辛伐他汀对血脂正常的老年单纯收缩期高血压患者内皮依赖性血管舒张功能的影响

目的探讨血脂正常老年单纯收缩期高血压患者应用不同剂量辛伐他汀治疗后对内皮依赖性血管舒张功能的影响。方法血脂正常高血压患者115例随机分成辛伐他汀20mg治疗组40例,辛伐他汀40mg治疗组39例,正常对照组30例。应用超声检测肱动脉血流介导的血管舒张功能（FMD）和内皮非依赖性血管舒张功能（EID）比较治疗4周前后变化。结果血脂正常高血压组患者内皮功能与健康对照组相比显著降低。辛伐他汀20mg组治疗前后FMD分别为（7.5±2.7）%与（10.5±3.1）%,P〈0.05,NMD为（16.6±4.1）%与（17.4±5.1）%,P〉0.05,辛伐他汀40mg组治疗前后FMD分别为（7.3±3.4）%与（13.7±2.5）%,P〈0.01,MND为（16.9±5.1）%与（17.1±5.6）%,P〉0.05。辛伐他汀20mg组与40mg组治疗后比较,以40mg组FMD改善明显（P〈0.05）。结论辛伐他汀具有降脂以外的改善内皮功能的作用,该作用与剂量相关。     

卡维地洛对高血压病并发2型糖尿病患者血管内皮功能及胰岛素抵抗的影响

目的:探讨卡维地洛对高血压合并糖尿病患者血管内皮功能及胰岛素抵抗的影响。方法:经2周导入期后熏将41例高血压合并2型糖尿病患者熏随机分为卡维地洛组(21例)和美托洛尔组(20例)。治疗前及治疗6月后熏采静脉血测定空腹胰岛素、空腹血糖熏计算胰岛素敏感性指数;采用高分辨率超声检测反应性充血和硝酸甘油介导的肱动脉舒张功能。结果:卡维地洛治疗6月后,患者收缩压和舒张压均有效下降熏空腹胰岛素降低,胰岛素敏感指数显著升高熏反应性充血和硝酸甘油介导的血管舒张功能均明显改善。美托洛尔治疗后,空腹血糖和空腹胰岛素均轻度升高,胰岛素敏感指数降低,但差异均不具有统计学意义;反应性充血和硝酸甘油介导的血管舒张功能均无明显变化。结论:卡维地洛可有效降低高血压合并2型糖尿病患者的血压,改善胰岛素抵抗及肱动脉内皮依赖性及非内皮依赖性的血管舒张功能。     

益心舒胶囊对冠心病患者血管内皮功能改善作用的研究

目的：观察服用益心舒胶囊3个月后对冠心病患者血管内皮功能的改善作用。方法：入选150例冠心病患者按2∶1比例分为益心舒胶囊组和常规治疗组。两组均给予冠心病常规治疗,益心舒胶囊组加用益心舒胶囊1次3粒,1日3次,疗程3个月。检测治疗前后肱动脉血流介导内皮依赖性舒张功能（FMD）、血浆一氧化氮（NO）、内皮素-1浓度,评价两组患者血管内皮功能。结果：与治疗前比较,治疗后两组患者（FMD）较治疗前改善（P〈0.05）,血浆一氧化氮（NO）较前升高（P〈0.05）,内皮素-1浓度较治疗前降低（P〈0.05）。且益心舒胶囊组（FMD）,血浆一氧化氮（NO）、内皮素-1浓度较常规治疗组改变明显（P〈0.05）。结论：冠心病患者在常规治疗基础上加用益心舒胶囊可明显改善血管内皮功能。     

罗格列酮对血糖正常的代谢综合征患者血管内皮功能和C反应蛋白的影响

目的评价罗格列酮对血糖正常的代谢综合征患者血管内皮功能和C反应蛋白的影响。方法用随机双盲对照方法,选择血糖正常的代谢综合征患者190例,用高分辨率超声检测肱动脉血流介导的血管活性(FMD)和硝酸甘油介导的血管活性(NTGMD),计算胰岛素抵抗指数(IR)。结果罗格列酮+常规治疗组(试验组)较常规治疗组(对照组)FMD和NTGMD明显改善,IR变化2组具有显著性差异,血清hs-CRP水平显著下降(P<0.05)。结论罗格列酮能明显改善血糖正常的代谢综合征患者的血管内皮功能,并可减轻炎症反应。     

丙丁酚对冠心病血管内皮功能的影响

目的观察丙丁酚（普罗布考）对冠心病血管内皮功能的影响。方法采用高分辨率超声诊断系统检测35例确诊冠心病的老年患者服用普罗布考前后肱动脉血流介导的舒张功能（即内度依赖性舒张功能，FMD）和硝酸甘油介导的舒张功能（非内皮依赖性舒张功能，NMD）的变化，同时检测治疗前后血浆一氧化氮（NO）、内皮素（ET）水平的变化，并与28例未接受调脂治疗的老年冠心病患者进行对照研究。结果接受普罗布考治疗的患者ET、总胆固醇（TC）、低密度脂蛋白胆固醇（LDL-C）水平明显降低，而NO和FMD明显增加，NMD无显著性改变。结论普罗布考在降脂的同时能够改善老年冠心病患者血管内皮功能，且该作用独立于高密度脂蛋白胆固醇（HDL-C）水平的降低。     

