冠心病病人血浆纤溶成分与血脂水平评价

探讨冠心病（ＣＨＤ）患者血浆组织型纤溶酶原激活剂（ｔ－ＰＡ）、纤溶酶原激活剂抑制剂（ＰＡＩ）、交联纤维蛋白二聚体（Ｄ－ｄｉｍｅｒ）及脂蛋白（ａ）［ Ｌｐ（ａ）］等血浆水平变化、临床应用价值以及其相互间的关系。方法： ｔ－ＰＡ、ＰＡＩ、ＬＰ［ａ］、Ｄ－ｄｉｍｅｒ采用ＥＬＩＳＡ双抗体夹心法检测,胆固醇、甘油三酯采用酶法测定。结果：４７例ＣＨＤ ,患者血浆ｔ－ＰＡ－ＰＡＩ及Ｄ－ｄｉｍｅｒ测值为（９．７±５．７）、（８０．５±３０．０）、（２０９±１２５）ｎｇ ／ｍｌ,其中ｔ－ＰＡ,和Ｄ－ｄｉｍｅｒ值明显高于健康对照组（Ｐ＜０．００１）,ＰＡＩ含量两组水平差别不明显（Ｐ＞０．０５）．血浆ＬＰ（ａ）、ＴＧ及ＨＤＬ浓度两组间差别有统计学意义（Ｐ＜０．０５）。用准确性评价各项指标临床应用价值,以Ｄ－ｄｉｍｅｒ为最佳,Ｌｐ（ａ）次之。血浆ｔ－ＰＡ与Ｌｐ（ａ）及ＴＧ含量呈正相关。ＰＡＩ与血浆ＴＧ呈正相关,和ＨＤＬ呈负相关。结论：ｔ－ＰＡ、Ｄ－ｄｉｍｅｒ、ＬＰ（ａ）与粥样斑块及血栓形成有密切关系。     

极化液对冠心病患者纤溶系统功能的影响

目的：观察极化液葡萄糖－胰岛素－氯化钾（ＧＩＫ）用于冠心病治疗时对纤溶系统功能的影响。方法：４６例确诊冠心病患者,其中陈旧性心肌硬塞１０例,不稳定性心绞痛１４例,稳定性心绞痛２２例。给予ＧＩＫ液,即１０％葡萄糖５００ｍｌ＋普通胰岛素１０μｌ＋氯化钾１ｇ静滴 ８～１２ ｄ。于用药前后测定组织型纤溶酶原激活物活性（ｔ－ＰＡ：Ａ）及其抑制物活性（ＰＡＬ：Ａ）,纤溶酶原活性（ＰＬｇ）,组织型纤溶酶原激活物（ｔ－ＰＡ）及其抑制物（ＰＡＩ－Ｉ）含量及Ｄ－二聚体（Ｄ－Ｄｉｍｅｒ）含量,空腹血清胰岛素水平。结果：用药前与正常比较,ｔ－ＰＡ活性降低,ＰＡＩ－１活性增高,胰岛素水平增高,高胰岛素者占７８．２％。用药后ｔ－ＰＡ活性及含量、纤溶酶原活性均较前降低（Ｐ＜０．０１）,ＰＡＩ－１含量较前增加（Ｐ＜０．００１）,而ＰＡＩ－１活性及Ｄ－Ｄｉｍｅｒ变化不明显。结论：冠心病特别伴有胰岛素水平增高患者,应用ＧＩＫ液可能通过其对纤溶系统功能的不良影响促使病变进展。     

肺心病急性加重期血管内皮细胞损伤与SOD间关系的观察

观察３３例肺心病急性加重期患者血浆内皮素（ＥＴ）、ＶＷ因子（ＶＷＦ）、组织型纤溶酶原激活物（ｔ－ＰＡ）及其抑制物（ＰＡＩ）和血清超氧化物歧化酶（ＳＯＤ）变化。结果：肺心病急性加重期ＥＴ、ＶＷＦ、ＰＡＩ升高，ＳＯＤ和ｔ－ＰＡ活性下降，与对照组比较差异显著（均Ｐ〈０．０１）。ＳＯＤ与ＰａＯ２、ｐＨ、ｔ－ＰＡ呈正相关（ｒ分别为０．３４８、０．２９５、０．３１４，Ｐ〈０．０５），与ＰａＣＯ２、ＥＴ、ＶＷＦ     

慢性肺心病急性发作期t—PA,PAI活性的变化

测定３２例肺心病急性发作期组织型纤溶酶原激活物（ｔ－ＰＡ）、纤溶酶原激活物抑制物（ＰＡＩ）、纤溶酶原（Ｐｇ）及纤维蛋白原降解产物（ＦＤＰ）。结果表明，肺心病患者ｔ－ＰＡ、ＰＡＩ、Ｐｇ明显下降，而ＦＤＰ明显升高，表明肺心病急性发作期处于高凝、低纤溶状态。ｔ－ＰＡ、Ｐｇ的变化与ＰａＯ２呈明显正相关，而ＦＤＰ与ＰａＯ２呈明显负相关。     

