射干抗病毒片与其含药血清对豚鼠离体气管平滑肌作用的比较研究

目的:比较射干抗病毒片原液与其含药血清对豚鼠离体气管平滑肌收缩作用。方法:制备豚鼠离体气管平滑肌螺旋条,加入组胺使其收缩,观察加入射干抗病毒片及其含药血清后5min的解痉百分率。结果:射干抗病毒片及其含药血清均能提高组胺引起的气管平滑肌收缩反应的解痉率,原液效果优于含药血清。结论:射干抗病毒片原液对His引起的气管平滑肌收缩反应的拮抗作用优于含药血清。     

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。     

化橘红提取物对豚鼠离体气管平滑肌收缩功能的影响

目的:研究化橘红提取物对豚鼠离体气管平滑肌收缩功能的影响.方法:以离体豚鼠螺旋条作为实验对象,建立不同浓度化橘红提取物孵育时各致痉剂的量效曲线,观察化橘红提取物对各致痉剂引起收缩的影响.结果:化橘红提取物对豚鼠离体气管平滑肌的静息张力和乙酰胆碱、组胺、氯化钙、氯化钾、氯化钡所致的收缩都有抑制作用,使以上各致痉剂的量效曲线非平行右移,最大效应降低,其强度依次为BaCl2》KCl》CaCl2》His》Ach,并明显抑制乙酰胆碱所致的外钙内流引起的收缩,以上作用均具剂量依赖性.结论:化橘红提取物是以上各激动剂的非竞争性拮抗剂,其作用机制可能与钙通道的阻滞作用有关.     

蝉蜕对豚鼠离体气管环的作用研究

目的：观察蝉蜕对豚鼠离体气管环平滑肌张力的影响,探讨蝉蜕的平喘作用机制。方法：分别以1g/ml、5g/ml、10g/ml三种不同浓度的蝉蜕提取物（CPE）作用于离体豚鼠气管环,观察气管环平滑肌张力的变化;同时观察中剂量蝉蜕提取物对磷酸组胺（His）和乙酰甲胆碱（Ach）诱发豚鼠支气管平滑肌收缩反应的影响。结果：蝉蜕提取物对离体豚鼠气管环的平滑肌张力无改变;对His和Ach引起的豚鼠支气管平滑肌的收缩反应无拮抗作用。结论：蝉蜕的平喘作用机制并非通过直接舒张支气管平滑肌发挥作用,可能是通过神经-体液-免疫系统的整体调节作用实现的。     

辛弗林对豚鼠离体气管平滑肌的作用及机制

目的:探讨辛弗林(synephrineon,Syn)对豚鼠离体气管平滑肌的作用及其机制。方法:采用离体气管恒温灌流的实验方法,取豚鼠气管,在K-H液中制备气管平滑肌环,通过BL-420S生物机能实验系统测定其张力的变化,观察Syn对豚鼠离体气管平滑肌静息张力及对4种致痉剂乙酰胆碱(Ach),组胺(His),Ca Cl2,β受体阻断剂普萘洛尔(Pro)诱导气管平滑肌收缩的影响。结果:Syn可剂量依赖性的舒张气管平滑肌,PD2值为(2.22±0.14);Syn 2个浓度(0.021 2,0.042 4 mmol·L-1)使Ach和His诱发的豚鼠气管平滑肌收缩的最大效应降低,且0.042 4 mmol·L-1的Syn溶液对其均有显著性差异(P<0.05);Syn溶液对Ca Cl2的诱发豚鼠气管平滑收缩效应降低但无显著性差异。Syn 3个浓度(0.010 6,0.021 2,0.042 4 mmol·L-1)对Ach引起的气管平滑肌细胞内钙的释放有显著的抑制作用(P<0.05,P<0.01),且具有剂量依赖关系;加入Pro孵育后,再累积加入Syn,对Ach引起的气管收缩略有降低,与Pro组比较,无显著性差异。结论:Syn可能是通过抑制M受体和组胺受体、兴奋β受体、拮抗内钙的释放从而舒张气管平滑肌。     

