依达拉奉与前列地尔脂微球载体靶向制剂联合治疗急性脑梗死的疗效观察

目的探讨依达拉奉与前列地尔脂微球载体靶向制剂联合治疗急性脑梗死的临床疗效。方法选择80例急性脑梗死患者随机分为治疗组(40例)和对照组(40例),治疗组在常规治疗的基础上给予依达拉奉和前列地尔脂微球载体靶向制剂。结果观察两组治疗后临床疗效,治疗组总有效率95.0%显著优于对照组(75.0%)。结论依达拉奉与前列地尔脂微球载体靶向制剂联合治疗急性脑梗死安全、有效。     

前列地尔脂微球载体制剂治疗急性脑梗死的临床观察

目的观察前列地尔脂微球载体制剂治疗急性脑梗死的疗效及安全性。方法 108例急性脑梗死患者随机分成治疗组和对照组,在基本及对症治疗基础上,治疗组给予前列地尔脂微球载体制剂治疗,对照组则给予复方丹参注射液治疗,共14d,评定治疗前后神经功能缺损程度评分(NIHSS)、日常生活活动能力Barthel指数(BI),并随访治疗后3个月后的BI指数。结果两组患者治疗后NIHSS评分均有降低而BI指数均升高,但治疗组变化更显著(P<0.05),而副作用比较无明显差异(P>0.05)。结论前列地尔脂微球载体制剂治疗急性脑梗死能减轻患者的神经功能缺损及改善日常生活活动能力,且副作用少,值得临床推广使用。     

前列地尔脂微球载体制剂治疗急性脑梗死临床研究

目的探讨研究急性脑梗死治疗中前列地尔脂微球载体制剂临床疗效。方法从2009年6月至2011年5月在我院住院治疗的患者中符合本次研究要求的急性脑梗死患者共116例,按照数字表法随机平分为观察组和对照组,对照组在常规治疗的基础上行丹参治疗,观察组则在常规治疗的基础给予前列地尔脂微球载体制剂治疗。结果经过1个疗程治疗,观察组治疗总有效率为64.15%,对照组总有效率为18.87%,观察组患者治疗效果显著高于对照组(P<0.01)。观察组日常活动能力和神经功能缺损改善程度明显高于对照组,两组差异具有显著性(P<0.01),观察组1例患者出现轻微恶性,未经特殊处理,自行消失;2例输液部位静脉出现红、痛反应,输液结束即自行消失,不良反应轻微。结论前列地尔脂微球载体制剂在急性脑梗死治疗方面具有较好疗效,且不良反应轻微,值得推广。     

前列地尔脂微球载体治疗急性脑梗死87例

目的观察前列地尔脂微球载体制剂治疗急性脑梗死的临床疗效与安全性。方法将169例急性脑梗死患者分为治疗组87例和对照组82例,两组均给予常规治疗,对照组加用丹参注射液,治疗组给予前列地尔脂微球载体制剂10 μg静脉滴注,qd,14 d为1个疗程。治疗7,14,21 d后评定疗效,记录神经功能缺损评分和日常生活活动能力评分, 监测用药前后凝血功能、肝肾功能等变化。结果治疗组治疗14,21 d后神经功能改善有效率分别为60.4%和62.1%,对照组分别为18.3%和29.3%;治疗组日常生活活动能力改善有效率分别为54.0%和57.5%,对照组分别为36.6%和39.0%,治疗组均显著高于对照组（均P＜0.05）;治疗期间治疗组2例、对照组1例丙氨酸氨基转移酶和（或）天冬氨酸氨基转移酶轻度增高。结论前列地尔脂微球载体制剂能有效改善急性脑梗死患者近期神经功能缺损和日常生活活动能力,未见严重不良反应。     

前列地尔脂微球载体制剂改善76例急性脑梗死患者预后

目的:评价前列地尔脂微球载体制剂治疗急性缺血性卒中的疗效及安全性。方法:发病1周内的76例急性脑梗死患者随机分为试验组和对照组,每组各38例。试验组接受前列地尔脂微球载体制剂治疗,对照组接受低分子右旋糖苷加丹参注射液治疗。疗程14 d。主要疗效评价指标为d 21的躯体日常生活活动能力Barthel指数(BI),BI>95分定义为良好预后。次要疗效评价指标为d 21欧洲卒中神经功能评分(ESS)。安全性评价指标为血小板聚集率、凝血时间、纤维蛋白原、D-Dimer、血脂和不良反应。结果:试验组和对照组预后良好率分别为26.3%与2.6%(P=0.007)。试验组和对照组ESS改善的总有效率为47.37%与21.05%(P=0.016)。治疗期间血小板聚集功能下降明显,试验组比对照组下降明显(P<0.05)。试验组与对照组不良反应发生率分别为7.89%与5.26%(P>0.05)。结论:前列地尔脂微球载体制剂治疗急性脑梗死安全性好,有一定疗效。     

