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Статті в журналах з теми "Antispasmodic activity"

Автор: Grafiati

Опубліковано: 6 жовтня 2023

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1

Martínez-Pérez, Edith Fabiola, Zaida N. Juárez, Luis R. Hernández, and Horacio Bach. "Natural Antispasmodics: Source, Stereochemical Configuration, and Biological Activity." BioMed Research International 2018 (October 8, 2018): 1–32. http://dx.doi.org/10.1155/2018/3819714.

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Анотація:

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.

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2

Ventura-Martinez, Rosa, Guadalupe Esther Angeles-Lopez, Maria Eva Gonzalez-Trujano, Omar F. Carrasco, and Myrna Deciga-Campos. "Study of Antispasmodic and Antidiarrheal Activities of Tagetes lucida (Mexican Tarragon) in Experimental Models and Its Mechanism of Action." Evidence-Based Complementary and Alternative Medicine 2020 (October 28, 2020): 1–10. http://dx.doi.org/10.1155/2020/7140642.

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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.

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3

Cechinel Filho, Valdir, Obdúlio Gomes Miguel, Ricardo José Nunes, João Batista Calixto, and Rosendo Augusto Yunes. "Antispasmodic Activity of Xanthoxyline Derivatives: Structure–Activity Relationships." Journal of Pharmaceutical Sciences 84, no. 4 (April 1995): 473–75. http://dx.doi.org/10.1002/jps.2600840416.

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4

Drozdov, V. N., K. I. Arefev, S. Yu Serebrova, I. A. Komissarenko, E. V. Shikh, and A. K. Starodubtsev. "Role of antispasmodics in the treatment of irritable bowel syndrome." Meditsinskiy sovet = Medical Council, no. 5 (May 13, 2021): 155–64. http://dx.doi.org/10.21518/2079-701x-2021-5-155-164.

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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.

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5

Romussi. "Antispasmodic Activity of Semi-Synthetic Secoisopimarane Deriva." Scientia Pharmaceutica 77, no. 1 (2009): 215. http://dx.doi.org/10.3797/scipharm.oephg.21.po-16.

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6

Khalid, S., E. Kalaflla, and O. Mohamed. "The Flavonoids ofSolanostemma argeland their Antispasmodic Activity." Planta Medica 58, S 1 (December 1992): 651. http://dx.doi.org/10.1055/s-2006-961661.

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7

Avramenko, T. V., and A. P. Moschich. "Efficacy and safety assessment of viburcol drug for preparation of uterine cervix for childbirth and prevention of labor anomalies." HEALTH OF WOMAN, no. 7(113) (September 30, 2016): 73–78. http://dx.doi.org/10.15574/hw.2016.113.73.

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The objective is to compare the effectiveness of complex bio-regulatory medication (CBRM) Viburcol, produced by «Biologishe Haylmittel Heel GmbH», Germany, with the reference product No-X-sha, produced by «Lekhim-Kharkov», which are used as antispasmodics, for preparation of uterine cervix for childbirth and prevention of labor anomalies. Patients and methods. 92 pregnant women aged 18 to 45 years, who were randomized into 2 groups: the main group (n=46) and the control (n=46) one, were involved in the study. Viburcol was used for the treatment of pathological preliminary period and prevention of development of labor anomalies. It was prescribed at the end of pregnancy and in the 1st stage of labor, in the morning and in the evening. Two Viburcol suppository every 3-4 hours were given at the onset of labor. Antispasmodic No-X-sha was used in the control group. It was studied the functional state of the sympathetic-adrenal system with fluorometric method, the concentration of noradrenaline (NA) and adrenaline (A) in the urine, to assess the neurohormonal regulation of labor. The plasma levels of b-estradiol and progesterone were determined to identify the risk of discoordination of labor activity and the state of uterine contractile function. Also, the parameters of uterine contractile activity were analyzed according to cardiotocography. Results. Usage of complex bio-regulatory medication Viburcol promotes adequate cervical ripening and incidence of discoordination of labor activity decreased by 1.5 times. CDRM Viburcol administration in childbirth facilitated the elimination of pathological levels of catecholamines, which led to the development of discoordination of labor activity. Conclusion. The results show the effectiveness of CDRM Viburcol (rectal suppositories) for the prevention of discoordination of labor activity. The medicine meets all modern requirements for antispasmodics and analgesics used during labor: it has analgesic, antispasmodic, anxiolytic effect, eliminates side reflex reactions, reduces the severity of birth stress, it has no adverse effect on the contractile activity of uterus and the fetus condition. Key words: complex bio-regulatory medications, bio-regulatory approach, labor amoralities, preparation of uterine cervix, Viburcol.

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8

Zoofishan, Zoofishan, Norbert Kúsz, Attila Csorba, Gábor Tóth, Judit Hajagos-Tóth, Anna Kothencz, Róbert Gáspár, and Attila Hunyadi. "Antispasmodic Activity of Prenylated Phenolic Compounds from the Root Bark of Morus nigra." Molecules 24, no. 13 (July 8, 2019): 2497. http://dx.doi.org/10.3390/molecules24132497.

