蜂斗菜不同提取物对豚鼠离体回肠收缩的影响

目的 比较蜂斗菜不同提取物对豚鼠离体回肠收缩的影响。方法 采用豚鼠离体回肠实验,以组胺、乙酰胆碱不同激动剂为研究模型,比较蜂斗菜CO₂超临界提取物、80%乙醇提取物、80%乙醇提取物的不同极性提取物及乙酸乙酯提取物经硅胶柱层析分离获得的不同馏分对豚鼠离体回肠的收缩作用,计算各个提取物对豚鼠回肠收缩幅度的抑制率。结果 蜂斗菜不同提取物对组胺、乙酰胆碱所致的豚鼠离体回肠收缩有显著拮抗作用,其中乙酸乙酯提取物硅胶柱色谱的馏分抑制作用最强。结论 蜂斗菜不同提取物均能抑制组胺、乙酰胆碱引起的豚鼠离体回肠收缩作用,脂溶性成分抑制作用最强,其机制可能与M、H₁受体的抑制有关。     

Evaluation of Antiasthmatic Activity of Curculigo orchioides Gaertn. Rhizomes

The ethanol extract of Curculigo orchioides was evaluated for antiasthmatic activity by using various in vitro and in vivo animal models. In vitro models like isolated goat tracheal chain preparation and isolated guinea pig ileum preparation were studied to know basic mechanism by which extract shows relaxant activity. The study showed that extract is effective against histamine-induced contraction. In isolated goat tracheal chain preparation and isolated guinea pig ileum preparation extract exhibits maximum relaxant effect (p< 0.01) against histamine at concentrations 100μg/ml and 25μg/ml respectively. Animal studies involved use of histamine induced bronchoconstriction in guinea pigs, egg albumin induced passive paw anaphylaxis in rats and haloperidol-induced catalepsy in mice. These studies showed significant (p< 0.01) protection at lower doses while further increase in the dose level showed reduced activity. Biochemical estimations in milk-induced total leukocytes count and milk-induced differential leukocyte count were also studied. In this study there was maximum increase in leucocytes and lymphocytes (99%) and maximum decrease in eosinophils up to 0% at dose 375mg/kg p.o. body weight was observed. The results of these studies indicated usefulness of ethanol extract of Curculigo orchioides in asthma.     

Pharmacological Activities of Gutenburgia cordifolia

A methanol extract of Gutenburgia cordifolia showed a greater fall in diastolic than systolic blood pressure in anaesthetised rats. The plant extract produced cardiodepressant activity on isolated rabbit heart and caused contraction on isolated rabbit ileum. The contraction was reduced but not abolished with atropine. On isolated guinea pig ileum, the contraction was abolished by atropine, the presence of an acetylcholine-like compound in the plant extract is indicated.     

Pharmacology of ASL-8052, a novel beta-adrenergic receptor antagonist with an ultrashort duration of action

ASL-8052, a novel beta-adrenergic receptor antagonist, was studied in isolated guinea pig cardiac and tracheal tissues, in isolated frog sciatic nerves, and in anesthetized dogs. The compound was a moderately potent beta-adrenoceptor antagonist in right atria (pA2 6.96) but was much less active in tracheal tissues (pA2 5.33), indicating cardioselective properties. ASL-8052 possessed a small degree of intrinsic sympathomimetic action in isolated guinea pig right atria and caused direct cardiac depression only at concentrations 1,000-fold higher than its cardiac pA2. Significant local anesthetic action in frog sciatic nerve occurred at extremely high concentrations of ASL-8052 (greater than 0.1 M). In anesthetized dogs, ASL-8052 produced steady-state levels of beta-blockade within 10 min during a 3-h intravenous infusion. In contrast, propranolol produced increasing levels of blockade throughout most of the infusion period. Recovery from beta-blockade occurred rapidly following termination of ASL-8052 infusion (80% recovery in approximately 12 min), whereas very little recovery occurred following cessation of propranolol infusion. Intravenous infusion of ASL-8052 produced dose-dependent blockade of cardiac responses to isoproterenol but only minimally decreased hindlimb vascular responses to isoproterenol. The results indicate that ASL-8052 is a novel cardioselective beta-blocker with an ultrashort duration of action.     

