响应面法优化复方体外培育牛黄凝胶中药物配比

目的：优选复方体外培育牛黄凝胶中药物的配比,为该制剂的开发应用提供参考。方法：采用体外抑菌实验,在单因素试验基础上,以痤疮丙酸杆菌抑菌圈直径为指标,进行响应面优化设计,考察不同药物配比后对痤疮丙酸杆菌的抑菌效果,最终找到最佳配比。结果：模拟预测最佳复方体外培育牛黄凝胶复配比例为体外培育牛黄∶盐酸小檗碱∶丹皮酚∶桉油= 1.69∶3∶3∶2.38,在此复配比例下可得到痤疮丙酸杆菌的平均抑菌圈直径为29.88 mm,与预测值29.56 mm的相对误差为1.1%。结论：用响应面优化法模拟预测的抑菌圈直径与实测值非常相似,响应面优化法可较好地用于复方体外培育牛黄凝胶配伍比例的研究。     

陶瓷膜技术和水提醇沉法对咽舒宁复方水提液精制的比较研究

目的考察并对比研究Al2O3陶瓷膜技术和水提醇沉法对咽舒宁复方指标成分、抑菌活性的影响。方法采用陶瓷膜技术和水提醇沉法精制咽舒宁复方水提液,用HPLC考察其对咽舒宁抗病毒的指标成分表告依春及除杂率的影响,同时,以对金黄色葡萄球菌等急性咽喉炎致病菌的抑制作用为指标,对两种精制方式进行比较。结果陶瓷膜能更有效地保留抗病毒的有效成分;两种精制方法对咽舒宁复方水提液抑菌效果的影响无明显差异。结论陶瓷膜技术比水提醇沉法更适合咽舒宁复方水提液的精制。     

植物精油对痤疮致病菌的体外抑菌活性分析

目的 探讨8种植物精油对痤疮致病菌的体外抑菌效果。方法 采用抑菌圈试验定性检测8种植物精油对痤疮丙酸杆菌和金黄色葡萄球菌的抑菌活性,随后通过二倍稀释法定量检测8种植物精油对痤疮丙酸杆菌、金黄色葡萄球菌和表皮葡萄球菌的最小抑菌浓度(MIC)和最小杀菌浓度(MBC)。结果 8种植物精油对痤疮致病菌均有不同程度的抑制作用;其中,广藿香的抑菌效果最好,对痤疮丙酸杆菌、金黄色葡萄球菌和表皮葡萄球菌的MIC分别为0.31、0.16和0.31μL/mL,MBC分别为1.25、1.25和5.00μL/mL。结论 8种植物精油对痤疮丙酸杆菌、金黄色葡萄球菌和表皮葡萄球菌均具有抑菌活性,可作为痤疮致病菌的天然抑菌剂应用。     

河北产蜂胶提取物对痤疮丙酸杆菌的抑制作用

目的探讨河北产蜂胶不同溶剂提取物对痤疮丙酸杆菌的抑制作用。方法采用微量板法培养痤疮丙酸杆菌,观察不同溶剂蜂胶提取物溶液对痤疮丙酸杆菌的抑菌效果,并确定其最低抑菌浓度(MIC)。结果蜂胶95%乙醇提取物对痤疮丙酸杆菌的MIC为512μg.mL-1;蜂胶75%乙醇提取物对痤疮丙酸杆菌的MIC为8μg.mL-1;蜂胶水提取物对痤疮丙酸杆菌的MIC为54μg.mL-1。结论河北产蜂胶不同溶剂提取物对痤疮丙酸杆菌均有较好的体外抑菌效果,蜂胶75%乙醇提取物的抑菌效果>蜂胶水提取物>蜂胶95%乙醇提取物。     

中药体外抑制痤疮丙酸杆菌的活性测定

目的:研究中药在体外对痤疮丙酸杆菌的抑制作用,筛选用于治疗痤疮的中药.方法:采用琼脂平板稀释法,测定14味中药水提液及4个中药单体成分对痤疮丙酸杆菌的抑制作用. 结果:大黄、黄芩、金银花的MIC为12.50 mg·mL-1,黄柏的MIC为25 mg·mL-1,连翘、甘草、苦参的MIC为50 mg·mL-1,栀子的MIC为200 mg·mL-1,白芷、赤芍、当归、丹皮、蒲公英、杏仁6味中药在测试的最高浓度200 mg·mL-1时仍未产生抑菌作用.大黄酸、黄芩苷、小檗碱的MIC分别为25、12.5、3.13 μg·mL-1,绿原酸在测试的的最高浓度50 μg·mL-1时仍未产生抑菌作用. 结论:药材黄芩、大黄、金银花和单体成分小檗碱表现出良好的抑菌效果,在进一步的药物筛选中可进行重点考查.     