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Black mulberry is a widely acknowledged ancient traditional medicine. Its extract and constituents have been reported to exert various bioactivities including antimicrobial, hypotensive, analgesic etc. effects. While black mulberry preparations are also used as antispasmodic agents in folk medicine, no related studies are available on its isolated constituents. Through an extensive chromatographic purification, seven phenolic compounds were isolated from the methanol extract of Morus nigra root bark, including morusin (1), kuwanon U (2), kuwanon E (3), moracin P (4), moracin O (5), albanol A (6), and albanol B (7). A complete NMR signal assignment of moracin P and O was achieved, and related literature errors confusing the identity of moracin derivatives are hereby clarified. Compounds 2, 5 and 7 were identified as strong antispasmodic agents on isolated rat ileum and tracheal smooth muscles, while compound 3, a methoxy derivative of 2, was inactive. Moracin O (5) inhibited the ileal and tracheal smooth muscle contractions with Emax values of 85% and 302 mg, respectively. Those actions were superior as compared with papaverine. Our findings demonstrate that prenylated arylbenzofurans, geranylated flavonoids and Diels-Alder adducts from Morus nigra are valuable antispasmodic agents. Compounds 2, 5 and 7 are suggested as marker compounds for quality control of antispasmodic mulberry preparations. Moracin O (5) is a new lead compound for related drug development initiatives.

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9

Lakshmanan, Baskar, Papiya Mazumder, Dinakar Sasmal, and Swastika Ganguly. "Synthesis, antispasmodic and antidiarrheal activities of some 1-substituted imidazole derivatives." Acta Pharmaceutica 61, no. 2 (June 1, 2011): 227–36. http://dx.doi.org/10.2478/v10007-011-0014-6.

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Synthesis, antispasmodic and antidiarrheal activities of some 1-substituted imidazole derivatives 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.

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10

Martin, M., M. Diaz, M. Montero, Pilar Prieto, Luis Roman, and Diego Cortes. "Antispasmodic Activity of Benzylisoquinoline Alkaloids Analogous to Papaverine." Planta Medica 59, no. 01 (February 1993): 63–67. http://dx.doi.org/10.1055/s-2006-959606.

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11

de Moura, Neusa F., Ademir F. Morel, Emilia C. Dessoy, Nilo Zanatta, Marilise M. Bürger, Neusa Ahlert, Gerusa P. Porto, and Bernardo Baldisserotto. "Alkaloids, Amides and Antispasmodic Activity of Zanthoxylum hyemale." Planta Medica 68, no. 6 (June 2002): 534–38. http://dx.doi.org/10.1055/s-2002-32550.

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12

Pohocha, Nazneen, and Nirmala D. Grampurohit. "Antispasmodic activity of the fruits ofHelicteres isora Linn." Phytotherapy Research 15, no. 1 (2001): 49–52. http://dx.doi.org/10.1002/1099-1573(200102)15:1<49::aid-ptr729>3.0.co;2-e.

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13

Barile, Elisa, Raffaele Capasso, Angelo A. Izzo, Virginia Lanzotti, S. Ebrahim Sajjadi, and Behzad Zolfaghari. "Structure-Activity Relationships for Saponins fromAllium hirtifoliumandAllium elburzenseand their Antispasmodic Activity." Planta Medica 71, no. 11 (October 2005): 1010–18. http://dx.doi.org/10.1055/s-2005-873134.

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14

Duangjai, Acharaporn, Vatcharin Rukachaisirikul, Yaowapa Sukpondma, Chutima Srimaroeng, and Chatchai Muanprasat. "Antispasmodic Effect of Asperidine B, a Pyrrolidine Derivative, through Inhibition of L-Type Ca2+ Channel in Rat Ileal Smooth Muscle." Molecules 26, no. 18 (September 9, 2021): 5492. http://dx.doi.org/10.3390/molecules26185492.

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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.

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15

Romussi, Giovanni, Giovanni Ciarallo, Angela Bisio, Nadia Fontana, Francesco De Simone, Nunziatina De Tommasi, Nicola Mascolo, and Luisa Pinto. "A New Diterpenoid with Antispasmodic Activity from Salvia cinnabarina." Planta Medica 67, no. 2 (2001): 153–55. http://dx.doi.org/10.1055/s-2001-11511.

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16

Venkataranganna, M. V., S. D. Anturlikar, S. Gopumadhavan, N. S. Prakash, Mohammed Rafiq, Girish S. Murthy, and S. K. Mitra. "Antispasmodic Activity of SJ-200 (Himcospaz): An Herbal Preparation." Pharmaceutical Biology 40, no. 6 (January 2002): 416–21. http://dx.doi.org/10.1076/phbi.40.6.416.8435.

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17

Sheridan, Helen, Neil Frankish, and Ronan Farrell. "Synthesis and antispasmodic activity of analogues of natural pterosins." European Journal of Medicinal Chemistry 34, no. 11 (November 1999): 953–66. http://dx.doi.org/10.1016/s0223-5234(99)00113-0.

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18

Görnemann, T., R. Nayal, H. H. Pertz, and M. F. Melzig. "Antispasmodic activity of essential oil from Lippia dulcis Trev." Journal of Ethnopharmacology 117, no. 1 (April 2008): 166–69. http://dx.doi.org/10.1016/j.jep.2008.01.009.

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19

Kaur, Jaskiran, Narendra Nath Ghosh, and Ramesh Chandra. "Synthesis and Antispasmodic Activity Evaluation of Bis-(Papaverine) Analogues." CHEMICAL & PHARMACEUTICAL BULLETIN 52, no. 3 (2004): 316–21. http://dx.doi.org/10.1248/cpb.52.316.