Pharmacological activities of Lantana trifolia on isolated guinea pig trachea and rat phrenic nerve diaphragm

A methanol extract of L. trifolia produced bronchodilation of isolated guinea pig trachea comparable to that of salbutamol. The plant extract reduced bronchoconstriction induced by histamine, 5-HT and acetylcholine on isolated guinea pig trachea. Physostigmine failed to inhibit neuromuscular blocking activity of the extract on rat phrenic nerve diaphragm.     

Pharmacological action of cattle prostate extracts (PE). V. Effect on the bladder]

As the extract of cattle prostate (PE) is clinically effective in treating prostatic hypertrophy, a study was carried out on urinary bladders of rat, guinea pig, rabbit and dog as well as on guinea pig ileum. Muscle strip of rat and/or dog bladder contracted with PE with increasing spontaneous movement, and was unaffected by atropine. The isolated ileum of guinea pig also contracted with PE, and the contraction was inhibited by papaverine, but not by atropine. A rise in intravesical pressure was observed with increasing spontaneous movement in guinea pig bladder treated with PE, as well as in rabbit bladder in vitro or in situ. The sphincter vesica of guinea pig was dilated by PE as well as by ACh and methacholine.     

Pharmacological Activities of Vernonia glabra

A 70% methanol aerial part extract of Vernonia glabra caused a fall in blood pressure in anaesthetised rats. After the 50 µg dose, systolic, diastolic, and mean blood pressures decreased by 56%, 66%, and 61% respectively below the baseline levels. The adrenaline-like activity of the extract was not antagonised by L(-) propranolol on isolated rabbit heart. The extract caused contraction on the isolated rabbit ileum and was abolished with atropine, suggesting the presence of a compound with acetylcholine-like activity. The extract on isolated guinea pig ileum caused contraction which was dose related.     

Isolation of Amentoflavone from Selaginella rupestris and its Pharmacological Activity on Central Nervous System, Smooth Muscles and Isolated Frog Heart Preparations.

Amentoflavone has been isolated from the leaves of SELAGINELLA RUPESTRIS S PRING (Selaginellacae). This biflavonoid was tested for its activity on central nervous system, smooth muscles and isolated frog heart preparations. It was observed that amentoflavone did not have any effect on central nervous system of rats and mice, but it had antispasmodic effect on isolated guinea pig ileum. Amentoflavone had also increased significantly the contractility of both nor-modynamic and hypodynamic frog hearts.     

戒毒康对吗啡依赖豚鼠离体回肠戒断性收缩的影响

目的研究戒毒康对吗啡依赖豚鼠离体回肠催促戒断反应的抑制作用。方法连续递增皮下注射吗啡,建立豚鼠身体依赖性模型,利用MD2000 Super Lab生物信息采集系统观察戒毒康对纳洛酮催促诱发吗啡身体依赖性豚鼠离体回肠的戒断性收缩的抑制作用。结果戒毒康高（0.6 mg.mL-1）、中（0.3 mg.mL-1）、低（0.15 mg.mL-1）3个剂量对吗啡依赖豚鼠离体回肠纳洛酮催促戒断性收缩的抑制率分别为：78.8%,46.8%,30.0%,并呈剂量相关性,其中高剂量组和中剂量组与模型组比较,有显著性差异。结论戒毒康在一定程度上能抑制吗啡依赖豚鼠离体回肠体外纳洛酮催促戒断性收缩。     

Pharmacological activity of alkaloids from poison-dart frogs (Dendrobatidae)

