活犀角与犀角抗炎作用的比较研究

摘 要 目的：比较活犀角与犀角的抗炎作用有无显著差异,为活犀角替代犀角提供实验依据。 方法: 通过大鼠足跖肿胀法和小鼠棉球肉芽肿法、耳廓肿胀法、腹腔染料通透法研究活犀角和犀角的抗炎作用。 结果: 与模型对照组比较,活犀角的高（440 mg·kg^-1）、中（220 mg·kg^-1）剂量组和犀角3个剂量组各时间点的足跖肿胀度差异有统计学意义（P＜0.05或P＜0.01）;活犀角和犀角的高（700 mg·kg^-1）、中（350 mg·kg^-1）剂量组能显著降低小鼠棉球肉芽肿的重量（P＜0.05）;活犀角和犀角3个剂量组（700,350,175 mg·kg^-1）均能明显降低二甲苯引起的小鼠耳廓肿胀（P＜0.05或P＜0.01）;犀角中（350 mg·kg^-1）剂量组,活犀角高（700 mg·kg^-1）、中（350 mg·kg^-1）剂量组的腹腔清洗液中伊文思兰的吸光度值显著降低（P＜0.05或P＜0.01）。活犀角与犀角相同剂量组间抗炎作用比较无显著差异。 结论: 活犀角与犀角均具有一定抗炎作用,本研究为活犀角在抗炎作用方面作为犀角的替代品进行使用提供了实验依据。     

乐食宝咀嚼片对幼龄厌食症大鼠模型的药理作用

摘 要 目的：研究乐食宝咀嚼片治疗厌食症的药理作用。方法: 大鼠随机分6组,每组10只,采用特制饲料喂养4周建立幼龄大鼠厌食症模型,从第8天起,每日给予乐食宝咀嚼片0.60,0.30,0.15 g·kg^-1,连续3周,期间观察大鼠一般状况并记录体质量和饮食量;测定胃液量、游离酸度、总酸度和胃蛋白酶活性;取血清采用测试盒方法测定总蛋白(TP)、白蛋白( Alb)、总胆固醇(TC)、胃动素（MTL）和胃泌素（GAS）的含量;以0.80,0.40,0.20 g·kg^-1剂量给予小鼠7 d,观察各组小鼠胃甲基橙排空率和小肠墨汁推进长度。结果: 乐食宝咀嚼片可明显增加幼龄厌食模型大鼠体质量和饮食量(P<0.05或P<0.01);促进胃液分泌和提高胃液中总酸及游离酸含量(P<0.05或P<0.01);能明显提高幼龄厌食模型大鼠胃蛋白酶活性(P<0.05或P<0.01);显著降低大鼠血清中TP、Alb及TC含量(P<0.05或P<0.01);升高血清中MTL和GAS水平(P<0.05或P<0.01)。同时能促进小鼠胃排空及小肠推进运动(P<0.05或P<0.01)。结论: 乐食宝咀嚼片可明显增加厌食症模型大鼠的摄食量和体质量,增强消化功能,对厌食症模型幼龄大鼠具有明显的治疗作用。     

耳复康口服液对小鼠微循环障碍的影响

摘 要 目的：观察耳复康口服液对肾上腺素致急性血瘀症小鼠微循环障碍的影响。方法: 将小鼠随机分为模型组,脑得生片组（1.35 g·kg^-1）,高(30 ml·kg^-1)、中(15 ml·kg^-1)、低(7.5 ml·kg^-1)剂量耳复康口服液组,用微循环仪观察正常小鼠给药1 h后毛细血管开放数。尾静脉注射肾上腺素造成耳廓微循环障碍,观察造模后2 min小鼠的毛细血管开放数及血流情况。结果:和模型组相比,高、中、低剂量耳复康口服液对正常小鼠耳廓毛细血管开放数无明显影响(P＞0.05);与模型组相比,高、中剂量耳复康口服液可显著改善肾上腺素致小鼠耳壳微循环障碍模型微循环血流情况(P＜0.05或P<0.01),可明显对抗肾上腺素所致小鼠耳壳微循环障碍模型毛细血管网开放数的减少(P<0.05)。结论:耳复康口服液有改善微循环障碍的作用。     

