氨杞精口服液对小鼠耐缺氧及抗疲劳作用的实验研究

目的:观察氨杞精口服液对小鼠耐缺氧能力和抗疲劳能力的影响。方法:将小鼠随机分为3组,分别为空白对照组、氨杞精口服液低剂量组、高剂量组,连续灌胃给药30 d后,测定小鼠的缺氧存活时间、负重游泳存活时间、血清尿素氮、血乳酸、肝糖原和肌糖原含量等指标的变化。结果:氨杞精口服液可以明显延长小鼠缺氧存活时间,并延长小鼠负重游泳持续时间,降低血乳酸、血清尿素氮含量,提高肝糖原含量和肌糖原含量。结论:氨杞精口服液具有提高小鼠耐缺氧及抗疲劳的作用。     

缢蛏水解物的抗疲劳作用

目的研究缢蛏水解物(HSC)的抗疲劳作用及机制。方法采用不同浓度HSC溶液灌胃给药,30 d后测定小鼠负重游泳时间及血清尿素氮含量、血浆乳酸浓度、血清乳酸脱氢酶活性、血红蛋白浓度、肝糖原与肌糖原含量等生化指标。结果 HSC可明显延长小鼠负重游泳时间,显著降低运动后小鼠的血清尿素氮含量和血乳酸水平,提高了血红蛋白浓度、肝糖原与肌糖原水平及乳酸脱氢酶的活性。结论 HSC具有良好的抗疲劳作用。     

板蓝根活性组分对小鼠耐缺氧及抗疲劳作用的实验研究

目的观察板蓝根活性组分(ACRI)对小鼠的耐缺氧及抗疲劳作用,并探讨其作用机制。方法根据体重将ICR小鼠随机分成5组:空白对照组、ACRI 25、50、100 mg·kg~(-1)3个剂量组及西洋参口服液3 m L·kg~(-1)组,连续给小鼠灌胃14 d,观察小鼠一般生长情况;分别采用常压耐缺氧实验和负重游泳实验,观察ACRI对小鼠的耐缺氧及抗疲劳作用;并通过检测血清与肝脏的超氧化歧化酶(superoxide dismutase,SOD)活性、丙二醛(maleic dialdehyde,MDA)含量及血尿素氮、血乳酸、肝糖原水平,探讨其可能机制。结果ACRI可以明显降低小鼠体重增长率,延长常压缺氧条件下小鼠存活时间和小鼠负重游泳时间;ACRI能够增强小鼠血清和肝脏SOD活性,降低MDA含量,提高肝糖原储备量,降低小鼠游泳后血尿素氮和血乳酸水平。结论 ACRI具有明显的耐缺氧和抗疲劳作用。     

蒙药那仁满都拉对小鼠的抗疲劳作用

目的 观察蒙药那仁满都拉对小鼠的抗疲劳作用.方法 通过小鼠负重游泳试验、肝糖原测定、耐缺氧实验以及耐热实验对那仁满都拉抗疲劳作用进行综合考察.结果 那仁满都拉能显著延长小鼠负重游泳时间、增加小鼠肝糖原的量、延长耐缺氧时间和耐热时间.结论 蒙药那仁满都拉具有显著抗疲劳作用.     

复方双参合剂对小鼠耐缺氧和抗运动疲劳能力的影响

目的：研究复方双参合剂对小鼠耐缺氧和抗疲劳的作用。方法：50只小鼠随机分为空白组（生理盐水10 ml·kg~（-1））、丹参组（丹参提取物0.2 g·kg~（-1））、人参组（人参皂苷0.1 g·kg~（-1））、复方双参组（丹参提取物0.2 g·kg~（-1）＋人参皂苷0.1 g·kg~（-1））和红景天组（阳性对照,红景天提取物0.6 g·kg~（-1））,每组10只。连续灌胃给药20 d后,测定小鼠常压密闭缺氧存活时间、减压缺氧存活率和负重游泳时间,并测定小鼠运动后血清尿素氮含量、肝糖原含量、血乳酸含量和乳酸脱氢酶活性。结果：与空白组相比,复方双参组小鼠常压密闭缺氧存活时间显著延长,延长率为45.95%（P〈0.01）;小鼠运动后血清尿素氮含量及乳酸堆积显著减少（P〈0.01）,肝糖原含量及乳酸脱氢酶活性显著增加（P〈0.01）,其作用强于红景天组。减压缺氧条件下,给药组存活率较空白组显著提高（P〈0.05或0.01）。红景天组与复方双参组与其他给药组相比,小鼠负重游泳时间显著延长（P〈0.05或0.01）。结论：复方双参合剂能显著增强小鼠耐缺氧和抗疲劳的能力。     

方格星虫多糖对运动小鼠抗疲劳作用实验研究

目的探讨方格星虫多糖对小鼠的抗疲劳作用。方法将小鼠随机分组,采用小鼠负重游泳实验,以方格星虫多糖0.2,0.4,0.6g.kg-1灌胃给药,测定各组游泳时间,并对游泳后小鼠的血清尿素氮、乳酸脱氢酶、肝糖原、肌糖原、超氧化物歧化酶、丙二醛等指标进行检测。结果与对照组相比,星虫多糖各剂量组明显延长了小鼠的游泳时间。相应剂量给药小鼠血清尿素氮有明显减低,乳酸脱氢酶显著升高,肝糖原、肌糖原也呈上升趋势,低剂量用药能显著提高SOD活性和降低MDA含量。结论星虫多糖对小鼠有明显抗疲劳效果。     

