木通提取物对实验性大鼠静脉血栓形成的影响

目的 探讨活血化瘀中药木通的提取物对大鼠实验性静脉血栓形成的影响,为木通提取物治疗静脉血栓提供实验依据。方法 利用大鼠静脉血栓形成模型测定给予木通提取物100,200 mg·kg-1后血栓湿重和干重,另有模型组(给予0.9%氯化钠溶液)和阳性对照组(华法林)进行对比,分别计算其各血栓形成抑制率。结果 木通提取物100 mg·kg-1组对大鼠静脉血栓形成有一定影响,木通提取物200 mg·kg-1组可以明显抑制大鼠静脉血栓形成,减轻血栓湿重和干重,对血栓湿重抑制率分别为19.9%和48.6%,对血栓干重抑制率分别为15.5%和42.8%。 结论 木通提取物可抑制大鼠实验性静脉血栓形成。     

木通提取物对实验性大鼠静脉血栓形成的影响

目的探讨活血化瘀中药木通的提取物对大鼠实验性静脉血栓形成的影响,为木通提取物治疗静脉血栓提供实验依据。方法利用大鼠静脉血栓形成模型测定给予木通提取物100,200mg·kg^-1后血栓湿重和干重,另有模型组（给予0.9%氯化钠溶液）和阳性对照组（华法林）进行对比,分别计算其各血栓形成抑制率。结果木通提取物100mg·kg^-1组对大鼠静脉血栓形成有一定影响,木通提取物200mg·kg^-1组可以明显抑制大鼠静脉血栓形成,减轻血栓湿重和干重,对血栓湿重抑制率分别为19.9%和48.6%,对血栓干重抑制率分别为15.5%和42.8%。结论木通提取物可抑制大鼠实验性静脉血栓形成。     

参桂提取物对实验性前列腺增生大鼠尿动力学的影响

目的 研究参桂提取物对大鼠实验性前列腺增生的治疗作用。方法将60只SD大鼠随机分为6组，每组10只。除假手术组外，其他5组大鼠均在无菌条件下行去势手术，术后1周分别皮下注射溶于橄榄油的丙酸睾丸酮，以制作前列腺增生模型。随后模型对照组给予0.9%氯化钠溶液，5 mL·kg 1；阳性对照组给予普乐安片，2.5 g·kg 1；参桂提取物低、中、高剂量组分别给予参桂提取物0.38 ，0.75和1.50 g·kg 1。假手术组给予假手术后，每天给予0.9%氯化钠溶液0.5 mL。所有大鼠均连续给药4周，末次给药后1 h称重，进行大鼠尿动力学测定，称取前列腺湿重和干重，计算湿重和干重指数。结果参桂提取物高、中剂量组大鼠每日以1.50和0.75 g·kg 1参桂提取物灌胃给药，连续4周后可抑制丙酸睾丸酮引起的大鼠前列腺增生，尿动力学参数明显改善，尿程延长，尿量增加，剩余尿量减少，排尿阈值压均有下降(P＜0.01或P＜0.05)；与模型组比较，前列腺湿重、湿重指数、干重及干重指数均下降（均P＜0.01）。结论参桂提取物可抑制大鼠前列腺增生，明显改善大鼠实验性前列腺增生导致的尿动力学参数。     

甘草酸二铵对动物静脉血栓形成及凝血时间的影响

目的：研究甘草酸二铵(diammonium glycyrrnizinate, DG)对实验动物静脉血栓形成及凝血时间的影响；方法：给家兔耳缘静脉、大白鼠颈外静脉及小白鼠尾静脉注射DG 10～20 mg·kg 1，静脉注射30 min后，观察其对动物体外血栓形成及凝血时间的影响。结果：10～20 mg·kg 1的DG对大白鼠体外血栓形成有抑制作用，抑制率分别为68.7%，72.5%；对家兔体外血栓形成有抑制的作用，抑制率分别为12.7%，26.7%；对小白鼠体外凝血时间有延长作用，与0.9%氯化钠注射液比较差异有极显著性(P＜0.01)。结论：10～20 mg·kg 1 DG对家兔、大白鼠体外血栓形成有抑制作用，对小白鼠凝血时间有延长作用。     

芎麻滴丸对血管性认知障碍大鼠社交行为的影响

目的 观察双侧颈总动脉结扎致血管性认知障碍大鼠社交行为的变化,探讨芎麻滴丸对其干预作用。方法 采用永久性结扎双侧颈总动脉法制备血管性认知障碍模型。实验大鼠随机分为假手术组（生理盐水10 mL·kg^-1）,模型组（生理盐水10 mL·kg^-1）,芎麻滴丸高剂量组（生药1.5 g·kg^-1）,芎麻滴丸低剂量组（生药0.75 g·kg^-1）。模型制备第28,42天采用Morris水迷宫对大鼠的学习记忆能力进行测试;模型制备第7,14,28,42天用社交行为仪检测大鼠社交能力的变化。结果 模型制备第7,14天大鼠社交行为无明显变化,模型制备第28天和第42天,模型组大鼠持续接触时间减少（P<0.05）;模型制备第42天,模型组大鼠接触次数减少,逃避潜伏期显著增加,穿越平台次数显著减少（P<0.01）。与模型组大鼠相比,模型制备第28天,芎麻滴丸高剂量组大鼠接触次数显著增加（P<0.05）;芎麻滴丸高、低剂量组大鼠持续接触时间显著增加（P<0.05或<0.01）;模型制备第42天,芎麻滴丸低剂量组大鼠接触次数和持续接触时间增加（P<0.05）,芎麻滴丸高、低剂量组大鼠逃避潜伏期显著减少（P<0.01）。结论 模型制备第42天大鼠出现学习记忆障碍;模型组大鼠第28天大鼠开始出现社交行为障碍,经芎麻滴丸干预后,接触时间和接触次数增加,即可认为其有效缓解由双侧颈总动脉结扎造成的社交能力障碍,且低剂量效果优于高剂量。     

