棉花根醇提物与水提物的止咳祛痰抗炎作用研究

制备棉花根醇提物和水提物,止咳实验采用小鼠浓氨水引咳法,祛痰实验采用气管酚红排泌法,抗炎实验采用二甲苯致耳肿胀法,观察棉花根醇提物和水提物的止咳祛痰抗炎作用。实验小鼠分正常对照组,醇提物与水提物高低剂量组及阳性药物对照组。结果发现棉花根醇提物、水提物均能延长小鼠的咳嗽潜伏期,减少咳嗽次数,均能增加气管内的酚红排泌量,对二甲苯所致的耳肿胀均有显著的抑制作用。     

玉郎伞提取物抗炎作用研究

研究玉郎伞水提物及从玉郎伞中提取纯化的三种活性成份—黄酮、皂苷、多糖的抗炎作用。以巴豆油致炎小鼠耳廓肿胀、角叉菜胶诱发小鼠足跖肿胀及小鼠棉球肉芽肿模型分别观察玉郎伞水提物及三种成份对小鼠耳廓肿胀、足跖肿胀及棉球肉芽肿形成的抑制作用。结果表明,玉郎伞水提物及三种成份可抑制小鼠耳廓炎症、足跖肿胀及棉球肉芽肿的形成。因此,玉郎伞水提物及三种活性成份具有较强的抗炎作用。     

小叶榕不同提取物的主要药效学研究

为研究小叶榕不同提取部位的镇咳、抗炎作用,采用氨水致咳小鼠动物模型、枸橼酸致咳豚鼠动物模型来评价小叶榕不同提取部位的镇咳作用;采用二甲苯滴耳廓致肿胀的小鼠动物模型、大鼠棉球肉芽肿动物模型来评价小叶榕不同提取部位的抗炎作用。结果表明:小叶榕醇沉不溶物能延长小鼠和豚鼠的咳嗽潜伏期,但不能减少咳嗽次数,小叶榕水提物、水提醇沉溶解物、大孔吸附树脂吸附洗脱物能延长小鼠和豚鼠的咳嗽潜伏期,并能减少咳嗽次数,其中水提醇沉溶解物镇咳作用最强;小叶榕醇沉不溶物不能减轻二甲苯引起的小鼠耳廓肿胀的程度,能减轻大鼠棉球肉芽肿足跖肿胀的程度,但效果不明显,小叶榕水提物、水提醇沉溶解物、大孔吸附树脂吸附洗脱物均能明显减轻二甲苯引起的小鼠耳廓肿胀的程度,并能明显减轻大鼠棉球肉芽肿足跖肿胀的程度。这表明国产小叶榕不同提取部位具有明显的镇咳、抗炎作用。     

杨桃水提物对小鼠抗炎镇痛作用研究

为了研究杨桃水提物(Averrhoa caramhola L. water extract, AWE)对小鼠的抗炎、镇痛作用,采用蛋清致小鼠足跖肿胀和二甲苯致小鼠耳廓肿胀来建立炎症模型,通过比较致炎侧小鼠足跖、耳廓与非致炎侧小鼠足跖、耳廓的质量关系来观测AWE的抗炎作用,采用热板法观测其镇痛作用。将90只小鼠采用完全随机设计分组法分成3组:空白对照组、阿司匹林组及杨桃水提物组,每组30只,分别进行抗炎和镇痛系列判定试验。其中杨桃水提物组给予AWE(10.00 g/kg)灌胃、阿司匹林组给予阿司匹林(0.20 g/kg)灌胃、空白对照组给予相同体积蒸馏水灌胃,均每天1次,连续给药7 d。各组在末次给药后分别进行抗炎镇痛作用的观测。试验结果与空白对照组相比较后显示,AWE可明显抑制蛋清所致小鼠足肿胀、抑制二甲苯所致小鼠耳廓的肿胀度,可提高热板所致小鼠痛阈值(p0.05,p0.01),因此AWE具有明显的抗炎镇痛作用。     

合萌水提物抗炎镇痛作用的实验研究

目的:观察合萌水提物的抗炎、镇痛作用。方法:采用二甲苯致小鼠耳肿胀、角叉菜胶致小鼠足跖肿胀、醋酸致小鼠腹腔毛细血管通透性增加及醋酸致小鼠扭体实验、热板实验模型,观察合萌水提物的抗炎镇痛作用,并测定丙二醛(MDA)、一氧化氮(NO)的含量及超氧化物歧化酶(SOD)活性。结果:合萌水提物可抑制二甲苯致小鼠耳肿胀,减轻小鼠足跖肿胀,降低小鼠毛细血管通透性,减少醋酸致小鼠扭体次数,增加热板小鼠痛阈值,降低血清MDA、NO含量,提高血清SOD活性。结论:合萌水提物具有抗炎镇痛作用,作用机制可能与降低血管通透性、抑制NO等炎症介质产生及增强清除自由基、抗脂质过氧化能力有关。     