Batrachotoxin, pumiliotoxin B, isodihydrohistrionicotoxin, pumiliotoxin C and gephyrotoxin represent five different classes of skin alkaloids from the dendrobatid poison dart frogs. In quinea pig ileum segments batrachotoxin and pumiliotoxin B caused rhythmic contractures which were prevented by tetrodotoxin. In quinea pig atria, batrachotoxin and pumiliotoxin B had positive inotropic and chronotropic effects, followed in the case of batrachotoxin by irregular arrhythmias and atrial arrest. Isodihydrohistrionicotoxin has no apparent effect in ileum or atrium, while gephyrotoxin was a potent muscarinic antagonist. In rat phrenic nerve-diaphragm, batrachotoxin blocked both direct and indirect-elicited twitch; pumiliotoxin B potentiated both direct and indirect-elicited twitch, isodihydrohistrionicotoxin blocked indirect-elicited twitch and gephyrotoxin had no apparent effect. Pumiliotoxin C had no apparent effect in any of the preparations.     

The presynaptic activity of huwentoxin-I, a neurotoxin from the venom of the chinese bird spider Selenocosmia huwena.

Three different types of isolated nerve-synapse preparations, guinea pig ileum, rat vas deferens and toad heart, were used to investigate the physiological activity of Huwentoxin-I, a neurotoxin from the venom of the spider Selenocosmia huwena. The twitch response of isolated guinea pig ileum induced by electrical stimulus can be inhibited by HWTX-I. After blockage, contraction of the ileum can be induced by exogenously applied acetylcholine. HWTX-I caused the inhibition of the twitch response to electrical nerve stimulation in the rat vas deferens. After the twitch was completely inhibited, noradrenaline triggered rhythmic contraction of the vas deferens. The inhibitory effect on heart of toad induced by stimulating sympathetic-vagus nerve can be reversed by HWTX-I, although exogenously applied acetylcholine still acts as an effective inhibitor. All of these results support the conclusion that HWTX-I has the presynaptic activity that effects the release of neurotransmitter from the nerve endings of both the cholinergic synapse and the adrenergic synapse.     

A new class of cardiotonic agents: structure-activity correlations for natural and synthetic analogues of the alkaloid A new class of A new class of cardiotonic agents: structure-activity correlations for natural and synthetic analogues of the alkaloid pumiliotoxin B (8-hydroxy-8-methyl-6-alkylidene-1-azabicyclo[4.3.0]nonanes)

Pumiliotoxin B (PTX-B, 6-(6',7'-dihydroxy-2',5'-dimethyl-(E)-4'-octenylidene)-8-hydroxy-8 -methyl-1- azabicyclo-[4.3.0] nonane) increases the force of contractures of spontaneously beating guinea pig atrial strips by 3- to 5-fold with half-maximal effects at about 3 microM and increases rates of atrial contractions by 2- to 3-fold with half-maximal effects at about 6 microM. The presence of an axial 7-hydroxy substituent (PTX 339A) decreases the efficacy but not the potency of PTX-B as a positive inotropic agent while having only slight effects on activity as a positive chronotropic agent. The presence of an equatorial 7-hydroxy substituent (PTX 339B) greatly decreases efficacy and potency of PTX-B as a positive chronotropic and inotropic agent. Pumiliotoxin A which lacks the side-chain 7'-hydroxy group of PTX-B causes only a 2-fold increase in force of contracture at 54 microM while having minimal effects on rate. The presence of an axial 7-hydroxy substituent (PTX 323B' and 323B", epimeric at the 6'-hydroxy) markedly enhances positive inotropic and chronotropic effects of PTX-A. Another congener, PTX 251D with a 6-(2'-methylhexylidene) side chain, and a synthetic analogue with a 6-(6'-heptenylidene) side chain are cardiac depressants. Both lack hydroxyl groups in the side chain. The presence of an omega-1 hydroxy group in the side chain of PTX 251D yields an alkaloid (267C) with weak positive inotropic effects and minimal chronotropic effects. The presence of an axial 7-hydroxy group in the indolizidine ring of PTX 251D results in a compound (PTX 267A) with very weak positive inotropic effects while retaining the negative chronotropic effects of PTX 251D. A synthetic analogue with a 6-(7'-hydroxyheptylidene) side chain is a cardiac depressant even though it contains a side-chain hydroxyl corresponding in position to the 7'-hydroxyl of the side chain of PTX-B. The positive chronotropic and inotropic effects of pumiliotoxin B are reversed only by relatively high concentrations of the calcium channel blockers nifedipine and verapamil, suggesting that pumiliotoxin B may owe its cardiotonic activities to effects on internal mobilization of calcium.     

