清肝利胆浸膏保肝、利胆的实验研究

目的：观察清肝利胆浸膏对急性肝损伤的保护作用和利胆、退黄作用。方法：用CCL4－和D－GaL致小鼠急性肝损伤，观察血清ALT和AST；用麻醉大鼠胆管收集胆汁，测定胆汁中胆固醇和总胆红素的含量；用异硫氰酸－1－萘酯造成黄疸模型，测定血液中ALT和AST、总胆红素。结果：清肝利胆浸膏能显著降低CCL4致小鼠ALT和AST升高，对D－GaL致小鼠ALT和AST升高亦有明显降低，对大鼠胆汁分泌有增加，对胆汁成份胆固醇、总胆红素升高有明显的降低。结论：清肝利胆浸膏具有一定的保肝降酶、利胆和退黄作用。     

复方丹参注射液退黄降酶保肝作用的实验研究

本实验主要研究复方丹参注射液的退黄降酶保肝作用。采用四氯化碳(CCl4)、D-半乳糖胺(D-Gla)致小鼠急性肝损伤模型,观察复方丹参注射液对肝损伤的保护作用;采用异硫氰酸萘酯(ANIT)致小鼠急性黄疸模型,观察复方丹参注射液对急性黄疸的退黄降酶作用。通过以上实验可以得出复方丹参注射液能明显降低CCl4和D-Gla致小鼠急性肝损伤模型血清中丙氨酸氨基转移酶(ALT)、天冬氨酸氨基转移酶(AST)活性和总胆红素(T-BIL)含量;复方丹参注射液能明显降低ANIT致小鼠急性黄疸模型血清中ALT、AST、T-BIL和丙二醛(MDA)含量,升高超氧化物歧化酶(SOD)活性。综上所述,复方丹参注射液具有退黄降酶保肝作用,其机制可能与抗氧化作用有关。     

茵陈郁金汤对小鼠急性肝损伤的影响

目的:观察茵陈郁金汤对四氯化碳(CCl4)致小鼠急性肝损伤MDA、GSH-Px 及SOD的变化.方法:采用腹腔注射CCl4致小鼠急性肝损伤为模型,联苯双酯作为阳性对照药物,测定高、中、低剂量的茵陈郁金汤对肝损伤时MDA的含量,GSH-Px 及SOD活性.结果:茵陈郁金汤能够明显降低CCl4致小鼠急性肝损伤肝组织中 MDA含量(P＜0.01),提高 GSH-Px 、SOD活力(P＜0.05).说明茵陈郁金汤对肝脏损伤具有明显的保护作用.     

复方茵虎汤对实验性肝损伤的保护作用

目的：本实验研究复方茵虎汤（复方茵虎汤）对四氯化碳致小鼠肝损伤的保护作用。方法：以腹腔注射四氯化碳（CCl4）建立小鼠肝损伤模型,以复方茵虎汤作为受试药物,以联苯双酯作为阳性对照药物,以肝指数（LJI）、血清中谷氨酸氨基转移酶（ALT）、天冬氨酸转氨酶（AST）、肝组织匀浆中超氧化物歧化酶（SOD）和丙二醛（MDA）水平为检测指标,观察复方茵虎汤对肝损伤的保护作用。结果：复方茵虎汤能够明显降低CCl4致小鼠肝损伤血清中ALT和AST水平,升高肝组织中SOD水平,降低肝组织中MDA水平,减轻四氯化碳对肝脏细胞的病理损伤。结论：复方茵虎汤对CCl4致小鼠急性肝损伤有一定的保护作用。     

雪域肝胆康胶囊对小鼠实验性肝损伤及胆汁的影响

目的 研究藏药雪域肝胆康胶囊(XYGD)的保肝利胆作用.方法 以CCl4制作动物急性肝损伤模型,测定血清ALT、AST、TBIL的含量,观察XYCD对动物急性肝损伤的影响;采用麻醉大鼠行胆汁引流术,测定正常大鼠的胆汁分泌量及胆汁成分.结果 雪域肝胆康胶囊能明显降低CCl4急性肝损伤动物血清ALT、AST水平;使正常大鼠的胆汁流量明显增加,降低胆汁中胆固醇的浓度.结论 XYGD有明显保肝、利胆作用.     