大血藤醇提物抗炎镇痛和止血活性研究初探

为观察大血藤醇提物抗炎、镇痛、止血活性,该文采用75%乙醇提取制备大血藤醇提物(AESC),利用HPLC法测定其绿原酸含量; KM鼠(或新西兰兔)在测定抗炎、镇痛、止血活性时随机分为空白对照组、阳性对照组(云南白药酊组)、AESC组,依次测定其抑制二甲苯致小鼠耳肿胀度作用、痛阈值和兔肝脏局部创面损伤出血的记分分值,分别考察其抗炎、镇痛、止血作用。结果表明:AESC中绿原酸含量为(0.294±0.013 5)%;与空白组比较,剂量为0.700 g·kg~(-1)的AESC组能显著减轻二甲苯所致的小鼠耳肿胀度(P0.01),抑制率达26.3%;与空白组及给药前比较,剂量为1.40 g·kg~(-1)的AESC组均能显著提高小鼠痛阈值(P0.01);与空白组相比,剂量为1.40 g·kg~(-1)的AESC组能显著提高兔肝脏局部创面损伤出血的记分分值(P0.001)。大血藤醇提取物具有显著的抗炎、镇痛、止血作用,有望将其开发为抗炎、镇痛、止血制剂。该结果也为大血藤的临床应用提供理论依据。     

通体结香技术产沉香的镇痛抗炎作用研究

探究通体结香技术产沉香(以下简称"通体沉香")的镇痛抗炎作用及可能机制。采用体外LPS诱导RAW264.7细胞炎症模型筛选,评价通体沉香不同温度加热熏香挥发性成分的抗炎活性;采用体内小鼠经典镇痛抗炎热板法、醋酸致小鼠扭体、二甲苯致耳肿胀及卵清蛋白(OVA)致脚趾肿胀等试验,评价通体沉香醇提物(WTAAE)预先给药处理的镇痛抗炎作用;通过检测药物处理炎症细胞培养上清中TNF-α和IL-1β的水平,探究通体沉香发挥镇痛抗炎的可能作用机制。结果显示,通体沉香加热熏香挥发性成分体外有较好抗炎活性,IC_(50)范围为30～50μg/mL;WTAAE能显著缩短小鼠痛阈时间,降低小鼠扭体次数,且同等剂量下WTAAE作用与野生沉香醇提物(WAAE)作用相当或略优,同时缓解小鼠耳和脚趾的肿胀程度,体内有较好镇痛抗炎作用;作用机制研究显示,通体沉香挥发性成分可显著降低炎性细胞因子TNF-α和IL-1β的水平。通体沉香体内外均有较好的镇痛抗炎作用,其机制可能与抑制炎性细胞因子和致痛物质的分泌有关。     

灵芝发酵液酸性醇提物抗慢性支气管炎疗效的研究

通过灵芝发酵液酸性醇提物对小鼠的镇咳、祛痰实验,及烟熏小鼠肺部组织的形态学观察,研究灵芝酸性醇提物抗慢性支气管炎的疗效。灵芝发酵全液,不同剂量的灵芝酸乙醇提取物、灵芝酸正丁醇提取物均能显著延长二氧化硫诱发的小鼠咳嗽潜伏期,并显著抑制小鼠咳嗽次数,有明显的镇咳作用。60mg/kg给药量的正丁醇提取物使小鼠气道酚红排泄量较对照组提高了50.7%,祛痰疗效也明显优于双黄连口服液。肺组织切片病理检查表明,灵芝酸性提取物明显减轻烟熏小鼠的气管、支气管粘膜损伤,慢性支气管炎的组织病理学变化明显轻于单纯烟熏模型组,且抗炎、抗损伤作用与双黄连相当,这可为灵芝酸产品的研究开发提供一定的药理依据。     

