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。     

小檗碱对大鼠胃窦平滑肌细胞收缩作用的影响(英文)

目的 :观察小檗碱对大鼠胃窦平滑肌细胞的收缩作用。方法 :采用Bitar法分离制备大鼠胃窦平滑肌细胞悬液 ;将 3种不同浓度的小檗碱加入细胞悬液中 ,用测微尺观察细胞长度的变化。结果 :与对照组相比 ,终浓度为 0 .5 g·L-1 ,1 g·L-1 的小檗碱可显著促进大鼠胃窦平滑肌细胞收缩 (P <0 .0 5 ) ,并呈剂量 效应关系。结论 :小檗碱对大鼠胃窦平滑肌细胞有直接收缩作用。     

Effects of Thymus species extracts on rat duodenum isolated smooth muscle contraction

The diethylether, ethylacetate and butanolic extracts from Thymus webbianus and Thymus leptophyllus were tested for spasmolytic activity. Pre-incubation of the isolated rat duodenum with these extracts for 10 min produced a concentration-dependent inhibition of acetylcholine-induced contractions. This effect was at least ten times greater with the apolar extracts than with the polar extracts.     

Antiinflammatory activity and effects on isolated smooth muscle of extracts from different Teucrium species

The present study analyses the antiinflammatory effects and the action on in vitro motility of methanol and dichloromethanol extracts and stems of four Teucrium species (T. flavum, T. cartaginenses, T. buxifolium and T. pumillum). The antiinflammatory activity was tested in the carrageenan-induced paw oedema in rats. T. flavum methanol (200 mg/kg, i.p.) and dichloromethanol (138 mg/kg, i.p.) extracts showed a significant anti-inflammatory effect through the 24 h experimental period and reduced the E_max induced by histamine and serotonin in vitro on guinea-pig ileum and rat uterus respectively. These extracts did not modify the contractile effects induced by acetylcholine on rat duodenum and noradrenaline on rat vas deferens. The methanol extracts of T. pumillum (50 mg/kg, i.p.) and T. buxifolium (26 mg/kg, i.p.) exhibited significant antiinflammatory effects only in the acute phase of the oedema (2 h) without affecting the chronic phase (24 h). In guinea-pig ileum, rat uterus and rat vas deferens, the methanol extract of T. pumillum reduced the maximal effect induced by histamine, serotonin and noradrenaline, respectively, whereas the methanol extract of T. buxifolium lacked any effect on the contractile activity induced by various agonists in vitro. When tested for antiinflammatory activity the methanol (200 mg/kg, i.p.) and dichloromethanol (200 mg/kg, i.p.) extracts of T. cartaginenses did not modify the oedematous response induced by carrageenan administration.     

Contractile response induced by a limonoid (humilinolide A) on spontaneous activity of isolated smooth muscle

The in vitro effect of the limonoid humilinolide A, isolated from Swietenia humilis (Meliaceae), on spontaneous contractions of guinea-pig ileum, and uterus from oestrus, dioestrus, ovariectomized and oestrogen-primed rats was studied. Humilinolide A caused a concentration dependent and non-reversible excitatory effect on intestinal and uterine smooth muscle, distinguished as spasmogenic and uterotonic action respectively. However, the potency of this compound to induce contraction was different in the distinct preparations assayed: in ileal musculature of male guinea-pigs, as well as in uterine muscle of dioestrus and ovariectomized rats, a slight excitatory effect was observed; in contrast to an intense excitatory effect displayed in rat uterus with high oestrogen levels (oestrus and oestrogenized). These data suggest that the contractile response induced by humilinolide A could be mediated by oestrogens, probably by occupancy of some receptors in myometrial plasma membranes to induce uterotonic response, which may be oestrogen-dependent. © 1997 John Wiley & Sons, Ltd.     

黄连水煎剂对未孕大鼠离体子宫平滑肌运动的影响

目的 :探讨黄连水煎剂对未孕大鼠离体子宫平滑肌运动的影响。方法 :利用BL 3 10智能型生物信号显示与处理系统记录平滑肌条的等长收缩活动。结果 :黄连水煎剂能明显延长收缩波持续时间 ,增加收缩波面积且有显著正相剂量效应关系 ,还可增加收缩波的振幅但无剂量效应关系 ,黄连水煎剂的这作用可被异搏定 (L型电压依赖性Ca2 通道阻断剂 )所阻断。结论 :黄连水煎剂在体外可增强子宫平滑肌的收缩 ,该作用是通过L型钙通道而发挥的。     

小檗碱对大鼠胃窦平滑肌细胞收缩作用的影响(英)

目的:观察小檗碱对大鼠胃窦平滑肌细胞的收缩作用.方法:采用Bitar法分离制备大鼠胃窦平滑肌细胞悬液;将3种不同浓度的小檗碱加入细胞悬液中,用测微尺观察细胞长度的变化.结果:与对照组相比,终浓度为0.5g·L-1,1g·L-1的小檗碱可显著促进大鼠胃窦平滑肌细胞收缩(P＜0.05),并呈剂量-效应关系.结论:小檗碱对大鼠胃窦平滑肌细胞有直接收缩作用.     

