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Eugen J. Verspohl - One of the best experts on this subject based on the ideXlab platform.
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bioassay guided fractionation of a thymol deprived hydrophilic thyme extract and its antispasmodic effect
Journal of Ethnopharmacology, 2012Co-Authors: Jonas Engelbertz, Matthias Lechtenberg, Lena Stud, A Hensel, Eugen J. VerspohlAbstract:Abstract Ethnopharmacological relevance Extracts from Thymus vulgaris L. and Thymus zygis L. are traditionally used for bronchitis, catarrhs of the respiratory tract and supportive treatment of pertussis. A potential spasmolytic effect is thought to be due to the presence of the monoterpenoid phenols thymol and carvacrol in the extract. Based on previous data the present investigation aimed to clarify if thymol-deprived thyme extracts (as been in use within German drug market) have antispasmodic activity. Additionally compounds responsible for this effect had to be identified. Materials and methods Thyme fluid extract was subsequently fractionated by FCPC, LPLC, and HPLC and compounds isolated were identified by spectroscopic methods. Bioassay testing was done by quantification of antispasmodic activity in the preconstricted rat smooth muscle trachea model against papaverin as positive control. Results Thymol-deprived spissum extract (SE) had good antispasmodic activity (−37%, related to the maximum contraction). Bioassay-guided fractionation indicated that rosmarinic acid and apigenin do not contribute to this effect. Luteolin contributed significantly to the antispasmodic activity (−9%). Conclusions Thyme extracts have antispasmodic activity, which is at least due to synergistic effects of phenolic volatile oil compounds and the flavone luteolin. Specifications of thyme-containing preparations should refer to this flavone in addition to focusing on the volatile phenols.
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impact of thymol in thyme extracts on their antispasmodic action and ciliary clearance
Planta Medica, 2010Co-Authors: Frank Egrow, Jonas Engelbertz, Jo Feistel, Romanus Lehnfeld, Katri Aue, Eugen J. VerspohlAbstract:: Thyme is a herb with broncholytic und secretomotoric effects. Its activity on beta (2) receptors as a possible mechanism of action was demonstrated. Major components are thymol and carvacrol which are claimed to be responsible for its effects and, therefore, used for standardization in the German pharmacopoeia (0.03 % phenols calculated as thymol). Our aim was to investigate the impact of thymol by using thyme extracts with either normal or extremely low thymol concentrations ( 0.038 %). The antispasmodic effect on smooth muscles of the trachea and the ileum and the effect on ciliary activity (respiratory clearance) were investigated. In addition, pure thymol and carvacrol were investigated separately and in spiking experiments. Thymol and carvacrol had a concentration-dependent antispasmodic effect in the rat trachea either being stimulated by acetylcholine, K (+) or Ba (++). The same result was observed with respect to the increase of mucociliary transport in mice. Extracts with very low thymol contents are effective in all models used except acetylcholine-induced rat ileum contraction. When thyme extracts with normal thymol contents or with very low thymol contents were compared, the extract with normal thymol contents was more effective, both as a relaxant (rat ileum) and as an antispasmodic compound (rat trachea contraction induced by either acetylcholine, Ba (++) or K (+)) and in ciliary transport experiments. Thyme extracts with very low thymol contents (practically free of volatile oil) were equally effective with respect to endothelin effects. When an extract with very low thymol contents is spiked with increasing concentrations of thymol, a concentration-dependent increase concerning the antispasmodic effect (Ba (++)-induced trachea contraction) is observed. In conclusion, the data show that in various models of antispasmodic effect (ileum and trachea) and by measuring ciliary activity, thymol (and carvacrol) is (are) active, although other not identified components of thyme extract appear to be very important as well, since extracts with very low thymol contents are active. On the basis of these results the standardization on thymol alone appears not to be justified.