枇杷花茶水提物的镇咳、抗炎与抗氧化作用研究

采用小鼠氨水致咳法研究枇杷花茶水提物镇咳效果,以二甲苯致小鼠耳肿胀法研究其抗炎效果,并从枇杷花茶的还原能力及对超氧阴离子和羟自由基的清除作用分析枇杷花茶水提物的抗氧化效果。结果表明,枇杷花茶的水提物高剂量组(3000 mg·kg-1)、低剂量组(700 mg·kg-1)均有镇咳抗炎效果,水提物的浓度越高,效果越好。各浓度枇杷花茶水提物均表现出一定的还原能力,对于羟基自由基和超氧阴离子都有一定的清除效果。其中,20 mg·mL-1水提物还原效果最好(吸光值0.903),超过0.2 mg·mL-1抗坏血酸(吸光值0.814);10 mg·mL-1的水提物对超氧阴离子的清除率为47.32%;20 mg·mL-1水提物对于羟基自由基的清除效果非常明显,清除率为91.62%。枇杷花茶水提物镇咳、抗炎、抗氧化效果明显。     

蕲蛇提取物抗炎镇痛药理作用的研究

目的 研究蕲蛇提取物的抗炎及镇痛作用,为蕲蛇的临床应用提供科学依据.方法 采用热板法、冰醋酸刺激致痛法研究蕲蛇提取物对小鼠痛阈的影响,利用二甲苯致小鼠耳廓炎症模型和腹腔染料渗出法测定蕲蛇提取物的抗炎作用.结果 蕲蛇提取物醇溶性和水溶性部位对小鼠热板及冰醋酸致痛反应有明显镇痛作用,对二甲苯致小鼠耳廓肿胀、冰醋酸致腹腔毛细血管通透性增高均有明显的抑制作用.结论 蕲蛇提取物醇溶性和水溶性部位有一定的抗炎及镇痛作用,并且水溶性部位较醇溶性部位的药效好,可为蕲蛇的临床应用提供指导作用.     

巴豆提取物对玉米象的生物活性

研究了巴豆(Croton tigliumL.)4种溶剂提取物对玉米象Sitophilus zeamais(Motschulsky)成虫的驱避作用和触杀作用。结果表明:巴豆的4种溶剂提取物对玉米象Sitophilus zeamais(Mostchulsky)成虫均有很好的触杀作用,7.86 mg/cm2的浓度处理后,4 d后的校正死亡率均达到100%。巴豆的4种溶剂提取物对玉米象成虫没有明显的驱避作用。     

Potent Anti-Inflammatory Activity of Novel Microtubule-Modulating Brominated Noscapine Analogs

Noscapine, a plant-derived, non-toxic, over-the-counter antitussive alkaloid has tubulin-binding properties. Based upon the structural resemblance of noscapine to colchicine, a tubulin-binding anti-inflammatory drug, noscapine and its semi-synthetic brominated analogs were examined for in vitro anti-inflammatory activity. Brominated noscapine analogs were found to inhibit cytokine and chemokine release from macrophage cell lines but did not affect cell viability. Brominated noscapine analogs demonstrated anti-inflammatory properties in both TLR- and non-TLR induced in vitro innate immune pathway inflammation models, mimicking septic and sterile infection respectively. In addition, electron microscopy and immunoblotting data indicated that these analogs induced robust autophagy in human macrophages. This study is the first report to identify brominated noscapines as innate immune pathway anti-inflammatory molecules.     

Antitussive and expectorant activities of licorice and its major compounds

Licorice has been used as an antitussive and expectorant herbal medicine for a long history. This work evaluated the activities of 14 major compounds and crude extracts of licorice, using the classical ammonia-induced cough model and phenol red secretion model in mice. Liquiritin apioside (1), liquiritin (2), and liquiritigenin (3) at 50?mg/kg (i.g.) could significantly decrease cough frequency by 30–78% (p?<?.01). The antitussive effects could be partially antagonized by the pretreatment of methysergide or glibenclamide, but not naloxone. Moreover, compounds 1–3 showed potent expectorant activities after 3?days treatment (p?<?.05). The water and ethanol extracts of licorice, which contain abundant 1 and 2, could decrease cough frequency at 200?mg/kg by 25–59% (p?<?.05), and enhance the phenol red secretion (p?<?.05), while the ethyl acetate extract showed little effect. These results indicate liquiritin apioside and liquiritin are the major antitussive and expectorant compounds of licorice. Their antitussive effects depend on both peripheral and central mechanisms.     

Effect of ethanol on corticosterone production by dispersed adrenal cells of the rat

The action of ethanol on adrenal steroidogenesis "in vitro" has been studied. It has been found that ethanol did not change the basal production of corticosterone by dispersed adrenal cells, but significantly reduced its response to ACTH stimulation. It is suggested that the inhibitory action of ethanol on steroidogenesis "in vitro" could have a physiological meaning, because the response to ACTH stimulation of adrenal cells from rats treated "in vivo" with ethanol showed a clear dose-related inhibition.     