柚皮苷对豚鼠离体气管平滑肌作用的机制研究

目的考察柚皮苷对正常及多种致痉剂诱导的豚鼠气管平滑肌收缩功能的影响及其作用机制。方法采用离体气管恒温灌流的方法,取豚鼠气管,在K-H液中制备豚鼠离体气管环,在其静息张力状态下以及用乙酰胆碱(Ach)、组胺(His)、氯化钙(Ca Cl2)、无钙时Ach诱导细胞内钙释放和高钙时诱发细胞外钙内流条件下,通过BL-420S生物机能实验系统测定其张力的变化,考察柚皮苷对离体豚鼠气管平滑肌张力的影响。结果柚皮苷低剂量浓度(0.0172~0.5504)mmol·L-1时,对静息状态下的豚鼠离体气管平滑肌有一定的收缩作用,高剂量浓度(0.5504~1.3780)mmol·L-1时舒张气管平滑肌,且呈剂量依赖性;使致痉剂Ach、His、Ca Cl2收缩豚鼠离体气管平滑肌的量效曲线非平行性右移,最大效应降低;抑制加入高钙后引发细胞外钙内流导致的收缩。结论柚皮苷舒张气管平滑肌作用机制可能与抑制豚鼠气管平滑肌上M受体、H1受体和阻断Ca2+通道从而抑制细胞Ca2+内流有关。     

胡颓子叶对豚鼠离体气管平滑肌收缩功能的影响

目的 研究胡颓子叶乙醇提取物正丁醇部位(胡颓子叶正丁醇部位)对正常及多种致痉剂诱导的豚鼠气管平滑肌收缩功能的影响.方法 制备豚鼠离体气管平滑肌螺旋条,在其正常状态下以及用乙酰胆碱、组胺、氯化钾、无钙下乙酰胆碱诱导细胞内钙释放和高钙下诱发细胞外钙内流条件下,观察胡颓子叶正丁醇部位对离体气管张力的影响.结果 胡颓子叶正丁醇部位对静息状态下的豚鼠离体气管平滑肌有明显的舒张作用,使乙酰胆碱和组胺的量效曲线发生明显右移,抑制加入高钾或高钙后引发细胞外钙内流导致的收缩.结论 胡颓子叶正丁醇部位能明显抑制正常状态及多种致痉剂诱发的豚鼠气管平滑肌收缩.     

思茅松松塔提取物对不同条件下豚鼠离体气管条张力的影响

目的研究思茅松松塔不同溶剂提取物对不同条件下豚鼠离体气管条张力的影响。方法制作豚鼠离体气管条,观察思茅松松塔不同溶剂提取物分别对静息、组胺(His)致痉和乙酰胆碱(Ach)致痉的豚鼠离体气管条张力变化率的影响。结果在静息、组胺(His)和乙酰胆碱(Ach)致痉条件下,与给药前比较,思茅松松塔乙醇提取物组、石油醚提取物组、氯仿提取物组和乙酸乙酯提取物组的给药后张力明显降低;与吐温-20组比较,思茅松松塔提取物组、石油醚提取物组、氯仿提取物组和乙酸乙酯提取物组的张力变化率明显增大。结论思茅松松塔乙醇提取物、石油醚提取物、氯仿提取物和乙酸乙酯提取物对不同条件下豚鼠离体气管条均有舒张作用。     

野马追对豚鼠离体气管平滑肌收缩功能的影响

目的 :研究野马追对豚鼠离体气管平滑肌收缩功能的影响。方法 :离体豚鼠气管螺旋条上建立不同浓度野马追孵育时各致痉剂的量效曲线 ,观察野马追对各致痉剂引起收缩的影响。结果 :野马追对豚鼠离体气管平滑肌的静息张力和乙酰胆碱、组胺、氯化钙、氯化钾、氯化钡所致的收缩都有抑制作用 ,使以上各致痉剂的量效曲线非平行右移 ,最大效应降低 ,其强度依次为BaCl2>KCl>CaCl2 >His >Ach ,并明显抑制乙酰胆碱所致的外钙内流引起的收缩 ,以上作用均具剂量依赖性。结论 :野马追为以上各激动剂的非竞争性拮抗剂 ,其作用机制可能与钙通道的阻滞作用有关。     

