盐酸戊乙奎醚对豚鼠离体回肠/结肠的解痉作用

目的　研究盐酸戊乙奎醚 (PHC)对豚鼠离体回肠 /结肠肌条的抑制收缩作用。方法　将豚鼠离体回肠 /结肠条悬吊于麦氏浴槽中 ,测量给药PHC后豚鼠离体肌条自主收缩及乙酰胆碱 (Ach)所致痉挛收缩的最大张力 ,计算抑制 5.0 %收缩的PHC的浓度。结果　PHC对豚鼠离体回肠 /结肠肌条的自主收缩有明显抑制作用 ,对乙酰胆碱 (Ach)所致的痉挛性收缩有明显的松弛作用。结论　PHC能有效地缓解离体回肠 /结肠的痉挛状态。     

蛇床子素抗变态反应的研究

蛇床子素能较强地抑制小鼠被动皮肤过敏(PCA)反应,对整体豚鼠组胺性喘息具有保护作用,对慢反应物质(SRS-A)引起的豚鼠离体回肠收缩以及豚鼠离体回肠的Schultz-Dzle反应呈明显的拮抗和阻断作用,并能抑制大鼠腹腔肥大细胞脱颗粒。上述作用均呈一定的剂量依赖关系。     

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。     

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。     

辛夷挥发油的抗过敏实验研究

目的：研究辛夷挥发油的抗过敏作用。方法：采用磷酸组织胺（HA）、氯化乙醇胆碱（Ach）所致豚鼠离体回肠收缩实验，卵白蛋白（OA）引起的致敏豚鼠离体回肠实验及大鼠肥大细胞脱颗粒实验法。结果：辛夷挥发油能显著抑制HA、Ach引起的豚鼠离体回肠收缩，对致敏豚鼠离体回肠的过敏性收缩有较强的抑制作用，并能明显阻止大鼠肥大细胞脱颗粒。结论：辛夷挥发油具有较强的抗过敏作用。     

粉防己碱对吗啡在离体豚鼠回肠中依赖性的作用(英文)

目的:研究粉防己碱(Tet)和尼莫地平(Nim)对吗啡在离体豚鼠回肠中戒断性反应的影响。方法:戒断性收缩由纳洛酮(1μmol·L~(-1))加入已在含吗啡(3μmol·L~(-1))的37.5℃ Krebs液中孵育4h的离体豚鼠回肠或加入从吗啡依赖豚鼠中取得的回肠引起。结果:离体豚鼠回肠在含吗啡的Krebs液中孵育4h,给Nim(0.01、0.05和0.1μmol·L~(-1))或Tet(1、10和50μmol·L~(-1))抑制其戒断性收缩。Nim和Tet体内或体外给药都能抑制吗啡依赖豚鼠离体回肠的戒断性收缩。结论:钙拮抗剂Nim和Tet抑制吗啡在离体豚鼠回肠的戒断性收缩。     

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。     

大黄素对动物离体回肠收缩作用的影响

大黄素对豚鼠、大鼠和家兔离体回肠的作用均与剂量相关,＜29.6μmol/L时收缩幅度随剂量增加而增强(P＜0.01和P＜0.05);＞29.6μmol/L时收缩幅度逐渐减弱直至停止;大黄素对家兔离体回肠的收缩频率无明显影响(P＞0.05);大黄素增强回肠收缩幅度的作用可被低剂量的阿托品拮抗,提示大黄素有类似乙酰胆碱的作用,但作用较弱.实验表明大黄素对豚鼠、大鼠和家兔离体回肠具有双向调节作用,这种作用对肠麻痹及痉挛可能有调节性治疗作用.     

