长松萝多糖抑瘤作用的初步研究

通过建立S180肉瘤模型,测定抑瘤率,研究长松萝多糖对S180荷瘤小鼠的抑瘤作用.通过碳粒廓清实验,测定多糖对小鼠单核-巨噬细胞吞噬功能的影响.结果ip该多糖100～150mg/kg@d,对S180荷瘤小鼠的抑瘤率为30%～45.3%;该多糖对小鼠单核-巨噬细胞的吞噬功能有增强作用.     

参苓胶囊对氟尿嘧啶增效减毒作用的研究

目的:研究参苓胶囊与氟尿嘧啶(FU)配伍对小鼠移植肿瘤S180,H22,Lewis抑瘤作用及对FU所致小鼠免疫功能抑制的保护作用.方法:按照抗癌药物筛选规程进行体内抑瘤实验;采用FU制备免疫功能低下模型,测定参苓胶囊与FU配伍对小鼠白细胞计数、腹腔巨噬细胞吞噬功能及NK细胞活性的影响.结果:不同剂量的参苓胶囊与FU配伍用均能明显提高FU对小鼠移植肿瘤S180,H22,Lewis的抑瘤率,其中高剂量组抑瘤效果最佳,配伍且能明显拮抗FU所致白细胞下降、腹腔巨噬细胞功能降低及NK细胞活性降低等毒副作用.结论:参苓胶囊与FU配伍能有明显提高FU抗肿瘤及降低其毒副作用.     

高乌甲素对S180荷瘤小鼠的免疫调节作用研究

目的:研究高乌甲素(LA)对S180荷瘤小鼠的免疫调节作用。方法:每只小鼠腋窝皮下接种S180荷瘤生理盐水混悬液,24h后肌肉注射LA,每天给药1次,连续10d。检测S180荷瘤小鼠的免疫功能。结果:LA能显著升高S180荷瘤小鼠血清免疫球蛋白G(IgG)抗体水平;对2,4-二硝基氟苯诱导的迟发性超敏反应有增强作用;能诱导淋巴细胞转化为淋巴母细胞;能显著提高S180荷瘤小鼠网状内皮系统的吞噬功能;且能增强其红细胞免疫功能。结论:LA对小鼠S180荷瘤的生长具有抑制作用,能显著增强S180荷瘤小鼠的细胞免疫功能。     

马甲子叶提取物的抗肿瘤活性研究

目的 研究马甲子叶提取物的体内外抗肿瘤活性.方法 采用系统溶剂萃取法萃取马甲子叶醇提物,采用MTT法分别检测马甲子叶水提物、醇提物、石油醚部位、乙酸乙酯部位和正丁醇部位对人肝癌HepG-2、人胃癌MGC-803、人宫颈癌Hela细胞的体外抗肿瘤活性;考察马甲子叶乙酸乙酯部位对S180荷瘤小鼠的体内抗肿瘤活性.结果 马甲子乙酸乙酯部位对3种肿瘤细胞均有明显抑制作用,呈一定量效关系,IC50分别为23.68、24.91、75.32 μg·mL-;乙醇提取物和石油醚部位对3种肿瘤细胞均有一定抑制作用;正丁醇部位和水提物的抑制作用不明显.乙酸乙酯部位对S180荷瘤小鼠的体内抗肿瘤作用明显,中剂量的抑瘤效果与环磷酰胺的相当,抑瘤率达49.38％.结论 马甲子叶乙酸乙酯部位的抗肿瘤活性最强.     

冬苓扶正液对氟尿嘧啶增效解毒作用研究

目的：研究冬苓扶正液与氟尿嘧啶(FU)配伍用对小鼠移植肿瘤S180、H222、Lewis的抑瘤作用及对FU所致小鼠免疫功能抑制的保护作用。方法：按照抗癌药物筛选规程进行体内抑瘤实验；采用FU制各免疫功能低下模型，测定冬苓扶正液与FU配伍用对小鼠白细胞计数、免疫器官重量、腹腔巨噬细胞吞噬功能的影响。结果：不同剂量的冬苓扶正液与FU配伍用均能明显提高FU对小鼠移植肿瘤S180、H22、Lewis的抑瘤率，其中高剂量组抑瘤效果最佳，配伍用又能明显拮抗FU所致白细胞下降、胸腺、脾脏萎缩及腹腔巨噬细胞功能降低等毒副作用。结论：冬苓扶正液与FU配伍用具有明显提高FU抗肿瘤及降低其毒性作用。     