前列地尔脂微球载体辅治颈动脉粥样斑块的疗效观察

目的观察前列地尔脂微球载体制剂对颈动脉粥样斑块的疗效。方法经颈部血管彩色B型超声检查80例患者,随机分为观察组42例和对照组38例,观察组给予前列地尔脂微球载体治疗,对照组给予常规治疗,比较2组临床效果。结果观察组的颈动脉粥样斑块厚度、颈内动脉血流速度与治疗前及对照组比较,差异有统计学意义（P〈0.05）。结论前列地尔脂微球载体组对颈动脉粥样斑块有明显治疗作用。     

前列地尔脂微球载体制剂治疗肝硬化腹水的临床观察

前列地尔脂微球载体制剂（商品名：kashi，凯时）为前列地尔（alpmstadil）封入脂微球中的一种新型载体制剂，利用脂微球（1iposome）易在病变部位及病变血管处聚集，靶向发挥前列地尔的药理作用，且为传统给药量的1／10，因而具有高效性。本研究于2004年9月至2005年4月应用前列地尔脂微球载体制剂治疗肝硬化腹水30例，取得良好效果，现报告如下。     

前列地尔脂微球载体制剂治疗急性脑梗死58例临床分析

目的观察前列地尔脂微球载体制剂治疗急性脑梗死的疗效及安全性。方法将嵩县人民医院106例经颅脑CT或MRI证实的急性脑梗死患者随机分为两组,其中治疗组58例,用前列地尔10μg加0.9%氯化钠溶液10mL静脉推注,1次/d;对照组48例,用低分子右旋糖酐500mL加丹参20mL静脉滴注,1次/d,并口服阿司匹林75mg/d,疗程均为14d。用药前及用药后21d进行神经功能缺损评分和日常生活能力评分。结果两组患者治疗前、后神经功能缺损和日常生活能力评分间差异均有显著性意义(P<0.05);治疗后,治疗组两项评分明显优于对照组(P<0.01)。治疗组总有效率为91.5%,对照组总有效率为64%,两组间差异有显著性意义(P<0.05)。治疗组未见明显不良反应。结论前列地尔脂微球载体制剂治疗急性脑梗死安全、有效。     

前列地尔脂微球载体制剂治疗肝硬化后血清AST、ALT的变化

目的研究肝硬化患者前列地尔脂微球载体制剂(LiPoPGE1)治疗后血清ALT、AST变化的临床意义。方法采用全自动生化测定70例肝硬化患者和30例正常人血浆ALT、AS的含量。肝硬化患者随机分成两组,对照组30例,为综合治疗组;实验组40例为综合治疗加前列腺素E1(PCE1)。两组治疗前以上观察指标差异无显著性(P>0.05)。按Child分级,治疗前肝硬化患者血清ALT、AST水平两组均为A级0.05)。结论前列地尔脂微球载体制剂(LiPoPGE1)治疗肝硬化A、B两级患者具有降低ALT.AST的作用,从而推论前列地尔脂微球载体制剂(LiPoPGE1)具有保护肝细胞的作用。     

前列地尔脂微球载体注射液治疗冠心病并闭塞性周围动脉粥样硬化的疗效

【摘要】目的观察前列地尔脂微球载体注射液治疗冠心病并闭塞性周围动脉粥样硬化的临床疗效。方法选取2010年6月～2012年6月于本院心内科住院治疗的患者98例，分为对照组和治疗组，对照组患者44例，治疗组患者54例。所有患者均给予常规治疗，包括硝酸酯类、ACEI、利尿剂、钙离子拈抗剂、β-受体阻滞剂、阿司匹林、洋地黄、调脂药等基础治疗。治疗组在常规治疗的基础上，加用前列地尔脂微球载体注射液10μg加0．9％氯化钠溶液20mL静脉滴注，每天1次，疗程2周。结果与对照组患者相比，治疗组患者6min步行距离有显著增加．血Hey水平显著降低，ABI明显升高，Bruce运动平板试验代谢当量METs显著增加。以上差异均具有统计学意义（P〈0．05）。而两组患者心排量的差异无统计学意义（P〉0．05）。结论前列地尔脂微球载体注射液治疗冠心病并闭塞性周围动脉粥样硬化有确切的疗效，且无明显的不良反应。     

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.     

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.