巴曲抗栓酶对肺原性心脏病病人血栓前状态的作用

目的：研究巴曲抗栓酶对肺原性心脏病（肺心病）病人的纤溶作用。方法：所有肺心病病人接受常规治疗（包括吸氧、抗生素及平喘药物），治疗组２０例（男性１６例，女性４例；年龄５７±ｓ７ａ）静脉滴注巴曲抗栓酶５ＢＵ加入０．９％氯化钠注射液１００ｍＬ，２次／ｗｋ，共２ｗｋ．对照组１０例（男性９例、女性１例；年龄５５±３ａ）不用巴曲抗栓酶。结果：巴曲抗栓酶组治疗后ＰＬＧ，ＰＡＩ比治疗前下降（Ｐ＜０．０５）．ＴＰＡ，Ｄ－ｄｉｍｅｒ比治疗前增加（Ｐ＜０．０５）。对照组治疗后仅ＰＬＧ比治疗前降低（Ｐ＜０．０５）。２组病人ＴＰＡ、ＰＡＩ比较有差异（Ｐ＜０．０５）。结论：巴曲抗栓酶对肺心病病人血栓前状态运用有一定价值。     

卡托普利对主动脉平滑肌细胞增殖的影响

目的：观察卡托普利（Ｃａｐ）对平滑肌细胞（ＳＭＣ）增殖的作用及其作用机制。 方法：用高脂血清（ＨＬＳ）造成体外培养猪主动脉ＳＭＣ增殖。 结果：ＨＬＳ培养促进ＳＭＣ增殖，加Ｃａｐ（０．２ｍｇ·Ｌ＾－１）后拮抗ＳＭＣ增殖，使丙二醇（ＭＤＡ）含量，纤溶酶原激活物抑制物（ＰＡＩ）活性明显减少，６－酮－前列腺素Ｆ１α（６－ｋｅｔｏ－ＰＧＦ１α）及环腺苷－磷酸（ｃＡＭＰ）含量明显增加（Ｐ〈０．０５－０．０１）     

慢性肾衰病人胰岛素和纤维蛋白溶解活性变化的观察

为探讨慢性肾衰（ＣＲＦ）病人胰岛素代谢异常和纤溶活性降低间的内在关系,采用邻苯胺法、放射免疫法和发色物显色法检测ＣＲＦ病人空腹血糖（ＦＢＳ）、血清Ｃ－肽（Ｃ－Ｐ）、胰岛素（ＩＮＳ）、纤溶酶原活性抑制物（ＰＡＩ）和组织型纤溶酶原激活剂９ｔ－ＰＡ）的变化。结果表明,ＣＲＦ病人ＦＢＳ、Ｃ－Ｐ、ＩＮＳ－ＰＡＩ均明显增高,而ｔ－ＰＡ明显降低。ＩＮＳ水平与ＦＢＳ、Ｃ－Ｐ及ＰＡＩ呈直线正相关。结论：ＣＲＦ病人Ｉ     

三七总皂苷对冠心病患者过氧化脂质及纤维蛋白溶酶原激活物的影响

目的：观察三七总皂苷对冠心病患者血清超氧化物歧化酶（ＳＯＤ）、过氧化脂质（ＬＰＯ）、组织型纤维蛋白溶酶原激活物（ｔＰＡ）及组织型纤维蛋白溶酶原激活物抑制剂（ＰＡＩ－１）的影响。方法：将４５例患者分成２组,三七总皂苷治疗组用三七总皂苷注射液５００ｍｇ加入２５０ｍｌ液体中静滴,ｑｄ,共１周,余治疗同对照组。结果：治疗组血清ＳＯＤ活力明显增高（Ｐ〈０．０１）,ＬＰＯ含量降低（Ｐ〈０．０１）。对照组ＳＯＤ活力及ＬＰＯ含量用药前后无明显改变（Ｐ均〉０．０５）,血清ＳＯＤ的含量在治疗组用药前后和对照组皆无明显差别（Ｐ均〉０．０５）。三七总皂苷治疗后ｔＰＡ明显高于治疗组,ＰＡＩ－１明显低于治疗前（Ｐ均〈０．０１）。而对照组治疗前后无明显变化（Ｐ均〉０．０５）。结论：三七总皂苷能升高冠心病患者ＳＯＤ活力,降低ＬＰＯ含量,提高纤     

卡托普利对兔血浆t—PA和PAI—1活性水平的影响

目的：观察卡托普利及兔血浆ｔ－ＰＡ和ＰＡＩ－１活性水平的影响。方法：选用新西兰白兔１１只，给予卡托普利０．５ｍｇ／ｋｇ，ｉｇ。用药及前用药后２ｈ各采集静脉血１ｍｌ，采用发色底物显色法测定血浆ｔ－ＰＡ和ＰＡＩ－１活性。结果：应用卡托普利２ｈ后血浆ｔ－ＰＡ活性显著增高，ＰＡＩ－１活性明显降低。ｔ－ＰＡ与ＰＡＩ－１比值显著升高。结论：卡托普利可以促进纤溶系统的功能。     

巴曲抗栓酶临床应用进展

巴曲抗栓酶是通过生物工程ＤＮＡ合成的单一酶,选择性地作用于凝血因子ＩＡ２链,释放血纤维蛋白肽Ａ,使纤维蛋白分解,并促使组织纤溶酶原激活物（ＴＰＡ）释放和活性增加．促进纤维蛋白溶酶生成,减少纤溶酶原激活抑制物（ＰＡＩ）和抗纤溶酶,促使血栓溶解,防止血栓继续生成,根据巴曲抗栓酶的上述药理作用,临床应用日趋广泛,现综述如下。１缺血性脑血管疾病［１］ 巴曲抗栓酶具有分解凝血因子Ｉ（ＦＧ）抑制血栓形成、诱发ＴＰＡ释放、增强ＩＰＡ的作用,促进纤维蛋白溶酶的生成,减少纤维蛋白溶酶抑制物（ａ２—ＰＩ）和 ＰＡＩ的…     

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.