Antispasmodic activity of extracts and compounds of Acalypha phleoides Cav

The aerial parts of Acalypha phleoides are usually prescribed in the Mexican traditional medicine for a variety of gastrointestinal complaints. The MeOH-CHCl(3) (1:1) extract of the aerial part of A. phleoides showed an inhibitory effect on the gastrointestinal propulsion of a charcoal meal in mice. In isolated guinea-pig ileum, this extract produced a concentration dependent inhibition of the contractions induced by 5-hydroxytryptamine, but it was unable to inhibit the contractions elicited by acetylcholine, histamine, KCl and BaCl(2). This extract produced also a concentration dependent inhibition of the spontaneous pendular movement of the isolated rabbit jejunum. This inhibitory activity was partially blocked by propranolol. The essential oil, obtained from the aerial part of this plant, was more potent than the MeOH-CHCl(3) (1:1) extract in inhibiting the spontaneous pendular movement of the rabbit jejunum. Thymol, camphor and gamma-terpinene were identified from the essential oil by GC-MS. These monoterpenes showed antispasmodic activity in the rabbit jejunum preparation, thymol was the most active compound, followed by camphor and gamma-terpinene. Thymol and camphor in high concentrations also showed tracheal relaxant properties, but gamma-terpinene did not. These in vivo and in vitro results tend to support the traditional use of A. phleoides as an antispasmodic agent.     

小半夏加茯苓汤及其拆方对家兔离体胃肠运动的影响

目的:研究小半夏加茯苓汤(Xiaobanxia Fuling decoction,XBFD)及其拆方水提物对家兔离体胃肠运动的影响.方法:用生物信号分析系统记录小半夏加茯苓汤及其拆方提取物对家兔正常离体胃、肠平滑肌和工具药乙酰胆碱、阿托品所致离体胃、肠平滑肌收缩的影响,采集胃、肠平滑肌收缩的曲线和数据,比较用药前后胃、肠平滑肌收缩的振幅、频率和张力变化.结果:小半夏加茯苓汤及其拆方提取物对正常离体胃底和胃窦平滑肌自主活动具有不同程度的兴奋作用,对家兔正常离体十二指肠平滑肌的正常舒缩活动有抑制作用,加药前后比较显著差异(P＜0.01);能拮抗氯化乙酰胆碱引起的胃肠平滑肌强直痉挛(P＜0.01);对阿托品引起的十二指肠平滑肌舒缩活动减弱具有协同作用(P＜0.05),而对阿托品作用后的胃底和胃窦平滑肌有兴奋作用(P＜0.01),原方及拆方的作用强度表现为:小半夏加茯苓汤＞小半夏汤＞生姜＞半夏.结论:小半夏加茯苓汤及其拆方提取物对家兔离体胃肠运动具有双向调节作用,复方药效优于拆方.其作用途径不仅与M胆碱受体有关,还可能与其他调节因素有关.     

Antispasmodic effect of three fractions of hydroalcoholic extract of Pycnocycla spinosa

Hydroalcoholic extract of Pycnocycla spinosa was shown to have spasmolytic action in vitro and antidiarroheal effect in vivo. The hydroalcoholic extract of P. spinosa is composed of alkaloid-, flavonoid- and saponin-rich components. These components were separated by fractional separation technique. The pharmacological objective of this study was to look for relaxant effect of these components of hydroalcoholic extract of P. spinosa on rat isolated ileum contractions. The alkaloid-, flavonoid- and saponin-rich fractions of P. spinosa inhibited the response to 80 mM KCl in a concentration-dependent manner. The alkaloid-rich fraction was the most and saponin-rich fraction the least effective relaxant of ileum contractions. The alkaloid-rich fraction also inhibited the response to acetylcholine (ACh) and 5-hydroxytryptamine (5-HT). From this study, it can be concluded that the antispasmodic action of hydroalcoholic extract of P. spinosa could be due to components in the alkaloid-rich fraction and to a lesser extent, to its flavonoid-rich fraction.     

Effects of an aqueous extract of Ferula ovina on rabbit and guinea pig smooth muscle

The effects of an aqueous extract of Ferula ovina were tested in vitro using isolated segments of rabbit and guinea pig intestine, trachea and aorta. The extract inhibited the spontaneous movements of rabbit jejunum and guinea pig ileum and the contractions induced by acetylcholine. The aqueous extract also inhibited the contractions of rabbit trachealis muscle induced by acetylcholine and the contractions of guinea pig trachealis muscle induced by histamine. These inhibitions were dose-dependent and reversible. However, the aqueous extract did not inhibit the contractions of rabbit and guinea pig aortic rings induced by norepinephrine. These data suggest that this plant has non-specific anticholinergic and antihistaminic antispasmodic effects.     