依那普利对高血压患者内皮依赖性舒张功能的影响

目的评价依那普利对高血压患者内皮依赖性舒张功能的影响。方法30例高血压患者应用依那普利治疗前后分别用高分辨率超声,测量右肱动脉在静息时、反应性充血(流量介导血管舒张)、舌下含服硝酸甘油(硝酸甘油介导舒张)时的舒张末期内径,取25例健康人对比分析。结果高血压病组流量介导血管舒张(FMD),较对照组明显减弱(P<0.01),而硝酸甘介导血管舒张(NCD)两组无显著性差异(P>0.05)。经治疗,收缩压、舒张压均显著降低(P<0.01),FMD较治疗前显著提高,NCD无改变。结论依那普利可显著改善高血压患者内皮依赖性舒张功能。     

普罗布考对老年单纯收缩期高血压患者血管内皮功能的影响

目的 评价普罗布考对老年单纯收缩期高血压患者血管内皮舒张功能的影响。方法 采用自身对照和组间对照，将64例老年单纯收缩期高血压患者随机单盲分为A、B两组，其中A组33例，在常规抗高血压药物的基础上加服用普罗布考：B组31例．常规抗高血压药物治疗．疗程均为12周。采用高分辨率超声技术测定两组治疗前后肱动脉内皮依赖性血管舒张功能及血脂的变化。结果 A组患者治疗前后比较血总胆固醇（TC）、低密度脂蛋白胆固醇（LDL-C）和高密度脂蛋白胆固醇（HDL-C）浓度明显降低（均P〈0．05），甘油三酯（TG）浓度则变化不明显（P〉0．05）。A、B两组FMD与治疗前比较均明显增高（P〈0．01和P〈0．05）。治疗后两组间比较血脂、FMD差异有统计学意义（P〈0．05）。结论 普罗布考可改善老年单纯收缩期高血压患者的血管内皮功能。     

针灸治疗大动脉炎对血管内皮舒张功能的影响

目的：应用高频超声评价针灸治疗对大动脉炎（头臂动脉型）患者依赖性血管内皮舒张功能（EDD）的影响。方法：针灸治疗组31例和药物治疗组30例，分别观察治疗前后肱动脉血管内皮舒张功能变化，测定血浆一氧化氮（NO）、内皮素（ET）等血管活性物质的浓度变化，并进行对比分析。结果：2组患者治疗后较治疗前EDD％、血浆中NO浓度升高（P〈0．01），ET浓度降低（P〈0．01），针灸疗法更显效。结论：针灸治疗大动脉炎（头臂动脉型）可以改善血管内皮舒张功能，疗效显著。     

3类活血化瘀中成药对冠心病稳定型心绞痛血管内皮功能的影响

目的：比较复方丹参滴丸、银杏叶片、维脑路通对冠心病稳定型心绞痛（Chronic Stable Angina）血管内皮功能的影响情况。方法：选取本院稳定型心绞痛患者200例,随机分为服用复方丹参滴丸、银杏叶片、维脑路通及安慰剂4组进行治疗（疗程均为4周）,通过超声方法检测肱动脉血流介导的血管扩张功能（flowmediated dilatation,FMD）、硝酸甘油介导的血管舒张反应（nitrogtycerin—mediated dilation,NMD）,采用酶联免疫吸附法（ELISA）或硝酸还原酶法检测血浆中的内皮素（Endothelin-1,ET-1）及NO水平,分析各组患者服药前后的血管内皮功能变化情况,比较3种活血化瘀类中成药对血管内皮功能的影响。结果：与安慰剂组比较治疗前后的丹参滴丸组和维脑路通组具有较大的FMD值变化（P〈0．05）,治疗前后的丹参滴丸组、维脑路通组和银杏叶组具有较大的NMD值变化（P〈0．05）,治疗前后的丹参滴丸组、银杏叶组和维脑路通组具有较大的ET值变化（P〈0．05）,其中以丹参滴丸组、银杏叶组最大,维脑路通组次之;与安慰剂组、维脑路通组比较,治疗前后的丹参滴丸组具有较大的NO值变化（P〈0．05）;其中以丹参滴丸组最大,银杏叶组、维脑路通组次之。结论：活血化瘀类中成药可改善冠心病稳定型心绞痛患者的血管内皮功能,其作用效果以复方丹参滴丸最为显著,维脑路通及银杏叶片次之。     

不稳定性心绞痛患者血管内皮功能及普罗布考干预研究

目的:观察普罗布考对不稳定性心绞痛患者内皮依赖舒张功能、血氧化低密度脂蛋白(ox-LDL)和高敏C反应蛋白(hs-CRP)水平的影响。方法:将53例不稳定性心绞痛患者随机分为普罗布考组和常规治疗组,治疗前、治疗3个月后应用高频超声测肱动脉内皮依赖性舒张功能(FMD),并观察外周血ox-LDL及hs-CRP等指标变化。结果:治疗后普罗布考组FMD较治疗前及常规治疗组治疗后均明显升高(P<0.01),血浆ox-LDL及hs-CRP水平较治疗前及常规治疗组治疗后均明显降低(P<0.01或P<0.05)。普罗布考组治疗后血浆ox-LDL与FMD呈负相关(r=-0.651,P<0.01)。结论:普罗布考具有较强的抗氧化及抗炎症作用并可改善不稳定心绞痛患者内皮依赖舒张功能。     

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.     

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.     

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.