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.     

海红豆化学成分研究

目的：研究海红豆的化学成分。方法：应用各种色谱技术分离纯化,通过理化性质和波谱学方法鉴定化合物的结构。结果：从95%乙醇提取物中分离得到9个化合物,分别鉴定为aridanin(1),3-［(2-acetamido-2-deoxy-β-D-glucopyranosyl)oxy］-16α-hydroxyolean-12-en-28-oic acid(2),(+)-pinitol(3),蔗糖(4),(-)-butin(5),芹菜素(6),异甘草素-4-甲基醚(7),齐墩果酸(8),胡萝卜苷(9)。结论：化合物1～7为首次从该植物中获得。     

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.     

Intestinal myorelaxant and antispasmodic effects of the essential oil of Croton nepetaefolius and its constituents cineole,methyl-eugenol and terpineol

The effects of the essential oil of Croton nepetaefolius (EOCN), a medicinal plant from the north-east of Brazil, and its constituents cineole, methyl-eugenol and terpineol, were studied on intestinal motility in vivo and on in vitro mechanical activity of intestinal smooth muscle. In mice, EOCN (10–100 mg/kg body weight, intragastrically) increased the intestinal transit of charcoal marker delivered to the stomach. This was also observed in animals pretreated with castor oil. In segments of guinea-pig ileum and cardial, pyloral and ileo-caecal sphincters, EOCN preferentially decreased basal tonus compared with the amplitude of spontaneous contractions with EC₅₀ values in the range 0.9 – 16 and 8 – 150 μg/mL respectively. In ileum, EOCN, cineole, methyl-eugenol and terpineol decreased tonus with EC₅₀ values of 16, 322, 9 and 71 μg/mL, respectively, and blocked 60 mM [K⁺]-induced contraction with IC₅₀ values of 18, 419, 12 and 95 μg/mL. The data show that EOCN possesses myorelaxant and antispasmodic properties in vitro, consistent with the use of Croton nepetaefolius in folk medicine as an intestinal antispasmodic. EOCN-induced stimulation of intestinal transit in vivo appears consistent with its in vitro effects, since a preferential decrease in tonus may reduce luminal resistance to bulk flow of intestinal contents. © 1998 John Wiley & Sons, Ltd.     

复方川贝颗粒含药血清对豚鼠离体气管平滑肌收缩功能影响随机平行对照研究

[目的]观察复方川贝颗粒含药血清对豚鼠离体气管平滑肌收缩功能影响。[方法]使用随机平行对照方法,将清洁级豚鼠12只按随机数字表法随机分为6组,用于制作含药血清：模型组,复方川贝颗粒低、中、高剂量组,二陈丸组,氨茶碱组,2只/组,雌雄各半。其余10只准备取气管制作气管螺旋条的豚鼠,根据抽签结果决定先后顺序。制作新鲜的豚鼠离体气管螺旋条,将其放入克氏液中,使用磷酸组胺（His）引发豚鼠气管螺旋条收缩。观测加入复方川贝颗粒含药血清后1,3,5min的解痉百分率。[结果]复方川贝颗粒含药血清中剂量组解痉率与模型组比较均有明显上升（P〈0.05）,复方川贝颗粒含药血清对His引起的气管平滑肌收缩反应具有拮抗作用,药物与标本接触5min后作用较好。[结论]复方川贝颗粒含药血清对His引起的气管平滑肌收缩反应具有一定拮抗作用。     