Antidiarrheal and Antispasmodic Activities of Buddleja polystachya are Mediated Through Dual Inhibition of Ca++ Influx and Phosphodiesterase Enzyme

This study describes the antidiarrheal and antispasmodic activities of the hydro‐alcoholic extract of Buddleja polystachya (Bp.Cr) with possible mode of action explored along with activity‐directed fractionation. Bp.Cr and its aqueous (Bp.Aq) and organic fractions, petroleum ether (Bp.Pet), dichloromethane (Bp.DCM), ethylacetate (Bp.EtAc) and butanol (Bp.But), were tested using the in‐vivo and in‐vitro assays. The crude extract (100–300 mg/kg) showed 20 and 60% protection of castor oil‐induced diarrhea in mice. In isolated rabbit jejunum, Bp.Cr like papaverine inhibited spontaneous and high K⁺ (80 mM)‐induced contractions equi‐potently. In guinea‐pig ileum, Bp.Cr showed a moderate spasmogenic effect. The activity‐directed fractionation revealed that the spasmolytic activity was concentrated in the organic fractions and spasmogenic component in the aqueous fraction. Amongst the organic fractions, BP.DCM and Bp.Pet inhibited spontaneous and high K⁺‐induced contractions equi‐potently, while Bp.But, like verapamil was more potent against high K⁺. The crude extract and its organic fractions caused rightward shift in the Ca⁺⁺‐concentration response curves (CRCs), similar to verapamil, and all except Bp.But potentiated the isoprenaline‐inhibitory CRCs to the left, similar to papaverine. The results of this study indicate that the crude extract of B. polystachya possesses antidiarrheal and antispasmodic activities, mediated possibly through dual inhibition of Ca⁺⁺ influx and phospodiesterase enzyme. Copyright © 2015 John Wiley & Sons, Ltd.     

Effects of ethanol extract of Moringa stenopetala leaves on guinea-pig and mouse smooth muscle.

The fresh leaf ethanol (LE) extract of Moringa stenopetala was tested in guinea-pig ileum and mouse duodenum and in uterus strips. There were significant dose and time dependent reductions of the acetylcholine (AC) response with initial stimulatory effects in both the guinea-pig ileum and the mouse duodenum preparations. Spontaneous rhythmic contractions were greatly reduced, suggesting an antispasmodic property of the crude LE extract. The LE extract showed some oxytocic activity on uterus strips of guinea-pigs and mice. The results are indicative of the traditional use of the leaves of Moringa stenopetala for stomach pain and to expel retained placentae by women.     

Spasmogenic effect of Datura metel root extract on rat uterus and rectum smooth muscles

The effect of Dautura metel leaf and root extracts, scopolamine and acetylcholine was studied on isolated smooth muscle preparations. Datura metel leaf extract and scopolamine showed antispasmodic effects, whereas Datura metel root extract and acetylcholine caused contracture in isolated rat uterus and rectum whole muscle. This suggests the presence of a spasmogenic factor in Datura metel root extract.     

麸煨肉豆蔻不同提取物对大鼠离体肠平滑肌的影响

目的研究麸煨肉豆蔻不同提取物对大鼠离体肠管自发活动的影响。方法采用RM6240B多道生理信号采集处理系统及大鼠离体十二指肠平滑肌进行实验,观察麸煨肉豆蔻不同提取物对离体肠运动功能的影响。结果麸煨肉豆蔻挥发油、醇提物、醇提物的石油醚提取物及乙酸乙酯提取物对离体大鼠十二指肠自主运动有抑制作用,抑制率分别为51.2%、29.2%、47.8%和59.2%(P<0.01);水提物、正丁醇提取物及醇提取物萃取后的水层无抑制作用。结论麸煨肉豆蔻的挥发油、醇提物的石油醚、乙酸乙酯提取物可能为麸煨肉豆蔻止泻的有效部位。     

