姜黄油提取物乳注射液体内抗癌活性的研究

中药姜黄为姜科植物姜黄（Curcuma longaL．）的干燥根茎。其挥发油及姜黄素为活性成分。药理实验表明姜黄挥发油对肿瘤有明显的抑制作用和增强免疫功能。多年来在姜黄油提取物抑癌作用的研究中我们发现，姜黄油中的倍半烯萜类化合物（C15H24）姜烯、姜黄烯、芳姜黄烯有一定的抑癌活性，但姜黄油中的另一类组分倍半萜酮类化合物：     

基于多指标评价优选炮姜砂烫工艺

目的：运用层次分析法（AHP）建立一种中药多指标的综合评价方法,优选炮姜最佳炮制工艺,明确其工艺参数,为炮姜的规范化生产和质量控制提供实验依据。方法：以7个姜辣素（姜酮、6-姜酚、8-姜酚、10-姜酚、6-姜烯酚、8-姜烯酚及10-姜烯酚）含量,外观性状评分和挥发油中共有成分的综合评分为指标,采用AHP和主成分权重赋值法确定各评价指标的权重系数,考察不同炮制时间对炮姜砂烫工艺的影响,并对优选工艺进行验证。结果：炮姜最佳炮制工艺是炮制温度195℃,炮制时间为7.5分钟。结论：结合炮姜内在质量和外观性状,优化的炮制工艺简单、稳定、可行,所得参数为炮姜的研究生产提供科学依据,并对优选工艺进行验证,所得结果更加合理可信,可用于该饮片的质量控制。     

生姜及其炮制品中姜辣素的研究进展

生姜不仅是日常调味品,也是一种常用良药,是人们平时生活中应用较多的药食两用品,生姜内服具有抗炎抗菌作用,外用可缓解风湿性疾病。姜辣素是其主要有效成分。姜辣素种类繁多,药效作用明显。常见含量较高的有6-姜酚、8-姜酚、10-姜酚、6-姜烯酚和姜酮5种,其在生姜及炮制品中的含量差异较大,如姜酮在生姜炮制品中含量较高,而在生姜中极低;而6-姜酚在生姜中的含量最高,经过炮制后含量逐渐降低。因此,生姜及其炮制品中姜辣素的研究一直是人们关注的重点,相关文献报道也较多。本文就生姜中5种姜辣素的理化性质、药理作用和检测方法进行综述,以期为生姜及其炮制品的开发利用及质量控制提供参考。     

姜酚胶丸与干姜的挥发油成分GC-MS对比分析

目的对姜酚胶丸与其原料药材干姜的挥发油成分进行分析和比较。方法利用顶空固相微萃取法分别对姜酚胶丸与干姜挥发油进行提取,并以气相色谱-质谱联用仪对其进行分离鉴定,采用峰面积归一化法确定各组分的相对含量。结果从姜酚胶丸和其原料药材干姜挥发油中分别分离鉴定了60种和66种挥发性成分,分别占其挥发油总量的93.4%和94.2%,其化学成分组成相似,均含有α-姜烯、β-水芹烯、β-倍半水芹烯、芳姜黄烯、莰烯、β-没药烯、α-蒎烯、α-金合欢烯、β-月桂烯、香树烯、α-水芹烯、1-龙脑、芳樟醇等主要成分,但组分比例略有差异。其挥发油的指标性成分α-姜烯在姜酚胶丸与药材干姜中的相对含量相当。结论姜酚胶丸与干姜中挥发油成分组成及相对含量基本一致。     

GC-MS结合保留指数分析紫花香薷不同部位挥发油的化学成分

摘要：目的:研究紫花香薷不同部位挥发油化学成分的差异。方法:采用水蒸气蒸馏法提取紫花香薷叶、茎中的挥发油,利用GC-MS计算机联用仪定性分析,按峰面积归一化法求出挥发油中化学成分的百分含量,并结合Kovats保留指数对其主要成分进行定性分析。结果:紫花香薷叶茎共分析出40种挥发性化合物,以单萜和倍半萜为主。其中26种化合物是两个部位均有成分,相对含量较高的有D-柠檬烯（叶9.368%、茎4.351%）、（Z）-β-柠檬醛（叶18.10%、茎8.097%）、柠檬醛（叶14.59%、茎10.84%）、（Z）-罗勒烯异构体混合物（叶16.83%、茎5.355%）、（E）-香叶醇（叶5.152%、茎3.397%）、石竹烯（叶3.154%、茎7.40%）及（Z）-β-法尼烯（叶13.59%、茎32.32%）等7种化合物,相对含量分别占总挥发油80.784%和71.76%。紫花香薷叶鉴定出36个化合物,占总离子峰的98.862%,单萜类占72.22%,倍半萜类占19.416%,紫花香薷茎鉴定出28个化合物,占总离子峰的96.277%,单萜类占42.578%,倍半萜类占46.735%。两个部位所含有成分的种类与含量显著差异。结论:唇形科香薷属植物紫花香薷具有潜在药用开发价值。     

