云南獐牙菜化学成分的分离与鉴定

目的 研究云南獐牙菜（Swertia yunnanensis Burk.）全草的化学成分。方法 用各种柱色谱方法进行分离纯化,根据理化性质和波谱解析鉴定其化学结构。结果 从云南獐牙菜的甲醇提取物中得到9个化合物,分别鉴定为：齐墩果酸 (oleanolic acid,I)、β-谷甾醇 (β-sitosterol,II)、豆甾醇 (stigmasterol, III)、雏菊叶龙胆酮 (bellidifolin,IV)、去甲基雏菊叶龙胆酮 (demethylbellidifolin,V)、龙胆黄素 (gentisin, VI)、当药醇苷 (swertianolin,VII)、2&;#61602;-间羟基苯甲酰獐牙菜苷(deacetylcentapicrin, VIII)、维太菊苷(vittadinoside, IX)。结论 化合物I~IX均为首次从该植物中分离得到。     

鱼胆草中獐牙菜苦苷的大孔树脂分离富集研究

目的研究大孔树脂对鱼胆草中獐牙菜苦苷富集作用,并确定其树脂分离纯化工艺参数。方法采用高效液相色谱法对獐牙菜苦苷进行分析测定,通过考察6种大孔树脂对鱼胆草中獐牙菜苦苷的静态吸附及解吸情况,选择吸附及解吸较好的树脂进行动态柱层析分离参数筛选。结果 6种大孔树脂中AB-8和SP825对鱼胆草中獐牙菜苦苷吸附效果较好,AB-8具有饱和静态吸附量及解吸率,分别为19.43 mg·g-1,92.6%,并对AB-8柱动态参数进行筛选,结果树脂动态饱和吸附量为40.5 mg·g-1;先采用2 BV水洗除杂,3.5 BV30%乙醇洗脱;树脂柱最佳径高比为1:8。结论采用AB-8大孔树脂对鱼胆草中獐牙菜苦苷进行分离纯化,可以将獐牙菜苦苷从原药的5.7%提纯至60%以上,工艺富集作用明显,且生产成本低,适合工业生产应用。     

高纯度獐牙菜苦苷的制备方法

目的从川西獐牙菜药材中制备高纯度獐牙菜苦苷。方法川西獐牙菜经醇提水沉后,上清液经HPD-300大孔吸附树脂吸附洗脱后得獐牙菜苦苷粗提物,再用闪式柱色谱对其进行分离。结果制备得到的獐牙菜苦苷,纯度在90%以上,工艺总收率为79.94%。结论本实验建立的制备高纯度的獐牙菜苦苷的方法,可操作性强,重现性较好,工艺收率和产品纯度均较为理想。     

獐牙菜苦苷的药理作用研究进展

獐牙菜苦苷是一个具有良好生物活性的天然环烯醚萜类化合物。现代药理研究表明,獐牙菜苦苷具有保肝、调血脂、抗糖尿病、镇痛镇静和抗炎等多种作用。综述獐牙菜苦苷药理作用的研究进展。     

高效液相色谱法测定川东獐牙菜中獐牙菜苦苷和去甲当药苷的含量

目的 建立测定川东獐牙菜中獐牙菜苦苷和去甲当药苷含量的高效液相色谱方法。方法 HYPERSILBDSC18(4.6 mm×200 mm,5μm)色谱柱,流动相为乙腈-磷酸二氢钠(0.03 mol·L-1,pH=3.0),梯度洗脱(ACN%;0 min 5％,20 min 15％),流速为0.8 mL·min-1,检测波长为250 nm,柱温为25℃。结果 獐牙菜苦苷和去甲当药苷分别在1.528-11.466μg,85.4-854 ng范围内线性良好,相关系数r分别为0.99992、0.99988, 平均回收率分别为99.1％和101.8％,RSD均<1％(n=5)。结论 本方法操作简便,分离效果好,灵敏度高,重 现性好,为控制川东獐牙菜质量提供参考。     

丽江獐牙菜化学成分研究

目的研究民族药丽江獐牙菜(Swertia delavayi)的化学成分。方法用系统溶剂提取,常规的硅胶柱色谱和薄层色谱进行分离纯化,根据化合物的物理、化学性质和波谱特征鉴定其结构。结果从丽江獐牙菜的脂溶性部分分离得到6个化合物,其中3个分别鉴定为1,8-二羟基-3,7-二甲氧基口山酮(Ⅰ)、1,7,8-三羟基-3-甲氧基口山酮(Ⅱ)和齐墩果酸(Ⅲ),另3个结构正在鉴定中。结论所有化合物均为首次从该植物中得到。     