基于平喘生物效价的麻黄品质评价研究

目的研究37个不同产地麻黄平喘作用及其生物效价的差异。方法取豚鼠离体气管平滑肌建立平喘药效模型,按累积计量法于麦氏浴槽中加入不同质量浓度梯度(剂间距1:0.5)的麻黄水煎液,计算不同产地麻黄解痉率;按照《中国药典》2010年版二部附录XIV生物检定统计法项下"量反应平行线法"(2,2)法计算生物效价值;采用HPLC法测定麻黄药材中麻黄碱和伪麻黄碱的量;对不同产地麻黄生物效价值进行聚类分析。结果麻黄对磷酸组胺(His)引起的豚鼠离体气管平滑肌收缩有解痉作用,与麻黄对照药材相比,有20个产地的麻黄达显著水平(P0.05),麻黄解痉作用与给药质量浓度呈剂量依赖性,草麻黄与中麻黄种间解痉率无显著差异(P0.05);37个产地的麻黄药材与对照药材相比平喘效价值存在显著差异(P0.05、0.01),平喘效价值为22.35~489.04 U/g,可信限率(FL)13.15%~38.97%,效价相差近21.88倍,麻黄平喘生物效价与麻黄碱及伪麻黄碱总量之间相关不显著;采用聚类分析法能够将不同平喘生物效价值的麻黄区分开来,37份麻黄药材中有24份生物效价值高于对照药材,占麻黄样品总数的64.86%。结论平喘生物效价值可以定量评价不同产地麻黄的质量。     

Chemical constituents of Aristolochia constricta: antispasmodic effects of its constituents in guinea-pig ileum and isolation of a diterpeno-lignan hybrid

Twenty constituents were isolated from the n-hexane and chloroform extracts of Aristolochia constricta, a plant whose aerial parts have been used empirically in folk medicine for various purposes. The inhibitory effects of these constituents on smooth muscle contraction in isolated guinea-pig ileum were studied in order to observe their antispasmodic effects. 3,4-Dibenzyldihydrofuran-type lignans [(-)-cubebin, (-)-hinokinin, and (-)-pluviatolide] and a kaurene-type diterpene [(-)-kaur-16-en-19-oic acid] were isolated as active principals. They inhibited electrically induced and acetylcholine-induced contraction in the isolated guinea-pig ileum. In addition, 9- O-[(-)-kaur-15-en-17-oxyl]cubebin was isolated as a new diterpeno-lignan hybrid, although this constituent did not exhibit antispasmodic activity.     

环氧橙皮油素对平滑肌肌球蛋白功能及肠平滑肌收缩性的影响

目的:探讨环氧橙皮油素对平滑肌肌球蛋白功能及肠平滑肌收缩性的影响.方法:在纯化的蛋白体系中进行平滑肌肌球蛋白Ca2+依赖性磷酸化反应,采用甘油聚丙烯酰胺凝胶电泳测定肌球蛋白轻链磷酸化程度,孔雀绿法测定肌球蛋白Mg2+-ATPase活性.以平滑肌肌球蛋白Mg2+-ATPase活性、肌球蛋白磷酸化以及在克氏液中孵育的肠平滑肌收缩振幅为指标,考察环氧橙皮油素对平滑肌肌球蛋白Mg2+-ATPase活性和肌球蛋白磷酸化程度的调节作用,以及环氧橙皮油素对大鼠离体小肠平滑肌收缩性的影响.结果:在肌球蛋白轻链的Ca2+依赖性磷酸化反应中,在40～320 μmol·L-1浓度内环氧橙皮油素能抑制磷酸化肌球蛋白Mg2+-ATPase活性及其轻链磷酸化程度(P＜0.01),这种抑制作用与1-(5-氯-1-萘-磺酰)-六氢-1,4-二氮杂卓(ML-9)具有协同作用;40 - 320μmol·L-1浓度内环氧橙皮油素可剂量依赖性抑制大鼠离体小肠平滑肌收缩,且可拮抗新斯的明、乙酰胆碱引起的促进收缩作用,相加阿托品引起的抑制收缩作用(P＜0.01).结论:环氧橙皮油素可通过抑制平滑肌肌球蛋白的功能,抑制胃肠平滑肌的收缩性.     

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。     

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.     

