烟酰水杨酸对鹌鹑实验性动脉粥样硬化的预防作用

目的探讨烟酰水杨酸(N icotinylsalicylic ac id,NSA)对高脂饲料诱导的鹌鹑实验性动脉粥样硬化的预防作用。方法91只♂朝鲜种鹌鹑,随机分为6组,组1:普通饲料组(对照组)、组2:高脂饲料组(造模组)、组3:高脂饲料+NSA150 mg.kg-1.d-1、组4:高脂饲料+NSA 300 mg.kg-1.d-1、组5:高脂饲料+烟酸75 mg.kg-1.d-1+乙酰水杨酸75 mg.kg-1.d-1、组6:高脂饲料+烟酸150 mg.kg-1.d-1。动态监测(0、4和8 wk)其血浆总胆固醇(TC)、甘油三酯(TG)、高密度脂蛋白胆固醇(HDL-C)、低密度脂蛋白胆固醇(LDL-C)和丙二醛(MDA),8 wk末处死动物,观察主动脉及左、右头臂动脉病理变化和TC、TG含量;观察心脏病理变化。结果高脂饲料可使鹌鹑血脂发生紊乱,血浆TC、TG水平增加,LDL-C、MDA明显升高,HDL-C水平下降;主动脉及左、右头臂动脉壁TC、TG含量升高,并有明显的动脉粥样硬化斑块形成。NSA可降低高脂饲料喂养的鹌鹑血浆TC、TG、LDL-C、MDA水平,升高HDL-C水平,动脉壁TC、TG含量降低,主动脉及左、右头臂动脉的AS斑块形成减轻。结论NSA对高脂饲料诱导的鹌鹑实验性动脉粥样硬化有预防作用。     

复方尼阿措提取物对高脂血症大鼠的调血脂作用

目的:探讨复方尼阿措提取物(CNAE)的调血脂作用。方法:通过灌胃脂肪乳剂制备实验性高脂血症大鼠模型。随机分为正常对照组、模型对照组、阳性对照组(1 mL.kg-1)、柳茶水提物(SAE)低、高剂量组(6.01,2.0 g.kg-1)、CNAE低、高剂量组(8.0,16.0 g.kg-1)。除正常组外,各给药组大鼠灌胃给予脂肪乳剂,基础饲料喂养,末次给药后,腹主动脉采血测定血清总胆固醇(TC)、甘油三脂(TG)、低密度脂蛋白胆固醇(LDL-C)、高密度脂蛋白胆固醇(HDL-C)和丙二醛(MDA)的含量及超氧化物歧化酶(SOD)、谷胱甘肽过氧化物酶(GSH-Px)活性。结果:CNAE能明显降低TC、TG、LDL-C和MDA含量(P<0.01),升高HDL-C浓度,显著提高SOD及GSH-Px酶活性(P<0.01),且降血脂作用优于SAE。结论:CNAE具有明显的调血脂和抗氧化作用,提示其可用于高脂血症的防治。     

降脂灵降血脂作用的实验研究

目的观察降脂灵药物对动物高血脂的影响。方法以降脂灵1.5g.kg-1.d-1、3g.kg-1.d-1、6.0g.kg-1.d-1低、中、高3个剂量分别给予腹腔注射蛋黄乳液致高血脂小鼠及高脂饲料喂养致高血脂大鼠,观察降脂灵对受试动物血清总胆固醇(TC)、甘油三酯(TG)、高密度脂蛋白胆固醇(HDL-C)、低密度脂蛋白胆固醇(LDL-C)及总胆固醇与高密度脂蛋白胆固醇比值(TC/HDL-C)的影响。结果该制剂中、高剂量显著降低高脂小鼠血清TC(P<0.05);高剂量组显著降低高脂小鼠血清TG(P<0.01);中剂量组可显著降低高脂大鼠血清TC(P<0.05)、TG(P<0.05)及TC/HDL-C(P<0.01),并且显著提高HDL-C的含量(P<0.05);高剂量组显著降低高脂大鼠血清TC(P<0.01)、TG(P<0.01)及LDL-C(P<0.05)、TC/HDL-C(P<0.05)。结论降脂灵对高血脂动物有明显的降脂和调节脂代谢作用。     