脑安胶囊萃取液对大鼠血栓形成的影响

目的 　评价脑安胶囊萃取液抗血栓形成的作用。方法 　采用超临界 CO2 流体萃取技术 ,分离出脑安胶囊的萃取液。参照动 -静脉旁路血栓形成法 ,建立大鼠血栓形成模型。以不同浓度的脑安胶囊萃取液及阳性药物阿司匹林用于实验大鼠 3 d后 ,分别测定血栓湿重。结果 　脑安胶囊萃取液高剂量组 ( 80 mg· kg- 1 )和阿司匹林 ( 3 0 0 mg· kg- 1 )对照组的血栓湿重显著减少 ,与溶剂对照比较 ,P均 <0 .0 5 ;但两组间比较 ,P>0 .0 5 ;而脑安胶囊萃取液 2 0 ,40 mg· kg- 1 组的血栓湿重与溶剂对照组比较 ,P均 >0 .0 5。结论　脑安胶囊萃取液高剂量对实验性大鼠血栓形成有拮抗作用     

复方藻酸双脂钠抗血栓作用的实验研究

目的探讨复方藻酸双脂钠(CoPss)对大鼠实验性血栓形成的影响。方法采用对大鼠连续两周灌胃给药,分别对体内,体外血栓形成的2种模型观察其药物作用,包括血栓的湿重,干重及两种模型血栓形成的时间。结果实验组大鼠体外形成的血栓其湿重和干重均低于生理盐水对照组(P<0.01)并可使大鼠体内血栓形成时间显著延长(P<0.01)。结论实验证明CoPss对血栓形成有抑制作用,且抗血栓作用与剂量有明显依赖关系。     

仙牛颗粒的降血糖作用研究

［摘要］目的观察仙牛颗粒对大鼠实验性糖尿病血糖的影响。方法采用链脲佐菌素复制糖尿病模型大鼠60只，随机分为6组，每组10只，分别给予仙牛颗粒0.30，1.20 g·kg-1·d-1,二甲双胍150 mg·kg-1·d-1 （阳性对照组），灵菊七1.00，4.00 g·kg-1·d-1， 羧甲基纤维素钠（CMC Na，模型对照组）20 mg·kg-1·d-1 。另设一组空白对照组（给予等体积0.5% CMC Na）。0.5%连续给药14 d后，分别测定大鼠的血糖。结果仙牛颗粒可显著降低糖尿病大鼠的血糖，与模型对照组比较，差异有显著性（P＜0.05）。结论仙牛颗粒剂具有降低糖尿病大鼠血糖的作用。     

贻贝多活素的药理学研究

观察了贻贝多海素（ＭＳＭ）对实验性血栓形成和血小板聚集的影响。大鼠经ｉｇＭＳＭ１．３５、２．７和５．４ｇ（ｋｇ．ｄ）连续２８天后，对“旋转环法”所形成的大鼠实验性血栓有明显抑制作用。其血栓湿重分别为１０５．１、９７３和８９．３ｍｇ，与生理盐水（ＮＳ）对照组的１４２．７ｍｇ相比较，差异非常显著；其血栓干重亦明显低于ＮＳ组。同样的给药途径和剂量，ＭＳＭ可抑制ＡＤ忸的大鼠血小板聚集，使其最大聚集率降低，     

痰咳净滴丸对豚鼠的平喘作用研究

目的研究痰咳净滴丸的平喘作用。 方法采用磷酸组胺制作豚鼠哮喘模型，将哮喘模型豚鼠随机分为空白组（给予糊精）、痰咳净片对照组（给予痰咳净片，0.4 g·kg 1）、痰咳净滴丸高、中、低剂量组(分别给予痰咳净滴丸0.4，0.2，0.1 g·kg 1)和拆方组（给予不含咖啡因的痰咳净滴丸0.4 g·kg 1），每组10只，记录各组豚鼠出现哮喘的时间。 结果与其他各组比较，痰咳净滴丸高、中剂量组平喘作用更明显，且均差异有极显著性（均P＜0.01）。结论痰咳净滴丸对哮喘豚鼠有显著的平喘作用。     

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.     

Pharmacological treatment of COVID-19: an opinion paper

The precocity and efficacy of the vaccines developed so far against COVID-19 has been the most significant and saving advance against the pandemic. The development of vaccines has not prevented, during the whole period of the pandemic, the constant search for therapeutic medicines, both among existing drugs with different indications and in the development of new drugs. The Scientific Committee of the COVID-19 of the Illustrious College of Physicians of Madrid wanted to offer an early, simplified and critical approach to these new drugs, to new developments in immunotherapy and to what has been learned from the immune response modulators already known and which have proven effective against the virus, in order to help understand the current situation.