Spasmolytic effect of Lonicera japonica extracts on isolated uterus smooth muscle contractions

Introduction: Honeysuckle (Lonicera japonica) is an ornamental flowering plant with numerous traditional medicinal uses. It has been claimed to have anti-spasmodic activities, but only limited studies have been done to support this. The objective of this research was to investigate anti-spasmodic effect of L. japonica flower extract on uterus contractions. Methods: Hydroalcoholic extract was prepared using the maceration technique. In addition, chloroform and ethyl acetate fractions were prepared using a solvent in solvent fractionation technique. Essential oils were collected using the hydro-distillation technique. Rat isolated uterus was suspended in an organ bath and contracted with oxytocin, acetylcholine (ACh), KCl, or application of electrical field stimulation (EFS). The relaxant effects of the extract, its fractions, and nifedipine were examined on uterine contrition induced by the above-mentioned stimuli. Results: Nifedipine in a concentration-dependent manner inhibited uterine contraction induced by oxytocin, KCl, ACh, and EFS. L. japonica flower extract also exhibited an inhibitory effect on the isolated rat uterus. Comparison of the hydroalcoholic extract with its chloroform and ethyl acetate fractions showed that the chloroform fraction was the most potent and the ethyl acetate the weakest part of the plant with antispasmodic activity. The relaxant effect of essential oil had close similarities to that of chloroform extract. Conclusion: Lipophilic compounds isolated by the chloroform partition of crude hydroalcoholic extract of L. japonica flower exhibited the most antispasmodic activity. Ethyl acetate partition of the same extract exhibited the least activity. Therefore, it can be concluded that the spasmolytic constituents of L. japonica flower reside in chloroform partitioning. The nonpolar essential oils may also have a contribution.

Role of antispasmodics in the treatment of irritable bowel syndrome

Introduction. IBS is a functional bowel disorder that has a significant impact on patients and society, especially in terms of quality of life and medical costs.Pathogenesis. It is believed that the pathogenesis of IBS consists of several mechanisms: the syndrome of intersection of functional disorders (gut-brain), stress, visceral hypersensitivity and changes in motor skills.Visceral hypersensitivity. Changes in visceral sensitivity in IBS are characterized by central abnormalities in areas of the cerebral cortex. Motility impairment in IBS manifests itself as abnormal myoelectric activity in the colon, resulting in repetitive contractions of the small intestine and colon, which appear to cause pain.Intestinal microflora. FODMAPs are found in high amounts in some fruits, artificial sweeteners, legumes, and green vegetables and are poorly absorbed by all people. FODMAPs have enzymatic and osmotic effects that may contribute to the onset of symptoms in some patients.The principles of IBS therapy. Treatment for IBS should be based on the type and severity of symptoms. For the treatment of IBS, drugs of various pharmacological groups are used, depending on the prevailing symptoms. These include opioid receptor agonists, bile acid sequestrants, guanylate cyclase agonists, chlorine channel activators, as well as antibiotics, probiotics, antidepressants, 5-HT3 receptor antagonists, and antispasmodics.Myotropic antispasmodics. Drugs with antispasmodic activity are used to treat functional and organic diseases of the gastrointestinal tract as a basic therapy or «on demand». Mebeverine quickly and effectively relieves spasm, pain and the entire complex of intestinal symptoms, in addition, the drug reduces visceral hypersensitivity due to a local anesthetic effect. The drug has a high safety profile and has a number of advantages over drugs of the same pharmacological group.Conclusion. Myotropic antispasmodics have been shown to be highly effective in the treatment of IBS. Mebeverine occupies a special place among myotropic antispasmodics. Its combined action provides a pronounced antispasmodic activity along with a high safety profile.

Metabolomic Profiling of Mango (Mangifera indica Linn) Leaf Extract and Its Intestinal Protective Effect and Antioxidant Activity in Different Biological Models

Mangifera indica Linn popularly known as mango is used in folk medicine to treat gastrointestinal disorders. The aim of this study was to identify the metabolomic composition of lyophilized extract of mango leaf (MIE), to evaluate the antioxidant activity on several oxidative stress systems (DPPH, FRAP, TBARS, and ABTS), the spasmolytic and antispasmodic activity, and intestinal protective effect on oxidative stress induced by H2O2 in rat ileum. Twenty-nine metabolites were identified and characterized based on their ultra-high-performance liquid chromatography (UHPLC) high-resolution orbitrap mass spectrometry, these include: benzophenone derivatives, xanthones, phenolic acids, fatty acids, flavonoids and procyanidins. Extract demonstrated a high antioxidant activity in in-vitro assays. MIE relaxed (p < 0.001) intestinal segments of rat pre-contracted with acetylcholine (ACh) (10−5 M). Pre-incubation of intestinal segments with 100 µg/mL MIE significantly reduced (p < 0.001) the contraction to H2O2. Similar effects were observed with mangiferin and quercetin (10−5 M; p < 0.05) but not for gallic acid. Chronic treatment of rats with MIE (50 mg/kg) for 28 days significantly reduced (p < 0.001) the H2O2-induced contractions. MIE exhibited a strong antioxidant activity, spasmolytic and antispasmodic activity, which could contribute to its use as an alternative for the management of several intestinal diseases related to oxidative stress.

