通心络胶囊预防垂体后叶素致实验性大鼠急性心肌缺血的研究

目的:研究通心络胶囊对垂体后叶素致实验性大鼠急性心肌缺血的预防作用。方法:对40只大鼠随机分成正常对照组、模型组、硝酸甘油组和通心络胶囊组,采用大鼠腹腔注射垂体后叶素建立急性心肌缺血模型,观察各给药组注射垂体后叶素后心电图ST段变化以及血清乳酸脱氢酶(LDH)、肌酸磷酸激酶同工酶(CK-MB)、肌钙蛋白I(TnI)、肌红蛋白(Myo)、超氧化物歧化酶(SOD)活性和丙二醛(MDA)等指标。结果:硝酸甘油组和通心络胶囊组能明显影响急性心肌缺血的心电图变化,抑制CK-MB、TnI、Myo的升高,提高血清SOD活性、降低MDA含量。结论:通心络胶囊能改善垂体后叶素致实验性大鼠急性心肌缺血的作用。     

海红果黄酮对垂体后叶素致急性心肌缺血的保护作用

目的初步研究海红果黄酮对大鼠急性心肌缺血的保护作用。方法用垂体后叶素制备心肌缺血大鼠模型,观察造模前后Ⅱ导联心电图T波、S点、P-P间期的变化,检测造模前后血清超氧化物歧化酶(SOD)、丙二醛(MDA)含量的变化。结果海红果黄酮各剂量组均可对抗垂体后叶素引起的心电图变化,且对血清SOD、MDA含量的变化都有明显的对抗作用(P<0.05,P<0.01)。结论海红果黄酮对实验性急性心肌缺血具有良好的保护作用。     

健心合剂对大鼠急性心肌缺血的保护作用

目的:观察健心合剂对实验性大鼠急性心肌缺血的保护作用.方法:采用垂体后叶素(pit)尾静脉注射法诱发大鼠急性心肌缺血,以健心合剂高、中、低剂量在不同时间对心电图T波改变及血清超氧化物歧化酶(SOD)、丙二醛(MDA)、乳酸脱氢酶(LDH)、肌酸肌酶(CK)含量变化为指标,以脉络通为阳性对照药物,观察比较健心合剂对大鼠实验性心肌缺血的保护作用.结果:健心合剂能显著降低大鼠心肌缺血心电图T波升高,减少血清MDA、LDH、CK含量,提高血清SOD的活性.结论:健心合剂对pit诱发大鼠急性心肌缺血具有保护作用 .     

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。     

丹参酮ⅡA静脉乳剂对大鼠急性心肌缺血的保护作用

目的:研究丹参酮ⅡA静脉乳剂对大鼠急性心肌缺血的保护作用。方法:采用垂体后叶素、异丙肾上腺素造成大鼠急性心肌缺血模型,以心电图T波变化,血清CK、LDH,心肌匀浆SOD、MDA、GSH-PX为指标,研究丹参酮ⅡA静脉注射乳剂对大鼠急性心肌缺血的保护作用。结果:丹参酮ⅡA静脉乳剂5.6,2.8,1.4mg·kg-1剂量组均能明显对抗垂体后叶素引起的大鼠急性心肌缺血T波高耸,并且能够显著降低异丙肾上腺素致心肌缺血的大鼠血清中CK和LDH的释放,降低心肌匀浆中MDA的水平(P<0.05),保护心肌SOD和GSH-PX的活性。结论:丹参酮ⅡA静脉乳剂对大鼠急性心肌缺血具有显著的保护作用。其机制与增加冠脉流量,抑制脂质过氧化和改善心肌能量代谢有关。     

延胡索乙素对大鼠实验性心肌缺血的保护作用

目的 研究延胡乙素（dl-THP)对大鼠实验性心肌缺血的保护作用。方法 观察dl-THP对垂体后叶素（pit)所致大鼠心电图急性缺血性改变的预防作用以及对异丙肾上腺素（Iso)引起心肌损伤大鼠的保护作用。结果 dl-THP对垂体后叶素所致心电图改变有明显预防作用。能对抗Iso所致ECG的ST段升高。显著抑制心肌组织中磷酸肌激酶（CPK）、乳酸脱氢酶（LDH）的释放,降低血清CPK和LDH水平,保护心肌组织超氧化物歧化酶（SOD）活性,减少丙二醛（MDA）生成。结论 dl-THP对实验性心肌缺血有明显的保护作用。     