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antispasmodic activity of an extract from plantago lanceolata l and some isolated compounds
Phytomedicine, 2007Co-Authors: H Flee, Eugen J. VerspohlAbstract:Abstract An ethanolic spissum extract of the aerial parts of Plantago lanceolata L. was examined for antispasmodic activity on isolated ileum and trachea of the guinea-pig. Isolated constituents were investigated as well. The P. lanceolata extract inhibited the contractions of the guinea-pig ileum that were induced by various agonists such as acetylcholine (ACh), histamine, potassium and barium ions. Additionally the trachea contractions induced by barium ions were inhibited. The compounds luteolin, acteoside, plantamajoside an catalpol peracetate but not catalpol, isoacteoside, lavandulifolioside and aucubin inhibited the ACh-induced contractions of the guinea-pig ileum. Luteolin and acteoside reduced the barium-induced contractions of the guinea-pig trachea. Two recently isolated compounds did not show antispasmodic activity: luteolin-3′,7-diglucuronide and β -hydroxy-acteoside.
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reduction of ach induced contraction of rat isolated ileum by coptisine caffeoylmalic acid chelidonium majus and corydalis lutea extracts
Planta Medica, 1996Co-Authors: Sabine C. Boegge, Eugen J. Verspohl, Stefanie Kesper, Adolf NahrstedtAbstract:The crude extracts of Chelidonium majus and Corydalis lutea were examined for antispasmodic activity against acetylcholine (ACh)-induced contraction on isolated rat ileal smooth muscle. Further, coptisine and caffeoylmalic acid as components of the alkaloid and the hydroxycinnamic acid ester fraction of both plants were similarly investigated. The ACh-induced contraction was found to be antagonized weakly by caffeoylmalic acid (6.9 % ; 2.5 x 10 -5 g/ml organ bath), C majus extract (12.7% ; 2.0 x 10 -4 g/ml), and a higher concentration of coptisine (16.5% ; 1.0 x 10 -5 g/ml) whereas the antispasmodic activity of C. lutea extract reached 45% (2.0 x 10 -4 g/ml). Antagonism by papaverine as a positive control amounted to 83.2 %.
Shafi Mussa - One of the best experts on this subject based on the ideXlab platform.
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duration of action of antispasmodic agents novel use of a mouse model as an in vivo pharmacological assay
European Journal of Cardio-Thoracic Surgery, 2004Co-Authors: Shafi Mussa, Tash Prio, Nicholas J Alp, Kathry J Wood, Keith M Channo, David P TaggaAbstract:OBJECTIVE: Radial arteries are increasingly used as conduits for coronary artery bypass grafts, but perioperative graft vasospasm remains a concern. In vitro testing has demonstrated the efficacy of phenoxybenzamine and verapamil/nitroglycerin as topical antispasmodic agents, but their duration of action in vivo is unknown. Using an in vivo mouse model, we measured their duration of action in functioning vascular grafts, and compared this to their in vitro duration of action in ungrafted vascular segments. METHODS: Two millimetre mouse aortic segments (C57/BL6) were incubated with phenoxybenzamine, verapamil/nitroglycerin, or buffer (controls) for 15 min in organ chambers. Isometric tension responses to phenylephrine and prostaglandin F2alpha were measured at 0, 2, 6 and 12 h post-incubation. In parallel, 36 murine infrarenal aortic interposition grafts (2 mm) were performed. Twelve grafts were pre-treated (15 min) with phenoxybenzamine, 12 with verapamil/nitroglycerin and 12 remained untreated (controls). Isometric tension responses to the same agonists were measured in grafts harvested 2, 6, 13 and 23 h after surgery. RESULTS: Phenoxybenzamine prevented alpha-adrenergic vasoconstriction for up to 16 h in vivo (grafts), and 12h in vitro (ungrafted segments). Verapamil/nitroglycerin was effective for at least 2 h in vitro, but did not prevent vasoconstriction after 2 h in vivo. CONCLUSIONS: The mouse model appears to be a useful technique for assessing the pharmacological properties of antispasmodic agents in vivo. Phenoxybenzamine has an extended action in arterial grafts in vivo. Verapamil/nitroglycerin is short-lived in vivo but lasts longer in vitro. Measurements of antispasmodic duration of action in vitro should be interpreted with caution.