诃子醇提物对动物胃肠运动和血清胃动素含量的影响

目的: 研究诃子醇提物对动物胃肠运动和血清胃动素含量的影响。 方法: 将实验动物随机分为空白对照组、吗丁啉（小鼠0.005 g·kg^-1,大鼠0.003 g·kg^-1）组,诃子提取物高、中、低剂量组（小鼠3.5,1.75,0.875 g·kg^-1,大鼠2.4,1.2,0.6 g·kg^-1）,按10 mL·kg^-1给药,采用小鼠在体胃肠运动实验、放免法检测大鼠血清胃动素含量和家兔离体肠平滑肌运动实验,观察诃子提取物对正常小鼠胃排空、小肠推进运动和大鼠血清胃动素含量以及家兔离体肠平滑肌收缩的影响。 结果: 诃子提取物高、中剂量对正常小鼠胃排空和小肠推进运动有显著抑制作用,可以降低大鼠血清胃动素的含量,对家兔离体肠平滑肌收缩有显著抑制作用,对氯化乙酰胆碱引起的肠平滑肌兴奋有显著拮抗作用（P<0.05或P<0.01）。 结论: 诃子醇提物对动物胃肠运动有抑制作用,其作用途径可能与M胆碱受体有关。     

Species Differences in the Antidiarrheal and Antispasmodic Activities of Lepidium sativum and Insight into Underlying Mechanisms

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.     

In vitro pharmacological investigations of Sapindus trifoliatus in various migraine targets

Phytotherapies have offered alternative sources of therapy for migraine and gained much importance in prophylactic treatment. The aqueous extract of pericarp of fruits of Sapindus trifoliatus Linn (ST), family Sapindaceae was evaluated for its affinity for 5-HT(1B/1D) receptors in rabbit saphenous vein, alpha-adrenoceptors in rabbit aorta, GABA receptors in guinea pig ileum, 5-HT(2B) receptors in rat fundus and vanilloid receptors in guinea pig trachea. The calcium blocking effect was studied in rabbit aorta while the modulatory role of ST on platelet serotonin release was evaluated in human platelets. The aqueous extract of Sapindus trifoliatus exhibited significant 5-HT(2B) receptor inhibition and moderate platelet serotonin release inhibition.     

枳壳及辛弗林对兔离体小肠运动的影响

目的 :观察枳壳及辛弗林对兔离体小肠运动的影响并探讨其作用机制。方法 :以家兔小肠收缩强度为指标 ,观察枳壳水煎剂及辛弗林对肠平滑肌收缩的影响。结果 :枳壳水煎剂 ( 12 5 %、2 5 %、5 0 %、75 %、10 0 % )和辛弗林 ( 0 1mg/ml、1mg/ml、5mg/ml、10mg/ml、2 0mg/ml)均能显著抑制家兔离体小肠 (十二指肠 )的自发活动 ,使收缩力降低 ,紧张性下降 ,且呈量效关系。枳壳对乙酰胆碱 (Ach)、氯化钡 (BaCl2 )、5 羟色胺 ( 5 HT)引起的收缩加强均有显著拮抗作用 ,能使先用阿托品、肾上腺素、多巴胺而紧张性降低的离体兔肠进一步松弛 ;枳壳能微弱拮抗酚妥拉明的作用 ,对心得安的抑制效应影响不大。辛弗林能显著拮抗BaCl2 、5 HT引起的小肠 (空肠和回肠 )收缩加强 ,并拮抗肾上腺素 (Adr)、多巴胺 (DA)引起的小肠 (空肠和回肠 )收缩抑制 ,协同酚妥拉明的作用。结论 :枳壳水煎剂和辛弗林均能抑制家兔离体小肠运动 ,随剂量加大而作用加强。枳壳的抑制效应通过以 5 HT受体介导 ,由直接对平滑肌抑制作用为主 ,以M受体介导为辅。辛弗林主要通过介导 5 HT、Adr受体和直接对平滑肌作用产生上述抑制效应。辛弗林对离体兔肠作用与枳壳有一定的一致性 ,可能是枳壳作用胃肠运动的有效成分之一。     

射干提取物含药血清对豚鼠离体气管平滑肌收缩功能的影响

目的:研究射干提取物含药血清对豚鼠离体气管平滑肌收缩功能的影响.方法:取豚鼠气管,在Kreb's液中制备气管平滑肌螺旋条,于恒温浴槽装置中,加入组胺(His)使其收缩,观察加入射干提取物含药血清后3,5,10 min的解痉率.结果:射干提取物含药血清对组胺引起的气管平滑肌收缩反应有一定拈抗作用,其中剂量(0.46 g?kg-1)3,5,10 min解痉率分别为44.29％,45.27％和48.30％;高剂量(0.92 g?kg-1)3,5 min解痉率分别为31.17％和31.83％,与空白对照组比较有显著性差异(P ＜0.05或P＜0.01),药物与标本接触5 min效果最好.结论:射干提取物含药血清对His引起的气管平滑肌收缩反应具有一定的拮抗作用.     

