女贞子提取物的体内抗肿瘤作用

目的：观察女贞子中含有熊果酸和齐墩果酸粗提物的抗肿瘤作用。方法：采用小鼠移植性肿瘤模型，观察了女贞子提取物（Extract of Nu Zhen Zi,ENZZ）对H22肝癌、S180肉瘤荷瘤小鼠的抑瘤作用，对S180荷瘤小鼠的生命延长作用。结果：女贞子提取物对小鼠移植性肿瘤H22有抑制，ENZZ250mg/kg，500mg/kg，1000mg/kg组平均抑瘤率分别为41.49%、48.32%、45.45%，对S180肉瘤实体型有抑制作用，上述三个剂量的抑瘤率分别为37.50%、44.23%、46.15%；女贞子提取物对S180肉瘤腹水型，H22肝癌腹水型无生命延长作用。结论：女贞子提取物对移植性肿瘤H22肝癌、S180肉瘤有抑制作用。     

盐酸小檗碱对小鼠移植性肿瘤的抑制作用

目的 研究盐酸小檗碱的体内抗肿瘤活性.方法 应用移植性实体瘤H22,宫颈癌U14,肉瘤S180荷瘤小鼠作为动物模型,腹腔给药观察小鼠生长情况,并计算抑瘤率.结果 盐酸小檗碱10,20,25 mg/kg剂量对肝癌H22的抑制率分别为25.82%,36.81%和40.66%;盐酸小檗碱10,20 mg/kg剂量对宫颈癌U14抑制率分别为37.80%和59.90%;盐酸小檗碱15,20 mg/kg剂量对肉瘤S180的抑制率分别为30.85%和39.80%.结论 盐酸小檗碱可抑制肝癌H22、宫颈癌U14、肉瘤S180在小鼠体内的生长.     

黄精多糖抗肿瘤作用的实验研究

目的研究黄精多糖对H22实体瘤、S180腹水瘤的生长抑制作用和对荷瘤小鼠免疫调节作用。方法小鼠接种H22实体瘤或S180腹水瘤后随机分组,灌胃给予不同剂量[100、200、400mg/(kg.d)]的黄精多糖,以生理盐水和环磷酰胺为空白对照组和阳性对照组,计算黄精多糖对小鼠H22实体瘤生长的抑制率,脾脏指数和胸腺指数,以及S180腹水型荷瘤小鼠的存活时间。结果给予黄精多糖灌胃的荷瘤小鼠的脾脏指数和胸腺指数显著增加;低、中、高剂量的黄精多糖对H22实体瘤的抑瘤率分别是(34.93、43.44、56.25)%;中、高剂量的黄精多糖可以显著延长S180腹水型荷瘤小鼠的存活时间。结论黄精多糖有显著的抗肿瘤作用和免疫调节活性。     

白花蛇舌草多糖对S180和H22荷瘤小鼠的抗肿瘤作用研究

目的研究白花蛇舌草多糖对S180和H22荷瘤小鼠的抑瘤作用及对免疫器官的影响。方法应用肉瘤S180、肝癌H22荷瘤小鼠作为动物模型,连续灌胃给药10 d后脱颈椎处死,剥离肿瘤、胸腺、脾脏,称质量,计算抑瘤率及胸腺、脾脏指数。结果分别以30,20和10 mg.kg-1剂量的白花蛇舌草多糖灌胃,对肉瘤S180的抑制率分别为36.09%,28.66%和17.54%,对肝癌H22的抑制率分别为49.68%,40.47%和27.19%,相比模型组有显著性差异(P<0.05),对荷瘤小鼠的胸腺指数、脾脏指数无明显影响。结论白花蛇舌草多糖对S180和H22荷瘤小鼠均有抗肿瘤作用,并呈现一定的量效关系。     

核桃楸树皮水提取物抗突变和抑瘤作用研究

目的 研究核桃楸树皮水提取物的抗突变和抑瘤作用.方法 以小鼠骨髓细胞微核试验和小鼠睾丸染色体畸变实验,观察核桃楸树皮水提取物的抗突变作用;以S-180和H-22移植性肿瘤观察其抑瘤效果.结果 核桃楸树皮水提取物高、低剂量组和环磷酰胺阳性对照组的微核率分别为17.6‰、25.3.5‰、35.7‰;核桃楸树皮水提取物高、低...     

肝乐康抗肿瘤作用的研究

目的 研究肝乐康对肝癌细胞株BeL-7402增殖的抑制作用和对S180实体瘤型小鼠的抗肿瘤作用.方法 以MTT法测定含药复方肝乐康血清对肝癌细胞株BBL-7402的增殖情况;将小鼠接种S180实体瘤后检测肝乐康对小鼠S180实体瘤生长的抑制作用以及对荷瘤小鼠脾脏指数和胸腺指数的影响.结果 不同剂量的肝乐康显著抑制肝癌细胞株BBL-7402的增殖,对S180实体瘤的抑瘤率分别为33.72%、41.36%、54.21%.结论 肝乐康具有较强的抗肿瘤作用.     

