知母中三个新的呋甾皂苷

从中药知母（ＡｎｅｍａｒｒｈｅｎａａｓｐｈｏｄｅｌｏｉｄｅｓＢｇｅ．）中分离出三种新的呋甾皂苷，初步鉴定为（２５Ｓ）－２６－Ｏ－β－Ｄ－葡萄糖－５β－呋甾－２０（２２）－双键－３β，２６－二醇－３－Ｏ－β－Ｄ－葡萄糖基（１→２）〔β－Ｄ－葡萄糖基（１→３）〕－β－Ｄ－葡萄糖基（１→４）－β－Ｄ－半乳糖苷（１），（２５Ｓ）－２６－Ｏ－β－Ｄ－葡萄糖基－２２－羟基－５β－呋甾－３β，２６－二醇－３－Ｏ－β－Ｄ－葡萄糖基（１→２）〔β－Ｄ－葡萄糖基（１→３）〕－β－Ｄ－葡萄糖基（１→４）－β－Ｄ－半乳糖苷（２），（２５Ｓ）－２６－Ｏ－β－Ｄ－葡萄糖基－２２－甲氧基－５β－呋甾－３β，２６－二醇－３－Ｏ－β－Ｄ－葡萄糖基（１→２）〔β－Ｄ－葡萄糖基（１→３）〕－β－Ｄ－葡萄糖基（１→４）－β－Ｄ－半乳糖苷（３）．分别命名为ｔｉｍｏｓａｐｏｎｉｎ－ＢⅣ，ｔｉｍｏ－ｓａｐｏｎｉｎ－ＢⅤ，ｔｉｍｏｓａｐｏｎｉｎ－ＢⅥ．     

云南甘草皂甙A和B结构鉴定

从云南甘草中分出２个新皂甙。根据理化性质和光谱数据，鉴定这两个新皂甙为：３β－羟基齐墩果－１１，１３－二烯－２９－羧酸－３－Ｏ－β－Ｄ－吡喃葡萄糖醛酸基（１→４）β－Ｄ－吡喃葡萄糖醛酸甙和３β，２１α－二羟基齐墩果－１１，１３二烯－２９－羧酸－３－Ｏ－β－Ｄ－吡喃葡萄糖醛酸基（１→４）β－Ｄ－吡喃葡萄糖醛酸甙，分别命名为：云南甘草皂甙Ａ和Ｂ。     

太白Song木根皮的三萜皂甙成分研究

从太原song木（Sralia taibaiensis Z.Z.Wang et H.C.Zheng)根皮中首次分离得到四个三萜皂甙，根据理化性质和光谱数据，分别鉴定为齐墩果酸－3－O－[β－D－吡喃木糖1－→2）][β-D-吡喃葡萄糖（1→3)]-β-D-吡喃葡萄糖醛酸甙（1），tarasaponin V(2),3-O-{[β-D-吡喃木糖（1→2）][β-D-吡喃葡萄糖（1→3）]-β-D吡喃葡萄糖醛酸乙酯}－齐墩果酸－28－O－β－D－吡喃葡萄糖甙（3）和3－O－{[β=D 吡喃木糖（1→2)][β－D吡喃葡萄糖（1→）]-β-D吡喃葡萄糖醛酸丁酯}－齐墩果酸28－O－β－D－吡喃葡萄糖甙（4），1为新天然产物，3和4为新化合物，分别命名为太白Song木皂甙VI（taibaienoside VI),太白Song木皂甙Ⅶ（taibaienosideⅦ)和太白Song木皂甙Ⅷ（taibaienosideⅧ)。     

从人参叶中得到的两个微量皂甙成分

从有参叶中分离得到两种微量皂甙成分，分别为3β，12β，20（S）－三羟基达玛－24（25）－烯－（20－O－α－L-呋喃阿拉伯糖基（1→6）－β－D－吡喃葡萄糖基）－3－O－β-D-吡喃葡萄糖甙（1），和3β，12β，20（S）-三羟基达玛-24（25）－烯－（20－O－α-L－吡喃阿拉伯糖基（1→6）-β-D－吡喃葡萄糖基－3－O－β-D吡喃葡萄糖甙（2），前者为三七参甙－Fe(notoginsenoside-Fe）,后者为一新的天然产物，命名为人参皂甙－Rd2(ginsenoside-Rd2）。     