番薯藤提取物抗痤疮丙酸杆菌有效部位筛选研究

目的 研究番薯藤提取物对痤疮丙酸杆菌的体外抑菌作用,并对其有效部位进行筛选。方法 采用固体平板法、试管2倍比稀释法测定番薯藤水、醇提物对痤疮丙酸杆菌的抑菌圈大小和最低抑菌浓度（minimum inhibitory concentration,MIC）,采用系统溶剂法对番薯藤醇提物进行梯度提取,分别得到石油醚层、二氯甲烷层、乙酸乙酯层、正丁醇层和水层5个不同极性部位,并确定其有效部位及相应的MIC、最低杀菌浓度（minimum bactericidal concentration,MBC）。结果 番薯藤醇提物对痤疮丙酸杆菌有较强抑制作用,其MIC为50 mg·mL^-1。其中石油醚部位的抑菌作用最强,MIC为12.5 mg·mL^-1,MBC为25 mg·mL^-1;其次为正丁醇部位,MIC为25 mg·mL^-1,MBC为100 mg·mL^-1。结论 番薯藤醇提物对痤疮丙酸杆菌存在体外抑制作用,其有效成分主要集中于石油醚和正丁醇部位。     

几种中药制剂的体外抑菌作用研究

目的:探讨蒲公英颗粒、黄柏胶囊、鞣酸苦参碱胶囊和复方瓜子金颗粒对大肠杆菌、金黄色葡萄球菌和枯草芽孢杆菌的体外抑菌作用.方法:采用琼脂平板扩散法测定药物的抑菌圈直径大小,采用试管连续稀释法测定药物的最低抑菌浓度(MIC,g/ml).结果:四种中药制剂对金黄色葡萄球菌抑菌圈直径为23.7～38 mm,对枯草芽孢杆菌抑菌圈直径为14.6～29.6 mm;对大肠杆菌的抑菌圈直径为22.4～32.6 mm(黄柏胶囊除外).结论:上述四种中药制剂中黄柏胶囊对金黄色葡萄球菌的抑制作用最强,其抑菌圈直径为38 mm,MIC为9.76×10-4 g/ml,复方瓜子金颗粒对大肠杆菌的抑制作用最强,其抑菌圈直径为32.6 mm,MIC为7.81×10-3 g/ml,黄柏胶囊对大肠杆菌无抑制作用.     

枇芩颗粒剂体外抑制金黄色葡萄球菌和痤疮丙酸杆菌的作用

目的 研究枇芩颗粒剂对金黄色葡萄球菌和痤疮丙酸杆菌的体外抑制作用。方法 采用滤纸片或牛津杯的琼脂扩散法观察枇芩颗粒剂对金黄色葡萄球菌和痤疮丙酸杆菌的体外抑菌作用,同时定量测定枇芩颗粒剂对这2种菌的最低抑菌浓度。结果 枇芩颗粒剂对金黄色葡萄球菌和痤疮丙酸杆菌均有明显抑菌作用,对金黄色葡萄球菌最低抑菌浓度为0.05 g·mL^-1,对痤疮丙酸杆菌最低抑菌浓度为0.10 g·mL^-1。结论 枇芩颗粒剂对金黄色葡萄球菌和痤疮丙酸杆菌均具有明显的抑制作用。     

黄芩等6味中药对多重耐药鲍曼不动杆菌的体外抑菌活性的实验研究

目的:探究黄芩、黄连等6味中药材对多重耐药鲍曼不动杆菌(MDR-AB)的体外抑菌和杀菌活性.方法:选用黄芩、黄连、连翘、乌梅、穿心莲、金银花药材的提取物,采用药敏纸片琼脂扩散法及肉汤稀释法,测定提取物对MDR-AB的体外抑菌圈的最低抑菌浓度(MIC).结果:黄芩、黄连提取物有较强的抑菌活性,抑菌圈直径大,MIC值较低;...     

余甘子醇提物不同萃取部位对人消化道常见菌的抑制作用研究

目的:研究余甘子醇提物4种不同萃取部位对人消化道常见菌的抑制作用。方法:采用管碟法进行余甘子醇提物及醇提物中石油醚、乙酸乙酯、三氯甲烷、水部位对大肠杆菌的抑菌试验,测量其抑菌圈直径以确定最佳抑菌部位,二倍稀释法测定最低抑菌浓度(MIC)。采用宏量肉汤稀释法(试管法)进行余甘子醇提物最佳抑菌部位对消化道菌群的抑菌试验,测定其MIC。结果:余甘子醇提物对大肠杆菌的MIC为0.625 mg/ml。余甘子醇提物乙酸乙酯部位为最佳抑菌部位,其对金黄色葡萄球菌、表皮葡萄球菌、枯草芽孢杆菌、白色念珠菌、变形杆菌、沙门氏菌的MIC均为2.5 mg/ml,对肺炎链球菌的MIC为0.625 mg/ml,对大肠杆菌和产气荚膜杆菌的MIC均为1.25 mg/ml,对破伤风杆菌的MIC为0.156 mg/ml。结论:余甘子醇提物乙酸乙酯部位对消化道常见菌群有较强的抑制作用。     

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.     

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.