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20

KRASNOV, V. A., V. K. GORSHKOVA, A. A. BAKIBAEV, and A. S. SARATIKOV. "ChemInform Abstract: Synthesis and Antispasmodic Activity of Fluorosubstituted Benzhydrylamides." ChemInform 28, no. 46 (August 3, 2010): no. http://dx.doi.org/10.1002/chin.199746111.

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21

Silva, Fabiana L., Joelmir L. V. da Silva, Juciléia M. Silva, Luiza S. A. Marcolin, Viviane L. A. Nouailhetas, Massayoshi Yoshida, Pedro H. Vendramini, Marcos N. Eberlin, José M. Barbosa-Filho, and Paulo R. H. Moreno. "Antispasmodic activity from Serjania caracasana fractions and their safety." Revista Brasileira de Farmacognosia 27, no. 3 (May 2017): 346–52. http://dx.doi.org/10.1016/j.bjp.2016.12.002.

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22

Tamilselvi, S., R. Sathyaseela, S. Iyswarya, U. Sowmiya, and B. Sowmiya. "Review on antispasmodic activity of crocus sativus and abies." International Journal of Pharmaceutical and Clinical Research 4, no. 1 (January 1, 2022): 26–31. http://dx.doi.org/10.33545/26647591.2022.v4.i1a.31.

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23

Strege, Peter R., Lei Sha, Arthur Beyder, Cheryl E. Bernard, Edward Perez-Reyes, Stefano Evangelista, Simon J. Gibbons, Joseph H. Szurszewski, and Gianrico Farrugia. "T-type Ca2+channel modulation by otilonium bromide." American Journal of Physiology-Gastrointestinal and Liver Physiology 298, no. 5 (May 2010): G706—G713. http://dx.doi.org/10.1152/ajpgi.00437.2009.

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Анотація:

Antispasmodics are used clinically to treat a variety of gastrointestinal disorders by inhibition of smooth muscle contraction. The main pathway for smooth muscle Ca2+entry is through L-type channels; however, there is increasing evidence that T-type Ca2+channels also play a role in regulating contractility. Otilonium bromide, an antispasmodic, has previously been shown to inhibit L-type Ca2+channels and colonic contractile activity. The objective of this study was to determine whether otilonium bromide also inhibits T-type Ca2+channels. Whole cell currents were recorded by patch-clamp technique from HEK293 cells transfected with cDNAs encoding the T-type Ca2+channels, CaV3.1 (α1G), CaV3.2 (α1H), or CaV3.3 (α1I) alpha subunits. Extracellular solution was exchanged with otilonium bromide (10−8to 10−5M). Otilonium bromide reversibly blocked all T-type Ca2+channels with a significantly greater affinity for CaV3.3 than CaV3.1 or CaV3.2. Additionally, the drug slowed inactivation in CaV3.1 and CaV3.3. Inhibition of T-type Ca2+channels may contribute to inhibition of contractility by otilonium bromide. This may represent a new mechanism of action for antispasmodics and may contribute to the observed increased clinical effectiveness of antispasmodics compared with selective L-type Ca2+channel blockers.

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24

Ali Haimoud, Safia, Rachida Allem, Meriem Medjekane, Khadidja Benyahla Djeffaland, Nour El Houda Lembarki, Khawla Boutara, and Fatiha Belhache. "Antispasmodic and nephroprotective potentials of native Algerian propolis and bee pollen: An experimental study in mice." International Food Research Journal 30, no. 1 (February 24, 2023): 109–18. http://dx.doi.org/10.47836/ifrj.30.1.08.

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The present work examined the in vivo antispasmodic and nephroprotective potentials of methanolic extracts obtained from Algerian native propolis and bee pollen. The in vivo antispasmodic activity was assessed by the intraperitoneal injection of acetic acid (1%) which induced long-lasting visceral pain in mice. The renal damage was modelled by intraperitoneal injection of a cisplatin (CP; 10 mg/kg) followed by histopathological changes in kidneys. In addition, the beehive by-products were screened for their bioactive content and in vitro antioxidant activities. The propolis and bee pollen are rich sources of bioactive compounds. The propolis showed the highest antioxidant potencies as evaluated by β-carotene bleaching system (87.16 ± 3.69%), DPPH (176.05 ± 0.20 µg/mL), and FRAP (0.61 ± 0.002 μmol Fe(II)/g) assays. The antispasmodic test revealed that propolis extract (250 mg/kg) significantly inhibited the number of spasms (61.04 ± 3.92%) induced by acetic acid. Based on histopathology examinations, bee pollen extract at 250 mg/kg significantly reduced nephrotoxic effects induced by CP injection. These results provided a good scientific basis for future research on antispasmodic and nephroprotective effects and/or mechanisms of propolis and bee pollen, which confer them a real application in drug discovery.

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25

Khan, Farman Ullah, Arif-Ullah Khan, Javid Hussain, Ihsan Ullah Khan, Nawshad Muhammad, Aslam Khan, Sultan Mehmood, Abdullah Mohamed Asiri, Sher Bahadar Khan, and Anwarul Hassan Gilani. "Spasmolytic and Ca++ Channel Blocking Potential of Nepetolide: Isolated from Nepeta Suavis." Natural Product Communications 11, no. 5 (May 2016): 1934578X1601100. http://dx.doi.org/10.1177/1934578x1601100507.