含二十二碳六烯酸和大豆磷脂复方制剂的抗疲劳实验

目的研究含二十二碳六烯酸和大豆磷脂复方制剂的抗疲劳功能。方法给小鼠口服不同剂量供试品 ,进行负重游泳试验 ,记录游泳时间并测定血清尿素氮 ;口服供试品测定肝糖原含量和运动后血乳酸升高和运动休息后血乳酸的消除。结果经口服供试品 ,能延长小鼠的游泳时间 ,增加肝糖原的储量 ,降低运动后血乳酸升高幅度。结论该制剂具有抗疲劳的功能。     

阿魏菇胶囊抗疲劳作用的实验研究

目的 研究阿魏菇胶囊的抗疲劳作用.方法 小鼠每日经口给予不同剂量阿魏菇胶囊,连续30 d后,对小鼠进行负重游泳实验,检测运动后小鼠的乳酸、肝糖原、尿素氮指标.结果 不同剂量阿魏菇胶囊均能延长小鼠负重游泳时间,同时小鼠运动后产生的乳酸含量、肝糖原消耗量、血清尿素氮较对照组明显减少.结论 阿魏菇胶囊有抗疲劳作用.     

黄秋葵提取物抗疲劳的实验研究

目的观察黄秋葵水提物对实验动物的抗疲劳作用,探讨黄秋葵水提物抗疲劳作用的机制。方法以观察小鼠负重力竭游泳时间探讨黄秋葵提取物抗疲劳作用;测定小鼠游泳前后血清尿素的变化、小鼠肝糖原含量、小鼠血乳酸等探讨抗疲劳机制。结果黄秋葵提取物能明显延长小鼠负重游泳时(P<0.05),减少小鼠血清尿素产生(P<0.01),减少小鼠血乳酸含量(P<0.05),对小鼠肝糖原含量无明显影响。结论黄秋葵提取物具有良好的抗疲劳作用。该作用可能与提高小鼠代谢能力和增强应激能力有关。     

珍珠粉抗疲劳作用的实验研究

目的:探讨珍珠粉对小鼠的抗疲劳作用.方法:经灌胃给予小鼠珍珠粉0.125,0.250,0.500 g·kg-1·d-1(分别相当于人体推荐摄入量的5,10和20倍),分别观察小鼠的体重、负重游泳时间、血清尿素含量、肝糖原含量和血乳酸含量.结果:珍珠粉对实验小鼠体重未见影响;在0.500g·kg-1·d-1时能延长小鼠负重游泳时间和降低运动后小鼠血清尿素含量;在0.250,0.500 g·kg-1·d-1时能增加小鼠肝糖原;且无降低运动小鼠血乳酸的作用.结论:珍珠粉具有增强小鼠抗疲劳的作用.     

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.

     

Synthesis,Cytotoxicity and Antileishmanial Activity of Some N-(2-(indol-3-yl)ethyl)-7-chloroquinolin-4-amines

We report herein the condensation of 4,7-dichloroquinoline (1) with tryptamine (2) and D-tryptophan methyl ester (3) . Hydrolysis of the methyl ester adduct (5) yielded the free acid (6) . The compounds were evaluated in vitro for activity against four different species of Leishmania promastigote forms and for cytotoxic activity against Kb and Vero cells. Compound (5) showed good activity against the Leishmania species tested, while all three compounds displayed moderate activity in both Kb and Vero cells.     

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.     

Glycofection: The Ubiquitous Roles of Sugar Bound on Glycoplexes

Glycofection (transfection by using sugar-substituted polylysine) was assessed in order to provide an alternative to viral vectors for the transfer of genes into vascular smooth muscle cells. A rabbit vascular smooth muscle cell line (Rb-1 cells) was selectively transfected by using glycoplexes (glycosylated polylysine/pSV2LUC complexes) in the presence of 10 mu M of the fusogenic peptide GALA. A sugar-specific transfection was obtained when the glycofection was conducted for 1 h with glycoplexes containing either alpha Gal, alpha -Glc, alpha -GalNAc, beta -GlcNAc, or beta -GalNAc residues. The gene expression was high after transfection, with glycoplexes bearing alpha Gal, alpha -GalNAc, or beta -GalNAc residues that were weakly internalized, and low with glycoplexes carrying Lact or Rha residues that were well taken up by cells. These results suggest that 1) glycofection can be a good approach for a selective transfer of genes intovascular smooth muscle cells, 2) an efficient uptake of the glycoplexes is not the unique limiting step for an efficient transfection, and 3) the sugar-dependent trafficking of the glycoplexes inside the cells may account for the transfection efficiency.     

直肠癌下切缘病理组织学分析

目的探讨直肠癌逆向浸润与下切缘的安全距离的关系。方法对36例直肠癌Miles手术和Dixon手术后标本的肿瘤下缘1.0cm、2.0cm、3.0cm的肠壁及对应的系膜病理组织学检查,观察直肠癌逆向浸润或转移的距离。结果36例直肠癌标本距癌肿下缘1.0 cm、2.0cm、3.0cm的肠壁及对应的系膜病理组织学检查均为阴性,结论直肠癌远恻逆向浸润或转移未见超过1.0cm,因此认为保肛手术时切除肿瘤远侧肠管(包括系膜)2.0cm是安全的。