苍术挥发油成分分析及光敏感性初步观察

目的 分析苍术挥发油的化学成分并初步观察其光敏感性。方法 用气—质联用仪(GC／MS)分离、分析鉴定苍术挥发油的成分，在室温下考察不同颜色容器(棕色和白色量瓶)中挥发油的变化从而考察挥发油的光敏感性。结果 分析鉴定了苍术挥发油中17种成分，其中以β-桉叶醇、茅术醇等为主要成分。室温下，两种颜色容器中苍术挥发油均逐渐发生变化，有的成分发生逐渐减少立至消失，β-桉叶醇、β-芹子烯、荜澄茄—1，4—二烯等成分含量至上升趋势，茅术醇等含量则变化不大。棕瓶中挥发油变化速度明显慢于白瓶。结论 苍术挥发油对光线敏感，对其中有些成分影响较大。避光保存可减缓苍术挥发油的变化，为保征苍术挥发油的稳定性，宜避光保存。     

苍术炮制前后指纹图谱及主要成分含量变化研究

摘要：目的:建立苍术及其炮制品的HPLC指纹图谱,并对其所含的6个有效成分进行定量分析。方法:采用HPLC,Waters XTERRA C18色谱柱（250 mm×4.6 mm,5μm）,流动相乙腈-0.8%磷酸溶液梯度洗脱,检测波长为220 nm（检测苍术酮、β-桉叶醇、苍术苷A和白术内酯Ⅲ）、270 nm（检测苍术素和苍术素醇）,流速为0.8 ml·min-1,建立生苍术和麸炒苍术的HPLC指纹图谱,通过相似度评价、聚类分析对苍术炮制前后指纹图谱进行分析,并对苍术素、苍术素醇、苍术酮、β-桉叶醇、白术内酯Ⅲ、苍术苷A进行含量测定。结果:建立了苍术及其炮制品的指纹图谱,以苍术素为参照峰,生苍术标定了21个共有峰,麸炒苍术标定了20个共有峰,与各自对照指纹图谱的相似度均大于0.955。苍术素、苍术素醇、苍术酮、β-桉叶醇、白术内酯Ⅲ、苍术苷A在炮制前的质量分数分别为3.157 3,0.663 6,1.026 2,1.001 4,0.242 7,0.238 5 mg·g-1;经炮制后,上述6种成分中的苍术酮消失,苍术素、苍术素醇、β-桉叶醇、白术内酯Ⅲ、苍术苷A在麸炒苍术中的含量分别为2.701 9,0.539 2,0.800 8,0.313 5,0.321 4 mg·g-1。结论:苍术的HPLC指纹图谱在炮制前后发生了明显变化,通过对比共有峰的保留时间和色谱图,指认出部分成分;并发现20号峰为苍术的特有峰,因此峰20可用于区别生苍术和麸炒苍术; 6个有效成分含量在炮制前后均发生了一定程度的变化,样品中苍术素、苍术素醇、苍术酮、β-桉叶醇含量排序为苍术>麸炒苍术,样品中白术内酯Ⅲ和苍术苷A含量排序则为麸炒苍术>苍术。     

野生茅苍术挥发油成分分析

目的:分析野生茅苍术挥发油的化学成分,测定各成分的含量。方法:水蒸气蒸馏法提取野生茅苍术挥发油,用气相色谱-质谱(GC-MS)联用技术分离各成分并鉴定其结构。结果:从野生茅苍术挥发油中分离出44个成分,鉴定出其中33个,主要成分为β-桉叶油醇、苍术酮、茅术醇和苍术素;用峰面积归一化法计算其含量,分别为18.894%、13.707%、11.053%和6.815%。结论:本研究有助于正确评价栽培茅苍术的品质。     

基于GC-MS和UPLC技术的河北产北苍术野生品与栽培品的比较研究

目的：研究河北产野生北苍术和栽培北苍术药材化学成分的异同。方法：水蒸气蒸馏法提取北苍术野生及栽培品药材的挥发油,GC-MS技术对挥发油成分进行分析,UPLC技术对样品中苍术素含量进行测定,并利用SPSS26.0软件对所测定的6份野生及栽培北苍术样品进行聚类分析。结果：北苍术野生品和栽培品的挥发油总含量均在2%左右;3个不同产地栽培品样品挥发油共鉴定出39种成分,其中共有成分34种,相对含量总和在总挥发油中占比90%以上,含量最高的挥发性成分为β-桉叶醇、苍术素和苍术酮。3个野生样品挥发油共鉴定出39种成分,其中共有成分20种,挥发油主成分β-桉叶醇和苍术素在各样品中含量差异较大。栽培品中苍术酮含量明显高于野生样品,栽培品中均含有一定量的香樟烯,该成分在野生品中未检测到。UPLC检测6份样品中指标性成分苍术素含量均能达到药典“不得少于0.30%”的标准。结论：河北产栽培北苍术指标性成分苍术素含量均能达到药典标准,栽培品总挥发油含量与野生品差别不明显,且挥发油的化学组成较稳定,野生样品之间挥发油含量和组成差异较大,可利用苍术酮和香樟烯来区分北苍术野生品和栽培品。     