扁桃酸的镇痛抗炎作用研究

摘 要 目的：观察扁桃酸的镇痛、抗炎作用。方法: 50只昆明种SPF级小鼠随机分为5组：空白对照组（生理盐水,0.1 ml/10 g）、扁桃酸高（300 mg·kg^-1）、中（200 mg·kg^-1）、低（140 mg·kg^-1）剂量组、阿司匹林阳性对照组,ig,qd。采用小鼠扭体法和热板法观察扁桃酸的镇痛作用。采用二甲苯涂耳致小鼠急性耳肿胀观察其抗炎作用。结果: 扁桃酸各剂量组均能使小鼠扭体次数明显减少,痛阈延长,与空白对照组比较差异有统计学意义（P＜0.01）。扁桃酸高剂量组的小鼠扭体次数少于阳性对照组,差异无统计学意义（P＞0.05）,扁桃酸中、低剂量组的小鼠扭体次数多于阳性对照组,其中低剂量组差异有统计学意义（P＜0.05）; 扁桃酸各剂量组用药前后小鼠的痛阈提高率均比阳性对照组高,其中高剂量组用药前后痛阈增加明显,与阳性对照组差异有统计学意义（P＜0.05）。扁桃酸各剂量组对小鼠耳肿胀的影响无显著作用,与空白对照组比较差异无统计学意义（P＞0.05）。结论: 扁桃酸具有显著的镇痛作用,抗炎作用不明显。     

小鼠体内五味子乙素抗炎和增强免疫功能研究

摘 要 目的：研究五味子乙素对小鼠的抗炎和免疫作用。方法: 选取SPF级昆明种小鼠,随机分为空白对照组、模型对照组、阳性对照组（盐酸地塞米松5 mg·kg^-1,盐酸左旋咪唑30 mg·kg^-1）、五味子乙素低剂量组(100 mg·kg^-1)、中剂量组 (200 mg·kg^-1 )和高剂量组 (400 mg·kg^-1,盐酸左旋咪唑30mg·kg^-1)。采用二甲苯致炎与环磷酰胺致免疫低下小鼠模型,通过耳肿胀、碳粒廓清和血清血溶素等实验,以肿胀率、肿胀抑制率、碳廓清指数、吞噬指数、半数溶血值、脾指数、胸腺指数等数据为考察指标进行研究。结果:与模型对照组比较,五味子乙素高、中剂量对致炎小鼠的耳肿胀率有显著的抑制作用(P<0.05),高剂量组与阳性对照组相比差异有统计学意义（P＜0.05）;五味子乙素高剂量与模型对照组比较对免疫功能低下小鼠的廓清指数和吞噬指数有显著增加(P<0.05),且高剂量组廓清指数和吞吐噬指数显著高于低剂量组,差异有统计学意义（P＜0.01）,五味子乙素各剂量组与模型对照组相比对免疫功能低下小鼠的半数溶血值有极显著升高(P<0.01);五味子乙素各剂量组与模型对照组比较对免疫功能低下小鼠的脾指数和胸腺指数均有极显著升高(P<0.01),且呈剂量依赖型。结论:五味子乙素具有良好的抗炎和增强免疫功能的作用。     

晕吐宁颗粒抗眩晕作用研究

摘 要 目的： 晕吐宁颗粒对小鼠及豚鼠抗眩晕作用及初步机制探讨,为该药临床应用提供实验支持。方法: 机械旋转使小鼠产生眩晕后,通过迷宫实验与跳台实验测定正常组,模型组,阳性对照组(盐酸地芬尼多片,10 mg·kg^-1·d^{-1),晕吐宁颗粒低、中、高剂量三组 (3,6,12 g·kg-1·d-1)小鼠逃避电击所用时间,并观察各组眩晕小鼠的进食量;观察外耳道注入三氯甲烷的眩晕模型豚鼠摇头和眼球震颤次数,观察晕吐宁颗粒的抗眩晕作用。结果: 晕吐宁颗粒各剂量组能够显著缩短眩晕小鼠逃避电击所用时间(P＜0.01或0.05),增加眩晕小鼠进食量;降低眩晕豚鼠的摆头和眼球震颤次数(P＜0.01, P＜0.05)。结论: 晕吐宁颗粒对眩晕具有显著的治疗效果。}     