小黄皮茎的化学成分及生物活性研究

目的研究小黄皮Clausenaemarginata茎的化学成分及其保肝活性。方法采用硅藻土、硅胶等多种柱色谱、中压制备液相色谱(MPLC)及制备型HPLC等方法对小黄皮茎的化学成分进行分离纯化,根据化合物理化性质结合现代波谱学方法鉴定化合物结构;并测试其对DL-半乳糖胺诱导肝细胞损伤的保护活性及其对脂多糖(LPS)诱导小鼠小胶质BV2细胞产生一氧化氮(NO)的抑制活性。结果从小黄皮茎的95%乙醇提取物的氯仿部位分离得到11个化合物,分别鉴定为nordentatin(1)、oxanordentatin(2)、5′-羟基葡萄内酯(3)、7-[(E)-7′-羟基-3′,7′-二甲基-2′,5′-二烯]-香豆素(4)、7-羟基香豆素(5)、claulamine A(6)、γ-崖椒碱(7)、开环异落叶松脂素(8)、2-{4-[(1E)-3-hydroxyprop-1-en-1-yl]-2,6-dimethoxyphenoxy}propane-1,3-diol(9)、2-[4-(3-hydroxy-1-propenyl)-2-methoxyphenoxy]-1,3-propanediol(10)、甲基-2-O-β-D-吡喃葡萄糖基苯甲酸(11)。其中,化合物1~5为香豆素类化合物,6为咔唑生物碱,7为呋喃喹啉类生物碱,8为木脂素类化合物,9、10为苯丙素类化合物,11为酚酸类化合物。结论化合物2~4、7~11为首次从该植物中分离得到,化合物5和7对DL-半乳糖胺诱导的肝细胞损伤具有一定的保护活性,化合物11对LPS诱导BV2细胞产生NO具有一定的抑制作用。     

罗汉果皂苷Ⅴ的镇咳、祛痰及解痉作用研究

 目的筛选罗汉果镇咳祛痰的有效部位,并进一步研究罗汉果皂苷Ⅴ的镇咳、祛痰及解痉作用。方法通过观察罗汉果水提部位、体积分数95%醇提部位及体积分数50%醇提部位对浓氨水致小鼠咳嗽次数及咳嗽潜伏期的影响,筛选出罗汉果镇咳的有效部位为体积分数50%醇提部分。进一步观察了50%醇提部分中的罗汉果皂苷Ⅴ对小鼠酚红排泄量及组胺致豚鼠离体回肠及离体气管痉挛的影响。结果罗汉果水煎剂50g生药·kg^-1,罗汉果体积分数50%醇提部位50g生药·kg^-1及罗汉果皂苷Ⅴ300,150,75mg·kg^-1能明显减少小鼠的咳嗽次数,罗汉果体积分数50%醇提部位50g生药·kg^-1及罗汉果皂苷Ⅴ300mg·kg^-1还能明显延长小鼠咳嗽潜伏期;罗汉果皂苷Ⅴ150mg·kg-1能明显增加小鼠气管酚红排泄量,提示有一定的祛痰作用;5g·L-1的罗汉果皂苷Ⅴ能明显拮抗组胺引起的回肠收缩;2.5及1.25g·L^-1剂量对组胺引起的气管痉挛有明显的拮抗作用。结论罗汉果皂苷Ⅴ显示出一定的镇咳、祛痰、解痉活性,推测为罗汉果镇咳的主要活性成分。     

Presence of cholinergic and calcium antagonist constituents in Saussurea lappa explains its use in constipation and spasm

This study was carried out to provide a scientific basis for the traditional use of Saussurea lappa, in constipation and spasms. Isolated tissue preparations were used to see if the aqueous-methanol crude extract of the S. lappa root (Sl.Cr) contains gut stimulatory and inhibitory constituents. In isolated guinea-pig ileum, a quiescent preparation, Sl.Cr caused a concentration-dependent (0.3-5.0 mg/mL) spasmogenic effect, with the maximum effect reaching 91% of the acetylcholine maximum. A further increase in concentration caused a declining effect, indicating the presence of spasmolytic constituent(s). The spasmolytic effect was more marked in the spontaneously contracting rabbit jejunum and in the atropinized preparations. The spasmolytic effect was mediated through calcium channel blocking (CCB) activity, as evident by its inhibitory effect against high K(+) (80 mm)-induced contraction and displacement of the Ca(++) concentration-response curves to the right. These data indicate that the crude extract of Sl.Cr contains gut stimulatory constituent(s) of cholinergic-type providing a scientific basis for its use in constipation. The presence of spasmolytic constituents of CCB-type more evident in the spontaneous contracting gut preparation may explain its use in spasms.     

