll lyophilized juice and waste extract indicated the beneficial effects of juice as an antioxidant and spasmolytic agent. Therefore, this red currant juice sample could be designated for the prevention or treatment of gastrointestinal disorders. Full article

Background: Community pharmacists are frequently approached by patients seeking health advice for minor ailments, particularly for common childhood diseases like diarrhea. Globally, approximately two million children under five years of age die each year due to diarrhea, which remains a significant health concern, especially in developing countries. Objectives: The purpose of this study was to assess the skills of community pharmacists in addressing and prescribing for simple viral diarrhea in children. Methods: A hundred community pharmacies were visited by simulated clients following a standard scenario of inquiring about simple childhood diarrhea. Subsequently, they filled out a standardized form after each visit to assess the skills of the community pharmacists. Results: It was found that 98% of the pharmacists were males. Approximately 80% of them inquired about the child’s age, while only 29% asked about the presence of fever. Around 2–6% of them only asked about the stool nature, child’s feeding behavior, and family symptoms. Around 10% of them suggested a potential bacterial origin, and 24% recommended the use of antibiotics. Only 43% of the community pharmacists suggested the use of oral rehydration solution, while 15–56% recommended using antidiarrheals, anti-emetics, and spasmolytics. The mean knowledge score of the pharmacists was 9.06 out of 17. Conclusions: The results indicated a relatively low level of knowledge about managing simple viral childhood diarrhea, which may reflect a similar level of knowledge about dealing with minor ailments in general. Full article

Background: Irritable bowel syndrome (IBS) has a major negative influence on quality of life, causing cramps, stomach pain, bloating, constipation, etc. Antispasmodics have varying degrees of efficacy. Mebeverine, for example, works by controlling bowel movements and relaxing the muscles of the intestines but has side effects. Therefore, more efficient medication is required. Methods: In the current study, we investigated the synthesis of novel mebeverine analogs and determined ex vivo their spasmolytic and in vitro and ex vivo anti-inflammatory properties. The ability to influence both contractility and inflammation provides a dual-action approach, offering a comprehensive solution for the prevention and treatment of both conditions. Results: The results showed that all the compounds have better spasmolytic activity than mebeverine and good anti-inflammatory potential. Among the tested compounds, 3, 4a, and 4b have been pointed out as the most active in all the studies conducted. To understand their mechanism of activity, molecular docking simulation was investigated. The docking analysis explained the biological activities with their calculated Gibbs energies and possibilities for binding both centers of albumin. Moreover, the calculations showed that molecules can bind also the two muscarinic receptors and interleukin-β, hence these structures would exert a positive therapeutic effect owed to interaction with these specific receptors/cytokine. Conclusions: Three of the tested compounds have emerged as the most active and effective in all the studies conducted. Future in vivo and preclinical experiments will contribute to the establishment of these novel mebeverine derivatives as potential drug candidates against inflammatory diseases in the gastrointestinal tract. Full article