蛹虫草子实体中多肽的提取分离及组成初探

目的获取蛹虫草子实体中的肽并对其分离纯化。方法采用水提醇沉法提取,葡聚糖凝胶色谱法分离纯化,继而用氨基酸自动分析仪分析组成。结果由单因素考察和正交试验法确定了最佳提取条件,经分离纯化后得到两个小分子量的肽组分,分别测定出了两组分的氨基酸组成及含量。结论分离出的肽类组分氨基酸种类丰富齐全,具有一定的营养和药用价值。     

伸筋草挥发油成分的固相微萃取分析

目的：分析伸筋草中挥发油化学成分。方法：采用固相微萃取气相色谱-质谱联用法分析挥发油化学成分。结果：共分离出98个组分，鉴定了81个组分，用归一化法测定其百分含量，占总挥发油组分峰面积的97．80％。结论：主要成分是癸酸（10．63％）、β-马榄烯（6．60G）、反-石竹烯（7．29％）、白菖蒲油烯（23．77％）、旷古芸烯（3．38％）、α-姜黄烯（1．38％）、α-蛇床烯（1．67％）、δ-杜松烯（2．16％）、α-雪松醇（15．50％）等组分。     

两个不同产区藏药刺柏叶中挥发油成分的GC-MS分析

摘 要 目的： 对甘肃榆中和碌曲的藏药刺柏叶中挥发油化学成分进行比较分析。 方法: 采用水蒸气蒸馏法提取挥发油,利用GC MS联用技术对其进行分离分析。结果:甘肃榆中和碌曲的得油率分别为0.21%和1.45%,两个地区刺柏叶中前者挥发油共分离出40个峰,鉴定出38个化合物,占分离物质的95%,后者挥发油共分离出51个峰,鉴定出47个化合物,占分离物质的92%。甘肃榆中刺柏叶中挥发油的主要成分为α-蒎烯（44.92%）,1-石竹烯（9.23%）、(-)-异喇叭烯（6.50%）、α-石竹烯（5.60%）、月桂烯（4.54%）、d-杜松烯（3.37%）;碌曲刺柏叶中挥发油的主要成分为二-非手性-α-柏木烯（31.87%）、环己烯（15.28%）、γ-榄香烯（10.05%）、澳白檀醇（5.80%）、α-蒎烯（5.79%）。结论: 两者刺柏叶挥发油成分有所不同,其得率及主要成分都有较大差异。该方法对建立刺柏质量标准控制有参考价值。     

大孔吸附树脂柱层析结合高速逆流色谱分离纯化环孢菌素小组分

应用大孔吸附树脂柱层析与高速逆流色谱相结合的方法．对环孢菌素A结晶母液中的两个小组分进行分离纯化。首先采用大孔树脂以丙酮-水（起始浓度50％，V／V）为洗脱液对母液进行梯度洗脱，达到去除色素杂质和富集环孢菌素小组分的目的，然后分别选择正己烷：乙酸乙酯：甲醇：水（5：6：6：5）和石油醚：甲醇：丙酮：水（3：1：3：2）为两相体系，以上相为固定相，下相为流动相对富集部分进行分离纯化。用高效液相色谱仪进行单组分纯度测定。结果表明采用大孔吸附树脂柱层析与高速逆流色谱相结合的方法可分离纯化这两个小组分，得到纯度97％以上的单组分，收率可达80％以上，初步质谱和HPLC分析判断其中一个组分可能为环孢菌素E，另一个可能为环孢菌素的未知组分。     

GC-MS和化学计量学解析法分析白术中挥发油成分

目的分析白术挥发油中的化学成分。方法采用气相色谱-质谱（GC-MS）联用技术对其进行分离检测,利用化学计量学解析法（CRM）对重叠色谱峰进行分辨解析,并结合程序升温保留指数辅助定性,从而对挥发油成分进行准确的定性定量分析。结果共分辨出了33个色谱峰,鉴定了其中29个组分,占白术挥发油总量的95.93%,其中主要化学成分为2-（2-甲氧基）苯甲氧基苯酚、γ-芹子烯和3,7（11）-蛇床二烯等,它们占总挥发油的70.07%,而其他26个组分只占25.86%。结论结合使用CRM解析重叠色谱峰,比单独使用GC-MS能更真实、全面地反映白术中的挥发油化学成分。     

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.     

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.