参麦注射液对离体人支气管平滑肌张力的影响

目的:探讨参麦注射液对离体人支气管平滑肌(HBSM)张力的影响及其作用机制。方法:采用体外等长张力测定法,观察参麦注射液对HBSM静息和收缩张力的影响。结果:与对照组比较,参麦注射液对支气管环的张力无明显作用;参麦注射液可显著抑制乙酰胆碱和KCl诱发的收缩反应;对内钙释放和外钙内流所引发的收缩均有明显的抑制作用(P均<0.05)。结论:参麦注射液能抑制乙酰胆碱和KCl诱发的支气管环的收缩作用,其作用机制可能是通过抑制细胞外钙进入细胞内及胞浆内钙的释放而抑制支气管的收缩。     

Contractile effect of some extracts from the leaves of Musanga cecropioides (Cecropiaceae) on uterine smooth muscle of the rat

Portions of the hot water extract, chloroform and n-butanol fractions of the leaves of Musanga cecropioïdes were used to challenge uterine strips from nonpregnant and early stage pregnant (3–8 days) female Wistar rats. Uterine strips were obtained from oestrogenized females. The aqueous and n-butanol extracts (10 mg/L showed very marked uterotonic effects which were more pronounced in the pregnant females. These contractile effects were dose-dependent and comparable to oxytocin and acetylcholine (100 μg/mL) but were all antagonized by ethanol, a potent Ca^2t channel antagonist. These effects may account for the abortifacient properties of the extracts observed in previous in vivo trials.     

远志皂苷H对离体平滑肌与心脏的作用

 目的:研究一种新的远志皂苷H对平滑肌和心肌的药理作用及其机制。方法:制备离体兔回肠,胸主动脉条,Langen-dorf心脏,豚鼠气管条和动情期未孕大鼠子宫标本,记录给药3min后的张力变化。结果:H对上述4种平滑肌均具兴奋作用,19和76μmol·L^-1分别使其张力提高64%和167%,30%和118%,20%和50%,以及100%和180%;对心脏则呈依剂量的抑制作用,19,38和76μmol·L^-1分别使心肌收缩力降低20%,23%和34%,使心率减少17%,20%和35%,但不影响冠脉流量。H对子宫的兴奋作用不受苯海拉明影响,但可被吲哚美辛部分抑制。结论:H对平滑肌具兴奋作用,对心肌具抑制作用,其中对子宫的作用可能部分地与前列腺素合成酶有关。     

苍术对大鼠离体小肠、结肠收缩活动的影响

30－200％浓度的苍术水煎剂剂量依赖性减小大鼠离体近端结肠纵行肌条的收缩波平均振幅,其作用可部分被心得安阻断,酚妥拉明、消炎痛和L－NNA对其活动无明显影响,提示苍术对大鼠结肠纵行肌的兴奋作用部分由肾上腺素能β受体介导。苍术对大鼠离体小肠、近端结肠环行肌和远端结肠纵、环行肌的收缩活动无明显影响。     

川芎嗪抑制大鼠气道平滑肌细胞增殖和诱导凋亡的研究

目的研究川芎嗪对大鼠气道平滑肌细胞(ASMCs)增殖和凋亡的影响。方法采用改良组织块和胰酶消化联合培养原代ASMCs,以血小板源生长因子(PDGF)诱导ASMCs增殖建立模型。采用MTT法检测不同浓度川芎嗪作用不同时间对ASMCs增殖的抑制,Hoechst33342染色检测细胞凋亡,Western blot检测ERK1/2蛋白表达情况。结果 MTT检测川芎嗪处理(6,12,24,36和48 h)后,与对照组比较,12.5μmol/L组、25μmol/L组、50μmol/L组和100μmol/L组的细胞平均抑制率均显著增加(P均<0.05)。Hoechst 33342染色观察到50μmol/L组、100μmol/L组和200μmol/L组川芎嗪中强荧光细胞比例随川芎嗪剂量增大而增多,细胞核内多个不均一蓝染现象。川芎嗪(200μmol/L组)和PDGF(20 pg/L)共同处理后,随作用时间增加,ERK1/2蛋白表达水平显著降低。结论川芎嗪对ASMCs增殖有抑制作用,同时高浓度的川芎嗪可促进ASMCs凋亡,可能与下调ERK1/2的表达有关。     