Ethnopharmacological evaluation of the anticonvulsant, sedative and antispasmodic activities of Lavandula stoechas L

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 Ca(2+) 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.     

Pharmacological Studies on the Antispasmodic,Bronchodilator and Anti‐Platelet Activities of Abies webbiana

This study evaluated the antispasmodic, bronchodilator and anti‐platelet activities of Abies webbiana to rationalize some of its folk uses in gut and airways disorders and inflammation. The crude extract of A. webbiana (Aw.Cr) caused a complete relaxation of both spontaneous and K⁺ (80 mM)‐induced contractions in isolated rabbit jejunum in a concentration‐dependent manner. Aw.Cr shifted the Ca⁺⁺ concentration–response curves (CRCs) to the right, in a fashion similar to verapamil, confirming its Ca⁺⁺ channel blocking (CCB) effect. In isolated rabbit tracheal preparations, it caused relaxation of carbachol (1 μM) and K⁺ (80 mM)‐induced contractions comparable to verapamil suggesting that the bronchodilatory effect may possibly be mediated through CCB activity. Aw.Cr was found to be the inhibitor of both ADP‐ and epinephrine‐induced aggregation of human platelets thereby suggesting therapeutic potential in this plant against thrombo‐embolic conditions. The exhibited anti‐platelet effect was observed at low doses against epinephrine as compared to ADP. This study confirmed the presence of spasmolytic activity in Abies webbiana through possible blockade of Ca⁺⁺ channels providing evidence for its folkloric use in gut and respiratory disorders in addition to anti‐platelet activity. Copyright © 2014 John Wiley & Sons, Ltd.     

Antispasmodic and antioxidant activities of fractions and bioactive constituent davidigenin isolated from Mascarenhasia arborescens

Ethnopharmacological relevance

Mascarenhasia arborescens A. DC. (Apocynaceae) is used in traditional medicine in the North of Madagascar to treat intestinal disorders, intestinal spasms and diarrhoea.

Aim of the study

The main objective of this work was to evaluate the antispasmodic activity of the crude methanolic extract of Mascarenhasia arborescens and of its four partitions and to identify the effective compound responsible for this effect.

Materials and methods

Isolation and structure elucidation techniques were performed in order to identify the bioactive constituent of Mascarenhasia arborescens and HPLC analysis was used for its quantification. Total phenolic content (TPC) of crude extracts and partitions were determined using the Folin–Ciocalteu method. Crude methanolic extract, partitions and the bioactive compound were investigated for their spasmolytic activity on several isolated organs. Their antiradical activity was also investigated by the DPPH test.

Results

Bioassay-guided fractionation using isolated guinea pig ileum pre-contracted with histamine 3 × 10⁻⁶ M led to the isolation of davidigenin (DG), a dihydrochalcone, as the main active constituent from the most promising methylene chloride partition (McP). This partition was effective on isolated guinea pig ileum pre-contracted with 3 × 10⁻⁶ M histamine, with a median effective concentration (EC₅₀) of 41.19 ± 3.74 μg/ml. The DG content of this partition was shown to be 26.5% by HPLC. DG induced a concentration-dependent relaxation of the histamine pre-contracted guinea pig ileum with an EC₅₀ of 8.04 ± 0.81 μg/ml and a concentration-dependent relaxation of the acetylcholine pre-contracted rat duodenum with an EC₅₀ of 9.35 ± 0.30 μg/ml. It inhibited in a non-competitive manner histamine-induced isolated ileum contraction and the acetylcholine-induced isolated duodenum contraction. Moreover, DG does not have any antiradical activity.

Conclusions

We demonstrated for the first time antispasmodic and antioxidant effects of Mascarenhasia arborescens. This study supports its use in traditional medicine. Furthermore, we highlighted the crucial role of davidigenin in the antispasmodic activity of this plant.     