百香果果汁对D-半乳糖致衰老小鼠抗氧化作用的研究

摘 要 目的：观察不同浓度百香果果汁对D 半乳糖致衰老小鼠肝脏、心脏抗氧化作用的影响。方法: 将小鼠随机分为6组：正常对照组、模型对照组、阳性对照组（维生素C,100 mg·kg^-1）、百香果果汁低、中、高浓度组,每组8只。除正常对照组外,其余各组小鼠腹腔注射 D 半乳糖（100 mg·kg^-1）建立亚急性衰老模型,正常对照组腹腔注射等量的生理盐水,1次/d,连续42 d。造模的同时,百香果果汁治疗组小鼠分别按高、中、低浓度均灌胃给予10 ml·kg^-1相应浓度的百香果果汁,阳性对照组小鼠按100 mg·kg^-1灌胃给予维生素C,模型对照组和正常对照组均灌胃给予10 ml·kg^-1的生理盐水。给药结束后测定各组小鼠肝脏中过氧化氢酶（CAT)、谷胱甘肽（GSH)、超氧化物歧化酶（SOD）和丙二醛（MDA) 的含量;心脏中总抗氧化活力（T AOC）、SOD和MDA的含量。结果:百香果果汁治疗组能把衰老小鼠的体质量维持在一定水平,与阳性对照组比较差异无统计学意义（P＞0.05）。与模型对照组比较,百香果果汁低、中、高3种浓度组小鼠肝组织中CAT、GSH、SOD活性均明显升高,MDA明显下降,差异有统计学意义（P＜0.05或P＜0.01）,小鼠心脏组织中的T-ADC和SOD活性均明显升高,MDA含量均明显下降,除T-AOC指标的百香果果汁低浓度组外,差异有统计学意义（P＜0.01）。结论:百香果果汁有延缓D 半乳糖致衰老小鼠的作用,其机制可能与提高小鼠肝脏、心脏的抗氧化能力有关。     

苦参素胶囊对BALB/c小鼠人肝癌细胞株SMMC 7721体外种植瘤的影响

摘 要 目的：观察苦参素胶囊对BALB/c小鼠人肝癌细胞株SMMC 7721体外种植瘤的影响。方法: 采用体外传代培养人肝癌SMMC 7721细胞株,建立体外种植瘤小鼠肝癌模型。随机分为模型组、氟尿嘧啶（5 Fu）组（25 mg·kg^-1）、苦参素胶囊高剂量组（90 mg·kg^-1）、苦参素胶囊低剂量组（45 mg·kg^-1）,另设空白对照组。每组10只,连续给药14 d后。眼球取血,分离血清,Elisa法测定IL 2水平。摘取瘤株,称量湿质量,计算抑制率;HE染色,观察肿瘤组织的病理改变。结果: 与模型组比较,苦参素胶囊高、低剂量组可显著升高小鼠血清IL 2含量（P<0.01或P<0.05）;抑制体外种植瘤生长（P<0.001或P<0.05）;高剂量组上述作用与5 Fu组相比无明显差异（P>0.05）。HE染色可见小鼠肿瘤细胞核染色变浅,肿瘤细胞数量减少。结论: 苦参素胶囊对BALB/c小鼠人肝癌细胞株体外种植瘤有一定的抑制作用。     