刘氏降脂化瘀口服液对实验性高脂血症兔血脂水平的影响

目的：观察刘氏降脂化瘀口服液对实验性高脂血症兔血脂水平的影响。方法：家兔喂高脂饲料连续4周造成高血脂模型，给药组同时灌服刘氏降脂化瘀口服液12，24g／kg，测定给药前及给药2周和4周时血清总胆固醇(TC)，甘油三醇(TG)，高密度脂蛋白胆固醇(HDL-C)和低密度脂蛋白胆固醇(LDL-C)。结果：刘氏降脂化瘀口服液灌胃2-4周可使血清TC和LDL-C水平显著降低，大剂量组(24g／kg)，也能降低血清TG。结论：刘氏降脂化瘀口服液对高脂血症兔具有较好的降血脂作用。     

栀子黄色素与栀子苷降血脂和体内抗氧化作用的比较

目的 比较栀子中栀子黄色素与栀子苷的降血脂和体内抗氧化作用.方法 饲喂小鼠高脂高胆固醇饲料8周,第5 ～8周分别每日ig给予栀子苷和栀子黄色素(100 mg· kg-1),以辛伐他汀(10 mg·kg-1)为阳性对照;检测小鼠血清中的总胆固醇(TC)、甘油三酯(TG)、低密度蛋白胆固醇(LDL-C)、高密度蛋白胆固醇(HDL-C)和丙二醛(MDA)的水平,测定血清中超氧化物歧化酶(SOD)和过氧化氢酶(CAT)的活力.结果 栀子黄色素能显著降低高脂血症小鼠血清中TC、TG、LDL-C的水平,升高HDL-C的水平;同时增强SOD和CAT酶的活力,降低MDA的含量;栀子苷虽能显著降低各血脂指标,但对体内抗氧化作用无明显效果.结论 栀子中的栀子黄色素与栀子苷均有降血脂的功能,但栀子黄色素的体内抗氧化作用效果更强.     

复方苦豆子颗粒对高脂血症大鼠血脂代谢的影响

目的:观察复方苦豆子颗粒对高脂血症大鼠血脂代谢的影响。方法:除空白对照组外,用喂饲高脂饲料法复制大鼠高脂模型,实验分空白对照组、高脂模型组、复方苦豆子颗粒组(低、中、高剂量组,分别喂饲生药7g.kg-1.d-1、15g.kg-1.d-1、22g.kg-1.d-1)、血脂康组(0.8g.kg-1.d-1),给药后每4wk抽1次血,连续3次,分别测定血浆总胆固醇(TC)、甘油三酯(TG)、低密度脂蛋白胆固醇(LDL-C)、极低密度脂蛋白胆固醇(VLDL-C)、高密度脂蛋白胆固醇(HDL-C)、丙二醛(MDA)含量变化。结果:高脂模型组血浆TC、TG、LDL-C、VLDL-C、HDL-C和MDA含量显著上升,同时动脉粥样硬化指数(AI)增加;给予复方苦豆子颗粒4wk后,各组血浆TC、TG、LDL-C、VLDL-C、MDA及AI水平均降低,且呈剂量依赖性。结论:复方苦豆子颗粒对高脂血症大鼠具有调血脂作用。     