舒心颗粒对垂体后叶素致心肌缺血模型大鼠的影响

目的:研究舒心颗粒对垂体后叶素致心肌缺血模型大鼠的影响。方法:利用静脉注射垂体后叶素的方法复制急性心肌缺血大鼠模型,观察大鼠心电图与大鼠血清精脒/精胺N1乙酰基转移酶(SAT)、血清肌酸激酶(CK)、血清肌酸激酶同工酶(CK-MB)、乳酸脱氢酶(LDH)、α-羟丁酸脱氢酶(HBDH)活性以及血小板聚集率。结果:舒心颗粒能减轻模型大鼠心电图缺血性改变(ST段的上移和T波的增高),抑制血清中SAT、CK、CK-MB、LDH、HBDH活性的升高,降低血小板聚集率。结论:舒心颗粒对垂体后叶素所致心肌缺血有较好的保护作用。     

芳香新塔花对大鼠急性心肌缺血和乳鼠心肌细胞的保护作用

目的比较芳香新塔花Ziziphora clinopodioides不同提取物对大鼠急性心肌缺血、对乳鼠心肌细胞缺氧-复氧损伤的影响。方法通过体内注射垂体后叶素造成大鼠急性心肌缺血模型,观察急性心肌缺血大鼠Ⅱ导联心电图J点的变化,以及试药对超氧化物歧化酶(SOD)、乳酸脱氢酶(LDH)、丙二醛(MDA)的影响。体外培养原代SD乳鼠心肌细胞,建立心肌细胞缺氧-复氧损伤模型,用MTT法测定药物对心肌细胞存活率的影响,测定给药后MDA的变化。结果芳香新塔花石油醚部位和氯仿部位0.3g/kg显著抑制注射垂体后叶素所致心电图J点升高,对心率、SOD、LDH、MDA的影响不显著;乙醇提取物和氯仿部位能明显降低缺氧-复氧模型下心肌细胞培养液中的MDA浓度。结论芳香新塔花具有潜在的心肌缺血保护作用。     

冠通活瘀胶囊对大鼠急性心肌缺血的保护作用

目的:观察冠通活瘀胶囊对小鼠注射异丙肾上腺素(ISO)后耐缺氧存活时间和注射垂体后叶素(Pit)所致的心肌缺血的影响。方法:采用腹腔注射ISO后观察小鼠耐缺氧存活时间和尾静脉注射Pit致大鼠急性心肌缺血模型,观察各给药组在腹腔注射ISO后耐缺氧存活时间和注射Pit后不同时间点Ⅱ导心电图T波变化百分率,心率变化及对血清肌酸激酶(CK)、乳酸脱氢酶(LDH)和谷草转氨酶(AST)的影响。结果:冠通活瘀胶囊低、中剂量组与模型组比较,均能明显延长小鼠耐缺氧存活时间和降低心肌缺血大鼠心电图T波峰值变化百分率(P<0.05);与注射Pit前比较,能对抗Pit致心率减慢的损伤,并能显著降低血清中CK、LDH和AST的含量。结论:冠通活瘀胶囊具有降低小鼠心肌耗氧量和抗Pit引起的大鼠急性心肌缺血作用。     

复方当归粉针剂对垂体后叶素诱导大鼠心肌缺血的保护作用

摘要目的：观察复方当归粉针剂对垂体后叶素诱导的大鼠缺血心肌的保护作用。方法：将60只大鼠分为空白对照组、模型对照组、复方当归粉针剂低、中、高剂量组,阳性对照组,大鼠腹腔注射垂体后叶素建立急性心肌缺血模型,观察复方当归粉针剂对各组大鼠血清中超氧化物歧化酶（SOD）、丙二醛（MDA）以及心肌梗死面积的影响。结果：复方当归粉针剂可对抗垂体后叶素所致的大鼠急性心肌缺血,增加血清中SOD活力,减少MDA生成,缩小心梗面积。结论：复方当归粉针剂对大鼠心肌缺血有保护作用,其机制可能与抗脂质过氧化有关。     

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.     

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.     

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.