芪防鼻敏颗粒对变应性鼻炎大鼠炎性因子表达的影响研究

摘 要 目的：观察芪防鼻敏颗粒对变应性鼻炎（AR）大鼠血清白介素 4(IL 4),白介素 17(IL 17）,肿瘤坏死因子（TNF α）及鼻黏膜γ干扰素（IFN γ）、白介素 6（IL 6）、TNF α表达的影响。方法: SD大鼠随机分为正常组,模型组,氯雷他定组（1.17 mg·kg^-1）,鼻炎康组（0.6 g·kg^-1）,芪防鼻敏颗粒高（26.48 g·kg^-1）、中（13.24 g·kg^-1）、低（6.62 g·kg^-1）剂量组。采用卵蛋白（OVA）建立AR大鼠模型。造模成功后分别灌胃给药,连续14 d。酶联免疫吸附法（ELISA）检测AR大鼠血清IL 4、IL 17、TNF α水平,免疫组化染色法（IHC）检测鼻黏膜IFN γ、IL 6、TNF α表达。结果:与正常组相比,模型组大鼠血清IL 4、IL 17水平明显上升（P<0.01）;鼻黏膜IFN γ阳性表达明显降低（P<0.05）,IL 6、TNF α阳性表达显著升高（P<0.01）。与模型组相比,氯雷他定组、芪防鼻敏颗粒中剂量组大鼠血清IL 4水平显著下降（P<0.05）,芪防鼻敏颗粒低剂量组大鼠血清IL 17水平明显下降（P<0.05）,氯雷他定组、鼻炎康组、芪防鼻敏颗粒高、中剂量组大鼠血清TNF α水平显著下降（P<0.05或P<0.01）;高、低剂量组大鼠鼻黏膜IFN γ阳性表达显著升高（P<0.05或P<0.01）,高、中剂量组IL 6阳性表达显著降低（P<0.01）,高剂量组TNF α阳性表达显著降低（P<0.01）。与氯雷他定组相比,鼻炎康组、芪防鼻敏颗粒高剂量组大鼠血清IL 17水平明显上升（P<0.05）,鼻炎康组、芪防鼻敏颗粒低剂量组大鼠血清IL 4水平明显上升（P<0.05）,芪防鼻敏颗粒高、中、低剂量组TNF α阳性表达显著升高（P<0.05）;与鼻炎康组比较,芪防鼻敏颗粒中剂量组大鼠血清IL 4水平明显下降（P<0.05）;与芪防鼻敏颗粒低剂量组相比,芪防鼻敏颗粒高剂量组大鼠血清IL 17水平明显上升（P<0.05）,芪防鼻敏颗粒中剂量组大鼠血清IL 4水平明显下降（P<0.05）。结论:芪防鼻敏颗粒可增加AR鼻黏膜IFN γ表达,降低血清IL 4、TNF α、IL 17水平及鼻黏膜TNF α、IL 6表达。     

三七总皂苷肠溶微丸对高脂血症家兔血液流变学的影响

摘 要 目的：探讨三七总皂苷（PNS）肠溶微丸对家兔血液流变学的影响。方法: 建立空白对照组、模型组、血栓通注射剂（冻干）组（15 mg·kg^-1·d^-1,im）、PNS肠溶微丸高剂量组（45 mg·kg^-1·d^-1,ig）、中剂量组（30 mg·kg^-1·d^-1,ig）、低剂量组（15 mg·kg^-1·d^-1,ig）,予高脂饲料配方灌胃造模;运用血液流变学检测方法测定各组全血黏度、血浆黏度 、红细胞聚集指数、红细胞刚性指数、红细胞电泳率5项指标。结果: 模型组血液流变学5项指标明显高于空白对照组(P<0.01),提示动物模型复制成功。与模型组比较, PNS肠溶微丸高、中剂量组均能明显降低全血黏度和血浆黏度（P<0.01或P<0.05）;PNS肠溶微丸低剂量组能显著降低中切黏度及血浆黏度（P<0.05）;PNS肠溶微丸高、中、低剂量组红细胞聚集指数显著降低（P<0.01）;PNS肠溶微丸高、中剂量组红细胞刚性指数显著降低（P<0.01或P<0.05）;PNS肠溶微丸高、中、低剂量有降低红细胞电泳率的趋势,但差异无统计学意义（P>0.05）。PNS肠溶微丸中剂量组降低中切黏度效果优于血栓通注射剂（冻干）组（P<0.05）。结论:PNS肠溶微丸能降低家兔全血黏度、血浆黏度、红细胞聚集指数、红细胞刚性指数、红细胞电泳率等指标,发挥PNS肠溶微丸活血化瘀、抑制血栓形成、增加心脑血管的血液供应的作用。     