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Анотація:

Nepeta suavis is used in traditional medicine for treatment of abdominal spasm (colic). The tricyclic clerodane type diterpene, nepetolide, isolated for the first time from Nepeta suavis. was evaluated for Ca++ antagonist and antispasmodic activities. When studied in isolated rabbit jejunum, nepetolide caused concentration-dependent (0.03–100 μM) relaxation of spontaneous and high K+ (80 mM)-induced contractions, like that caused by verapamil, indicating that nepetolide exhibits spasmolytic activity, possibly mediated through Ca++ channel blocking action, which provides scientific explanation for the medicinal application of Nepeta suavis as an antispasmodic agent.

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26

Xu, Yanli, Chenxi Li, Ting Chen, Xiaochun Li, Xiaoyu Wu, Qili Zhang, and Lei Zhao. "Quantitative Analysis of the Multicomponent and Spectrum–Effect Correlation of the Antispasmodic Activity of Shaoyao-Gancao Decoction." Journal of Analytical Methods in Chemistry 2022 (December 2, 2022): 1–13. http://dx.doi.org/10.1155/2022/2279404.

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Shaoyao-Gancao Decoction (SGD) is a well-known classic traditional Chinese medicine (TCM) with antispasmodic, anti-inflammatory, and analgesic effects. This preparation has been widely used to treat spasticity diseases in the clinic. To date, the material basis of SGD remains unclear, and the spectrum-effect correlation of its antispasmodic activity has not been reported yet. In this study, high-performance liquid chromatography (HPLC) was used to establish the fingerprint and determine the multiple components of SGD. The common peaks of fingerprints were evaluated by the similarity with the chromatographic fingerprints of the TCM. Meanwhile, the multiple components were quantified and analysed using the heatmap and box size analysis. Furthermore, data on the antispasmodic effect were extracted through in vitro smooth muscle contraction assay. Grey relational analysis combined with partial least square regression was used to study the spectrum–effect correlation of SGD. Finally, the potential antispasmolytic components were validated using an isolated tissue experiment. The HPLC fingerprint was established, and 20 common peaks were identified. The similarities of 15 batches of SGD were all above 0.965. The HPLC method for simultaneous determination of the multiple components was accurate and reliable. The contents of albiflorin, paeoniflorin, liquiritin, and glycyrrhizic acid were higher than the other components in SGD. The heatmap and box size also showed that X3 (albiflorin), X4 (paeoniflorin), X5 (liquiritin), X11 (liquirtigenin), and X16 (glycyrrhizic acid) could be used as quality indicators in the further establishment of quality standards. The spectrum–effect correlation results indicated that X4, X11, and X16 were highly correlated with antispasmolytic activity. Verification tests showed that paeoniflorin (11.7–29.25 μg/mL) and liquirtigenin (17.19–28.65 μg/mL) could significantly reduce the maximum contractile ( P < 0.01 ). These compounds exerted concentration-dependent spasmolytic effects with the inhibitory response for acetylcholine (Ach)-evoked contraction. Thus, SGD had a significant antispasmodic effect, which resulted from the synergistic activity of its multiple components. These findings can be used for the pharmacodynamics study of SGD and are of great significance for the determination of quality markers and quality control.

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Ali, N., S. W. A. Shah, and I. Shah. "Preliminary Phytochemical Screening and Antispasmodic Activity of Artemisia macrocephala Jacquem." Journal of Young Pharmacists 3, no. 2 (April 2011): 125–28. http://dx.doi.org/10.4103/0975-1483.80300.

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Saini, Navdeep, and GajendraKamal Singh. "Pharmacological evaluation of a polyherbal formulation for its antispasmodic activity." International Journal of Green Pharmacy 9, no. 2 (2015): 104. http://dx.doi.org/10.4103/0973-8258.155056.

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Aoki, Kazuko, Alma Rosa Cortés, María del Carmen Ramírez, Martín Gómez-Hernández, and Francisco J. López-Muñoz. "Pharmacological study of antispasmodic activity of Mirabilis jalapa Linn flowers." Journal of Ethnopharmacology 116, no. 1 (February 2008): 96–101. http://dx.doi.org/10.1016/j.jep.2007.11.004.

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Astudillo, Adela, Enrique Hong, Robert Bye, and Andrés Navarrete. "Antispasmodic activity of extracts and compounds of Acalypha phleoides Cav." Phytotherapy Research 18, no. 2 (February 2004): 102–6. http://dx.doi.org/10.1002/ptr.1414.

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Kandsi, Fahd, Raffaele Conte, Mohamed Marghich, Fatima Zahra Lafdil, Mohamed F. Alajmi, Mohamed Bouhrim, Hamza Mechchate, Christophe Hano, Mohammed Aziz, and Nadia Gseyra. "Phytochemical Analysis, Antispasmodic, Myorelaxant, and Antioxidant Effect of Dysphania ambrosioides (L.) Mosyakin and Clemants Flower Hydroethanolic Extracts and Its Chloroform and Ethyl Acetate Fractions." Molecules 26, no. 23 (December 1, 2021): 7300. http://dx.doi.org/10.3390/molecules26237300.

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Анотація:

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.