美洲大蠊多肽提取物对荷瘤小鼠肿瘤生长及免疫功能的影响

目的:研究美洲大蠊多肽提取物的体内抗肿瘤作用及其对荷瘤小鼠免疫功能的影响。方法:制备美洲大蠊多肽提取物,TLC薄层色谱法鉴别美洲大蠊多肽提取物;建立小鼠肉瘤S180及小鼠肝癌H22移植性肿瘤模型,观察美洲大蠊多肽提取物对荷瘤小鼠肿瘤生长的抑制作用;采用腹腔巨噬细胞吞噬实验、淋巴细胞转化实验及Elisa法测定细胞因子IL-2,IL-6,IL-12,TNF-α的水平,检测美洲大蠊多肽提取物对荷瘤小鼠免疫功能的影响。结果:美洲大蠊多肽提取物含多种氨基酸和多肽;在25,50,100 mg·kg-1时美洲大蠊多肽提取物对S180的抑瘤率分别为29.08%,45.92%,55.61%,对H22的抑瘤率分别为16.51%,25.94%,46.23%,且能提高荷瘤小鼠的脾指数和胸腺指数;美洲大蠊多肽提取物能增强荷瘤小鼠腹腔巨噬细胞的吞噬功能,促进淋巴细胞转化反应,升高荷瘤小鼠细胞因子IL-2,IL-6,IL-12,TNF-α的水平。结论:美洲大蠊多肽提取物有较强的体内抗肿瘤活性,其抗肿瘤机制可能与增强荷瘤机体免疫功能有关。     

银耳孢糖对荷瘤小鼠环磷酰胺化疗的增效作用

目的:研究银耳孢糖(Tremella fuciformis spores polysaccharide,TSP)对环磷酰胺(CTX)化疗H22及S180荷瘤小鼠的增效作用.方法:建立小鼠肝癌H22及小鼠肉瘤S180的体内移植性肿瘤模型,随机分为对照组,TSP小、中、大剂量组,CTX小、大剂量组,TSP(小、中、大剂量) CTX小剂量组,TSP(小、中、大剂量) CTX大剂量组等12组,接种肿瘤次日开始每天分别腹腔给予0.9%氯化钠注射液、TSP(25,50及100 mg·kg-1)、CTX(10,20 mg·kg-1)、TSP(25,50,100 mg·kg-1) CTX 10 mg·kg-1及TSP(25,50及100 mg·kg-1) CTX 20 mg·kg-1,连续12～14 d,称小鼠的瘤重,测定TSP对CTX的增效作用,每批实验重复3次.结果:TSP 25,50,100 mg·kg-1可明显增加CTX(10,20 mg·kg-1)对H22及S180荷瘤小鼠的抑制作用,抑瘤率分别提高6.82～92.01%,3.90～24.27%(P<0.05,0.01);9.50～87.04%,2.41～21.51%(P<0.05,0.01).结论:TSP与CTX合用对抑制荷瘤小鼠H22及S180有明显的增效作用.     

中药仙鹤复方水提取物对S180肉瘤和H22肝癌细胞在小鼠体内的抗肿瘤作用研究

目的观察中药仙鹤复方水提取物对移植型鼠源S180肉瘤和H22肝癌细胞在荷瘤动物体内抗肿瘤作用。方法昆明种受试小鼠,接种S180肉瘤和H22肝癌细胞后随机分为空白对照组、阳性对照组及中药仙鹤复方水提取物高、中、低3个剂量组。观察中药仙鹤复方水提取物对肿瘤的抑制作用及动物体质量、免疫器官重量的影响。结果中药仙鹤复方水提取物对鼠源移植型S180肉瘤细胞和H22肝癌细胞在荷瘤小鼠体内的增殖均有明显的抑制作用;且对两种荷瘤小鼠的免疫器官脾脏及胸腺均有显著性的保护作用影响。结论中药仙鹤复方水提取物在动物体内具有较好的抑瘤作用,且对荷瘤小鼠免疫器官有保护作用,具备减毒的功效。     

槐属植物生物碱衍生物施普睿达抗肿瘤作用的研究

目的:对槐属植物生物碱衍生物施普睿达体内抗肿瘤作用进行研究,并通过肝、脾、胸腺指数等多项指标综合考查施普睿达对荷瘤动物免疫机能的影响。方法:将昆明种小鼠移植宫颈癌U14、肉瘤S180和肝癌H22细胞后,腹腔注射施普睿达,观察施普睿达对实体瘤的抑瘤率。结果:施普睿达对3种移植瘤均有明显的抑制作用,最佳抑瘤率分别为U1474.3%、S18073.9%和H2279.3%,对小鼠的肝、脾指数和胸腺指数几乎无影响;而阳性对照药顺铂使小鼠的肝重、脾指数和胸腺指数明显下降。结论:施普睿达具有抑制S180、U14及H22等多种小鼠移植性肿瘤生长的作用,而且不影响荷瘤动物体重及免疫功能,属于低毒的抗肿瘤新药。     

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.