Selective modulatory effects of the essential oil of Croton zehntneri on isolated smooth muscle preparations of the guinea-pig

The effects of the essential oil of the plant Croton zehntneri (EOCz) in the concentration range 1–200 μg/mL were studied on the mechanical activity of various in vitro smooth muscle preparations of the guinea-pig. In isolated ileum EOCz induced a variable response such that in 57% of tissues basal tone was reduced (EC₅₀ 5 μg/mL) whereas the rest remained unaffected by the oil. In concentrations above 10 μg/mL EOCz induced spontaneous oscillatory contractions in all preparations. In contrast the basal tone of the aorta, portal vein and bladder remained unaltered by the oil. In the portal vein EOCz concentration-dependently inhibited the amplitude of spontaneous contractions (IC₅₀ 109 μg/mL) without reducing frequency, whereas in the bladder such activity was increased by the oil (EC₅₀ 44 μg/mL). In ileum precontracted with 60 mM KCl, EOCz induced a complete and concentration-dependent relaxation with an IC₅₀ value of approximately 26 μg/mL. In contrast EOCz did not relax KCl-induced tone in the aorta or bladder, whilst eliciting less than 20% relaxation of the precontracted portal vein. Thus our data show that EOCz exerts differential modulatory effects on the contractility of various smooth muscles of the guinea-pig. That EOCz appears to selectively relax intestinal smooth muscle may support its use in folk medicine as a gastrointestinal antispasmodic. © 1998 John Wiley & Sons, Ltd.     

心舒口服液对大鼠主动脉血管平滑肌细胞增殖和家兔体外血小板聚集功能的影响

 目的探讨心舒口服液治疗动脉硬化,抑制血管平滑肌增生和抗血小板聚集作用。方法通过血清药理学方法,考察心舒口服液对大鼠血管平滑肌体外增殖作用及家兔体外血小板聚集功能的影响。结果心舒口服液不同时间点含药血清能够明显抑制血管平滑肌细胞的增殖,对花生四烯酸(AA)和ADP诱导的体外血小板聚集功能均有明显的抑制作用。结论心舒口服液治疗心肌缺血作用机制与抑制血管平滑肌细胞增殖和抗血小板聚集有关。     

Effects of crinum glaucum aqueous extract on intestinal smooth muscle activity

Crinum glaucum aqueous extract (1–8 mg/mL) produced a concentration dependent, non-competitive inhibition of contractions induced by acetylcholine (1.1 × 10⁻⁸–3.3 × 10⁻⁷M ) and calcium chloride (CaCl₂, 0.05–2 mM ) on the rat duodenum. Contractions of the guinea-pig ileum induced by acetylcholine (1.1 × 10⁻⁸–3.3 × 10⁻⁷M ) and histamine (1.1 × 10⁻⁸–3.3 × 10⁻⁷M ) were inhibited by the extract (1–4 mg/mL). The extract (0.125–2.0 mg/mL) also, produced a concentration dependent relaxation of the guinea-pig taenia coli, precontracted with potassium chloride (40 mM ). It is concluded that the extract is a non-specific relaxant of the gastrointestinal smooth muscles used. © 1998 John Wiley & Sons, Ltd.     

喘可治注射液对哮喘小鼠气道炎症和豚鼠离体气道平滑肌的作用

目的:研究中药喘可治注射液(Chuankezhi injection,CKZ)雾化吸入对哮喘小鼠气道炎症的治疗作用,CKZ对豚鼠离体气道平滑肌的扩张作用,为哮喘急性发作期CKZ的合理应用提供依据。方法:利用卵白蛋白诱发小鼠哮喘模型,将小鼠按给药不同随机分为雾化吸入CKZ低、中、高剂量组(分别以0.2,0.4,0.8 mL.kg-1,每天2次)、腹腔注射CKZ组(0.4 mL.kg-1,每天2次)、腹腔注射地塞米松组(0.5 mg.kg-1.d-1)、模型组和空白对照组,采用支气管肺泡灌流法和病理切片观察CKZ的抗炎作用;采用离体气管条法观察CKZ对豚鼠气道的直接扩张和对抗氨甲酰胆碱(carbamylcholine,CCH)和组胺引起的气道平滑肌收缩的作用。结果:在整体试验中,与模型组比较,雾化吸入CKZ高剂量组、腹腔注射CKZ组和地塞米松组,哮喘小鼠支气管肺泡灌流中白细胞总数和嗜酸性粒细胞增加显著减少(P0.01),病理切片中炎症损伤明显减轻;在离体试验中,CKZ对豚鼠气道无直接舒张作用,对CCH和组胺引起的气道平滑肌收缩无对抗作用。结论:CKZ对卵白蛋白诱导的小鼠哮喘有抗炎治疗作用;对豚鼠离体气道平滑肌无明显扩张作用;在哮喘急性发作期的治疗中,CKZ雾化吸入并非首选给药方式。     