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Rauf, Abdur, Muhammad Akram, Prabhakar Semwal, Adil A. H. Mujawah, Naveed Muhammad, Zerfishan Riaz, Naveed Munir, et al. "Antispasmodic Potential of Medicinal Plants: A Comprehensive Review." Oxidative Medicine and Cellular Longevity 2021 (November 11, 2021): 1–12. http://dx.doi.org/10.1155/2021/4889719.

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Анотація:

Numerous medicinal plants have been utilized for the treatment of different types of diseases and disorders including gastrointestinal (GI) diseases. GI diseases are the most common complaints that normally affects the largest proportion of children and adolescents with overlapping clinical manifestation in diagnosis and medical needs. Drugs with antispasmodic effects are normally applied for the symptomatic treatment of contraction and cramping of smooth muscles in gastrointestinal diseases as well as in other critical clinical situations. In alternative system of medicines, the antispasmodic herbs played a significant role in the cure of GI diseases. These medicinal plants and their herbal products are used from generation to generation because of multiple nutritional and therapeutic benefits. The multiple uses might be attributed to the presence on biologically active chemical constitutes. The main aim of this review is to focus on the medicinal potential of plants possessing antispasmodic activities with their proposed mechanism of action. Several databases such as Google Scholar, Cochrane database, Scopus, and PubMed were used to search the relevant literature regarding “plants with antispasmodic activities.” This present study highlights the updated and quantified information on several medicinal plants with antispasmodic activity like Zanthoxylum armatum, Matricaria chamomilla, Foeniculum vulgare, Pycnocycla spinosa, Atropa belladonna, Lavandula angustifolia, Mentha pulegium, Glycyrrhiza ularensis, Anethum graveolens, and Origanum majorana. Moreover, recent studies on other medicinal plant species also have been included in this review article. Additionally, the study also revealed that the active compounds of all these plants possess significant spasmolytic effect which is safest, efficacious, and cost effective as compared to the available synthetic drugs.

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Amrani, Ouafa, Mohamed Marghich, Hanane Makrane, Chakib Alem, and Mohammed Aziz. "Antispasmodic activity of Warionia saharae Benthem ex Benth. & Coss. on the rabbit and rat jejunums." Journal of Pharmacy & Pharmacognosy Research 9, no. 5 (September 1, 2021): 677–84. http://dx.doi.org/10.56499/jppres21.1049_9.5.677.

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Context: Warionia saharae Benthem ex Benth. & Coss has been widely used for gastrointestinal problems in Morocco and Algeria. Aims: To explore the possible mechanism for its use to such ailments in order to rationalize some of these folkloric uses. We investigated the aqueous extract of this plant (AqWs) for antispasmodic activity on isolated rat and rabbit jejunums. Methods: To investigate the contractile activity of isolated jejunum preparations of rat and rabbit we had used in vitro techniques. Jejunums were suspended in tissue baths filled with KHB culture medium (37°C) and connected to force transducers. AqWs (0.1–3 mg/mL) was used with or without carbachol (10-6 M), KCl (25 mM), yohimbine (10-5 M), prazosin (10-5 M), propranolol (10-5 M), hexamethonium (10-4 M), atropine (10-6 M), methylene blue (10-5 M), L-NAME (10-4 M) and nifedipine (10-6 M). Results: AqWs at 0.1–3 mg/mL produced a relaxation on basal rabbit contractions with an IC50 = 1.55 ± 0.06 mg/mL. This effect was reversible and was not affected by pretreatment with the inhibitors of α and β adrenergic receptors yohimbine, prazosin and propranolol. The extract had an antispasmodic activity with an IC50 = 1.25 ± 0.02 mg/mL on rat jejunum precontracted with KCl rich medium (25 mM). This result suggests that the extract had a Ca2+ antagonist effect. This was fortified when pretreatment of the intestine with the extract induced a rightward shift in the Ca2+ concentration-response curves. AqWs exhibited also antispasmodic effect on carbachol (10-6 M)-induced contractions of rat jejunums with an IC50 = 1.53 ± 0.04 mg/mL. The extract at 3 mg/mL on rat jejunums pre-incubated with hexamethonium (10-4 M), atropine (10-6 M), and methylene blue (10-5 M), then contracted by KCl, decreased the maximum contraction but not totally like KCL alone without these inhibitors. For the jejunum pre-incubated with L-NAME (10-4 M), the spasmolytic effect of AqWs was comparable with KCL. Conclusions: These results suggest that the myorelaxant and antispasmodic effects are mediated possibly via Ca2+ antagonist, anticholinergic, and guanylate cyclase mechanisms but not by adrenergic and nitric oxide pathway.

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Paula, A. C. B., L. S. S. Hayashi, and J. C. Freitas. "Anti-inflammatory and antispasmodic activity of Ipomoea imperati (Vahl) Griseb (Convolvulaceae)." Brazilian Journal of Medical and Biological Research 36, no. 1 (January 2003): 105–12. http://dx.doi.org/10.1590/s0100-879x2003000100014.

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35

Rigano, Daniela, Gabriella Aviello, Maurizio Bruno, Carmen Formisano, Sergio Rosselli, Raffaele Capasso, Felice Senatore, Angelo A. Izzo, and Francesca Borrelli. "Antispasmodic Effects and Structure−Activity Relationships of Labdane Diterpenoids fromMarrubium globosumssp.libanoticum." Journal of Natural Products 72, no. 8 (August 28, 2009): 1477–81. http://dx.doi.org/10.1021/np9002756.