Antispasmodic and blood pressure lowering effects of Valeriana wallichii are mediated through K+ channel activation

Crude extract of Valeriana wallichii rhizome (Vw.Cr) and its fractions were studied for possible antispasmodic and blood pressure lowering activities to rationalize some of the folkloric uses. In rabbit jejunum preparations, Vw.Cr (0.1–3.0 mg/mL) caused relaxation of spontaneous contractions. When tested against high K⁺ (80 mM)-induced contractions it produced weak inhibitory effect, while caused complete relaxation of the contractions induced by low K⁺ (20 mM). In the presence of glibenclamide (3 μM), the inhibitory effect of low K⁺ was shifted to the right, similar to that produced by cromakalim while, verapamil caused no differentiation in its inhibitory effect against low and high K⁺-induced contractions. In guinea pig ileum, the plant extract produced similar results as in rabbit jejunum. Intravenous administration of Vw.Cr, produced fall in arterial blood pressure in normotensive anaesthetized rats and this effect was partially blocked by glibenclamide. In rabbit aortic preparations, plant extract also caused a selective and glibenclamide-sensitive relaxation of low K⁺ (20 mM)-induced contractions. Activity-directed fractionation studies revealed that the observed activity was distributed both in the chloroform and aqueous fractions. These results indicate that the antispasmodic and hypotensive effects of Valeriana wallichii are mediated possibly through K_ATP channel activation, which justify its use in gastrointestinal and cardiovascular disorders.     

Inhibition of ethyl phenylpropiolate-induced rat ear oedema by compounds isolated from Ipomoea pes-caprae (L.) R. Br.

The extract (IPA) of leaves from Ipomoea pes-caprae (L.) R. Br. has previously been shown to reduce the development of rat ear oedema induced by ethyl phenylpropiolate (EPP) in a dose-dependent manner. Using this bioassay to guide fractionation of the extract, two diastereomeric compounds, the actinidols 1a and 1b, were isolated (0.8% of IPA). The actinidols constitute part of the active principle of IPA. Compounds, previously isolated from IPA, with either prostaglandin synthesis inhibiting activity in vitro [2-hydroxy-4,4,7-trimethyl-1(4H)-naphthalenone, (?)-mellein and eugenol] or antispasmodic activity (E-phytol) were also assayed for inhibitory effects on the development of EPP-induced rat ear oedema. They all reduced oedema formation dose-dependently. The results suggest that IPA consists of several active compounds which interfere with the process of inflammation in different ways.     

CNS depressant effects,anti-inflammatory activity and anti-cholinergic actions of Santolina chamaecyparissus extracts

The pharmacological activity of several extracts together with the lyophilized infusion of S. chamaecyparissus ssp. squarrosa were investigated. The lethal dose 50% (LD₅₀), effect on animal metabolism, mechanical and thermic analgesia and spontaneous, anti-inflammatory, and anti-ulcer activity have been determined. Studies on isolated organs (rat duodenum and rat uterus) were also carried out. The hexanic and chloroformic extracts were potent antagonists of the thermic analgesia test; the former extract was also active in the mechanical analgesia test. The chloroformic extract and, to a lesser extent, the ethyl acetate extract and lyophilized infusion demonstrated noteworthy activity as anti-inflammatory agents. No extract produced an ulcerogenic effect. The hexanic extract had the highest inhibitory effect on ACh induced contraction of rat duodenum and the ethyl acetate extract of oxytocin induced contraction of rat uterus.     

胃疡宁丸对胃肠运动影响的研究

目的:研究胃疡宁丸对胃肠运动的影响.方法:将实验动物随机分为对照组、胃疡宁低、中、高剂量(0.395,0.79,1.58 g·kg-1)组、胃康宁组(0.4 g.kg-1)、吗丁啉组(0.05 g·kg-1),进行硫酸酮致家鸽呕吐实验,测定呕吐潜伏期和呕吐频率;进行大鼠在体肠运动实验、正常离体兔肠运动实验、乙酰胆碱所致痉挛离体兔肠运动实验,测定给药前后张力,并计算抑制率.结果:胃疡宁丸能够减少家鸽呕吐频率(P＜ 0.05或P＜0.01),抑制大鼠在体肠的收缩(P＜0.01),并且对正常离体兔肠收缩与乙酰胆碱所致离体兔肠痉挛有明显抑制作用.结论:胃疡宁丸有胃肠解痉、止呕的作用与其抑制胃肠运动有关.