Pharmacological evidence for a spasmogenic agent in Datura root extract tested on dispersed smooth muscle cells of guinea-pig ileum

The effect of acetylcholine, scopolamine, and Datura leaf and root extracts on the contractility of dispersed muscle cells of guinea-pig ileum was studied. Scopolamine and crude Datura leaf extract alone or together had no significant effect on contraction of smooth muscle cells. Acetylcholine and Datura root extract either alone or together caused a significant (30%) contraction. Datura root extract reversed the effect of both scopolamine and Datura leaf extract suggesting the presence of an unknown spasmogenic factor in Datura root extract.     

Further studies on the antidiarrhoeal activity of bisnordihydrotoxiferine,a tertiary indole alkaloid in rodents

The dimeric tertiary indole alkaloid bisnordihydrotoxiferine isolated from the root bark of Strychnos trinervis (Vell.) Mart. inhibited, on i.p. administration, Escherichia coli-induced diarrhoea and cholera toxin-stimulated intestinal fluid accumulation in mice. The respective ED₅₀ values were 10.6 and 20.0 mg/kg. The activity of bisnordihydrotoxiferine was unaffected by nalorphine or yohimbine, suggesting that the opioid and α₂-adrenoceptors respectively, are not important for its antidiarrhoeal action. In smooth muscle studies, bisnordihydrotoxiferine antagonized in a noncompetitive and reversible manner, the contractions produced by histamine, acetylcholine and substance P in guinea-pig ileum and by 5-hydroxytryptamine and arachidonic acid in rat fundic strip. The respective pD'₂ values (mean ± SEM) were 5.21 ± 0.29, 5.20 ± 0.29, 5.35 ± 0.12, in the ileum and 4.95 ± 0.13 and 3.66 ± 0.12 in the fundic strip. The values of slopes of the regression lines differed significantly from unity in all cases. Bisnor was inactive against PGE₂-induced contractions in the ileum. The mechanism of action of the alkaloid may be related to nonspecific antagonism of gastrointestinal smooth muscle stimulant activity of several endogenous substances.     

Effect of Desmodium adscendens fraction F1 (DAF1) on tone and agonist-induced contractions of guinea pig airway smooth muscle

Cumulative concentration-response curves (CCRC) of histamine, carbachol and leukotriene D, (LTD₄), and relaxation curves were used to evaluate the nature of the modulation of allergic airway smooth muscle contraction of Desmodium adrcendens fraction F1 (DAF1). DAM significantly increased the maximal contractions (E_max) of tracheal spirals for all three agonists, and significantly increased the pD, values for histamine and carbachol, but decreased that for LTD₄. On lung parenchymal strips DAM had no significant effect on the shape of the CCRC, the pD, value or E_max for histamine and carbachol. A significant decrease in the pD, value for LTD₄, was observed at DAM concentrations of 0.3 and 0.9mg/mL. At the higher concentration, the decrease was accompanied by an equally significant decrease in the E_max. DAF1 per se, caused relaxation of tracheal spirals. The results indicate that DAF1's effect includes a reduction in sensitivity and responsiveness to LTD₄-induced contractions.     

丹皮酚对脂多糖诱导损伤的与平滑肌细胞共培养的大鼠血管内皮细胞黏附功能的影响

目的：观察脂多糖（LPS）诱导的与平滑肌细胞（SMC）共培养的内皮细胞（VEC）与大鼠单核细胞黏附功能的改变及丹皮酚（paeonal,Pae）的干预作用。方法：组织块预消化贴壁法原代培养大鼠血管内皮细胞和大鼠血管平滑肌细胞;采用Transwell小室建立VEC-SMC共培养模型;采用LPS诱导VEC的损伤;MTT法和LDH法检测VEC活力;ELISA法检测VEC分泌IL-1β和TNF-α的水平;免疫细胞化学法检测ICAM-1表达水平;孟加拉玫瑰红染色法检测VEC与单核细胞的黏附功能。结果：LPS诱导VEC损伤的质量浓度为100 μg·L^-1,时间为7 h;Pae（15,30,60 μmol·L^-1）对以上细胞模型作用24 h可有效抑制LPS诱导的VEC损伤,显著提高LPS导致的VEC存活率的下降;降低损伤VEC分泌IL-1β和TNF-α的水平,同时减少ICAM-1的表达;从而抑制LPS诱导的VEC与单核细胞的黏附。结论：Pae通过抑制IL-1β和TNF-α表达而保护VEC免受LPS的损伤,可以通过降低ICAM-1的表达水平达到抑制VEC与单核细胞的黏附的作用。