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36

Sheridan, H., S. Lemon, N. Frankish, P. McArdle, T. Higgins, JP James, and P. Bhandari. "Synthesis and antispasmodic activity of nature identical substituted indanes and analogues." European Journal of Medicinal Chemistry 25, no. 7 (September 1990): 603–8. http://dx.doi.org/10.1016/0223-5234(90)90185-6.

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37

Nagai, Hidemasa, Ju-Xiu He, Tadato Tani, and Teruaki Akao. "Antispasmodic activity of licochalcone A, a species-specific ingredient ofGlycyrrhiza inflataroots." Journal of Pharmacy and Pharmacology 59, no. 10 (October 2007): 1421–26. http://dx.doi.org/10.1211/jpp.59.10.0013.

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38

Pongprayoon, U., P. Baeckström, U. Jacobsson, M. Lindström та L. Bohlin. "Antispasmodic Activity of β-Damascenone andE-Phytol Isolated fromIpomoea pes-caprae". Planta Medica 58, № 01 (лютий 1992): 19–21. http://dx.doi.org/10.1055/s-2006-961381.

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39

Sheridan, Helen, Neil Frankish, and Ronan Farrell. "ChemInform Abstract: Synthesis and Antispasmodic Activity of Analogues of Natural Pterosins." ChemInform 31, no. 9 (June 10, 2010): no. http://dx.doi.org/10.1002/chin.200009179.

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40

Khalaidzheva, K. N., V. N. Drozdov, E. V. Shikh, and S. Yu Serebrova. "The place of antispasmodic drugs in modern therapy of irritable bowel syndrome." Meditsinskiy sovet = Medical Council, no. 8 (May 25, 2023): 189–95. http://dx.doi.org/10.21518/ms2023-127.

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Анотація:

Irritable bowel syndrome (IBS) is a common functional disease of the gastrointestinal tract, affecting a large number of adults worldwide, and leads to a significant decrease in the quality of life. IBS places a heavy burden on patients, most of whom are able-bodied population, as well as doctors and the healthcare system. The pathogenesis of this disease is multifactorial and includes the brain-intestine axis, disorders of the immune function of the mucous membrane, visceral hypersensitivity, changes in the motility of the gastrointestinal tract, changes in the microbial composition of the intestine. Based on the fact that changes in intestinal motility and visceral hypersensitivity are among the key factors in the pathogenesis of the disease, he use of antispasmodic drugs as part of complex therapy is justified. Mebeverin is a myotropic antispasmodic drug recommended for use in patients with IBS according to Rome IV Criteria, as well as clinical recommendations of the Russian Gastroenterological Association and the Association of Coloproctologists of Russia. According to available data, mebeverin has proven to be an effective and safe antispasmodic used to treat patients with IBS. The article presents a clinical case demonstrating the experience of effective use of the drug Mebespalin®. A patient with a diagnosis of IBS with a predominance of constipation is recommended to take an antispasmodic, as well as lifestyle modification – the addition of fiber-rich foods, sufficient drinking regime and increased physical activity. A week after the start of treatment, the patient noted an improvement in her condition – abdominal pain did not bother, the stool normalized.

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41

Okoye, TC, PA Akah, CO Okoli, AC Ezike, and FN Mbaoji. "Antimicrobial and antispasmodic activity of leaf extract and fractions of Stachytarpheta cayennensis." Asian Pacific Journal of Tropical Medicine 3, no. 3 (March 2010): 189–92. http://dx.doi.org/10.1016/s1995-7645(10)60006-5.

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Bakibaev, A. A., L. G. Tignibidina, V. D. Filimonov, V. K. Gorshkova, A. S. Saratikov, A. V. Pustovoitov, N. S. Dobychina, and A. G. Pechenkin. "Synthesis of arylmethylureas and the influence of structure on their antispasmodic activity." Pharmaceutical Chemistry Journal 25, no. 5 (May 1991): 296–301. http://dx.doi.org/10.1007/bf00772117.

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43

Çetinus, Şenay Akkuş, İsmihan Göze, Bülent Saraç, and Nilüfer Vural. "Scavenging effect and antispasmodic activity of the essential oil of Cyclotrichium niveum." Fitoterapia 78, no. 2 (February 2007): 129–33. http://dx.doi.org/10.1016/j.fitote.2006.10.006.

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44

dos Santos, Rodrigo, Carlos Alberto Kuhnen, and Rosendo Augusto Yunes. "Molecular Structure and QSAR Study on Antispasmodic Activity of some Xanthoxyline Derivatives." Archiv der Pharmazie 339, no. 5 (May 2006): 227–37. http://dx.doi.org/10.1002/ardp.200500192.

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Spadaro, Federica, Rosaria Costa, Clara Circosta, and Francesco Occhiuto. "Volatile Composition and Biological Activity of Key Lime Citrus aurantifolia Essential Oil." Natural Product Communications 7, no. 11 (November 2012): 1934578X1200701. http://dx.doi.org/10.1177/1934578x1200701128.

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Анотація:

The essential oil of Citrus aurantifolia (Christm) Swingle fruits (limes) was studied for its potential spasmolytic effects in relation to its chemical composition. The essential oil, extracted by hydrodistillation (HD), was analyzed by GC-FID and GC-MS. The antispasmodic activity was evaluated on isolated rabbit jejunum, aorta and uterus. The results indicated that the essential oil of C aurantifolia possesses important spasmolytic properties, which are likely to be due to its major constituents, limonene (58.4%), β-pinene (15.4%), γ-terpinene (8.5%), and citral (4.4%).