二苯氰胂对毒蕈碱性受体的抑制作用

目的研究了日本在我国遗弃的化学武器———二苯氰胂(DC)对离体豚鼠回肠纵肌和毒蕈碱性受体的作用机制,为评估DC的毒理学作用及其对环境的影响提供依据。方法取豚鼠8只,分离豚鼠回肠纵肌16条,分4组,用累积给药法,从低到高分别给予不同浓度的DC,记录离体豚鼠回肠纵肌收缩的幅度,求出DC作用于离体回肠纵肌的EC50值,并通过DC与乙酰胆碱(AChR)的相互作用,研究DC的作用机制。在放射性配体-受体结合实验中,从10只大鼠大脑中提取受体,通过DC与[3H]QNB的竞争结合作用,研究了DC对毒蕈碱性受体的作用。结果DC可抑制离体豚鼠回肠纵肌的收缩作用,其对离体豚鼠回肠纵肌的EC50值为(7.335±2.377)×10-7mol/L,AChR可收缩离体豚鼠回肠,并可反转DC引起离体豚鼠回肠纵肌的舒张作用。在放射性配体-受体结合实验中,DC与毒蕈碱性受体结合的Ki值为(9.19±1.52)nmol/L,IC50值为(16.00±2.65)nmol/L。结论DC可作用于mAChR受体上,初步断定为AChR的拮抗剂。     

干酪菌发酵产物对豚鼠离体回肠平滑肌收缩功能的影响

目的 观察干酪菌发酵产物对豚鼠离体回肠平滑肌收缩功能的影响。方法采用豚鼠离体回肠平滑肌标本,观察加入干酪菌发酵产物前后肌紧张的变化以及加入几种受体阻断剂对其药效的影响。结果 干酪菌发酵产物能提高豚鼠离体回肠平滑肌肌紧张,且呈剂量-效应依赖关系,组织胺H1受体阻断剂苯海拉明能阻断其兴奋作用。结论 干酪菌发酵产物能提高豚鼠离体回肠平滑肌肌紧张,其作用途径与组织胺H1受体有关。     

Pharmacological properties of MM-706, a new prostacyclin derivative

• 1.1. In human platelet-rich plasma, platelet aggregation induced in vitro by collagen (10 μg/ml) or thrombin (50 mU/ml) was dose-dependently inhibited by increasing concentrations of prostacyclin or of the new derivative (±)(5E)-13,14-didehydro-ω-hexanor(1-hydroxycyclohexyl)-9a-carbaprostacyclin (MM-706) with an IC₅₀ of 20–50 nM and 250–500 nM, respectively. In human platelets loaded with fura-2, the intracellular rise of [Ca²⁺] induced by thrombin was dose-dependently inhibited by MM-706 with an approximate IC₅₀ of 100 μM.
• 2.2. In rabbit isolated femoral artery, MM-706 (10nM–10μM) was completely ineffective in relaxing the vessel, which was different to prostacyclin which was able to relax vessels at the same concentrations.
• 3.3. In in vitro guinea-pig ileum, prostacyclin produced a contractile effect in the concentration range 1 nM-10μM, but the derivative MM-706 was ineffective at the same concentrations. Preventive addition of MM-706 did not inhibit prostacyclin contraction.
• 4.4. On isolated guinea-pig tracheal preparation, prostacyclin induced a concentration-dependent contraction but the new compound MM-706 showed a lower activity, in the concentration range 10nM–10μM. The activity of prostacyclin was not affected by the contemporary presence of MM-706.
• 5.5. It is concluded that MM-706 is a prostacyclin analogue with antiaggregating properties but without evident effects on smooth muscle of different regions.