T-cadinol: a pharmacologically active constituent of scented myrrh: introductory pharmacological characterization and high field 1H- and 13C-NMR data.

Fractionation of an ethyl acetate extract of scented myrrh (resin of Commiphora guidottii Chiov., Burseraceae), using the guinea pig ileum test to monitor pharmacological activity, resulted in isolation of the sesquiterpene (+)-T-cadinol. High field NMR spectroscopy yielded new detailed 1H- and 13C-NMR data for the compound. T-cadinol was shown to have a concentration-dependent smooth muscle relaxing effect on the isolated guinea pig ileum and a dose-dependent inhibitory effect on cholera toxin-induced intestinal hypersecretion in mice.     

A potent factor in extracts of the skin of the Australian frog, Pseudophryne coriacea--III. Potentiation of contractions elicited in avian and mammalian isolated skeletal muscle preparations by direct and indirect electrical stimulation

Extracts of the skin of the Australian frog Pseudophryne coriacea displayed a striking potentiating effect on contractions evoked in isolated skeletal muscle preparations of mammals (phrenic nerve diaphragm) and birds (chick biventer cervicis and semispinalis muscles) by indirect and direct electrical stimulation. There was both a conspicuous increase in the amplitude of the twitch, up to 10-fold, and a remarkable prolongation of the duration of the twitch. The effect was dose- and frequency-dependent. In the presence of the extract, fusion of twitches after tetanic stimulation occurred earlier. No tachyphylaxis upon repeated stimulation by the extract was observed and the response to large doses persisted, declining slowly, for hours. These effects must be ascribed to an alkaloid related in structure to pumiliotoxin B. Response to the extract of Pseudophryne coriacea by indirectly-stimulated preparations was potentiated by physostigmine and blocked by tubocurarine and alpha-bungarotoxin, demonstrating that in these preparations the extract acted pre-synaptically to facilitate the release of acetylcholine from motor nerve endings. However, the extract of Pseudophryne coriacea displayed equally potent effects in directly stimulated preparations, insensitive to physostigmine and to blockers of nicotinic acetylcholine receptors, indicating a direct action on the skeletal muscle. It is suggested that, like pumiliotoxin B, the Pseudophryne coriacea alkaloid may interfere in the regulation of calcium channels in both nerve and muscle fibres.     

Relaxant and antispasmodic effects of extracts of the orchid <Emphasis Type="Italic">Encyclia michuacana</Emphasis> on isolated guinea pig ileum

The antispasmodic effects of hexane-, chloroform-, methanol- and water-extracts of the orchid Encyclia michuacana were studied in vitro on guinea pig ileum against three spasmogens: acetylcholine (Ach), histamine and barium chloride. The chloroform extract exerted a significant antispasmodic effect on ileum contractions induced by Ach, histamine and barium chloride (IC₅₀ = 90.64, 73.12 and 115.2 μg/mL, respectively). Furthermore, the chloroform extract of E. michuacana provoked a concentration-dependent inhibition of spontaneous contractions of guinea pig ileum with potencies comparable to those of papaverine. The antagonism against the spasmogens used suggests that the action of the chloroform extract of E. michuacana could be due mainly to the presence of gigantol. Hexane-, methanol- and water-extracts did not elicit any significant spasmolytic activity.     