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comparative efficacies and durations of action of phenoxybenzamine verapamil nitroglycerin solution and papaverine as topical Antispasmodics for radial artery coronary bypass grafting
The Journal of Thoracic and Cardiovascular Surgery, 2003Co-Authors: Shafi Mussa, Tomasz J Guzik, Edward Black, Michelle Dipp, Keith M Channon, David P TaggartAbstract:Abstract Objective Radial arteries are increasingly used as conduits for coronary artery bypass grafts, but perioperative graft vasospasm continues to be a concern. Phenoxybenzamine, verapamil/nitroglycerin solution, and papaverine have been advocated as topical antispasmodic agents. We compared the relative efficacies and durations of action of these agents. Methods Isometric tension developed in response to clinically important vasoconstrictors was measured in 100 radial artery rings (from patients undergoing coronary artery bypass grafting, n=25) after 15 minutes of ex vivo incubation with phenoxybenzamine, verapamil/nitroglycerin solution, papaverine, or vehicle (control). Duration of action was assessed by measuring responses to vasoconstrictors in antispasmodic pretreated and control rings at intervals through 5 hours. Results Verapamil/nitroglycerin solution reduced vasoconstriction in response to epinephrine, angiotensin II, prostaglandin F 2α , and phenylephrine but its effect had almost completely waned after 5 hours. Phenoxybenzamine prevented vasoconstriction in response to epinephrine, dopamine, and phenylephrine, with its effect lasting at least 5 hours. Papaverine had limited antispasmodic efficacy and prevented vasoconstriction in response to potassium (60 mmol/L) and phenylephrine for only 1 hour at the longest. Conclusions Verapamil/nitroglycerin solution has a broad efficacy against a range of vasoconstrictors but a limited duration of action. Papaverine has the shortest duration of action. Phenoxybenzamine is an effective agent with a prolonged duration of action, specifically preventing catecholamine mediated vasospasm of radial artery conduits.
Khalid M. Alkharfy - One of the best experts on this subject based on the ideXlab platform.
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species differences in the antidiarrheal and antispasmodic activities of lepidium sativum and insight into underlying mechanisms
Phytotherapy Research, 2013Co-Authors: Malik Hassan Mehmood, Najeeb Ur Rehman, Anwarul Hassan Gilani, Khalid M. AlkharfyAbstract:The aim of this study was to see if the crude extract of Lepidium sativum (Ls.Cr) exhibits species specificity in its antidiarrheal and antispasmodic activities along with insight into the underlying mechanisms using the in-vivo and in-vitro experiments. Ls.Cr inhibited castor oil-induced diarrhea in mice at doses (300 and 1000 mg/kg) three times higher dose than for rats. In isolated rat ileum and jejunum, Ls.Cr completely inhibited carbachol (CCh), low K+ (25 mM) and high K+ (80 mM)-induced contractions, while in guinea-pig tissues, Ls.Cr caused complete inhibition of only CCh-induced contraction. In rabbit tissues, Ls.Cr completely inhibited CCh and low K+-induced contractions sensitive to K+ channel antagonists. Pretreatment of guinea-pig and rat tissues with Ls.Cr caused a rightward shift in CCh-induced contractions in a pattern similar to dicyclomine, while in rabbit and rat tissues, Ls.Cr shifted isoprenaline curves to the left similar to papaverine. These data indicate that the antidiarrheal and antispasmodic activities of L. sativum are species dependent, mediating its antispasmodic effect through combinations of multiple pathways including activation of K+ channels, and inhibition of muscarinic receptors, Ca++ channels and PDE enzyme. Rat tissues showed the highest potency. Based on the results, we recommend using multiple species to know the real pharmacological profile of medicinal products. Copyright © 2012 John Wiley & Sons, Ltd.