     

秦皮乙素对过敏豚鼠离体肠系膜血管的作用

致敏豚鼠离体肠系膜血管,经抗原攻击后,产生强烈的收缩作用,3min时每分流量减少到攻击前(2.1±0.3ml,n=8)的32±12％(P<0.01)。经生物检定,提示产生收缩作用的物质中含有白三烯(LTs)。泰皮乙素7.5×10~(-6)mol/L能对抗抗原攻击引起的灌流量的减少。结果提示泰皮乙素对过敏反应释放LTs引起的血管收缩具有保护作用。     

The in vitro exposure to cypermethrin does not inhibit the proliferative response of peripheral blood mononuclear cells

This study evaluated the effect of in vitro exposure to cypermethrin on peripheral blood mononuclear cells proliferative response, considering reduced peripheral blood mononuclear cells proliferative response observed in individuals occupationally exposed to pyrethroids. Peripheral blood mononuclear cells were obtained from 21 healthy subjects (28.0?±?9.0 years old). The effect of cypermethrin (at 0.5, 1.0 and 5.0?mg/ml) on cell viability was evaluated by flow cytometry using an apoptosis detection kit. Cell proliferation (PI) was evaluated by 5-(and 6)-carboxyfluorescein diacetate succinimidyl ester (CFSE) fluorescence decay using flow cytometry. Cells labeled with CFSE were exposed, in vitro, to cypermethrin (0.5, 1.0, 2.0, 2.5 and 4?μg/ml) and stimulated with phytohemagglutinin (PHA 1.0 or 5.0?μg/ml) for 5?d (37?°C, 5% CO₂). The in vitro treatment of peripheral blood mononuclear cells with cypermethrin did not induce apoptosis or necrosis after 5?d in culture. Stimulation by PHA induced cell proliferation (PI?=?1.29?±?1.09 and 2.01?±?0.62, PHA at 1.0 and 5.0?μg/ml, respectively, mean?±?SD) and in vitro exposure to cypermethrin did not alter cellular proliferative response to PHA (PI?=?1.80?±?0.50, 2.60?±?0.05 and 2.10?±?1.20 for cypermethrin at 1.0, 2.0 and 4.0?μg/ml, respectively, and PHA at 5.0?μg/ml). In vitro treatment of peripheral blood mononuclear cells with cypermethrin, at the doses tested, does not affect cell viability or proliferation. These findings suggest that the reduction of proliferation observed on lymphocytes derived from individuals occupationally exposed to pesticides may be related to other mechanisms than direct action of cypermethrin on lymphocytes.     

Muscle relaxing activity of Hyssopus officinalis essential oil on isolated intestinal preparations

The muscle relaxing activity of the essential oil of Hyssopus officinalis L. (Lamiaceae) and some of its main components (isopinocamphone, limonene and beta-pinene) was studied on isolated preparations of guinea-pig and rabbit intestine. The essential oil and isopinocamphone inhibited the acetylcholine- and BaCl2-induced contractions in guinea-pig ileum in a concentration-dependent manner (IC50 42.4 microg/ml and 61.9 microg/ml to acetylcholine; 48.3 microg/ml and 70.4 microg/ml to BaCl2) whereas limonene or beta-pinene left tissue contraction unchanged. In guinea-pig ileum H. officinalis essential oil also blocked the contractions induced by CaCl2. In isolated rabbit jejunum the essential oil reduced the amplitude of spontaneous movements and decreased the basal tone; neither haemoglobin, methylene blue, N(omega)-nitro-L-arginine methyl ester (L-NAME) or propranolol blocked the myorelaxant effect.     

蛇床子素对豚鼠离体回肠和结肠带的作用

以豚鼠离体回肠和结肠带为标本,观察蛇床子素(Ost)的作用与Ca²⁺)的关系。结果表明:Ost和钙拮抗剂Ver产生剂量依赖性抑制乙酰胆碱(ACh)、组胺及KCl所致回肠条或结肠带的收缩;非竞争性拮抗CaCl₂累积量—效曲线,pD₂分别为4.41±0.15,7.0±0.2。Ost 100μmol/L和Ver 1μmol/L均能对抗小剂量Ca²⁺所致结肠带收缩,但被加入较大量Ca²⁺所取消。Ost和Ver均能抑制ACh诱导的依内钙性收缩,不影响依外钙性收缩。结果提示Ost具有钙拮抗作用,其作用方式与Ver类似。     