The constituents of licorice (Glycyrrhiza uralensis) differentially suppress nitric oxide production in interleukin-1β-treated hepatocytes

Licorice (Glycyrrhizae radix) is the roots and stolons of Glycyrrhiza uralensis Fischer or Glycyrrhiza glabra Linnaeus in the Japanese Pharmacopoeia. Glycyrrhizae radix has been widely used as a sweetener and a traditional medicine. A Glycyrrhizae radix extract contains many constituents and has antispasmodic, antitussive, anti-ulcer, and anti-inflammatory effects. However, reports comparing the anti-inflammatory effects of these constituents are very few. Here, we purified several constituents from the roots and stolons of G. uralensis and examined and compared their anti-inflammatory effects by monitoring the levels of the inflammatory mediator, nitric oxide (NO), in interleukin (IL)-1β-treated rat hepatocytes. From the G. uralensis extract, we purified the main constituent glycyrrhizin and the constituents that are characteristic of G. uralensis (chalcones and flavanones). These constituents suppressed NO production in IL-1β-treated rat hepatocytes, and isoliquiritigenin showed the greatest suppression activity. Isoliquiritigenin, isoliquiritin, and liquiritigenin significantly decreased both protein and mRNA for the inducible nitric oxide synthase. These constituents reduced the levels of mRNAs encoding tumor necrosis factor α and IL-6. In contrast, although glycyrrhizin is abundant, it showed a 100-fold lower potency in NO suppression. Therefore, both glycyrrhizin and the minor constituents (isoliquiritigenin, isoliquiritin, and liquiritigenin) may be responsible for the anti-inflammatory effects of G. uralensis. It is also implied that these constituents may have a therapeutic potential for inflammatory hepatic disorders.     

GABA-ergic mechanisms in the central control of cough

The antitussive activity of gabalinoleamide (Gabalid U CB) was studied in 40 non-anaesthetized cats. The antitussive action of the substance was compared to that of codeine (Codein Spofa). Cough was induced by mechanical stimulation using a chronic tracheal cannula. Single cough parameters were evaluated from changes in the side tracheal pressure. When gabalinoleamide was administered in a dose of 100 mg/kg b.w. intramuscularly all the studied parameters of cough showed a statistically significant decrease, only the intensity of maximum cough effort remained unaffected. Gabalinoleamide administered in the same dose induced a statistically significant decrease of respiratory frequency and breathing amplitude, and prolonged the cycle of breathing by delaying the expiratory phase. Higher doses (200 and 300 mg/kg b.w.) did not have an increased cough suppressing effect. The quality and quantity of cough parameters were similar after codeine and gabalinoleamide.     

Interaction of noscapine with the bradykinin mediation of the cough response

Angiotensin Converting Enzyme Inhibitors (ACEI) like captopril and enalapril, can induce persistant cough in man. Noscapine, an antitussive alkaloid, can be used to suppress ACEI-induced cough. Some workers have suggested a role for bradykinin in precipitation of ACE-induced cough. Work carried out in our laboratory has shown noscapine to be a non-competitive inhibitor of bradykinin in guinea pig ileum. It is therefore possible that noscapine suppresses cough by blocking the effect of bradykinin receptor activation in the airways. Guinea pigs were placed in a cough-chamber connected to an air pump and a pressure transducer. Capsaicin was sprayed into the chamber and cough was recorded as a distinctive change in air pressure inside the cough-chamber. Animals treated with 1 mg/kg captopril and enalapril for 7 days, showed increased cough response. Ten microgram/kg FR190997, a non-peptide agonist of the bradykinin B2 receptor, also increased the cough response. Noscapine at 0.5, 1 and 2 mg/kg was able to reverse the effects of ACEI and FR190997. Naloxone, a specific opioid receptor inhibitor, did not block the antitussive effects of noscapine in enalapril or FR190997 treated guinea pigs. This antitussive effect of noscapine is not mediated via the mu, kappa or delta opioid receptors. It is therefore possible that noscapine exerts its antitussive action by interfering with the bradykinin cough mediation.     

直链脂肪醇对豚鼠乳头肌慢动作电位的影响

本工作用相平面法观察和分析了乙醇、丁醇、己醇和辛醇对豚鼠乳头肌慢动作电位(APA,APD50,APD90,(?)_(max),(?)′_(max))及其所对应的钙电流(I_(max))和钾电流(I′_(max))的影响。结果表明:这四种脂肪醇对钙电流均有抑制作用,而对钾电流的影响,随碳原子数的加大从增强(乙醇)逐渐转化为削弱(已醇,辛醇)。并且碳链越长,产生这些效应所需脂肪醇的浓度越低,这提示醇的作用可能与它们的疏水性相关。