Flavonol glycosides from Aristeguietia discolor reduce morphine withdrawal in vitro

The effects of extracts, partially purified fractions and four flavonol glycosides 1-4 from Aristeguietia discolor were investigated on the naloxone-precipitated withdrawal contraction of the acute morphine dependent guinea-pig ileum in vitro. After a 4 min in vitro exposure to morphine a strong contraction of guinea-pig isolated ileum was observed after the addition of naloxone. Both MeOH extract (50, 100 and 200 mg/mL), the partially purified fractions I, L, M and N (50, 100 and 200 mg/mL) and flavonol glycosides 1-4 (1 x 10(-4) 5 x 10(-5) 1 x 10(-5) M), injected 10 min before morphine, were capable of blocking the naloxone-induced contraction after exposure to morphine in a concentration-dependent fashion. The results of the present paper suggest that flavonol glycosides from Aristeguietia discolor may play an important role in the control of morphine withdrawal.     

细柱五加皮化学成分的研究

目的 系统地研究五加属植物细柱五加皮Acanthopanax gracilistylus的化学成分。方法 用热甲醇分别对细柱五加皮的根进行提取后，采用Diaion HP-20P，Chromatorex ODS，Sephadex LH-20和硅胶色谱进行分离纯化，通过光谱分析以及直接和标准品对照进行结构确认。结果 从根皮中得到二萜类等6个化合物：五加酸(Ⅰ)，异贝壳杉烯酸(Ⅱ)，l芝麻素(Ⅲ)，豆甾醇(Ⅳ)，β-谷甾醇(Ⅴ)和刺五加苷B(Ⅵ)。结论 化合物Ⅰ，Ⅳ，Ⅴ为首次从该植物中分离得到。     

Effects of Crocus sativus petals' extract on rat blood pressure and on responses induced by electrical field stimulation in the rat isolated vas deferens and guinea-pig ileum

We have investigated the effects of Crocus sativus petals' extract on blood pressure in anaesthetised rats and also on responses of the isolated rat vas deferens and guinea-pig ileum induced by electrical field stimulation (EFS). Aqueous and ethanol extracts of C. sativus petals reduced the blood pressure in a dose-dependent manner. For example administration of 50 mg/100 g of aqueous extract changed the blood pressure from 133.5+/-3.9 to 117+/-2.1 (mmHg). EFS of the isolated rat vas deferens and guinea-pig ileum evoked contractions were decreased by aqueous and ethanol extracts of C. sativus petals. The aqueous extract (560 mg/ml) significantly reduced the contractile responses of vas deferens to epinephrine (1 microM) without any change in contraction induced by KCl (300 mM). The present results may suggest that the relaxatory action of C. sativus petals' extract on contraction induced by EFS in the rat isolated vas deferens is a postsynaptic effect.     

Pharmacological analysis of paregoric elixir and its constituents: in vitro and in vivo studies

Paregoric elixir is a phytomedicinal product which is used widely as an analgesic, antispasmodic and antidiarrheal agent. Here, we investigated the pharmacological actions and some of the mechanisms of action of paregoric elixir and compared its action with some of its components, the alkaloids morphine and papaverine. The paregoric elixir given orally to mice did not present relevant toxic effects, even when administered in doses up to 2000-fold higher than those used clinically. However, it showed an antinociceptive action that was more potent, but less efficacious, than morphine. In contrast to morphine, its effect was not dose-dependent and not reversed by the non-selective opioid antagonist naloxone. Moreover, paregoric elixir produced tolerance, but did not cause cross-tolerance, with the antinociceptive actions of morphine. When assessed in the gastrointestinal motility in vivo, paregoric elixir elicited graduated reduction of gastrointestinal transit. Finally, like morphine and papaverine, paregoric elixir concentration-dependently inhibited electrically-induced contraction of the guinea pig isolated ileum. In vivo and in vitro gastrointestinal actions of paregoric elixir were not reversed by naloxone. Collectively, the present findings lead us to suggest that the pharmacological actions produced by paregoric elixir are probably due to a synergic action of its constituents.     