Isolation of a bronchodilator flavonoid from the Thai medicinal plant Clerodendrum petasites

The ethanolic extract of Clerodendrum petasites was tested to evaluate the spasmolytic activity on isolated guinea-pig tracheal smooth muscle. The crude extract (2.25-9.0 mg/ml) dose-dependently caused relaxation of tracheal smooth muscle which was contracted by exposure to histamine. A bioassay-guided fractionation of the crude extract was performed by means of partitioning and centrifugal partition chromatography. Finally the active principle was isolated and identified as the flavonoid hispidulin (EC(50): (3.0+/-0.8)x10(-5) M). These results suggest that hispidulin may be beneficial in the treatment of asthma.     

Antispasmodic and relaxant effects of the hidroalcoholic extract of Pimpinella anisum (Apiaceae) on rat anococcygeus smooth muscle

The present work describes the mechanisms involved in the muscle relaxant effect of ethanol:water (40:60, 60:40 and 80:20) aerial parts extracts of Pimpinella anisum. Three hidroalcoholic extracts in which the proportion of ethanol was 40% (HA(40%)), 60% (HA(60%)) or 80% (HA(80%)) were tested for activity in the rat anococcygeus smooth muscle. The three extracts (50 microg/mL) inhibited acetylcholine-induced contraction. The extract HA(60%) (5-50 microg/mL) concentration dependently relaxed acetylcholine-pre-contracted tissues (31.55+/-3.56%). Conversely, HA(40%) and HA(80%) did not exert relaxant action. Pre-incubation of the preparations with N(G)-nitro-L-arginine methyl ester (L-NAME, 100 microM), 1H-[1,2,4]oxadiazolo[4,3-a]quinoxalin-1-one (ODQ, 3 microM) and oxyhemoglobin (10 microM) reduced the relaxation induced by HA(60%) (percentage of relaxation: 6.81+/-1.86%, 13.13+/-5.87% and 2.12+/-1.46%, respectively). Neither indomethacin (10 microM) nor tetraethylammonium (1 mM) affected the relaxation induced by HA(60%). Incubation of the tissues with L-NAME significantly enhanced the maximal contraction induced by acetylcholine, indicating an inhibitory role for NO in the modulation of the contractile response of anococcygeus smooth muscle to acetylcholine. However, simultaneous addition of L-NAME and HA(60%) resulted in an effect similar to that observed with L-NAME alone, further confirming the observation that Pimpinella anisum acts by realizing NO. Additionally, HA(60%) did not alter CaCl(2)-induced contraction. Collectively, our results provide functional evidence that the effects elicited by the hidroalcoholic extract of Pimpinella anisum involve the participation of NO and subsequent activation of the NO-cGMP pathway. The relaxant action displayed by Pimpinella anisum justifies its use in the folk medicine as an antispasmodic agent.     

Pharmacological basis for the use of Borago officinalis in gastrointestinal, respiratory and cardiovascular disorders

AIM OF THE STUDY: In this study, we investigated the crude extract of Borago officinalis leaves (Bo.Cr) for its antispasmodic, bronchodilator, vasodilator and cardio-depressant activities to rationalize some of the traditional uses. MATERIALS AND METHODS: Bo.Cr was studied using different isolated tissue preparations including rabbit jejunum, trachea, aorta, and guinea-pig atria. RESULTS: Bo.Cr which was tested positive for flavonoids, coumarins, sterols and tannins produced a concentration-dependent relaxation of spontaneous and K+ (80mM)-induced contractions in isolated rabbit jejunum preparations, suggestive of Ca++ antagonist effect, which was confirmed when pretreatment of the tissue with Bo.Cr produced a rightward shift in the Ca++ concentration-response curves like that caused by verapamil. In rabbit tracheal preparations, Bo.Cr relaxed the carbachol (1microM) and K+-induced contractions. Verapamil also produced non-specific inhibitory effect. In rabbit aorta preparations, Bo.Cr exhibited vasodilator effect against phenylephrine and K+-induced contractions similar to verapamil. When tested in guinea-pig atria, Bo.Cr caused inhibition of both atrial force and rate of contractions. CONCLUSIONS: These results suggest that the spasmolytic effects of Bo.Cr are mediated possibly through Ca++ antagonist mechanism, which might explain the traditional use of Borago officinalis in hyperactive gastrointestinal, respiratory and cardiovascular disorders.