Relaxant effect of the volatile oil of Rosmarinus officinalis on tracheal smooth muscle

The effects of the volatile oil of Rosmarinus officinalis leaves on the tracheal smooth muscle of rabbit and guinea pig were tested in vitro using isolated tracheal strips. The volatile oil of R. officinalis leaves inhibited the contractions of rabbit tracheal smooth muscle induced by acetylcholine stimulation and the contractions of guinea pig tracheal smooth muscle induced by histamine stimulation. Also, the volatile oil inhibited the contractions of rabbit and guinea pig tracheal smooth muscle induced by high potassium (K+) solution. This inhibition was dose-dependent and reversible. Furthermore, the volatile oil inhibited the contractions of rabbit and guinea pig tracheal smooth muscle induced by acetylcholine and histamine stimulation, respectively, in Ca(2+)-free solution. These data suggest that the volatile oil of R. officinalis leaves has a calcium antagonistic property.     

Direct relaxant effects of garlic juice on smooth and cardiac muscles

The effects of garlic juice on smooth and cardiac muscles of rabbit and guinea pig were tested in vitro using isolated segments of aorta, trachea and intestines and isolated rabbit hearts. Garlic juice inhibited the contractions of rabbit and guinea pig aortic rings induced by norepinephrine in Ca(2+)-free and Ca(2+)-containing Krebs-Henseleit solutions. Also, garlic juice inhibited the contractions of rabbit and guinea pig tracheal smooth muscles induced by acetylcholine and histamine, respectively, in both Ca(2+)-free and Ca(2+)-containing Krebs-Henseleit solutions. Furthermore, garlic juice inhibited the spontaneous movements of rabbit jejunum and guinea pig ileum and inhibited the force of contraction of isolated rabbit hearts in a concentration-dependent manner. All inhibitions were reversible. These data suggest that the hypotensive action of garlic juice may be due, at least in part, to a direct relaxant effect on smooth muscles.     

Effects of a Ferula sinaica root extract on the uterine smooth muscle of rat and guinea pig

The effects of an ethanolic extract of Ferula sinaica roots on the uterine smooth muscles of rats and guinea pigs were tested in vitro using isolated uterine horns. The extract inhibited the spontaneous movements of rat and guinea pig uterine smooth muscle and also the contractions induced by oxytocin stimulation. These effects were concentration-dependent and reversible by tissue washing. These data suggest that this plant extract may have some antioxytocic potential.     

The Prokinetic,Laxative, and Antidiarrheal Effects of Morus nigra: Possible Muscarinic,Ca2+ Channel Blocking,and Antimuscarinic Mechanisms

Morus nigra Linn. (black mulberry) is used in gastrointestinal ailments. This study demonstrates gut modulatory properties of M. nigra. The prokinetic, laxative, and antidiarrheal activities of M. nigra were assessed in mice, while isolated rabbit jejunum and guinea‐pig ileum were used to explore insight into mechanism(s). At 30 and 70 mg/kg, the crude extract of M. nigra (Mn.Cr) exhibited atropine‐sensitive prokinetic and laxative effects, similar to carbachol (CCh). While at higher doses (100, 300, and 500 mg/kg), Mn.Cr offered protection against castor oil‐induced diarrhea. In rabbit jejunum, Mn.Cr and its chloroform fraction inhibited CCh‐induced contractions more potently compared with high K⁺ (80 mm ). Conversely, petroleum fraction was more potent against high‐K⁺‐induced contractions. At 0.01 mg/mL, Mn.Cr caused a parallel shift in acetylcholine concentration–response curves (CRCs) followed by a non‐parallel shift at 0.03 mg/mL, similar to dicyclomine. At further tested concentrations, Mn.Cr (0.1 and 0.3 mg/mL) and petroleum fraction suppressed Ca²⁺ CRCs, similar to verapamil. In guinea‐pig ileum, Mn.Cr, its aqueous and ethyl acetate fractions exhibited atropine‐sensitive gut stimulant activity along with additional uncharacterized excitatory response in the aqueous fraction only. These results suggest that black mulberry possesses prokinetic, laxative, and antidiarrheal effects, putatively mediated through cholinomimetic, antimuscarinic, and Ca²⁺ antagonist mechanisms, respectively. Copyright © 2016 John Wiley & Sons, Ltd.     

