3,6-(二甲氨基)-二苯并碘杂六环葡萄糖酸盐对大鼠心肌缺血的保护作用

采用结扎冠状动脉制备心肌缺血模型和iv垂体后叶素诱导心肌缺血模型 ,观察了 3,6 (二甲氨基 ) 二苯并碘杂六环葡萄糖酸盐 (IHC 93)对大鼠心肌损伤的影响 .结果表明 ,IHC 930 .2 5及 0 .50mg·kg- 1能够缩小大鼠缺血心肌的梗死范围 ;明显减少缺血心肌乳酸脱氢酶及肌酸磷酸激酶的释放 ;对抗结扎冠脉和iv垂体后叶素所致的心电图ST段 T波抬高 ;明显改善缺血心肌光镜下的细胞损伤 .结果提示 ,IHC 93对大鼠急性缺血心肌损伤有保护作用 .     

人工麝香对抗动物心肌缺血的作用

目的研究人工麝香对抗动物心肌缺血的作用。方法实验动物随机分为模型组、阳性对照硝酸甘油组(小鼠为0.083mg·kg-1,大鼠为0.042mg·kg-1)、人工麝香低、中、高剂量组(小鼠为5、10、20mg·kg-1,大鼠为2.5、5.0、10mg·kg-1)5组。进行小鼠耐缺氧实验,记录存活时间;垂体后叶素诱发大鼠实验性心肌缺血实验,记录大鼠心电图变化;阻断大鼠冠状动脉引起急性心肌缺血,记录心电图变化、心肌酶指标、缺血范围及形态学检查。结果人工麝香延长动物耐缺氧时间(P<0.01或P<0.05);能够改善垂体后叶素引起的心电变化(P<0.05);抑制心肌酶活性的升高,减少心肌缺血范围(P<0.05)。结论通过实验研究表明人工麝香具有抗动物心肌缺血的作用。     

蝙蝠葛碱对动物耐缺氧及实验性心肌缺血和梗塞的影响

本文报道蝙蝠葛碱(Dau)对小白鼠耐缺氧和大鼠实验性心肌缺血及梗塞的影响。异丙肾上腺素(Iso)诱发耗氧量增加后,Dau,维拉帕米(Ver)和普萘洛尔(Pro)均能提高小鼠常压耐缺氧能力、延长存活时间、降低耗氧速率.Dau和Ver延长存活时间与其降低耗氧速率有关,而Pro的这一作用可能与降低耗氧速率和提高对氧的利用能力有关。 Dau明显降低iv垂体后叶素(Pit)所致的大白鼠心电图L—Ⅱ的J点和T波抬高幅度,降低大鼠冠脉结扎所致的心电图L—Ⅱ的J点抬高幅度和病理性Q波的出现率,明显缩小结扎24小时后心肌梗塞范围,提示Dau对实验性心肌缺血和梗塞具有保护作用。     

龙血竭总黄酮对动物心肌缺血的保护作用

目的:观察龙血竭总黄酮对大鼠、犬急性心肌缺血的保护作用。方法:股静脉注射垂体后叶素致大鼠急性心肌缺血,观察心电图变化;结扎麻醉犬冠状动脉致心肌缺血,测定缺血范围、心外膜电图及血清CK、LDH、LD浓度。结果:与模型对照组相比,360、180mg·kg-1龙血竭总黄酮灌胃给药能对抗垂体后叶素所致大鼠心肌缺血心电图J点、T波的变化;120、60、30mg·kg-1龙血竭总黄酮十二指肠给药能缩小冠状动脉结扎所致犬心肌缺血梗死范围,降低心电图的ST段比结扎前抬高≥2mv以上的个数(△NST)和心电图的ST段于结扎前抬高的差值(△ΣST);减少血清中CK、LDH、LD释放。结论:龙血竭总黄酮对大鼠、犬急性心肌缺血有较好的保护作用。     

松树皮提取物原花青素对抗动物心肌缺血的研究

目的:研究松树皮提取物原花青素对抗动物心肌缺血的作用.方法:实验动物随机分为空白组、阳性对照复方丹参组(小鼠为20 mg·kg-1,大鼠为10 mg·kg-1)、原花青素低、中、高组(小鼠为10.0、20.0、30.0 mg· kg-1,大鼠为5.0、10.0、20 mg·kg-1)共5组,进行小鼠常压耐缺氧及抗亚硝酸钠中毒实验,记录小鼠的存活时间;垂体后叶素诱发大鼠实验性心肌缺血,记录大鼠心电图的变化,颈动脉取血,测量血清的LDH、MDA等指标.结果:原花青素能延长动物耐缺氧时间(P＜0.01或P＜0.05);能够改善垂体后叶素引起的心电变化(P＜0.05).结论:松树皮提取物原花青素对动物的心肌缺血有一定的保护作用.     