朝鲜苍术挥发油成分GC—MS分析

目的研究朝鲜苍术挥发油成分,为朝鲜苍术的药用价值及合理开发利用提供参考。方法采用水蒸气蒸馏法提取挥发油,GC毛细管柱色谱法进行分析,峰面积归-化法确定其相对含量,气相色谱-质谱联用技术辅助人工检索鉴定其化学成分。结果从朝鲜苍术的挥发油中分离出58种,鉴定出55种化学成分,鉴定出的挥发性化学成分占挥发油总量的79．94％,主要成分有苍术酮（31．1831％）、3-羟基-6β-环丙烷-5β-胆甾烷（12．3086％）、5α-螺甾烷（11．2161％）、巴伦西亚橘烯（7．05606％）、γ-榄香烯（4．24732％）、菜油甾醇（2．11089％）、石竹烯（1．44473％）、β-桉叶烯（1．43541％）、9,10-脱水-异长叶烯（1．21445％）、α-石竹烯（0．72132％）。结论朝鲜苍术挥发油的主要化学成分为倍半萜类化合物。     

蜜糠炒苍术炮制工艺优选及其抗胃溃疡作用研究

目的 优选蜜糠炒苍术的炮制工艺,并对其炮制前后的抗胃溃疡作用进行比较。方法 采用L₉(3⁴)正交实验设计,结合熵权逼近理想解排序(TOPSIS)模型,以苍术酮、β-桉叶醇、白术内酯Ⅲ、苍术素含量的综合评分为评价指标,以辅料与药材比例、炒制温度、炒制时间为考察因素,优选蜜糠炒苍术的炮制工艺并验证。以无水乙醇灌胃建立胃溃疡小鼠模型,以复方氢氧化铝片为阳性对照,以血清炎症因子[白细胞介素2(IL-2)、IL-6、肿瘤坏死因子α(TNF-α)]含量、溃疡指数和胃溃疡抑制率为评价指标,比较生苍术和蜜糠炒苍术的抗胃溃疡作用。结果 蜜糠炒苍术的最优炮制工艺为辅料与药材比例3∶10(g/g)、炮制温度140℃、炒制时间4 min。3次验证实验结果显示,最优工艺炮制所得蜜糠炒苍术中苍术酮等4种成分的含量较为稳定(RSD为3.47%～5.80%,n=3),综合评分为95.53%～95.89%(RSD=0.21%,n=3)。生苍术和蜜糠炒苍术均可不同程度地升高胃溃疡模型小鼠血清IL-2含量,降低其血清IL-6、TNF-α含量,蜜糠炒苍术可显著降低其溃疡指数(P&l...     

气相色谱—质谱法测定苍术挥发油包合前后的成分与含量

本文采用气相色谱——质谱法测定了苍术挥发油β-环糊精包合物(包合前后)的成分与含量,共分离出28种组分并鉴定出20种已知化合物,其中含量较多的主要成分有苍术素(12.5%),苍术酮(9.3%)和β-按叶醇(14.1%)。挥发油β-环糊精包合前后成分相同,相对含量有一定变化     

基于功效关联的苍术质量标准研究

摘 要 目的：针对现有苍术质量标准缺乏与功效关联的质量控制指标问题，探究“燥湿”功效的活性部位，基于功效关联的指标性成分建立质量标准。方法：采用大鼠水钠潴留模型，将雄性SD大鼠分为模型组、阳性药组、苍术总提物组、挥发油组和剩余部位组，造模后收集1 ~ 5 h的尿液并检测电解质离子浓度，考察苍术的利尿活性部位，进而以活性部位中的主要成分β-桉叶醇、苍术素和苍术酮为指标建立HPLC含量测定方法。结果：苍术的挥发油部位显著增加水钠潴留大鼠的尿量和尿液中Na+和Cl－的排出量，为苍术发挥利尿作用的有效部位。HPLC含量测定方法结果显示该方法线性关系良好，精密度、重复性、稳定性的RSD均小于3.0%，加样回收率为99.4% ~ 101.9%。β-桉叶醇为茅苍术与北苍术的主要差异性成分，通过聚类分析可区分茅苍术和北苍术。结论：根据“燥湿”功效特点，结合利尿活性评价，确定苍术挥发油中的β-桉叶醇、苍术素和苍术酮为功效关联的质量控制指标，建立的含量测定方法可反映其有效性，且能反映茅苍术和北苍术的差异，对苍术的质量控制具有一定借鉴意义。     

苍术抗炎、抗肿瘤和免疫调节作用的研究进展

苍术为菊科植物茅苍术Atractylodes lancea或北苍术A.chinensis的干燥根茎,具有燥湿健脾、祛风散寒的功效。药理研究显示苍术及其提取物具有抗炎、抗肿瘤和免疫调节等作用。其对细胞免疫、体液免疫和非特异性免疫都有增强作用;对肺癌细胞、消化系统肿瘤细胞、白血病细胞、黑色素瘤细胞、宫颈癌细胞和肉瘤生长均有抑制作用;苍术烯内酯、苍术酮、茅术醇、β-桉叶醇、苍术多糖可能是苍术的重要活性成分。     

气-质联用法分析苍术、麸炒苍术及其辅料麦麸的挥发性成分

目的:分析生苍术及麸炒苍术挥发油的化学成分的变化,并对辅料麦麸在炮制前后挥发性成分进行分析。方法:采用水蒸气蒸馏法和超声提取法提取挥发油,用气相色谱-质谱联用法(GC-MS)对其进行定性和定量分析。结果:与苍术相比,麸炒苍术挥发油有7个成分显著降低;与单炒麦麸相比,炒苍术麦麸新增了4个成分。结论:苍术炮制前后挥发油的成分发生了明显量变;麸炒苍术的挥发油降低是由于加热和麦麸的吸附所致,实验结果为阐述苍术炮制机理提供了实验依据。     

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.