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species differences in the antidiarrheal and antispasmodic activities of lepidium sativum and insight into underlying mechanisms
Phytotherapy Research, 2013Co-Authors: Anwarul Hassa Gilani, Najeeb U Rehma, Malik Hassa Mehmood, Khalid M. AlkharfyAbstract:The aim of this study was to see if the crude extract of Lepidium sativum (Ls.Cr) exhibits species specificity in its antidiarrheal and antispasmodic activities along with insight into the underlying mechanisms using the in-vivo and in-vitro experiments. Ls.Cr inhibited castor oil-induced diarrhea in mice at doses (300 and 1000 mg/kg) three times higher dose than for rats. In isolated rat ileum and jejunum, Ls.Cr completely inhibited carbachol (CCh), low K+ (25 mM) and high K+ (80 mM)-induced contractions, while in guinea-pig tissues, Ls.Cr caused complete inhibition of only CCh-induced contraction. In rabbit tissues, Ls.Cr completely inhibited CCh and low K+-induced contractions sensitive to K+ channel antagonists. Pretreatment of guinea-pig and rat tissues with Ls.Cr caused a rightward shift in CCh-induced contractions in a pattern similar to dicyclomine, while in rabbit and rat tissues, Ls.Cr shifted isoprenaline curves to the left similar to papaverine. These data indicate that the antidiarrheal and antispasmodic activities of L. sativum are species dependent, mediating its antispasmodic effect through combinations of multiple pathways including activation of K+ channels, and inhibition of muscarinic receptors, Ca++ channels and PDE enzyme. Rat tissues showed the highest potency. Based on the results, we recommend using multiple species to know the real pharmacological profile of medicinal products. Copyright © 2012 John Wiley & Sons, Ltd.
Anwarul Hassa Gilani - One of the best experts on this subject based on the ideXlab platform.
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antispasmodic and antidiarrheal activities of rhizomes of polygonatum verticillatum maneuvered predominately through activation of k channels components identification through tlc
Toxicology and Industrial Health, 2016Co-Authors: Anwarul Hassa Gilani, Naveed Muhammad, Najeeb U Rehma, Malik Hassa Mehmood, Muhammad Saeed, Haroo Kha, Nadeem AshrafAbstract:Polygonatum verticillatum has traditionally been used for various purposes. The present study was aimed to validate the antispasmodic and antidiarrheal properties of crude methanolic extract of rhizomes of P. verticillatum (PR). Isolated rabbit jejunum preparations were suspended in tissue baths to measure the isotonic responses using Power Lab data acquisition system for the antispasmodic activity of PR, while the antidiarrheal activity was conducted in vivo in mice. PR caused complete relaxation of the spontaneous contractions of isolated rabbit jejunum preparations in a dose-dependent mode. A complete inhibition was observed against low potassium (K+; 25 mM)-induced contractions, while the plant extract partially inhibited the high K+ (80 mM)-induced contractions. From a mechanistic point of view, the spasmolytic effect of PR against low K+ was antagonized by glibenclamide similar to the effect of cromakalim, thus showing the presence of constituents in PR mediating spasmolytic activity predominantly t...
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species differences in the antidiarrheal and antispasmodic activities of lepidium sativum and insight into underlying mechanisms
Phytotherapy Research, 2013Co-Authors: Anwarul Hassa Gilani, Najeeb U Rehma, Malik Hassa Mehmood, Khalid M. AlkharfyAbstract:The aim of this study was to see if the crude extract of Lepidium sativum (Ls.Cr) exhibits species specificity in its antidiarrheal and antispasmodic activities along with insight into the underlying mechanisms using the in-vivo and in-vitro experiments. Ls.Cr inhibited castor oil-induced diarrhea in mice at doses (300 and 1000 mg/kg) three times higher dose than for rats. In isolated rat ileum and jejunum, Ls.Cr completely inhibited carbachol (CCh), low K+ (25 mM) and high K+ (80 mM)-induced contractions, while in guinea-pig tissues, Ls.Cr caused complete inhibition of only CCh-induced contraction. In rabbit tissues, Ls.Cr completely inhibited CCh and low K+-induced contractions sensitive to K+ channel antagonists. Pretreatment of guinea-pig and rat tissues with Ls.Cr caused a rightward shift in CCh-induced contractions in a pattern similar to dicyclomine, while in rabbit and rat tissues, Ls.Cr shifted isoprenaline curves to the left similar to papaverine. These data indicate that the antidiarrheal and antispasmodic activities of L. sativum are species dependent, mediating its antispasmodic effect through combinations of multiple pathways including activation of K+ channels, and inhibition of muscarinic receptors, Ca++ channels and PDE enzyme. Rat tissues showed the highest potency. Based on the results, we recommend using multiple species to know the real pharmacological profile of medicinal products. Copyright © 2012 John Wiley & Sons, Ltd.