Study of Antispasmodic and Antidiarrheal Activities of Tagetes lucida (Mexican Tarragon) in Experimental Models and Its Mechanism of Action

Tagetes lucida has been used in traditional medicine as a remedy to alleviate several gastrointestinal disorders that provoke stomachaches, abdominal cramps, and diarrhea. However, there is not enough scientific evidence that supports these effects. Therefore, the purpose of this study was to evaluate antispasmodic and antidiarrheal activities of aqueous extract of T. lucida (AqExt-TL) as well as its mechanism of action in experimental models. Antispasmodic activity and the mechanism of action of AqExt-TL were assessed on segments of the guinea pig ileum precontracted with KCl, acetylcholine (ACh), or electrical field stimulation (EFS). Furthermore, the antispasmodic effect of two coumarins (umbelliferone and herniarin) previously identified in this species was evaluated. Antidiarrheal activity of AqExt-TL was determined using the charcoal meal test in mice. AqExt-TL showed antispasmodic activity in segments of the guinea pig ileum precontracted with KCl (83.7 ± 1.9%) and ACh (77.2 ± 5.3%) at the maximal concentration; however, practically, it did not alter the contractions induced by EFS (10.1 ± 2.2%). Antispasmodic activity of AqExt-TL was not significantly altered by hexamethonium (a ganglionic blocker) or L-NAME (an inhibitor of nitric oxide synthase). However, this extract decreased the maximal contractile response to calcium (82.7 ± 8.5%), serotonin (68.1 ± 8.5%), and histamine (63.9 ± 5.9%) in their concentration-response curves. Umbelliferone and herniarin also induced an antispasmodic effect on tissues precontracted with KCl. In addition, low doses of AqExt-TL reduced to 50% the distance traveled by charcoal meal in the gastrointestinal transit model in mice as loperamide, an antidiarrheal agent, did. These results provided evidence of the antispasmodic and antidiarrheal activity of T. lucida, which supports its use in the folk medicine in relieving symptoms in some gastrointestinal disorders. In the antispasmodic effect, the blockade of histaminergic and serotoninergic pathway as well as the calcium channels seems to be involved. Finally, umbelliferone and herniarin could be partially responsible for the antispasmodic activity induced by T. lucida.

Evaluation of Ficus retusa L. Leaves with special reference to Anti-diarrheal and Anti-spasmodic activity

: Diarrhea is considered as a major cause of mortality, especially in children and aged persons. Because of diarrhea, 17% of admitted children get die. In order to treat the diarrhea, natural drugs may be useful. The objective of the present investigation was to evaluate the traditional claim of Ficus retusa as an anti-diarrheal and anti-spasmodic agent using different pharmacological models. In very first step, phytochemical test was done to evaluate the presence of secondary metabolites. Quantitative test revealed that flavanoid is present in 24.48±0.40 mg/100g of extract, which is in highest among all the secondary metabolites present. The anti-diarrheal activity was evaluated by magnesium sulphate induced diarrhea and 5-hydroxy tryptamine (5HT) induced diarrhea. Further, the extract was subjected to gastrointestinal motility test using standard procedure. Finding of the present study suggested that significant response was exhibited by an ethanolic extract (400mg/kg bw.) of Ficus retusa (EEFR). The highest diarrhea protection was 78.12% and 70.32% due to EEFR 400mg/kg bw in magnesium sulphate induced diarrhea and 5HT induced diarrhea respectively. In case of gastrointestinal motality test, 81.42% inhibition was observed which was maximum due to EEFR 400mg/kg bw. Dose response relationship at (0.4ml to 0.4 ml) of Ach+ EEFR revealed the confirmation of EEFR as potent antispasmodic agent. The response towards bioactivity was dose dependent. It was concluded that 400mg/kg bw of ethanolic extract is most potent in antidiarrheal and antispasmodic activity.

Antimicrobial, Antiquorum-sensing and Ex-vivo Antispasmodic Activity of Adhatoda vasica

Aims: To investigate the antimicrobial, antiquorum-sensing and Ex-vivo antispasmodic activity of the stem extract, fractions and isolated compounds of Adhatoda vasica. Study Design: Preparation of the total extract, fractions of A. vasica and isolation of its phytoconstituents for investigation of antimicrobial, antiquorum-sensing and Ex-vivo antispasmodic activity. Place and Duration of Study: Faculty of Pharmacy, Mansoura University, Egypt and College of Pharmacy, Prince Sattam Bin Abdulaziz University, KSA, between November 2014 and May 2019. Methodology: Different phytoconstituents in obtained liquid-liquid fractionations were isolated by repeated column chromatography. The preliminary antimicrobial activity was measured via agar disc-diffusion method. The minimum inhibitory concentration (MIC) was further determined using broth microdilution method in 96-well plates. Antiquorum-sensing activity was tested against Chromobacterium violaceum in LB agar medium. While, antispasmodic activity was performed using Ach-induced contraction on rat ileum. Results: Seven compounds have been isolated from the stems extract of Adhatoda vasica viz., β-sitosterol, daucosterol palmitate, monopalmitin, vanillin, vanillic acid, vasicinolone and vasicinone. The petroleum ether fraction, daucosterol palmitate, monopalmitin, vanillin and vanillic acid showed strong antibacterial activity towards E. coli and S. aureus. Whereas daucosterol palmitate and vanillic acid showed pronounced antifungal activity against C. albicans. Antiquorum-sensing assay showed that β-sitosterol, vanillin and vanillic acid were the most active compounds. While, petroleum ether and methylene chloride fractions, vasicinolone and daucosterol palmitate showed moderate antiquorum-sensing activity. For antispasmodic activity, petroleum ether fraction showed a remarkable inhibition of Ach-induced contraction at 200 and 250 μg/mL (89.5 and 95.2%, respectively). Also, methylene chloride fraction showed remarkable inhibition (97.6%) at 150 μg/mL. Vasicinone and vasicinolone showed significant inhibition at 150 μg/mL (89.9% and 84.8%, respectively). Conclusion: The isolated compounds and extracts from the stem of the studied plant showed remarkable activities. This work provides further evidences for the traditional medicinal uses of A. vasica in treatment of various ailments.

Natural Antispasmodics: Source, Stereochemical Configuration, and Biological Activity

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.