Effects of the volatile oil of Nigella sativa seeds on the uterine smooth muscle of rat and guinea pig

The effects of the volatile oil of Nigella sativa seeds on the uterine smooth muscle of rats and guinea pigs was tested in vitro using isolated uterine horns. The volatile oil of Nigella sativa seeds inhibited the spontaneous movements of rat and guinea pig uterine smooth muscle and also the contractions induced by oxytocin stimulation. These effects were concentration-dependent and reversible by tissue washing. These data suggest that this volatile oil may have some anti-oxytocic potential.     

胸腺免疫抑制提取物对豚鼠支气管平滑肌的影响及平喘作用

 目的：研究胸腺免疫抑制提取物(thymic immunosuppressive extract,TISE)对正常及致敏豚鼠支气管收缩的影响及平喘作用。方法：通过离体和整体实验，观察TISE对以组胺和乙酰胆碱引起正常豚鼠支气管的收缩和以卵白蛋白诱发的致敏豚鼠支气管收缩的影响。结果：离体实验，TISE760,380mg·L^-1对组胺致正常豚鼠气管片的收缩具有对抗作用，对卵白蛋白所致的致敏豚鼠支气管平滑肌收缩有极显著的抑制作用(P<0.01)，而对乙酰胆碱所致气管片收缩无明显影响；整体实验，TISE25,18mg·kg^-1可显著延长卵白蛋白所致的致敏豚鼠呼吸困难、抽搐和跌倒的潜伏期(P<0.01)。结论：TISE能拮抗组胺刺激引起的正常豚鼠和卵白蛋白引起的致敏豚鼠离体气管片的收缩，抑制致敏豚鼠哮喘的发生。     

Smooth muscle contraction induced by Indigofera dendroides leaf extracts may involve calcium mobilization via potential sensitive channels

The contractile effects of the aqueous extract of the leaves of Indigofera dendroides (ID) were studied on the gastrointestinal motility in mice and isolated smooth muscle preparations obtained from rats and guinea pigs. The contractile effects of 10(-6) M acetylcholine, 80 mM KCl and 1.6 mg/ml ID were measured on the rat ileal smooth muscle exposed to calcium-free buffer or physiological solution, to determine the calcium pools mobilized by extract for activation of contraction. Acute toxicity test (LD(50)) was also carried out in mice. The result showed that ID (0.05-3.2 mg/ml) produced a concentration-dependent contraction of the guinea pig and rat ileum. These responses were not blocked by mepyramine (2.49 x 10(-9) M), verapamil (8.14 x 10(-9) M), or pirenzepine (4.7 x 10(-7) M), but were blocked completely by atropine (2.92 x 10(-9) M). A significant increase in propulsion of gastrointestinal motility was observed. Acetylcholine, KCl and ID produced contractions in Ca(2+) free media. The phasic components of the contractile responses to Ach as well as the tonic component of K(+) and ID-induced contractions were relatively resistant to short periods of calcium-free exposure. Ach, K(+) and ID still caused contractions in the presence of verapamil. The data revealed that ID-induced contractions were not mediated by histaminergic receptors, calcium channels, M1 muscarinic receptors. It also suggests that Ach mobilize Ca from some tightly bound or intracellular pool, whereas high K(+) and ID may mobilize Ca from some superficial or loosely-bound pool.     

