小红参不同溶剂提取物对心肌缺血实验性指标的影响

目的通过对心肌缺血实验性指标的测定，筛选出小红参不同溶剂提取物中抗心肌缺血的主要活性部位，并研究其抗垂体后叶素（Pit）致心肌缺血的活性。方法通过小鼠常压耐缺氧试验、二磷酸腺苷（ADP）诱导家兔体外血小板聚集影响试验、去甲肾上腺素（NE）诱导大鼠离体主动脉环收缩试验，比较小红参石油醚、乙酸乙酯、正丁醇、水4种溶剂提取物抗心肌缺血的活性强度，以确定其抗心肌缺血活性的主要部位，再进行小红参主要活性部位抗Pit致大鼠心肌缺血的活性研究。结果小红参乙酸乙酯提取物在各试验中均有明显活性，并在NE诱导大鼠离体主动脉环收缩试验中对动脉环的舒张效应明显较强；还能明显对抗Pit所致心肌缺血大鼠心电图第1期和第2期的T波抬高（P〈0．01），且能明显增强超氧化物歧化酶（SOD）活性、降低丙二醛（MDA）含量。结论小红参乙酸乙酯提取物为其抗心肌缺血的主要活性部位，能够对抗由Pit引起的大鼠急性心肌缺血。     

中药茜草的研究进展

<正> 茜草为我国传统常用中药之一,具有行血、止血、通经活络、止咳祛痰等功效,其商品主要为茜草科茜草属植物茜草(Rubia cordifolia L.)的根。茜草属植物达60余种,分布于欧洲、亚洲、南非和美洲,我国有12种之多(见表1),分布于25个省市自治区。其中长叶茜草、黑果茜草、中华茜草、狭叶茜草、大叶茜草、大茜草、新疆茜草、小红参亦作茜草药用。自19世纪末始,国内外学者就开始对茜草的化学成分、药理作用进行了大量的研     

应用Ames试验对含与不含欧茜草消石素的致突变性

消石素（胶囊）临床上主要用于治疗泌尿系统的结石，其药用成分欧茜草所含的化学成分——Ｌｕｃｉｄｉｎ，据国外文献报道具有强致突变性及潜在的致癌性，经我们用Ａｍｅｓ试验方法研究也证实它是强致突变物。因此消石素能否继续在临床上安全使用，以及消石素中除欧茜草以...     

茜草与欧茜草的化学成分研究 Ⅱ.反相高效液相色谱法测定茜草素和芦西定的含量

采用ＲＰ—ＨＰＬＣ法，对茜草（Ｒｕｂｉａｃｏｒｄｉｆｏｌｉａ）和欧茜草（Ｒ．ｔｉｎｃｔｏｒｕｍ）中所含蒽醌类成分茜草素（ａｌｉｚａｒｉｎ）和芦西定（ｌｕｃｉｄｉｎ）进行含量测定．２种成分的平均回收率分别为９８．１％和１０１．４％，ＲＳＤ分别为４．０％和５．７％．     

茜草双酯的免疫抑制作用

茜草双酯的免疫抑制作用杨胜利，刘发（空军乌鲁木齐医院，新疆医学院药理教研室，乌鲁木齐８３００１１）中国图书分类号Ｒ９７５．５茜草双酯（Ｒｕｂｉｄａｔｅ，Ｒｕｂ）是人工合成的萘酚化合物，系茜草提取物升白主要成元成分，本文探讨其免疫药理作用。１材料ＮＩＨ...     

云南茜草根的化学成分研究

从云南茜草[Rubia yunnanensis(Franch.)Diels]根部的乙醚提取物中分离得到六个化合物，经光谱（UV，IR，MS，^1HNMR and ^13CNMR）分析和文献对照，证明其中五个为已知化合物：茜草乔木醇A，茜草乔木醇G，茜草乔木酮A，1，3，6－三羟基－2－甲基蒽醌和β－谷甾醇，一个新化合物7β，19α，28－三羟基乔木－9（11）－烯－3－酮（Ⅲ)，命名为茜草乔木酮B。     