Mode of action of peppermint oil and (-)-menthol with respect to 5-HT3 receptor subtypes: binding studies, cation uptake by receptor channels and contraction of isolated rat ileum

Peppermint oil (Mentha × piperita L. (Lamiaceae) has been shown to exert potent antiemetic properties, but its mode of action has not yet been elucidated. Among its active constituents (-)-menthol is the most important. Three different in vitro models were used to investigate the effects on 5-HT(3) receptors (serotonin receptor subtype): [(14)C]guanidinium influx into N1E-115 cells which express 5-HT(3) receptors, isotonic contractions of the isolated rat ileum and equilibrium competition binding studies using a radioactively labelled 5-HT(3) receptor antagonist ([(3)H]GR65630) (3-(5-methyl-1H-imidazol-4-yl)-1-(1-methyl-1H-indol-3-yl)-1-propanone). Both peppermint oil and (-)-menthol inhibited [(14)C]guanidinium influx through 5-HT(3) receptor channels as well as contractions of the ileum induced by serotonin. Neither the peppermint oil nor (-)-menthol, however, was able to displace [(3)H]GR65630 from 5-HT(3) binding sites. It may be concluded that peppermint oil and (-)-menthol exert their antiemetic effect at least partly by acting on the 5-HT(3) receptor ion-channel complex, probably by binding to a modulatory site distinct from the serotonin binding site.     

生姜抗运动病药理作用研究

干姜乙醇提取液(简称姜液)静脉注射,可使家兔皮层脑电图由低幅快波变为高幅慢波;使家兔在体胃运动幅度短暂抑制。姜液对离体大鼠胃底条运动幅度有先兴奋后抑制作用,且抑制胃底条运动频率。姜液致离体豚鼠回肠的收缩效应有快速耐受性,该收缩效应不受六烃季铵、5-羟色胺(5-HT)预处理影响,但可被冷冻、东茛菪碱、吗啡、苯海拉明、异丙嗪及P物质脱敏预处理所抑制。纳络酮可消除吗啡的作用。姜液对离体豚鼠回肠Ach、组胺性量效关系呈现非竞争性拮抗。提示生姜通过P物质介导兴奋M、H_1受体,并对MH_1受体有先兴奋后抑制作用;生姜通过中枢及外周抗胆碱和抗组胺效应而发挥抗运动病作。     

Bullatacin, bullatacinone, and squamone, a new bioactive acetogenin, from the bark of Annona squamosa

Activity-directed fractionation of the stem bark of Annona squamosa, monitoring with brine shrimp lethality, led to the isolation of the highly bioactive acetogenins bullatacin [1] and bullatacinone [2], thus demonstrating a new abundant plant source for these potent compounds. A new keto-monotetrahydrofuran acetogenin with a ketolactone terminus, as first seen in bullatacinone [2], was also isolated, characterized by spectral analyses, and named squamone [3]. The cytotoxicities of 3 were increased significantly by reduction of the two keto groups to hydroxyls, and the tetrahydrosquamone [7] and bullatacinone [2] both showed selective cytotoxicities to MCF-7 human breast carcinoma. Liriodenine and (-)-kaur-16-en-19-oic acid were also isolated.     

