超声法提取黄连中紫外吸收剂的试验研究

目的：研究超声提取法提取黄连中天然紫外吸收剂的优化工艺。方法：用分光光度法测定所提取紫外吸收剂的含量，考察了超声时间、乙醇浓度、料液比、超声温度以及萃取次数对黄连萃取液吸光度的影响。结果：较佳工艺为50％乙醇水溶液为萃取剂，料液比1：25（g/ml），在50℃超声提取50min，萃取一次。结论：超声提取法用于黄连中紫外吸收剂的提取是一种简单、快捷、高效的提取方法。     

正交设计优化超临界CO2萃取姜油工艺

目的：优化超临界CO2萃取生姜工艺参数。方法：建立生姜指标成分6-姜酚的分析方法,以萃取压力、萃取温度、分离釜Ⅰ压力、萃取时间为考察因素,采用L9（3^4）正交试验表,以姜油收率和6-姜酚百分含量为评价指标进行姜油萃取工艺优选。结果：超临界CO2萃取姜油的最佳萃取条件为：萃取压力20MPa;萃取温度40％;萃取时间3h;分离釜Ⅰ压力6MPa;分离釜Ⅱ压力3MPa。此时姜油的收率为2．117％,姜油中6-姜酚的百分含量为23．164％（n=3）。结论：优化后的超临界CO2萃取生姜工艺具有保持药物原有生物活性、提取效率高、提取物纯净无溶剂残留等优点。     

超临界萃取当归挥发油及阿魏酸正交试验研究

目的：优选超临界二氧化碳流体（SFE-CO2）萃取当归挥发油和阿魏酸的工艺条件。方法：以阿魏酸的提取量和挥发油的得率为考察指标，以高效液相色谱法测定阿魏酸含量，采用正交试验对提取条件优选。结果：优选萃取条件是：当归粉碎为20—60目，75％的乙醇作为夹带剂，萃取压力30Mpa，萃取温度60℃。结论：优选工艺萃取的挥发油和阿魏酸提取量较高，所得浸膏量较低。     

中药复方三棱颗粒的研制及成型工艺优化

目的：制备中药复方制剂"复方三棱颗粒",并优选其提取及制备工艺。方法：采用超临界二氧化碳萃取法（supercritical CO₂ fluid extraction,SFE-CO₂）萃取三棱、川芎挥发油,通过正交试验法优选萃取工艺条件;将萃取完挥发油的药渣与其余六味药材（制大黄、黄芪、杜仲、金樱子、连翘、蒲公英）共同采用冷凝回流法提取,采用正交试验法优选提取工艺条件;提取液进一步浓缩并制备成颗粒剂。结果：SFE-CO₂萃取挥发油的最佳工艺：萃取压力为25 MPa,萃取温度为50℃,萃取时间为2 h;回流提取最佳工艺：乙醇浓度为50%（V/V）,料液比为1∶12,提取时间为1 h,提取3次;成功制备了复方三棱颗粒剂,收得率为90.80%。结论：所采用提取工艺简单合理,提取效率高,颗粒剂制备工艺可行,为复方三棱颗粒剂制备工艺的确定及生产条件的控制提供了科学的实验依据。     

藏药白沙蒿挥发油超临界CO2萃取工艺优化及其抗氧化活性研究

目的 采用Box-Behnken响应面法优化白沙蒿挥发油超临界CO₂萃取的最佳萃取工艺,并考察萃取物的抗氧化活性。方法 以白沙蒿挥发油的萃取得率为响应值,通过单因素试验筛选出萃取时间、萃取温度和萃取压力3个主要因素,进行Box-Behnken中心组合试验设计,建立挥发油提取得率的二次回归方程,得到优化组合条件。通过测定挥发油对1,1-二苯基-2-三硝基苯肼（1,1-diphenyl-2-picrylhydrazyl,DPPH）和2,2'-联氮-双-3-乙基苯并噻唑啉-6-磺酸[2,2'-azino-bis（3-ethylbenzothiazoline-6-sulfonic acid）,ABTS]自由基的清除能力评价其抗氧化活性。结果 白沙蒿挥发油的最佳萃取工艺为萃取时间55 min,萃取温度59℃,萃取压力32 MPa,在此条件下挥发油萃取得率为（1.99±0.087）%,约为传统的水蒸气蒸馏法（萃取得率为1.05%）的1.9倍。超临界CO₂萃取的白沙蒿挥发油DPPH和ABTS自由基的IC₅₀值分别为0.264和0.045 mg·mL^-1。结论 优化后的白沙蒿挥发油萃取工艺稳定可靠,萃取的挥发油具有良好自由基清除作用,有望成为一种新的天然抗氧化剂。     

超临界CO2萃取樱桃叶中总黄酮的研究

目的：考察提取樱桃叶中总黄酮的最佳工艺条件。方法：以无水乙醇做夹带剂,采用超临界CO2萃取法．通过设计Lg（3^3）正交实验,考察萃取压力、萃取温度和萃取时间对提取率的影响。结果;优化后的提取条件为萃取温度为45℃,萃取压力为20MPa,萃取时间3h。结论：采用超临界CO2萃取樱桃叶中总黄酮的方法可行,产品质量好,收率高。     