茜素型蒽醌化合物体外Pig-a基因突变性试验研究

目的 对具有相同母核结构的7种茜素型蒽醌化合物开展体外Pig-a基因突变试验，分析不同茜素型蒽醌化合物取代基结构与其致突变性的关联。方法 小鼠淋巴瘤细胞L5178Y（tk^+/--3.7.2.C）分别与系列浓度的茜草素、异茜草素、甲基异茜草素、羟基茜草素、甲基异茜草素-1-甲醚、茜草素-1-甲醚和光泽汀作用4 h（有S9）或24 h（无S9），给药24 h后应用细胞计数仪进行计数，计算细胞相对倍增速率（RPD）评价受试物细胞毒性；细胞培养8 d后经APC-anti-CD45和PE-antiCD90.2抗体孵育后，使用流式细胞仪检测细胞突变（CD45⁺CD90.2^-）率。结果 所有受试物在有或无代谢活化条件下所设浓度组RPD均大于50%，未见明显细胞毒性作用，可排除试验中假阳性结果。在无S9代谢活化条件下，光泽汀（16 μg· mL^-1）组、羟基茜草素（10 μg· mL^-1）组、甲基异茜草素-1-甲醚（31.25 μg·mL^-1）组Pig-a基因突变率与溶媒对照组比较显著升高（P<0.05、0.01、0.001）；在有S9代谢活化条件下，光泽汀（4、8 μg· mL^-1）、羟基茜草素（10 μg· mL^-1）、茜草素-1-甲醚（3.75、15.00 μg· mL^-1）、甲基异茜草素（12.5、25.0、50.0、100.0 μ g · mL^-1）、甲基异茜草素-1-甲醚（15、30、60 μ g · mL^-1）、异茜草素（2.50、5.00 μg·mL^-1）组Pig-a基因突变率与溶媒对照组比较显著升高（P<0.05、0.01、0.001）。结论 羟基取代基所在位点是茜素型蒽醌化合物致突变性强弱的决定性因素，其体内致突变性有待进一步确证。     

银屑病患者用小红参治疗外周血T淋巴细胞亚群的变化

目的 探讨银屑病外周血Ｔ淋巴细胞亚群的变化及小红参治疗银悄病的免疫学机理。方法 单克隆抗体间接免疫芝光法测定３２例进行期银屑病患者在小红参治疗前后外周血Ｔ淋巴细胞亚群的变化。结果 ①进行期银屑病外周血中ＣＤ８＾＋Ｔ细胞升高ＣＤ４＾＋／ＣＤ８＾＋比值降低。②ＣＤ＾＋Ｔ细胞经小红参治疗后降至正常（Ｐ〈０．０１）,ＣＤ４＾＋／ＣＤ８＾＋比值也恢复正常。③小红参治疗前后ＣＤ３＾＋,ＣＤ４＾＋及ＣＤ２＾＋Ｔ     

茜草与欧茜草的化学成分研究II.反相高效液相色谱法测定茜草…

采用ＲＰ－ＨＰＬＣ法，对某草（Ｒｕｂｉａｃｏｒｄｉｆｏｌｉａ）和欧茜草（Ｒ．ｔｉｎｃｔｏｒｕｍ）中所含蒽醌类成分茜草素（ａｌｉｚａｒｉｎ）和芦西定（ｌｕｃｉｄｉｎ）进行含量测定，２种成分的平均回收率分别为９８．１％和１０１．４％，ＲＳＤ分别为４．０％和５．７％。     

以标准汤剂为基准的小红参配方颗粒量值传递研究

目的 以标准汤剂中出膏率、小红参萘酚苷A含量和特征图谱为基准,研究配方颗粒的量值传递规律。方法 制备小红参标准汤剂样品,建立小红参萘酚苷A含量及特征图谱测定方法,以其为基准进行药材-饮片-标准汤剂-配方颗粒量值传递研究。结果 15批标准汤剂结果表明,出膏率范围为15.3%～28.4%;小红参萘酚苷A的含量范围为15.83～29.39 mg·g^-1,转移率范围为21.79%～40.47%;共标定6个特征峰,指认峰1小红参萘酚苷A、峰4小红参醌苷乙2个特征峰。收集不同来源15批次小红参药材、饮片及3批中试配方颗粒,并测定小红参萘酚苷A含量及特征图谱,小红参药材中小红参萘酚苷A含量范围为14.32～19.79 mg·g^-1;小红参饮片中小红参萘酚苷A含量范围为12.71～18.81 mg·g^-1;小红参配方颗粒中小红参萘酚苷A含量范围为18.71～19.80 mg·g^-1;其饮片-药材转移率范围为64.41%～119.62%;标准汤剂-饮片转移率范围为21.79%～40.47%;饮片-配方颗粒转移率为26...     

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.

---

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.     

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.