太白Chong木根皮中两个新的齐墩果酸皂甙

从新种太白Chong木（Aralia taibaiensis Z.Z.Wang et H.C.Zheng)根皮中分离得到两个新的齐墩果酸皂甙和一个已知化合物，齐墩果酸－28－O－β-D-吡喃葡萄糖甙（1），经理化性质和光谱数据分析，鉴定两个新化合物结构为：3－O－β-D－吡喃葡萄糖甙（2）和3－O－β－D吡喃葡萄糖醛酸癸酯－齐墩果酸－28－O－β－D－吡喃葡萄糖甙（3），分别命名为太白Chong木皂甙IV和太白Chong木皂甙V。     

用动力学方法探讨葡萄糖注射液二次消毒的稳定性

鉴于葡萄糖注射液（１０％）生产及存放过程中，其中间分解产物５－羟甲基糖醛（５－ＨＭＦ）的量在不断增长，故药典规定了其限量检查。二次消毒后的葡萄糖，因采用了先进的自动化喷淋技术，故消毒后的５－ＨＭＦ仅在０．１０左右。为保证二次消毒后的葡萄糖产品质量，对葡萄糖的有关检测指标进行了一系列考证，用动力学，实测二次消毒葡萄糖注射液的５－ＨＭＦ的含量，推导了有效期［１］。     

胀果甘草根中胀果皂甙Ⅱ和Ⅵ的结构鉴定

从胀果甘草（Glycyrrhiza inflata Bat.）根的10％乙醇浸出物中分得七个新三萜皂甙，依理化性质及波谱分析，其中二个的结构分别鉴定为：甘草次酸－3－O－β－D－6‘‘－乙基－吡喃葡萄糖醛酸基－（1→2）-β-D－6‘－正丁基吡喃葡萄糖醛酸甙（1）和甘草次酸－3－O－β－D－6‘‘－正丁基－吡喃葡萄糖醛酸基－（1→2)-β-D-6‘-乙基－吡喃葡萄糖醛酸甙（2），分别命名为胀果皂甙Ⅱ和Ⅵ。     

Effect of artemether on glucose uptake and glycogen content in Schistosoma japonicum

研究蒿甲醚（Ａｒｔ）对血吸虫摄入葡萄糖和糖原含量的影响．方法：用Ａｒｔ３００ｍｇ·ｋｇ－１ｉｇ治疗感染小鼠后２４－４８ｈ取虫，作体外培养，测定♀、♂虫糖原含量，对［Ｕ１４Ｃ］葡萄糖的摄入及［Ｕ１４Ｃ］葡萄糖掺入虫糖原的量．结果：感染小鼠用Ａｒｔ治疗后２４－４８ｈ取虫作体外培养１－２４ｈ，♂和♀虫的糖原含量分别减少２７％－６１％和３９％－７８％；６组♂虫中，仅３组的葡萄糖摄入减少２３％－３５％，而♀虫各组的均明显减少，减少率为１８％－３８％．除２组♂虫外，［Ｕ１４Ｃ］葡萄糖掺入虫的糖原量无明显变化．结论：Ａｒｔ引起血吸虫糖原的减少，可能与干扰糖酵解而不是与葡萄糖的摄入有关．     

中药红花的化学成份研究

从中药红花（ＣａｒｔｈａｍｕｓｔｉｎｃｔｏｒｉｕｓＦｌｏｗｅｒｓ）中分离得八种黄酮醇化合物，经理化分析和光谱鉴定是山奈酚Ｋａｅｍｐｆｅｒｏｌ（Ｉ）槲皮素ｑｕｅｒｃｅｔｉｎ（Ⅱ）６－羟基山萘酮６－ｈｙｄｒｏｘｙｋａｅｍｐｆｅｒｏｌ（Ⅲ），山萘酚－３－葡萄糖甙Ｋａｅｍｐｆｅｒｏｌ－３－ｇｌｕｃｏｓｉｄｅ（Ⅳ），槲皮素－７－葡萄糖甙ｑｕｅｒｃｅｔｉｎ－７－ｇｌｕｃｏｓｉｄｅ（Ｖ），槲皮素－３－葡萄糖甙ｑ     

加拿大产西洋参茎叶中的一个新三萜皂苷

从加拿大产西洋参（ＰａｎａｘｑｕｉｎｑｕｅｆｏｌｉｕｍＬ．）的茎叶中分离得到一种新达玛烷型三萜皂苷，利用理化性质和光谱数据，鉴定为３－Ｏ－〔β－Ｄ－吡喃葡萄糖基－（１－２）－β－Ｄ－吡喃葡萄糖基〕－１２－羟基达玛－２３，２５－二烯－２０－β－Ｄ－吡喃葡萄糖苷，命名为西洋参皂苷Ｌ１．     

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.