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ethnopharmacological evaluation of the anticonvulsant sedative and antispasmodic activities of lavandula stoechas l
Journal of Ethnopharmacology, 2000Co-Authors: Anwarul Hassa Gilani, Nauma Aziz, Munasib Kha, Farhana Shahee, Qaise Jabee, Ina S Siddiqui, Joachim W HerzigAbstract:Lavandula stoechas L. (Lamiaceae) has been used for a long time in traditional medicine as an anticonvulsant and antispasmodic. The aqueous-methanolic extract of L. stoechas flowers (LS) was studied for its possible anticonvulsant and antispasmodic activities. When tested in mice, LS (600 mg/kg) significantly reduced the severity and increased the latency of convulsions induced by pentylene tetrazole (PTZ). LS likewise reduced PTZ's lethality. LS up to a dose of 600 mg/kg was found devoid of any hypnotic effect in mice, however, animals were found to be dull, calm and relaxed. The sedative effect of the plant extract was confirmed, as it prolonged the pentobarbital sleeping time in mice similar to that of diazepam. In isolated rabbit jejunum preparations, LS caused a dose-dependent (0.1–1.0 mg/ml) relaxation of spontaneous contractions. LS also inhibited K+-induced contractions in a similar dose range, thereby suggesting calcium channel blockade. This effect was confirmed when pretreatment of the jejunum preparation with LS produced a dose-dependent shift of the Ca2+ dose-response curve to the right, similar to the effect of verapamil, a standard calcium channel blocker. These data indicate that the plant extract exhibits anticonvulsant and antispasmodic activities. Its calcium channel blocking property may be mechanistically related to these activities. Its usefulness in folk medicine appears thus to be based on a sound mechanistic background.
David P Taggart - One of the best experts on this subject based on the ideXlab platform.
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comparative efficacies and durations of action of phenoxybenzamine verapamil nitroglycerin solution and papaverine as topical Antispasmodics for radial artery coronary bypass grafting
The Journal of Thoracic and Cardiovascular Surgery, 2003Co-Authors: Shafi Mussa, Tomasz J Guzik, Edward Black, Michelle Dipp, Keith M Channon, David P TaggartAbstract:Abstract Objective Radial arteries are increasingly used as conduits for coronary artery bypass grafts, but perioperative graft vasospasm continues to be a concern. Phenoxybenzamine, verapamil/nitroglycerin solution, and papaverine have been advocated as topical antispasmodic agents. We compared the relative efficacies and durations of action of these agents. Methods Isometric tension developed in response to clinically important vasoconstrictors was measured in 100 radial artery rings (from patients undergoing coronary artery bypass grafting, n=25) after 15 minutes of ex vivo incubation with phenoxybenzamine, verapamil/nitroglycerin solution, papaverine, or vehicle (control). Duration of action was assessed by measuring responses to vasoconstrictors in antispasmodic pretreated and control rings at intervals through 5 hours. Results Verapamil/nitroglycerin solution reduced vasoconstriction in response to epinephrine, angiotensin II, prostaglandin F 2α , and phenylephrine but its effect had almost completely waned after 5 hours. Phenoxybenzamine prevented vasoconstriction in response to epinephrine, dopamine, and phenylephrine, with its effect lasting at least 5 hours. Papaverine had limited antispasmodic efficacy and prevented vasoconstriction in response to potassium (60 mmol/L) and phenylephrine for only 1 hour at the longest. Conclusions Verapamil/nitroglycerin solution has a broad efficacy against a range of vasoconstrictors but a limited duration of action. Papaverine has the shortest duration of action. Phenoxybenzamine is an effective agent with a prolonged duration of action, specifically preventing catecholamine mediated vasospasm of radial artery conduits.