獐牙菜总苷高效液相色谱指纹图谱研究

目的研究獐牙菜总苷的高效液相色谱指纹图谱，为科学评价及有效控制其工艺和质量提供可靠方法。方法利用HPLC-DAD方法，梯度洗脱，测定了10批獐牙菜总苷样品。色谱条件为：Kromusil C₁₈分析柱(250 mm×4.6 mm ID, 5 μm)；柱温40 ℃；流动相A为10%甲醇-水，流动相B为80%甲醇-水，流动相A梯度洗脱(100%→0%)，分析时间32 min，0-15 min A∶B从100%∶0 → 0∶100%，15-32 min保持在0% A；流速为1.0 mL·min^-1；检测波长为260 nm。结果10批獐牙菜总苷样品得到的色谱指纹图谱有16个共有峰，分为3个部分：保留时间0-10 min，出现1个峰；保留时间10-15 min，出现9个峰，主要特征峰1-7号峰均在此区域，保留时间15-30 min出现5个峰。通过与对照品的保留时间、紫外光谱及LC/MS所得分子量信息，1-7号峰分别鉴定为獐牙菜苦苷、龙胆苦苷、獐牙菜苷、异荭草苷、当药黄素、异当药黄素、獐牙菜山酮苷；时间15-30 min，出现6个峰。通过峰面积及含量测定结果，确定最强峰为1号峰。相同色谱条件下测定了不同工艺提取的獐牙菜提取物及獐牙菜药材的HPLC图谱，其结果与獐牙菜总苷有很好的相关性。结论獐牙菜总苷的指纹图谱特征性及专属性强，可结合含量测定用于全面控制獐牙菜总苷的质量，确保每批产品的均一性。     

常用“蒂达”类藏药材四数獐牙菜的成分分析

目的：建立高效液相色谱法同时测定四数獐牙菜中獐牙菜苦苷、龙胆苦苷、当药苷、当药醇苷、1-羟基-3,4,5三甲氧基■酮含量的方法。方法：采用Waters SunFire C18柱（4.6 mm×250 mm,5μm）;以0.05%磷酸溶液-甲醇为流动相进行梯度洗脱;柱温30℃,流速1.0 mL·min-1,检测波长254 nm。结果：獐牙菜苦苷、龙胆苦苷、当药苷、当药醇苷、1-羟基-3,4,5三甲氧基■酮分别在0.0320～0.3202μg(r=0.9997)、0.3788～3.7881μg(r=0.9998)、0.0124～0.1237μg(r=0.9995)、0.0032～0.0321μg(r=0.9998)、0.0031～0.0308μg(r=0.9994)进样质量范围内呈良好的线性关系,加样回收率分别为98.69%、97.81%、92.21%、93.44%、92.77%,RSD(r=6)分别为0.76%、1.77%、1.98%、1.59%、1.79%。7批样品中獐牙菜苦苷、龙胆苦苷、当药苷、当药醇苷、1-羟基-3,4,5三甲氧基■酮的测定结果分别为0.1924%～0.3740%、...     

国产日本当药中獐牙菜苦苷与当药苷的HPLC含量测定及其品质评价

目的建立一种可以同时测定日本当药中獐牙菜苦苷与当药苷的方法,对我国引种与日本产的日本当药进行品质评价和比较。方法采用高效液相色谱法,色谱柱为Phenomenex C18(4.6 mm×250 mm,5μm);流动相为乙腈-水,梯度洗脱,流速为1 m L·min-1,柱温为30℃,进样量为10μL,检测波长分别为238、247 nm。结果獐牙菜苦苷、当药苷分别在0.019~1.234 mg·m L-1(r=1)、0.002~0.232 mg·m L-1(r=0.999 8)内呈良好的线性关系,平均加样回收率分别为99.50%、99.90%,RSD值分别为1.58%、2.10%。我国引种日本当药与日本产样品相比,个别成分相对含量略有差异,其中獐牙菜苦苷含量较高,达到了97.21 mg·g-1,而当药苷含量则较低;不同产地的日本当药均以花中有效成分含量最高。结论我国引种的日本当药中的獐牙菜苦苷含量高,很有开发价值,该文所建方法为我国对国产日本当药的合理开发利用和质量控制提供了依据和技术。     

裂环环烯醚萜苷类化合物的药理作用研究进展

裂环环烯醚萜苷类化合物是一类具有保肝、降血糖、调血脂、抗炎、抗肿瘤和神经保护作用的天然活性分子。本文对龙胆苦苷、獐牙菜苷和獐牙菜苦苷3个代表化合物的药理作用进行了综述，以期为裂环环烯醚萜苷类化合物的进一步研究与开发奠定基础。     

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.