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 Daniellia oliveri bark on isolated rat bladder.

The stem bark of Daniellia oliveri was screened phytochemically and a methanol extract prepared.-Condensed tannins, saponins, cyanogenetic and cardiac glycosides were identified in the crude drug. The cardiac glycoside components in the methanol extract were precipitated with acetone to yield a reddish-brown residue. The n-butanol soluble fraction of an aqueous solution of this residue tested positive for cardiac glycosides and was shown by TLC to contain steroidal compounds. This fraction was subjected to pharmacological studies on isolated rat bladder smooth muscle. It had no effect on purinergic neurotransmission but was a noncompetitive antagonist for muscarinic receptors.     

Effects of the essential oil of Croton zehntneri,and its constituent estragole on intestinal smooth muscle

The effects on isolated guinea-pig ileum of the essential oil of Croton zehntneri (CZEO) and of its main constituent estragole (57% of CZEO by weight) were studied. CZEO and estragole (0.1–100 μg/mL) decreased the tonus in 56% and 61.5%, respectively, of the muscles. At concentrations above 10 μg/mL, they induced spontaneous rhythmic movements of small amplitude (less than 11% of the potassium contraction peak to peak). At concentrations from 1 to 100 μg/mL and with similar potencies, these agents blocked the contractions induced by acetylcholine, histamine and 50 mM K⁺ and caused relaxation of already established potassium contractures. Tested separately, CZEO, estragole and anethole (28% of CZEO by weight) blocked the contraction induced by Ca⁺⁺ in the presence of 50 mM K⁺, but CZEO was more potent than estragole or anethole in blocking the Ca⁺⁺-induced contractions than those induced by K⁺. With large increases in the agonist concentration, the action of the oils on the contractions induced by Ca⁺⁺ was reversible; however, their effect on contractions induced by histamine or ACh was not. The data show that the essential oil of Croton zehntneri has an effect on intestinal smooth muscle that is predominantly antispasmodic, and attributable in part to the effect of estragole, a major constituent. © 1997 John Wiley & Sons, Ltd.     

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。     

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。     

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.     

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.     

雷公藤内酯醇对血管平滑肌细胞增殖的影响

目的　探讨雷公藤内酯醇对血管平滑肌细胞 (VSMC)增殖的影响及作用机制。方法　体外培养大鼠胸主动脉平滑肌细胞 ,通过3 H -TdR掺入试验 ,观察雷公藤内酯醇对血清诱导的细胞增殖的影响 ;采用流式细胞技术 ,观察该药对细胞增殖周期的影响。结果　雷公藤内酯醇在 (0 .5～ 4 )× 10 -5g/L的浓度范围内 ,以一种剂量依赖性的方式抑制了血清诱导的VSMC增殖 ;雷公藤内酯醇可显著增加细胞周期中G0 /G1期细胞百分含量 ,减少S期细胞的百分含量 ,阻断细胞由G0 /G1期向DNA合成的S期转化 ,作用呈剂量依赖性。结论　雷公藤内酯醇可能通过影响细胞周期的转化而抑制VSMC的增殖。     

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。     

左旋四氢巴马汀对肠道平滑肌的作用

左旋四氢巴马汀 (1 THP) 2 0 3 2 0mg/kg灌胃给药能剂量依赖性减慢小鼠小肠推进运动。在离体器官实验中 ,1 THP能抑制家兔十二指肠和豚鼠回肠的自发活动 ,非竞争性拮抗His和Ach引起的豚鼠回肠收缩 ,并能松弛高钾去极化和氯化钡引起的豚鼠结肠带收缩。     

The biological activity of eugenol,a major constituent of nutmeg (Myristica fragrans): Studies on prostaglandins,the intestine and other tissues

Studies have been made of eugenol on isolated tissues from man and laboratory animals, and on rats in vivo. Eugenol inhibited prostaglandin synthesis, and reduced the tone of isolated gut muscle and myometrium. With rats in vivo, the compound reduced the rate of intestinal transit, the intestinal accumulation of fluid induced by prostaglandin E₂, and the diarrhoea induced by castor oil. Eugenol showed anti-inflammatory activity in the rat paw carrageenin oedema test.     

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。     

Effect of Backebergia militaris cactus extract on intestinal smooth muscle contractility

The branches of the giant cactus Backebergia militaris contain at least one biologically active compound, corresponding to an alkaloid. This activity was not dependent on cactus age. Methanol crude extracts of B. militaris showed a clear inhibitory effect on rabbit intestinal smooth muscle contractility. The inhibitory activity was concentration-dependent, and reversible upon removal of the extract from the medium. B. militaris extract did not display any anticholinergic action on the rabbit intestine. Copyright © 1998 John Wiley & Sons, Ltd.     