侧柏叶乙酸乙酯提取物对豚鼠离体气管平滑肌的作用

用离体豚鼠气管条,探讨侧柏叶乙酸乙酯提取物对气管平滑肌作用。结果表明,侧柏叶乙酸乙酯提取物能抑制乙酰胆碱,氯化钾所致气管平滑肌收缩,而且能使乙酰胆碱收缩气管平没肌的量效曲线右移,并抑制最大效应,其作用为剂量依赖性心肌肥厚提示侧柏叶乙酸乙酯提取物松驰气管平滑肌作用机制可能与影响Ｃａ＾２＋的跨膜转运有关。     

Intestinal smooth muscle spasmolytic actions of the aqueous extract of the roots of Taverniera abyssinica

A room temperature aqueous extract of the roots of Taverniera abyssinica antagonized the contractile responses of the guinea-pig ileum to acetylcholine and histamine. The extract also relaxed the smooth muscle of the rabbit duodenum, abolished the pendular contractions and antagonized the effects of acetylcholine and histamine on this tissue. The results confirm that there may be a sound pharmacological basis for the ethnomedical use of the roots of this plant to treat stomach ache.     

Effect of Aqueous Extract of Brickellia veronicaefolia on the Gastrointestinal Tract of Guinea-pig,Rats and Mice

The aqueous extract of Brickellia veronicaefolia inhibited gastric emptying time in rats and intestinal motility in mice, both effects were manifested in a dose-related fashion. The crude extract inhibited the contractions induced by acetylcholine and histamine concentration-dependently in the guinea-pig ileum. In the castor oil diarrhoea test, the extract showed 90% protection from diarrhoea at 150 mg/kg.     

云木香对豚鼠离体肠及小鼠胃肠道的影响

目的:研究云木香挥发油、4种水提液萃取物对豚鼠离体肠平滑肌及小鼠胃排空和小肠推进功能的影响。方法:采用BL-420F生物机能实验系统、改良的酚红含量测定法,观察挥发油、4种水提液萃取物对豚鼠离体肠平滑肌及小鼠胃排空和小肠推进功能的作用情况。结果:云木香挥发油(4.0×10-2g生药/ml)、水提液萃取物(1.0×10-2g生药/ml)能够显著降低豚鼠正常状态下;挥发油(2.0×10-2g生药/ml)、水提液萃取物(1.5×10-2g生药/ml)能够显著降低Ach所致痉挛状态下豚鼠离体肠平滑肌的平均振幅;挥发油(2.4×10-2g生药/ml)、水提液萃取物(2.4×10-2g生药/ml)能够显著降低正常小鼠胃酚红排空率,显著提高阿托品所致抑制状态下的小鼠胃酚红排空率,并显著降低新斯的明所致亢进状态下的小鼠胃酚红排空率并降低小肠酚红推进百分率。结论:云木香挥发油、水提液萃取物能够抑制豚鼠离体肠平滑肌的自主活动及拮抗乙酰胆碱所致痉挛状态下离体肠平滑肌;同时抑制正常小鼠胃排空,改善阿托品所致抑制状态下的小鼠胃排空障碍,拮抗新斯的明所致的小鼠胃排空和小肠推进功能亢进。     

Effects of leaf extract of Caesalpinia bonduc (Caesalpiniaceae) on the contractile activity of uterine smooth muscle of pregnant rats

The calcium dependency and the cholinergic effect of the leaf extract of Caesalpinia bonduc Roxb. (Caesalpiniaceae) was studied in isolated pregnant rat myometrium preparations. Isometric contractions were recorded. The extract (Cebo) increased the contractile force in the isolated strips in a concentration-dependent manner. The effects were comparable to those obtained with acetylcholine. Contractions induced by Cebo or acetylcholine were inhibited in the presence of atropine. The stimulating action of Cebo on the contractile responses of isolated myometrium preparations inhibited by atropine may be mediated by cholinergic receptors. In calcium-free solution Cebo induced a tonic contraction (contracture) of the muscle. Moreover, in high-potassium calcium-free solution Cebo caused contracture of the uterine smooth muscle. Cebo was still able to elicit contractions in calcium-free solution containing EDTA or EGTA. These findings suggest the existence of cholinergic receptors sensitive to Cebo which could influence the influx of calcium (phasic contraction) and mobilization of calcium from cellular stores (tonic contraction), both of which are responsible for the increase of contractile activity and development of the contracture of uterine smooth muscle.     