肝康灵胶囊对化疗药物的增效减毒作用研究

目的:研究肝康灵胶囊(GKL)对化疗药物的增效减毒作用。方法:以体内抑瘤实验测定GKL单独使用及与顺铂(DDP)伍用时对小鼠移植性肿瘤(S180肉瘤、H22肝癌和Lewis肺癌肿瘤)的抑癌率,并考察GKL分别与DDP和丝裂霉素(MMC)伍用时对荷瘤小鼠白细胞数、免疫器官质量、巨噬细胞吞噬功能和自然杀伤(NK)细胞活性的影响。结果:GKL对小鼠移植性肿瘤(S180肉瘤、H22肝癌和Lewis肺癌肿瘤)均有抑制作用;当其分别与MMC和DDP伍用时,能显著提高2种化疗药物的抑癌率(P<0.01);GKL还可显著减少MMC和DDP所致小鼠白细胞下降、免疫器官萎缩、巨噬细胞吞噬功能下降和NK细胞活性降低等副作用。结论:GKL具有显著的抗肿瘤和增效减毒作用。     

荔枝核的抑瘤作用及对肝癌组织端粒酶活性的影响

目的:建立肝癌荷瘤小鼠模型,研究荔枝核水提物对小鼠模型实体瘤生长的影响。方法:小鼠S180肿瘤细胞与肝癌细胞混悬液用生理盐水按1∶1进行稀释,制成含瘤腹水混悬液;在给药前24h每只小鼠腋窝皮下接种0.2mL,整个操作在无菌条件下60min内完成。对小鼠S180肿瘤细胞、肝癌细胞连续10d给予荔枝核水提物,观察S180肿瘤细胞和肝癌细胞的生长情况、肝癌荷瘤小鼠体内Bcl -2的水平及肝癌细胞的凋亡情况。结果:荔枝核水提物能显著抑制S180肿瘤细胞和肝癌细胞的生长(P<0.01) ;荔枝核能显著升高肝癌荷瘤小鼠体内Bcl -2的水平(P<0.05或P<0.01) ;荔枝核能够显著促进肝癌细胞的凋亡。结论:荔枝核的抑瘤作用可能与升高动物体内的Bcl -2水平及促进癌细胞的凋亡有关。     

传统中药白花蛇舌草的抗肿瘤活性研究(英文)

研究了传统中药白花蛇舌草的乙醇提取有效部位对S180小鼠模型的肿瘤生长抑制作用、免疫系统及小鼠生存天数的影响。该醇提部位能有效抑制S180小鼠的肿瘤生长,并延长荷瘤小鼠的生存天数。通过灌胃给药,醇提有效部位在10mg/kg的剂量下与阳性对照药物环磷酰胺(20mg/kg)相比,能够有效降低荷瘤小鼠体内的肿瘤大小与重量。对荷瘤小鼠的脾指数,胸腺指数及血常规参数研究表明,该醇提有效部位对荷瘤小鼠未见明显的毒副作用。总之,研究结果表明白花蛇舌草的醇提部位具有有效的抗肿瘤活性。     

百多宁乳剂对荷S_(180)肉瘤小鼠免疫功能的影响

目的研究百多宁乳剂对荷S180肉瘤小鼠免疫功能的影响。方法建立小鼠体内荷S180肉瘤模型,以脾指数、胸腺指数、炭粒廓清指数、吞噬系数以及其对脾脏T、B淋巴细胞增殖能力作为免疫学指标,考察百多宁乳剂对荷S180肉瘤小鼠免疫功能的影响。结果静脉给予荷S180小鼠百多宁乳剂1、2 g.kg-1,7 d后能够显著提高其脾指数、炭粒廓清指数、吞噬系数,作用强于相同剂量的康莱特和鸦胆子;而对其胸腺指数则影响不大。同时,BDN既能够直接促进小鼠脾淋巴细胞增殖作用,又能协同促进刀豆蛋白A、脂多糖诱导的脾T、B淋巴细胞增殖。结论百多宁乳剂能够显著提高荷S180肉瘤小鼠的免疫能力。     

兔儿伞醇提物的抗肿瘤实验

目的:研究兔儿伞醇提物的抗肿瘤作用。方法:以S180小鼠模型研究兔儿伞醇提物的体内抗肿瘤作用,及对脾脏、胸腺指数的影响。结果:兔儿伞醇提物对S180有显著的抑制作用,明显增加胸腺指数,但对脾脏指数没有明显影响。结论:兔儿伞醇提物具有一定的体内抗肿瘤活性。     

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.     

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.