金线莲甲醇提取物降脂作用研究

目的研究金线莲甲醇提取物对高血脂大鼠血脂及肝酯水平的影响。方法采用高脂饲料喂养致大鼠高脂血症模型,给予不同剂量的金线莲甲醇提取物给药后治疗,实验设正常组,模型组,辛伐他汀组,非诺贝特组和金线莲总膏高、中、低剂量(1 000、500、250 mg·kg-1)组,分别测定血清总胆固醇(TC)、三酰甘油(TG)、高密度脂蛋白胆固醇(HDL-C)、低密度脂蛋白胆固醇(LDL-C)和肝脏组织匀浆中TC和TG的含量,并做肝脏病理学观察。结果金线莲总膏500、1 000 mg·kg-1剂量组可明显降低大鼠血清TC、TG和LDL-C的水平,并能显著提高血清HDL-C含量,其中高剂量组效果最好。另外高剂量组可显著降低肝脏TC和TG的水平。结论金线莲甲醇提取物在高血脂大鼠模型中具有显著地降血脂和肝脂作用。     

南极磷虾油对高脂血症大鼠血脂和抗氧化力的影响

目的探讨南极磷虾油对实验性高脂血症大鼠血脂和抗氧化力的影响。方法高脂饲料建立高脂血症大鼠模型,分别灌胃50,100和500 mg.kg-1南极磷虾油,连续30 d,测定大鼠血清总胆固醇(TC),甘油三酯(TG),低密度脂蛋白胆固醇(LDL-C),高密度脂蛋白胆固醇(HDL-C)、血清一氧化氮(NO)、超氧化物歧化酶(SOD)、谷胱甘肽过氧化物酶(GSH-PX)以及丙二醛(MDA)水平。结果南极磷虾油能显著降低高脂血症大鼠血清中的TC、TG和LDL-C含量,降低动脉粥样硬化指数(AI)。提高大鼠血清中NO含量,提高SOD和GSH-PX活性,降低MDA含量。结论南极磷虾油对高脂血症大鼠具有调血脂的作用和抗氧化作用,其抵抗动脉粥状硬化方面的作用优于深海鱼油。     

山楂叶总黄酮对家兔实验性动脉粥样硬化的影响

目的 研究山楂叶总黄酮对家兔实验性动脉粥样硬化的影响。方法 饲喂高脂饲料建立动脉粥样硬化家兔模型,测定家兔血清总胆固醇(TC)、甘油三酯(TG)、高密度脂蛋白(HDL-C)及低密度脂蛋白(LDL-C)含量。取主动脉做病理检查,免疫组化分析Bax、Bcl-2在粥样硬化斑块中的表达。结果 病理检查结果表明,山楂叶总黄酮能明显减轻模型家兔动脉粥样硬化性损伤。山楂叶总黄酮能降低动脉粥样硬化家兔血清TG含量,升高HDL-C含量。免疫组化显示,与模型组比较,山楂叶总黄酮组Bax的表达显著降低,Bcl-2的表达显著升高,而且Bax/Bcl-2的比值降低。结论 山楂叶总黄酮通过降低血脂,调节Bax、Bcl-2表达而发挥抗家兔实验性动脉粥样硬化作用。     

野山杏果肉总有机酸对高脂血症小鼠血脂及肝脏的影响

目的 研究野山杏果肉总有机酸(TOAWA)对高脂血症小鼠血脂的影响及其保肝作用.方法 ig给予小鼠高脂乳剂,建立小鼠高脂血症模型,每日ig给予小鼠不同剂量的TOAWA(0.1、0.2、0.4g·kg-1),连续4周,测定小鼠血清中总胆固醇(TC)、低密度脂蛋白-胆固醇(LDL-C)、高密度脂蛋白-胆固醇(HDL-C)及三酰甘油(TG)的含量和肝脏匀浆液中超氧化歧化酶(SOD)、丙二醛(MDA)的水平,计算肝脏的脏器指数,观察肝脏组织的病理学变化.结果 TOAWA能显著降低小鼠血清中TC、LDL-C、TG的水平,升高HDL-C的含量,提高肝脏中SOD的活性,减少MDA的形成,同时降低肝脏的脏器指数;对高血脂症小鼠肝脏细胞的病理变化具明显的改善作用.结论 TOAWA能调节高血脂症小鼠的血脂水平,并具一定的保护肝脏和改善肝功能的作用.     

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.     

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.     

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.