冠心丹参口腔崩解片对缺血缺氧心肌的保护作用

目的观察冠心丹参口腔崩解片对缺血缺氧心肌的保护作用。方法采用小鼠常压耐缺氧法、小鼠气管夹闭法及垂体后叶素(Pit)和异丙肾上腺素(Iso)致大鼠急性心肌缺血法观察冠心丹参口腔崩解片抗心肌缺血的作用。结果冠心丹参口腔崩解片能显著延长小鼠常压耐缺氧和气管夹闭的存活时间,减轻垂体后叶素和异丙肾上腺素所致心肌缺血大鼠的心电图变化。结论冠心丹参口腔崩解片具有显著的抗心肌缺血缺氧作用。     

养心复脉饮对心血管系统的作用

目的:研究养心复脉饮对实验性心肌缺血动物的保护作用。方法:应用垂体后叶素等造成动物心肌缺血和其他心功能改变。结果:养心复脉饮对注射垂体后叶素(p it)大鼠血清中磷酸肌酸激酶(CK)和乳酸脱氢酶(LDH)的升高有一定的缓解作用,能明显减少p it大鼠心肌组织丙二醛(MDA)的生成,保护大鼠心肌组织超氧化物歧化酶(SOD)的活性;对氯仿所致小鼠心律失常有明显的保护作用;能明显延长异丙肾上腺素(Iso)小鼠耐缺氧时间。结论:养心复脉饮对心功能有一定的保护作用。     

阿魏硝胺对心血管系统的作用

合成的阿魏硝胺(乙醇胺硝酸酯的阿魏酸盐),具有明显的心血管效应,可使麻醉兔降低全身血压39±12mmHg,但对心电图无明显影响(iv)。它对抗垂体后叶素所致急性心肌缺血(iv),能增强小鼠耐缺氧能力(ip),并能增加麻醉狗的冠脉血流量(iv);并能明显抑制去甲肾上腺素(NE)引起的动脉血管条收缩。本品对小鼠的 LD_(50)为857mg/kg(iv),>1200mg/kg(PO)。     

复方益母草膏药效学实验研究

目的观察复方益母草膏对大鼠未孕子宫张力、对缩宫素诱发子宫痉挛性疼痛反应、血液流变学、对体外血栓形成的影响和抗炎作用,进一步证实其药效。方法采用出生后即与雄性大鼠隔离的雌性大鼠,观察用药后离体子宫对垂体后叶素的收缩反应;观察雌性大鼠腹腔注射缩宫素15分钟内扭体次数;用肾上腺素加冰水刺激制备大鼠血瘀模型,观察对全血粘度及血浆粘度、红细胞变形和聚集性的影响;用体外血栓仪测定血栓形成的长度和重量;用蛋清致大鼠足跖肿胀和二甲苯致小鼠耳廓肿胀观察其抗炎作用。结果复方益母草膏对垂体后叶素引起的子宫平滑肌收缩具有明显抑制作用;复方益母草膏20.0g·kg-1、10.0g·kg-1、5.0g·kg-1剂量组能明显减少缩宫素所致大鼠扭体次数、显著改善肾上腺素诱导的大鼠全血粘度增高;20.0g·kg-1和10.0g·kg-1组可显著抑制肾上腺素诱导的红细胞聚集、降低蛋清所致大鼠足跖肿胀;10.0g·kg-1、5.0g·kg-1和2.5g·kg-1剂量组能明显抑制正常大鼠体外血栓形成;28.0g·kg-1、14.0g·kg-1、7.0g·kg-1剂量组对二甲苯所致小鼠耳廓急性炎症有明显抑制作用。结论复方益母草膏能明显抑制垂体后叶素所致离体子宫收缩反应和对缩宫素所致扭体反应;可显著改善血瘀型大鼠血液流变性;能明显抑制正常大鼠体外血栓形成;可有效抑制蛋清所致大鼠足跖肿胀反应和二甲苯所致小鼠耳廓的急性炎症反应,具有良好的解痉、活血化瘀、抗炎作用。     

薤白提取物对心肌缺氧缺血及缺血再灌注心肌损伤的保护作用

采用异丙肾上腺素致小鼠常压缺氧模型、垂体后叶素致大鼠急性心肌缺血模型及大鼠心肌缺血再灌注模型 ,考察薤白提取物抗心肌缺氧缺血及缺血后再灌注损伤的保护作用。结果表明薤白提取物能延长异丙肾上腺素作用的小鼠常压缺氧存活时间 ,对抗垂体后叶素所致的大鼠急性心肌缺血作用 ,并能明显保护缺血再灌注引起的大鼠心肌的损伤     

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.     

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.