刺五加的化学成分研究

目的研究五加科五加属植物刺五加Acanthopanax senticosus的化学成分。方法利用各种色谱技术进行分离,根据光谱数据鉴定结构。结果从刺五加中分离得到12个已知成分,分别鉴定为刺五加酮(1)、刺五加苷B1(2)、4-羟基-2-甲氧基苯基-1-O-β-D-葡萄糖苷(3)、alimoxide(4)、赤式-1-(4-羟基-3-甲氧基苯基)-2-{4-[(E)-3-羟基-1-丙烯基]-2-甲氧基苯氧基}-1,3-丙二醇(5)、erythro-1,2-bis(4-hydroxy-3-methoxyphenyl)-1,3-propanediol(6)、tortoside A(7)、表丁香脂素4′-O-β-D-葡萄糖苷(8)、(+)-lyoniresinol(9)、苯甲基-O-α-L-鼠李吡喃糖基(1→6)-β-D-葡萄吡喃糖苷(10)、2,6-二甲氧基-4-(3-羟基丙烯基)苯基-1-O-α-L-鼠李吡喃糖基-(1→6)-β-D-葡萄吡喃糖苷(11)、β-氨甲酰基吡啶(12)。结论化合物3～5、10～12为首次从该植物中分离得到。     

Antispasmodic and hypotensive effects of Ferula asafoetida gum extract

The effects of Ferula asafoetida gum extract on the contractile responses of the isolated guinea-pig ileum induced by acetylcholine, histamine and KCl, and on the mean arterial blood pressure of rat were investigated. In the presence of extract (3 mg/ml), the average amplitude of spontaneous contractions of the isolated guinea-pig ileum was decreased to 54 +/- 7% of control. Exposure of the precontracted ileum by acetylcholine (10 microM) to Ferula asafoetida gum extract caused relaxation in a concentration-dependent manner. Similar relaxatory effect of the extract was observed on the precontracted ileum by histamine (10 microM) and KCl (28 mM). However, when the preparations were preincubated with indomethacin (100 nM) and different antagonists, such as propranolol (1 microM), atropine (100 nM), chlorpheniramine (25 nM) then were contracted with KCl, exposure to the extract (3 mg/ml) did not cause any relaxation. Furthermore, Ferula asafoetida gum extract (0.3-2.2 mg/100g body weight) significantly reduced the mean arterial blood pressure in anaesthetised rats. It might be concluded that the relaxant compounds in Ferula asafoetida gum extract interfere with a variety of muscarinic, adrenergic and histaminic receptor activities or with the mobilisation of calcium ions required for smooth muscle contraction non-specificly.     

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.     

滑桃树茎皮的化学成分研究

目的：研究滑桃树茎皮的化学成分。方法：利用硅胶、凝胶柱色谱法进行分离纯化，波谱法进行结构鉴定。结果：从滑桃树茎皮乙醇提取物的醋酸乙酯部分分离得到10个化合物，分别鉴定为：豆甾-4-烯-6α-醇-3-酮(1)，豆甾-4-烯-6β-醇-3-酮(2)，7β-羟基谷甾醇(3)，7α-羟基谷甾醇(4)，schleicheol 2(5)，蒲公英赛酮(6)，abbeokutone(7)，β-hydroxypropiovanillone(8)，邻香兰醇(9)，单棕榈酸甘油酯(10)。结论：化合物1～5，7～9为首次从该植物中分离得到。     

南蛇藤茎的化学成分(英文)

目的:研究南蛇藤Celastrus orbiculatus Thunb.茎的化学成分。方法:采用硅胶、Sephadex LH-20和ODS柱色谱方法进行化合物的分离和纯化。根据理化性质和光谱数据鉴定化合物结构。结果:从南蛇藤茎的乙酸乙酯部位分离得到11个化合物,经鉴定分别为:3β-hydroxy-2-oxoolean-12-ene-22,29-lactone(1),2,6-二甲氧基苯醌(2),3-氧代齐墩果酸(3),24-去甲基齐墩果烷-12-烯-28-酸-3-酮(4),白头翁酸(5),香草酸(6),23-羟基齐墩果烷-12-烯-28-酸-3-酮(7),丁香酸(8),齐墩果酸(9),β-谷甾醇(10),β-胡萝卜苷(11)。结论:化合物1为新三萜化合物,化合物2-5和7为首次从该属植物中分离得到,化合物8和9为首次从该植物中分离得到。