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.     

Antispasmodic,bronchodilator and blood pressure lowering properties of Hypericum oblongifolium – possible mechanism of action

The crude extract of Hypericum oblongifolium (Ho.Cr), which tested positive for flavonoids, saponins and tannins caused concentration‐dependent (0.1–1.0 mg/mL) relaxation of spontaneous and high K⁺ (80 mM)‐induced contractions in isolated rabbit jejunum preparations, suggesting a Ca⁺⁺ antagonistic effect, which was confirmed when pretreatment of the tissue with Ho.Cr produced a rightward shift in the Ca⁺⁺ concentration‐response curves, like that caused by verapamil. Ho.Cr relaxed carbachol (1 μM) and high K⁺‐induced contractions in guinea pig tracheal preparations. It caused a dose‐dependent (3–100 mg/kg) fall in arterial blood pressure of rats under anesthesia. In isolated guinea pig atria, Ho.Cr caused inhibition of both atrial force and rate of spontaneous contractions. When tested in rabbit aortic rings, Ho.Cr exhibited a vasodilator effect against phenylephrine (1 μM) and high K⁺‐induced contractions. These results indicate that Ho.Cr possesses gastrointestinal, respiratory and cardiovascular inhibitory effects, mediated via a Ca⁺⁺ antagonist mechanism. Copyright © 2009 John Wiley & Sons, Ltd.     

The antianaphylactic effects of Crinum glaucum aqueous extract

The aqueous extract of Crinum glaucum was evaluated for its effects on antigen and histamine induced contraction of the ileum and on mediator release from the lungs of sensitized guinea pigs. The results show that the extract dose dependently inhibited the contractions induced by antigen and histamine in vitro and in vivo. The extract also inhibited, in a dose-dependent manner, the quantity of mediators antigenically released from the lungs and reduced the mepyramine resistant activity from the lungs. The results obtained indicate that the extract possesses antianaphylactic properties, which may account for its use as an antiasthmatic in traditional medicine.     

Relaxant effects of the essential oil of Ocimum gratissimum on isolated ileum of the guinea pig

The effects of the essential oil of Ocimum gratissimum L. (Labiatae) (EOOG) on guinea pig ileum were studied. EOOG (0.1-1000 microg/ml) reversibly and concentration-dependently relaxed the basal tone of the ileum and reversed the tonic contractions induced by 60 mM KCl and 10 microM acetylcholine, with IC(50) values of 23.8+/-5.2, 18.6+/-4.0 and 70.0+/-4.6 microg/ml, respectively. Our results show that EOOG exerts relaxant effects on intestinal smooth muscle, consistent with the popular use of the plant to treat gastrointestinal disorders.     

Phytochemical screening and effect of aqueous extract of Ficus sycomorus L. (Moraceae) stembark on muscular activity in laboratory animals

The stembark of Ficus sycomorus was collected, dried and extracted, to screen for some chemical constituents and study its effect on muscle contraction. The duodena and recti abdominis of 10 guinea pigs weighing between 330 and 345 g and 10 frogs weighing between 180 and 201 g, respectively, were isolated and used for this study. The extract was tested to see its effect on acetylcholine (ACH) induced contraction on kymograph. The extract reduced the acetylcholine contractile responses of guinea pigs duodena and recti abdominis muscles of frogs significantly, thus showing inhibitory effect on muscle contraction. The extract showed the presence of gallic tannins, saponins, reducing sugars, alkaloids and flavone aglycones. It was concluded that the extract has inhibitory effect on both smooth and skeletal muscles contractions and contains important constituents for pharmacological activities.     