Efficacy of gut lavage,hemodialysis, and hemoperfusion in the therapy of paraquat or diquat intoxication

Clinical and in vitro investigations were carried out to test the efficacy of gut lavage, hemodialysis, and hemoperfusion in the treatment of poisoning with paraquat or diquat. In a patient suffering from diquat intoxication 130 times more diquat was removed by gut lavage 30 h after ingestion than was removed by complete aspiration of the gastric contents.Determination of in vitro clearances for paraquat and diquat by hemodialysis showed that, at serum concentrations of 1–2 ppm, such as are frequently encountered in poisoning in man, toxicologically relevant quantities of herbicide cannot be removed from the body. At a concentration of 20 ppm, on the other hand, hemodialysis proved to be effective, the clearance being 70 ml/min at a blood flow rate of 100 ml/min. The efficacy of hemoperfusion with coated activated charcoal was on the whole better. Especially at concentrations around 1–2 ppm, the clearance values for hemoperfusion were some 5–7 times higher than those for hemodialysis.In a patient suffering from paraquat poisoning, both hemodialysis as well as hemoperfusion were carried out. The in vitro results could be confirmed: At serum concentrations of paraquat less than 1 ppm no clearance could be obtained by hemodialysis while by hemoperfusion with activated charcoal quite high clearance values were measured and the serum level dropped down to zero.

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Zusammenfassung Klinische Untersuchungen und Laboratoriumsversuche wurden durchgeführt, um die Wirksamkeit von Darmspülung, Hämodialyse und Hämoperfusion bei Paraquat- und Deiquat-Vergiftungen zu prüfen.Bei einem Patienten wurde 30 Std nach Deiquat-Aufnahme durch Darmspülung 130mal mehr Deiquat entfernt als durch vollständige Aspiration des Mageninhaltes. In vitro-Versuche ergaben, daß bei Blutserumkonzentrationen von 1–2 ppm, die bei Vergiftungen oft gemessen werden, durch Hämodialyse keine toxikologisch relevanten Paraquat- oder Deiquat-Mengen entfernt werden können. Dagegen erwies sich die Hämodialyse bei 20 ppm und einer Blutumlaufgeschwindigkeit von 100 ml/min mit einer Clearance von 70 ml/min als wirksam. Die Hämoperfusion mit beschicheter Aktivkohle war in diesen Versuchen aber eindeutig überlegen, denn insbesondere bei Konzentrationen um 1–2 ppm waren die Clearance-Werte 5–7mal höher als bei der Hämodialyse.Die in vitro-Ergebnisse wurden bei einem Patienten mit einer Paraquat-Vergiftung bestätigt: Bei Konzentrationen unter 1 ppm war die Hämodialyse wirkungslos, während durch Hämoperfusion relativ hohe Clearance-Werte erreicht wurden, so daß der Serumspiegel rasch unter die Nachweisgrenze abfiel.

     

In vitro studies on sterically stabilized liposomes (SL) as enzyme carriers in organophosphorus (OP) antagonism

This study describes a new approach for organophosphorous (OP) antidotal treatment by encapsulating an OP hydrolyzing enzyme, OPA anhydrolase (OPAA), within sterically stabilized liposomes. The recombinant OPAA enzyme was derived from Alteromonas strain JD6. It has broad substrate specificity to a wide range of OP compounds: DFP and the nerve agents, soman and sarin. Liposomes encapsulating OPAA (SL)* were made by mechanical dispersion method. Hydrolysis of DFP by (SL)* was measured by following an increase of fluoride ion concentration using a fluoride ion selective electrode. OPAA entrapped in the carrier liposomes rapidly hydrolyze DFP, with the rate of DFP hydrolysis directly proportional to the amount of (SL)* added to the solution. Liposomal carriers containing no enzyme did not hydrolyze DFP. The reaction was linear and the rate of hydrolysis was first order in the substrate. This enzyme carrier system serves as a biodegradable protective environment for the recombinant OP-metabolizing enzyme, OPAA, resulting in prolongation of enzymatic concentration in the body. These studies suggest that the protection of OP intoxication can be strikingly enhanced by adding OPAA encapsulated within (SL)* to pralidoxime and atropine.     