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46

Ybañez-Julca, Roberto O., Daniel Asunción-Alvarez, Ivan M. Quispe-Díaz, Javier Palacios, Jorge Bórquez, Mario J. Simirgiotis, Shagufta Perveen, Chukwuemeka R. Nwokocha, Fredi Cifuentes, and Adrián Paredes. "Metabolomic Profiling of Mango (Mangifera indica Linn) Leaf Extract and Its Intestinal Protective Effect and Antioxidant Activity in Different Biological Models." Molecules 25, no. 21 (November 5, 2020): 5149. http://dx.doi.org/10.3390/molecules25215149.

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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.

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47

Palla, Amber Hanif, Anwar-ul-Hassan Gilani, Samra Bashir, and Najeeb Ur Rehman. "Multiple Mechanisms of Flaxseed: Effectiveness in Inflammatory Bowel Disease." Evidence-Based Complementary and Alternative Medicine 2020 (July 13, 2020): 1–16. http://dx.doi.org/10.1155/2020/7974835.

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Анотація:

Ethnopharmacological Relevance. Natural products, like Flaxseed (Linum usitatissimum), have traditionally been used in inflammatory bowel disease (IBD). It is known to contain multiple constituents which may account for its effectiveness, as IBD is a multifaceted disease. Aim of the Study. In the current study, we aimed to assess pharmacological basis for the medicinal use of Flaxseed in IBD. Materials and Methods. Aqueous-methanolic crude extracts of Flaxseed (Fs.Cr) and Flaxseed oil were tested against 6% acetic acid- (AA-) induced colitis in BALB/c mice. Microscopic damage parameters of the hematoxylin and eosin-stained and periodic acid-Schiff-alcian blue-stained sections of the colon were scored to be assessed. Possible antispasmodic mechanism was studied on isolated rabbit jejunum, while antibacterial activity was assessed in vitro for microbes implicated in IBD. Results. In AA-induced colitis, Flaxseed oil was found to be more effective in reducing mortality and colonic ulcers than Fs.Cr at 500 mg/kg dose. Fs.Cr was more efficacious in increasing mucin content as compared to oil, exhibiting slightly greater anti-inflammatory effect (50% vs 35%) and reducing depth of lesion (55% vs 42.31%, respectively). Antispasmodic activity of Fs.Cr (0.03 and 0.1 mg/ml) was mediated by phosphodiesterase inhibitors (PDEI, possibly PDE-4 subtype) with a resultant increase in cAMP levels. Flaxseed oil PDEI activity was mild (1 and 3 mg/ml). Fs.Cr (0.1 and 0.3 mg/ml) was potent in exhibiting anticholinergic activity, similar to dicyclomine, whereas Flaxseed oil showed anticholinergic effect at 1 and 3 mg/ml. Flaxseed oil (9 and 14 µg/ml) was bactericidal against enteropathogenic E.coli (EPEC), enterotoxigenic E.coli (ETEC), and enteroaggregative E.coli (EAEC), whereas Fs.Cr exhibited bactericidal effect against EPEC at 100 µg/ml. Conclusions. Results of this study, taken together with previous studies, suggest that Flaxseed possesses anti-inflammatory, antibacterial, and antispasmodic action through multiple pathways and thus offers promising potential to be developed for IBD.

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Naboka, Olga, Alla Kotvitska, Alina Volkova, Oksana Tkachenko, Yuliya Voronina-Tuzovskykh, Olga Filiptsova, and Inna Pasynchuk. "Study of analgesic and myotropic spasmolytic activity of alkylcarb." ScienceRise: Biological Science, no. 2(35) (June 30, 2023): 4–11. http://dx.doi.org/10.15587/2519-8025.2023.285648.

