槐角颗粒的主要药效学研究

目的观察槐角颗粒的主要药理作用.方法采用断尾凝血法、体外凝血法、扭体法、热板致痛法、耳廓肿胀法、腹腔毛细血管通透性观察法、棉球肉芽肿法、体内外抑菌试验等方法.结果槐角颗粒可明显缩短小鼠断尾后的出血时间及血管内凝血时间;对抗0.6%冰醋酸所致小鼠的扭体次数增加,提高小鼠的痛阈值;抑制致炎液所致小鼠耳廓的肿胀度;抑制冰醋酸所致小鼠腹腔毛细血管通透性的增加;抑制大鼠棉球肉芽肿的增长;并具有明显的抑菌作用.结论槐角颗粒与原丸剂型一样具有明显的止血、凝血及镇痛、抗炎、抗菌等药理作用.     

清胃黄连丸抗炎作用的实验研究

目的观察清胃黄连丸的抗炎作用。方法采用醋酸所致小鼠腹腔毛细血管通透性增高,大鼠蛋清性足肿胀及二甲苯所致小鼠耳廓肿胀的方法来评价清胃黄连丸的抗炎效果。结果清胃黄连丸可以显著抑制醋酸所致小鼠毛细血管通透性增高,抑制蛋清所引起的大鼠足肿胀,抑制二甲苯所致小鼠的耳廓肿胀。结论清胃黄连丸具有抗炎作用。     

活血壮筋片的主要药效学实验研究

目的观察活血壮筋片抗炎、活血及对机体的免疫调节作用。方法采用二甲苯致小鼠耳廓肿胀，以肿胀度比较活血壮筋片的抗炎作用。用倒置生物显微镜观察对小鼠耳廓微循环的影响。通过观察吞噬鸡红细胞的巨噬细胞数计算吞噬百分率及吞噬指数。结果活血壮筋片高、中剂量组对二甲苯所致小鼠耳廓肿胀有明显抑制作用（P＜0.01＝，而低剂量不能减小耳廓肿胀度。 高、中、低剂量对小鼠耳廓三级小动脉与三级小静脉有扩张作用，并能增加毛细血管开放数，与阴性对照组比较，差异有显著性（P＜0.05＝。活血壮筋片高、中剂量能增加小鼠腹腔吞噬细胞的吞噬百分率和吞噬指数，与对照组比较其差异有显著性，而低剂量作用不明显。结论活血壮筋片有较好的抗炎、活血及免疫调节功能。     

眼络通冲剂对血小板聚集和微循环的作用研究

目的探讨眼络通冲剂(YLTG)对血小板聚集和微循环的作用。方法实验用体外ADP诱导法,测定大鼠血小板聚集作用;小鼠灌胃给予眼络通冲剂连续10d,观察对小鼠耳廓微循环的作用。结果YLTG能抑制ADP诱导的大鼠血小板聚集;能明显扩张小鼠耳廓微动脉,使毛细血管开放数增加,血流速度加快。结论YLTG具有预防抑制血栓形成,改善微循环,从而起到改善视力的作用。     

清喉口含片抗炎作用实验研究

目的：研究清喉口含片的抗炎作用。方法通过考察高、中、低剂量清喉口含片对巴豆油所致小鼠耳廓肿胀度的抑制作用,组织胺所致小鼠腹腔毛细血管通透性改变的影响及角叉菜胶所致大鼠足跖肿胀度的抑制作用,研究清喉口含片对不同炎症模型的抗炎作用。结果与空白对照组及阳性药对照组相比,清喉口含片高、中、低剂量均能够降低小鼠毛细血管通透性,抑制角叉菜胶致大鼠足跖肿胀及巴豆油致小鼠耳廓肿胀。结论清喉口含片具有较明显的抗炎作用。     

小儿退热贴抗炎作用的实验研究

目的:评价小儿退热贴的抗炎作用.方法:参考相关文献制成小鼠耳廓炎性肿胀及醋酸致小鼠腹腔毛细血管通透性增高的模型,随机分为小儿退热贴大、中、小剂量组,0.9%氯化钠溶液组和西药组各10只,分别给予治疗.治疗后处死动物,测量致炎耳廓的肿胀度和腹腔冲洗液的吸光度,以评价小儿退热贴的抗炎作用.结果:小儿退热贴对二甲苯所致小鼠耳廓炎症有明显的抑制作用,对醋酸所致小鼠腹腔毛细血管通透性增高有明显抑制作用.结论:小儿退热贴有抗炎作用.     

复方生肌膏的药效学研究

目的 进行复方生肌膏的药效学研究。方法 分别制备小鼠耳廓肿胀模型和小鼠腹腔毛细血管通透性增加模型，观察耳廓局部外用复方生肌膏对小鼠耳廓肿胀的作用，以及背部涂抹复方生肌膏对小鼠腹腔毛细血管通透性增加的影响。结果 复方生肌膏对小鼠耳廓肿胀有显著的抑制作用，能明显抑制醋酸所致的小鼠腹腔毛细血管通透性增加。结论 复方生肌膏具有明显的抗炎作用。     

鼻渊灵口服液的抗炎作用

目的：研究鼻渊灵口服液的抗炎作用。方法：用二甲苯致小鼠耳廓肿胀、蛋清致大鼠足跖肿胀、醋酸至小鼠腹腔毛细血管通透性增加及大鼠棉球肉芽肿等动物实验模型研究其抗炎作用。结果：对二甲苯致小鼠耳廓肿胀、蛋清致大鼠足跖肿胀、醋酸致小鼠腹腔毛细血管通透性增加及大鼠棉球肉芽肿等均有显著的抑制作用。结论：鼻渊灵口服液具有明显的抗炎作用。     

前列宁栓抗炎镇痛作用实验

目的:研究前列宁栓的抗炎、镇痛作用。方法:采用二甲苯所致小鼠耳廓肿胀实验、角叉菜胶致大鼠足跖肿实验、大鼠棉球肉芽肿的影响实验、小鼠腹腔毛细血管通透性实验,细菌性(大肠杆菌)前列腺炎的抗炎作用。采用醋酸致小鼠扭体反应实验和小鼠热板法实验观察了前列宁栓的镇痛作用。结果:前列宁栓可明显抑制二甲苯所致的小鼠耳廓炎症;在多数时间降低角叉菜胶致大鼠足跖肿胀;明显抑制大鼠棉球肉芽肿的生成;明显降低小鼠腹腔毛细血管通透性;明显抑制大鼠细菌性前列腺炎;明显降低醋酸致小鼠扭体反应数;明显升高小鼠痛阈值。结论:前列宁栓具有明显的抗炎、镇痛作用。     

引流熊胆的肮炎免疫抑制作用

引流熊胆Ｉｇ能明显地抑制二甲苯，巴豆油所致小鼠耳壳肿胀，抑制小鼠腹腔毛细血管通透性，抑制角叉菜胶所致大鼠足肿胀及Ｐｒｅｕｎｄ完全佐剂所致大鼠关节炎，对肾上腺，胸腺，脾脏及淋巴结重量无明显影响。抑制小鼠棉球肉芽肿增生，抑制小鼠单核巨噬细胞吞噬功能。表明引流熊胆具有抑制急，慢性及免疫性炎症作用免疫抑制作用。引流熊胆还抑制大鼠热烫足肿胀，减少大鼠炎平部位ＰＧＥ２含量。提示引流熊量的抗炎作用与抑制炎症部位     

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.