Aquatic Insects and Trace Metals: Bioavailability,Bioaccumulation, and Toxicity

Abstract

The uptake of metals from food and water sources by insects is thought to be additive. For a given metal, the proportions taken up from water and food will depend both on the bioavailable concentration of the metal associated with each source and the mechanism and rate by which the metal enters the insect. Attempts to correlate insect trace metal concentrations with the trophic level of insects should be made with a knowledge of the feeding relationships of the individual taxa concerned. Pathways for the uptake of essential metals, such as copper and zinc, exist at the cellular level, and other nonessential metals, such as cadmium, also appear to enter via these routes. Within cells, trace metals can be bound to proteins or stored in granules. The internal distribution of metals among body tissues is very heterogeneous, and distribution patterns tend to be both metal and taxon specific. Trace metals associated with insects can be both bound on the surface of their chitinous exoskeleton and incorporated into body tissues. The quantities of trace meals accumulated by an individual reflect the net balance between the rate of metal influx from both dissolved and particulate sources and the rate of metal efflux from the organism. The toxicity of metals has been demonstrated at all levels of biological organization: cell, tissue, individual, population, and community. Much of the literature pertaining to the toxic effects of metals on aquatic insects is based on laboratory observations and, as such, it is difficult to extrapolate the data to insects in nature. The few experimental studies in nature suggest that trace metal contaminants can affect both the distribution and the abundance of aquatic insects. Insects have a largely unexploited potential as biomonitors of metal contamination in nature. A better understanding of the physico-chemical and biological mechanisms mediating trace metal bioavailability and exchange will facilitate the development of general predictive models relating trace metal concentrations in insects to those in their environment. Such models will facilitate the use of insects as contaminant biomonitors.     

Steroidal sapogenin contents in some domestic plants

In order to find out the values of the steroid resources for the future use. the compositions and contents of steroidal sapogenins from 13 domestic plants have been investigated. As a result,Dioscorea nipponica, D. quinqueloba andSmilax china were found to have large amount of diosgenin. And pennogenin inTrillium kamtschaticum andParis verticillata, yuccagenin inAllium fistulosum, hecogenin inAgave americana and neochlorogenin inSolanum nigum were appeared to be major steroidal sapogenins.     

Alzheimer’s disease – current trends in basic and clinical research. Highlights from the 16th ECNP

Advances in the molecular biological knowledge of neuronal nicotinic acetylcholine receptors (nAChRs) have led to a growing interest by the pharmaceutical industry in the development of novel compounds that selectively modulate nAChR function. The ability of (-)-nicotine, an activator of nAChRs, to enhance attentional aspects of cognition in animals and humans, to exert neuroprotective and anxiolytic-like effects, and presumably to mediate the negative correlation between smoking and Alzheimer's (and Parkinson's) Disease, has focused interest on the potential therapeutic utility of modulators of nAChR function for treatment of some of the deficits associated with these progressive, neurodegenerative conditions. Numerous compounds are known which activate nAChRs and which might serve as lead compounds toward the development of such agents. The pharmacologic diversity of neuronal nAChR subtypes suggests the possibility of developing selective compounds which would have more favourable side-effect profiles than existing agents. This broader class of agents, collectively called cholinergic channel modulators (ChCMs), is anticipated to encompass compounds which would have more favourable side-effect profiles than existing agents, which generally exhibit low selectivity. This selectivity may be achieved by preferentially activating some subtypes of nAChRs (i.e., Cholinergic Channel Activators, ChCAs) or inhibiting the function of other subtypes (Cholinergic Channel Inhibitors, ChCIs). An overview of the biology of nAChRs and the rationale for the use of ChCMs for the treatment of dementia related to neurodegenerative diseases are presented, followed by a discussion of lead compounds and compounds under consideration for clinical evaluation.