吡喹酮对体外培养的日本血吸虫的作用

吡喹酮(Praziquantel,Embay 8440)系一种具有抗绦虫和抗血吸虫作用的广谱抗寄生虫新药。动物实验证明,该药对小鼠、家兔和犬的日本血吸虫病都有很好的疗效,且毒性低,疗程短;临床上用吡喹酮的1～2天疗法治疗日本血吸虫病,总剂量为45～90mg/kg时,治后半年的粪检虫卵转阴率达99.7％。本文报道吡喹酮对体外培养的日本血吸虫的作用。     

Optimization and evaluation of pluronic lecithin organogels as a transdermal delivery vehicle for sinomenine

The purpose of the present study was to prepare and optimize sinomenine (SIN) pluronic lecithin organogels system (PLO), and to evaluate the permeability of the optimized PLO in vitro and in vivo. Box–Behnken design was used to optimize the PLO and the optimized formulation was pluronic F127 of 19.61%, lecithin of 3.60% and SIN of 1.27%. The formulation was evaluated its skin permeation and drug deposition both in vitro and in vivo compared with gel. Permeation and deposition studies of PLO were carried out with Franz diffusion cells in vitro and with microdialysis in vivo. In vitro studies, permeation rate (J_ss) of SIN from PLO was 146.55?±?2.93?μg/cm²/h, significantly higher than that of gel (120.39?μg/cm²/h) and the amount of SIN deposited in skin from the PLO was 10.08?±?0.86?μg/cm², significantly larger than that from gel (6.01?±?0.04?μg/cm²). In vivo skin microdialysis studies showed that the maximum concentration (C_max) of SIN from PLO in “permeation study” and “drug-deposition study” were 150.27?±?20.85?μg/ml and 67.95?μg/ml, respectively, both significantly higher than that of SIN from gel (29.66 and 6.73?μg/ml). The results recommend that PLO can be used as an advantageous transdermal delivery vehicle to enhance the permeation and skin deposition of SIN.     

In vitro study of the effects of plaunotol on oral cell proliferation and wound healing

Plaunotol is an acyclic diterpene alcohol extracted from a medicinal plant called plau-noi, Croton stellatopilosus Ohba, and has been widely used for the treatment of gastric ulcers in Japan. The aim of this study was to examine the effects of plaunotol on human gingival fibroblasts (HGFs) and human oral keratinocytes (HOKs). To assess the cytotoxic effect, HGFs and HOKs were treated with plaunotol. Subsequently, the morphology of cells was recorded and cells were subjected to MTT assay. To investigate cell proliferation effect, cells were treated with plaunotol and counted with a haemocytometer. To determine wound healing effect, the number of cells repopulated into the wounded areas in monolayer culture and in fibroblast-populated collagen lattice (FPCL) was measured. The results showed that 10 and 1 μg/ml (33 and 3.3 μmol/l) plaunotol induced toxicity in HGFs and HOKs, respectively. However, 0.1 μg/ml (0.33 μmol/l) plaunotol promoted HGF proliferation and wound healing in monolayer and FPCL models. In contrast, 0.1 μg/ml plaunotol could not induce HOK proliferation nor in vitro wound healing using monolayer culture, but it induced wound healing in a modified FPCL model. Our data suggested that plaunotol could promote oral cell proliferation and wound healing in vitro and may have an implication on oral wound healing.     

“8204”对心血管系统和支气管平滑肌的药理作用

“8204”是新合成的化合物。动物实验表明:可使冠脉流量增加,心肌耗氧置降低,提高动物常压和低压情况下的缺氧耐力;对垂体后叶素诱发的缺血性心电图有保护作用,还能松弛离体豚鼠气管平滑肌,对抗乙酰胆碱和组胺引起的气管、支气管平滑肌收缩,增加豚鼠肺灌流量;对豚鼠吸入组胺引起的哮喘有明显保护作用。这些结果提示“8204”对治疗心肌缺血和支气管哮喘是有益的。