超临界CO2萃取猪肺表面活性物质的工艺研究

目的：用超临界CO2流体萃取技术提纯猪肺表面活性物质，并对萃取工艺条件进行优化。方法：通过单因素对比实验以及正交试验设计对其萃取过程中的主要影响因素进行了考察，以优化萃取工艺。结果：确定最佳萃取条件为：压力30MPa，温度50℃，动态萃取时间5h，0．3mL无水乙醇为夹带剂。结论：该提纯方法简便、高效、有机溶剂污染少。     

桔梗叶醇提工艺优化及其不同部位镇咳祛痰活性研究

目的 优化桔梗叶醇提工艺并研究其醇提物不同萃取部位的镇咳祛痰活性。方法 在单因素试验基础上，以乙醇体积分数、液料比、提取时间、提取温度为考察因素，综合评分（浸膏得率、总黄酮提取量、总皂苷提取量得分）为评价指标，采用Box-Behnken响应面法优化桔梗叶醇提工艺，并验证。实验设空白组[A组，等体积0.5%羧甲基纤维素钠（CMC-Na），模型组（B组，等体积0.5%CMC-Na），强力枇杷露组（C组，5.65 mL/kg），石油醚萃取部位组（D组，360 mg/kg），二氯甲烷萃取部位组（E组，6.67 mg/kg），乙酸乙酯萃取部位组（F组，228 mg/kg），正丁醇萃取部位组（G组，106 mg/kg），水萃取部位组（H组，449.54 mg/kg）。各组小鼠予相应药物或0.5%CMC-Na灌胃，每天1次，连续7 d。以氨水引咳法复制咳嗽小鼠模型，记录小鼠引咳后3 min内的咳嗽次数和咳嗽潜伏期；采用酚红法测定酚红排泌量；苏木素-伊红（HE）染色，观察小鼠肺组织病理形态。结果 桔梗叶最佳醇提工艺为，乙醇体积分数44%，液料比23∶1(mL/g),56℃提取2次，每次43 min；此...     

丙戊酸磁性分子印迹聚合物的制备及性能评价

目的：建立丙戊酸（valproic acid，VPA）磁性分子印迹聚合物（VPA MMIPs）的固相分散萃取方法，并与气相色谱-质谱法（GC-MS）联用，评价VPA MMIPs的吸附性能。方法：（1）以VPA为模板分子，甲基丙烯酸（MAA）为功能单体，乙二醇二甲基丙烯酸酯（EGDMA）为交联剂，乙腈为致孔剂，制备VPA MMIPs。通过傅里叶变换红外光谱（FTIR）、扫描电子显微镜（SEM）、透射电子显微镜（TEM）对材料进行表征。（2）通过对VPA MMIPs投加量、吸附时间及吸附测试液浓度的优化，确定最佳吸附条件并评价VPA MMIPs的特异性吸附能力。结果：（1） VPA MMIPs的制备条件为：模板分子/功能单体/交联剂的物质的量之比为1：8：40，致孔剂乙腈50 mL，引发剂偶氮二异丁腈（AIBN）50 mg，磁性材料0.40 g。SEM和TEM分析表明，制备的VPA MMIPs粒径分布为50~300 nm。FTIR显示VPA MMIPs材料合成成功。（2）吸附条件为：VPA MMIPs最佳投加量为20 mg，室温下吸附60 min。吸附特异性考察中，VPA MMIPs和丙戊酸磁性非分子印迹聚合物（VPA MNIPs）对VPA的最大平衡吸附量分别为3 423.68 μg·g^-1和1 403.81 μg·g^-1。结论：制备的VPA MMIPs对VPA具有较强的特异性吸附能力，该研究可为临床上VPA的检测提供新的思路。     

ω-3鱼油脂肪乳剂对实验性急性胰腺炎IL-1β、TNF-α和红细胞膜稳定性的影响

目的：观察急性胰腺炎大鼠模型经ω-3鱼油脂肪乳剂静脉治疗后，红细胞膜稳定性的变化与炎症细胞因子白细胞介素-1β（IL-1β）和肿瘤坏死因子-α（TNF-α）表达水平的关系，探讨ω-3鱼油脂肪乳剂对急性胰腺炎早期炎症发展过程的影响。方法：雄性SD大鼠随机分为假手术组（n=18）以及胰腺炎不同治疗组（n=54）。通过胰管逆行注射法建成急性胰腺炎模型，并分别静脉注射ω-3鱼油脂肪乳剂、大豆油和生理盐水治疗。检测2、6、24h大鼠血清淀粉酶及IL-1β和TNF-α的水平，并观察红细胞膜稳定性的变化。胰腺组织进行病理学评分。结果：与大豆油和生理盐水比较，ω-3鱼油脂肪乳剂能显著下调IL-1β和TNF-α的表达（P〈0．05），增加红细胞膜稳定性（P〈0．001），而且稳定性的增加与两种因子的表达下调之间表现出一定的相关趋势（r分别为0．555和0．756）。结论：ω-3鱼油脂肪乳剂能下调大鼠急性胰腺炎模型IL-1β和TNF-α的表达水平，从而减轻全身过度炎症反应；在急性胰腺炎病程早期静脉使用ω-3鱼油脂肪乳剂能增强红细胞膜的稳定性，且药效优于大豆油。     

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.     

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.