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The work is devoted to the search for new biologically active substances in a series of alkylamides of dihydroquinoline-3-carboxylic acid. Analgesic properties of 30 newly synthesized substances were studied, which made it possible to identify the leader compound (provisional name alkylcarb) and recommend its effectiveness for further research as an antispasmodic agent for pain relief. It has been established experimentally, that the substance alkylcarb exhibits concentration-dependent vasodilatory properties in vitro on segments of the thoracic aorta of rats. The data, obtained in the work, justify the prospect of using the leader substance as a new analgesic and antispasmodic drug. The research expands and deepens knowledge about the pharmacological properties of alkylamide derivatives of dihydroquinoline-3-carboxylic acid. The aim of the work was to conduct screening studies to establish the analgesic activity of a newly synthesized series of chemical compounds among alkylamides of dihydroquinoline-3-carboxylic acid and to study the myotropic spasmolytic activity of the leader substance. Materials and methods. Analgesic properties of alkylamides of dihydroquinoline-3-carboxylic acid were studied on outbred white mice in the "acetic acid convulsions" test. During the experiment, the animals were treated in accordance with the International Principles of the European Convention for the Protection of Vertebrate Animals Used for Experiments and Other Scientific Purposes (Strasbourg, March 18, 1986). The studied substances were administered intragastrically to experimental animals at a dose of 10 mg/kg in the form of a finely dispersed aqueous suspension, stabilized with Tween-80. Voltaren at a dose of 8 mg/kg, recommended for preclinical studies, and analgin at a dose of 50 mg/kg were chosen as reference drugs. The studies of the contractile activity of smooth muscle vessels were carried out on segments of the thoracic aorta of rats of both sexes weighing 180-200 g. The studies of dilator reactions were carried out against the background of preliminary contraction with phenylephrine at a concentration of 10-6 mol/l. The antispasmodic efficiency of the new compound was determined in comparison with the classic antispasmodic drotaverine. The statistical processing of the results was carried out using the package of statistical analysis of electronic spreadsheets Exel, with the help of the program "Statgraphics Plus v. 3.0.” and the standard package of statistical programs "Statistica, V. 6.0". We used the Student's test, a non-parametric analog of univariate variance analysis - the Kruskal-Wallis test, and the Mann-Whitney test. Differences were considered statistically significant at p<0.05. Results. The study of the analgesic activity of substances АO1-АO30 in the "acetic acid convulsion" test in mice showed that a compound АO26 (provisional name alkylcarb) has the most pronounced analgesic activity when administered intragastrically. In the "acetic acid convulsion" test, alkylcarb (10 mg/kg, per os) probably reduces the number of convulsions, caused by acetic acid. The level of activity of this compound is comparable to the activity of diclofenac (8 mg/kg, per os) and exceeds analgin (50 mg/kg, per os). The substance alkylcarb relieved vasospasm at the level of the comparison drug drotaverine in in vitro experiments on a model of an isolated fragment of the thoracic aorta of rats against the background of previous constriction with phenylephrine. Conclusion. Today, the search for new highly effective non-opioid analgesics is an urgent problem of modern pharmacology, since painkillers used in clinical practice do not meet the requirements of efficiency and safety. In this regard, in recent years, scientists of the National Pharmaceutical University have been intensively searching for new, highly effective substances with antinociceptive, anti-inflammatory and antipyretic effects among alkylamides of dihydroquinoline-3-carboxylic acid.

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AHMED, SAIMA, and Muhammad ASADULLAH. "PSYCHOPHARMACOLOGICAL ACTIVITY;." Professional Medical Journal 19, no. 02 (February 22, 2012): 264–69. http://dx.doi.org/10.29309/tpmj/2012.19.02.2029.

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Objective: The purpose of this study was to screen some herbal medicine as psychotropic drugs those has strong modulatingeffect on brain and behavior. Material & methods: Herbal drug Reserpine, Nux- Vomica, Anacardium and Chlorpromazine with a wide range ofpharmacological actions. In our present study, we evaluate the effectiveness of these drugs as Psychotropic agents and accessed bybiochemical-parameters. Rats (weighing 180-250g) and Mice (22-32g) either sex were used in this study. One group was kept as control fordrugs. Mice were kept under room temperature. Tap-water was allowed ad-Libitum. Animals were observed during and after 21 days. A tabletcrushed in 10ml of water, 1cc was given. Screening method used was swimming induced-despair. Results: Among these, Strychnos Nux-Vomica has strong action on cholinergic system, CNS activity and observed as an antispasmodic. Rauwolfia serpentine is an active alkaloidparticularly present in reserpine are used to treat essential hypertension and in certain neuropsychiatry disorders. It has sedative andtranquilizing effects, as it depletes catecholamine from the central nervous system. Keeping in view, the medicinal importance of these herbs,our present study was designed to screen these herbs as for CNS activity on Albino mice and rats.

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Valero, Marta Sofía, Víctor López, Marta Castro, Carlota Gómez-Rincón, María Pilar Arruebo, Francisco Les, and Miguel Ángel Plaza. "Involvement of NO/cGMP Signaling Pathway, Ca2+ and K+ Channels on Spasmolytic Effect of Everlasting Flower Polyphenolic Extract (Helichrysum stoechas (L.) Moench)." International Journal of Molecular Sciences 23, no. 22 (November 20, 2022): 14422. http://dx.doi.org/10.3390/ijms232214422.

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Анотація:

Functional gastrointestinal diseases (FGID) are worldwide prevalent conditions. Pharmacological treatments can be ineffective, leading the population to turn to herbal or traditional remedies. Helichrysum stoechas (L.) Moench is a medicinal plant traditionally used in the Iberian Peninsula to treat digestive disorders, but its effects on gastrointestinal motility have not been scientifically demonstrated. The aim of this work was to evaluate the antispasmodic effect of a polyphenolic extract of H. stoechas (HSM), its mechanism of action and its antioxidant activity. Isometric myography studies were performed in rat ileum, and malondialdehyde (MDA) and 4-hydroxyalkenals (4-HDA) levels were measured in rat jejunum. HSM reduced the integrated mechanical activity of spontaneous contractions. In Ca2+-free medium, HSM reduced the concentration–response curve of CaCl2 similarly to verapamil. Pre-incubation with the extract blocked the contraction induced by Bay K8644, KCl and carbachol. L-NAME, ODQ, Rp-8-Br-PET-cGMPS, KT-5823, apamin, TRAM-34 and charybdotoxin reduced the relaxant effect of the extract on spontaneous contractions. MDA+4-HDA levels in LPS-treated tissue were reduced by the extract, showing antioxidant activity. In conclusion, HSM showed antispasmodic activity through inhibition of Ca2+ influx, activation of the NO/PKG/cGMP pathway and opening of Ca2+-activated K+ channels. The results suggest that H. stoechas could help in the prevention or treatment of FGIDs.

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