Effect of shakuyaku-extract on electrical stimulation induced contraction of guinea pig ileum

It was reported that Paeoniae Radix extracts (S) depressed the contraction induced by electrical stimulation on the isolated guinea pig ileum. In the present study, the mechanisms of the inhibitory action of S on the contraction of guinea pig ileum were investigated. Theophylline and phentolamine are respective antagonists of adenosine and norepinephrine, decreased the inhibitory action by S on the contraction of guinea pig ileum about 50%. Thus these data suggest that some unknown substances with adrenergic and adenosine like actions may be contained in S. Furthermore the possibility of other inhibitors in S was suggested.     

Some pharmacological actions of furazan hydrazides and of 2 correspondent furoxan derivatives]

A study has been made of the acute toxicity, action on the guinea pig ileum, on the ventricle edge, on frog spinal reflex, and on the respiratory and cardiac activity and pulse of the following compounds: 3-methyl-4-furazancarbohydrazide (I); 3-methyl-4-furoxancarbohydrazide (II); 4-methyl-3-furoxancarbohydrazide (III). The compounds had no action on guinea pig ileum or ventricle edge. Compound (I) showed depressant activity on frog spinal reflex whereas compound (II) showed excitation and compound (III) had no direct spinal action. The compounds tested affected respiration and ECG only at the highest doses used. The pulse rate was raised by substance (I) in all cases whereas substances (II) and (III) raised pulse rate only at low doses.     

款冬花不同提取物对豚鼠离体回肠收缩作用的研究

目的研究比较款冬花各个不同提取物对豚鼠离体回肠收缩的作用。方法通过石油醚、乙酸乙酯、CO2超临界萃取等方法制备款冬花多个提取物,将离体豚鼠回肠悬吊于克-亨试液中,观察给药后豚鼠回肠的收缩作用,计算豚鼠回肠收缩幅度抑制率。结果款冬花各个不同提取物均能降低组胺引起的豚鼠离体回肠收缩幅度。结论款冬花各个提取物能明显抑制豚鼠回肠收缩运动。     

Magnolol and honokiol account for the anti-spasmodic effect of Magnolia officinalis in isolated guinea pig ileum

Magnolia officinalis is a commonly used traditional Chinese medicine for treating gastrointestinal disorders. HPLC quantification analysis revealed that magnolol and honokiol were the most abundant constituents of M. officinalis extracts, with their contents in the ethanol extract being the highest, the water extract the least and the 50 % ethanol extract in between. In guinea pig isolated ileum, both magnolol and honokiol inhibited contraction to acetylcholine. The herbal extracts also produced inhibitory responses, in an order of decreasing efficacy: ethanol extract > 50 % ethanol extract > water extract. The differences in inhibitory efficacies among the three extracts were similar to the differences in their magnolol and honokiol contents. Further examination demonstrated that two mixtures containing solely magnolol and honokiol at concentrations identical to those determined in the ethanol and water extracts exhibited similar levels of anti-spasmodic effects as their respective extracts while a "blank" ethanol extract free of magnolol and honokiol failed to produce any response. These observations suggest that the magnolol and honokiol contents account for the anti-spasmodic effects of M. officinalis extracts in guinea pig isolated ileum.     

Pharmacological Activity of Prunus spinosa on Isolated Tissue Preparations.

The pharmacological action of the aqueous extract of PRUNUS SPINOSA L. branches has been studied in tissue preparation IN VITRO. The influence of the extract on rat vas deferens and duodenum was tested using norepinephrine and acetylcholine on spasmogens as well as on guinea pig ileum and taenia coli using histamine and calcium chloride, respectively. The extract reduced responses to norepinephrine, epinephrine and histamine. Responses to cumulative increased Ca (2+) concentrations in depolarizing bathing medium were also blocked. The P. SPINOSA L. extract had effects PER SE on rat vas deferens and guinea pig ileum.