五苓散含药血清对家兔离体输尿管平滑肌作用的实验研究

[目的]观察五苓散含药血清对正常家兔离体输尿管平滑肌活动的影响,并初步探讨其作用机制。[方法]应用Powerlab生物机能信号采集处理系统,观察不同浓度五苓散含药血清及不同受体阻滞剂对离体输尿管平滑肌的影响。[结果]空白血清组和不同浓度五苓散含药血清组均可增强正常家兔离体输尿管平滑肌的张力和活动力,与空白对照组相比,均有显著性差异(P<0.01)。阿托品组和酚妥拉明组可阻断中浓度血清对输尿管平滑肌的收缩作用(P<0.05)。[结论]五苓散含药血清在离体情况下对正常家兔输尿管平滑肌具有收缩作用,有利于尿液的输送。     

大蒜素抑制胰岛素诱发血管平滑肌细胞增殖和迁移实验研究

目的:探讨大蒜素(allicin)抑制胰岛素(insulin)诱导的血管平滑肌细胞(VSMCs)增殖和迁移及其作用机制。方法:采用组织贴块法培养大鼠的VSMCs,并进行平滑肌α-肌动蛋白(α-SMA)免疫荧光鉴定,取3~5代细胞进行实验。建立胰岛素刺激的VSMCs模型。实验分5组:对照组、胰岛素组、大蒜素组、ERK抑制剂PD98059组、大蒜素+PD98059组。噻唑蓝(CCK8)比色法检测VSMCs的增殖;细胞计数法检测VSMCs的迁移;免疫印迹实验(Western blotting)测定total ERK,PhosphoERK(p-ERK),PCNA蛋白表达的情况。结果:原代培养的VSMCs生长良好,光镜下呈长梭形及“峰与谷”样生长。α-SMA免疫荧光显示培养的细胞具有典型的VSMCs特征。胰岛素能刺激VSMCs的增殖和迁移,且以100 nmol·L-1浓度时效果最明显。大蒜素预处理能显著抑制胰岛素刺激的VSMCs的增殖和迁移,且呈剂量依赖性。PD98059、大蒜素+PD98059预处理亦能显著抑制胰岛素刺激的VSMCs的增殖和迁移。胰岛素可明显促进VSMCs表达p-ERK,PCNA蛋白。大蒜素能显著抑制VSMCs表达p-ERK,PCNA蛋白,且呈剂量依赖性。结论:大蒜素能显著抑制胰岛素诱导的VSMCs的增殖与迁移,其作用机制可能是抑制ERK信号通路的激活。     

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.     

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。     

Inhibitory effects of emodin on the proliferation of cultured rat vascular smooth muscle cell-induced by angiotensin II

Rhubarb, used as a traditional Chinese medicine for centuries, offers therapeutic potential for cardiovascular and other diseases. Emodin, extracted from the root extract of rhubarb has sparked increasing interest for therapeutic application. The main objective was to study the effect of emodin on cultured vascular smooth muscle cells (VSMCs) proliferation induced by angiotensin II (Ang II) and the expression of proto-oncogene c-myc. VSMCs were cultured by the explant method, then incubated for 24, 48 and 72 h with emodin (10-80 microm) and Ang II, or were left untreated (control). Cell proliferation was measured by MTT assay and immunohistochemical staining for proliferating cell nuclear antigen (PCNA), respectively. The expression of c-myc was measured by immunohistochemical staining and image analysis technique. Ang II increased the cell proliferation compared with the control group (p < 0.01). The expression of PCNA and c-myc was increased compared with the control group (p < 0.01). After pretreatment with emodin, the above indexes were obviously reduced compared with the Ang II group (p < 0.01). These findings suggested that emodin inhibited VSMCs proliferation induced by Ang II. Inhibition of the expression of c-myc might be correlated with the inhibitory effects.     

Pharmacological activity of the extracts of two Satureja obovata varieties on isolated smooth muscle preparations

Aqueous extracts of two varieties of Satureja obovata Lag. subsp. obovata: var. valentina and var. obovata, exhibited a dose-dependent inhibitory effect on the contractions induced by acetylcholine (Ach) (3.4 × 10^?8?6.8 × 10^?5M) and CaCl₂ (2 × 10^?4?1.28 ? 10^?2M) in rat duodenum and by noradrenaline (NA) (10^?9?5.12 × 10^?7 M) and CaCl₂ (2 × 10^?4?1.28 × 10^?2 M) in rat aorta. The extracts also produced relaxant effects in both tissue preparations precontracted with K⁺ (75 mM) and in rat aorta precontracted with NA (10^?6 M). Vasodilatory effects of the two extracts were attenuated when the endothelium was removed. The inhibitory effects of var. valentina were stronger. These results indicated a smooth muscle relaxant effect that could account for the use of these extracts in traditional medicine.