Studies on Prokinetic,Laxative and Spasmodic Activities of Phyllanthus emblica in Experimental Animals

This study was aimed to provide pharmacological basis for the medicinal use of Phyllanthus emblica fruit in indigestion and constipation using the in‐vivo and in‐vitro assays. The crude extract of the dried fruits of Phyllanthus emblica (Pe.Cr) and its fractions were tested positive for alkaloids, saponins, tannins, terpenes, flavonoids, sterols and coumarins. Pe.Cr at the doses of 100 and 300 mg/kg exhibited the prokinetic and laxative activities in mice, which were found partially sensitive to atropine. In isolated guinea‐pig ileum and rabbit jejunum, the crude extract and its aqueous fraction (Pe.Aq) caused concentration‐dependent and partially atropine‐sensitive stimulatory effects followed by relaxation at higher tested concentrations, being more efficacious in guinea pig, while more potent in rabbit tissues. The petroleum fraction (0.003–0.1 mg/mL) exhibited fully atropine‐sensitive contractions in both guinea‐pig and rabbit tissues. However, the ethyl acetate and chloroform fractions (0.003–1.0 mg/mL) showed only spasmolytic activity when studied in spontaneously contracting rabbit jejunum. This study showed that the Phyllanthus emblica possesses prokinetic and laxative activities in mice along with spasmodic effect in the isolated tissues of guinea pig and rabbit, mediated partially through activation of muscarinic receptors; thus, this study provides a rationale for the medicinal use of Phyllanthus emblica fruits in indigestion and constipation. Copyright © 2012 John Wiley & Sons, Ltd.     

Antispasmodic property of the aqueous extract of Aristolochia albida Duch

The antispasmodic property of the underground parts of Aristolochia albida Duch (family: Aristolochiaceae) was evaluated. The evidence was provided by the aqueous extract of the plant's rhizome which exhibited significant relaxation of the spontaneous pendular contraction of isolated rabbit duodenum. The extract at moderate doses abolished acetylcholine (Ach), histamine and 5-hydroxytryptamine (5-HT) induced contractions on isolated rabbit duodenum and guinea-pig ileum. The effects of the extract mimicked antagonists (atropine, mepyramine and methysergide). Therefore, the extract evoked its antispasmodic actions by antagonism via muscarinic, histaminic and 5-HT receptors. © 1997 John Wiley & Sons, Ltd.     

Pharmacological Evaluation of Gut Modulatory and Bronchodilator Activities of Achyranthes aspera Linn.

Achyranthes aspera L. is traditionally used to relieve constipation, diarrhea, and asthma. Its crude extract (Aa.Cr) was evaluated through in vivo and ex vivo experiments to rationalize these medicinal uses of A. aspera and to provide their scientific basis. Aa.Cr, at 3 and 10 mg/kg, increased fecal output, similar to castor oil, whereas at 30, 100, 300, and 700 mg/kg, it protected against castor oil‐induced diarrhea in mice when administered orally. Aa.Cr caused spasmogenic effect on rabbit jejunum and guinea pig ileum preparations, which was partially inhibited by atropine while completely blocked by cyproheptadine preincubation. Aa.Cr also relaxed high K⁺ (80 mM)‐induced contraction in rabbit jejunum. Aa.Cr inhibited CCh (100 μg/kg)‐induced bronchospasm in rats, similar to aminophylline. Like dicyclomine, Aa.Cr relaxed high K⁺ and CCh (1 μM)‐induced contractions in guinea pig trachea and caused rightwards parallel shift of CCh concentration–response curves at the lower concentrations followed by non‐parallel shift at the higher concentrations. On activity‐directed fractionation, spasmogenic and spasmolytic activities of Aa.Cr were concentrated in aqueous and organic fraction, respectively. This study suggests the presence of dose‐specific laxative and antidiarrheal effects in A. aspera, possibly mediated through cyproheptadine‐sensitive receptors and dual cholinergic and calcium channel blockade, respectively. The latter combination is also a suggested mechanism underlying its bronchodilator effect. Copyright © 2017 John Wiley & Sons, Ltd.