紫草大黄合剂对四氯化碳致小鼠急性肝损伤保护作用的观察

目的：观察不同浓度的紫草大黄合剂对四氯化碳（CCl4）致小鼠急性肝损伤的保护作用。方法：采用腹腔注射CCl4致小鼠急性肝损伤为模型，测定高低剂量的紫草大黄合剂对肝损伤ALT、AST值，同时对肝组织进行病理组织检查。结果：高剂量紫草大黄合剂同联苯双酯一样能够明显降低CCl4致小鼠肝损伤血清ALT、AST值升高（P＜0．01），减轻CCl4对肝脏细胞的病理损伤。结论：紫草大黄合剂对CCl4致急性肝损伤具有一定的保护作用。     

降脂利肝颗粒对小鼠急性肝损伤的保护作用

目的：研究降脂利肝颗粒对急性肝损伤小鼠的保护作用。方法：以四氯化碳（CCl4）诱导急性肝损伤制作肝损伤小鼠模型，分别给予低（100mg／kg）、中（300mg／kg）、高（900mg／kg）3个剂量的降脂利肝颗粒浸膏，以联苯双酯（200mg／kg）为阳性对照药物，检测血清中丙氨酸氨基转移酶（ALT）和门冬氨酸氨基转移酶（AST）的水平，并进行病理学检查。结果：与模型对照组比较，降脂利肝颗粒浸膏低、中、高3个剂量组ALT和AST水平显著降低（P〈0．05）。降脂利肝颗粒浸膏低剂量组降低ALT水平的作用不如阳性对照联苯双酯组明显，中、高剂量组作用与联苯双酯组相似。降脂利肝颗粒浸膏低、中、高3个剂量组均能减轻肝组织病理损伤程度。结论：降脂利肝颗粒对小鼠急性肝损伤具有较好的保护作用。     

赤丹退黄颗粒对大鼠实验性肝损伤的保护作用

赤丹退黄颗粒是由赤芍、瓜娄、丹参等组成的复方中药制剂，具有凉血活血，清热祛湿等功效，主治血淤血热，湿热中阻所致重症黄疸肝炎。本文通过对α-萘异硫氰酸酯造成实验性大鼠肝内胆汁淤积模型，观察赤丹退黄颗粒对胆汁排泄的影响。     

姜黄素保肝作用的实验研究

目的：研究姜黄素的肝脏保护作用。方法：采用H22肝癌细胞移植模型、CCl4所致小鼠急性肝损伤模型和CCl4所致大鼠慢性肝损伤模型,检测移植小鼠瘤重、急性肝损伤小鼠血清谷丙转氨酶（ALT）水平和大鼠血清ALT、谷草转氨酶（AST）、总蛋白（TP）、白蛋白、羟脯氨酸水平。结果：姜黄素可减轻肝癌H22荷瘤小鼠的瘤重,且对荷瘤小鼠白细胞的降低有一定的升高作用;姜黄素能显著降低CCl4所致小鼠血清ALT的升高,且对大鼠慢性肝损伤过程中的肝纤维化也有一定的保护作用。结论：姜黄素有一定保肝作用,但其机制需要进一步研究。     

陆英提取物对急性化学性肝损伤的保护作用

目的研究陆英中保肝降酶活性部位提取物(LY)保肝降酶的功效。方法采用急性CCl4肝损伤模型、D半乳糖胺盐酸盐大鼠急性肝损伤模型、ConA致小鼠急性肝损伤模型研究LY灌胃给药对急性实验性肝损伤的保护作用,同时采用碳粒廓清实验考察了LY灌胃给药对小鼠非特异性免疫功能的的影响。结果LY对CCl4致小鼠急性肝损伤有明显的保护作用,其保肝作用可能与对抗脂质过氧化有关;对D半乳糖胺盐酸盐致大鼠急性肝损伤和ConA所致小鼠急性肝损伤亦有明显的保护作用;能增强小鼠非特异性免疫功能。结论LY对多种急性实验性肝损伤有明显的保护作用并且能增强小鼠非特异性免疫功能的作用。     

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.