异叶梁王茶中三萜皂苷的研究

从异叶粱王茶树皮的醇提取物中分离得到两种新的三萜皂苷化学物，异叶梁王茶苷Ⅶ［ｌ］和异叶梁王茶苷Ⅷ［２］；以及一种已知化合物梁王茶苷Ⅱ［３］。经光谱和化学分析，分别鉴定为３－Ｏ－β－（２’，４’－Ｏ－二乙酰基）－Ｄ－吡喃木糖－３β－羟齐墩果－１２－烯－２８，２９－双羧酸－２８－Ｏ－［α－Ｌ－吡喃鼠李糖（１－４）－β－Ｄ－吡喃葡萄糖（１－６）－β－Ｄ－吡喃葡萄糖］酯苷［１］；３－Ｏ－β－（３’－Ｏ－乙酰基）－Ｄ－吡喃木糖－３β－羟齐墩果－１２－烯－２８，２９－双羧酸－２８－Ｏ－［α－Ｌ－吡喃鼠李糖（１－４）－β－Ｄ－吡喃葡萄糖（１－６）－β－Ｄ－吡喃葡萄糖］酯苷［２］。     

异叶梁王茶甙Ⅲ和Ⅳ的结构

继前报后,又从异叶梁王茶[Nothopanax davidii(France)Harms]树皮中分离得到两种五环三萜皂甙。经化学和波谱(IR,~1HNMR,~(13)CHMR,~1H-~1HCOSY,~(13)C-~1H COSY,MS)分析,分别鉴定为3-O-α-(2’,4’-O-二乙酰基)-L-吡喃阿拉伯糖-3β-羟基齐墩果-12-烯-28,29-双羧酸-28-O-[α-L-吡喃鼠李糖(1-4)-β-D-吡喃葡萄糖(1—6)-β-D-吡喃葡萄糖]酯甙(Ⅲ),命名为异叶梁王茶甙Ⅲ和3-O-β-(2-O-乙酰基)-D-吡喃木糖-3β-羟齐墩果-12-烯-28,29-双羧酸甙(Ⅳ),命名为异叶梁王茶甙Ⅳ。这两种皂甙均系首次从植物中分出的新化合物。     

异叶梁王茶化学成分的研究

从异叶梁王茶[Nothopanax davidii(Franch)Harms]树皮中分离得到两种五环三萜皂甙,经化学和光谱(IR,¹HNMR,¹³CNMR,¹H-¹H COSY,¹H-¹³C COSY,NOESY,MS)分析,分别鉴定为3-O-α-(3′,4′-O-二乙酰基)-L-吡喃阿拉伯糖-β-羟齐墩果-12-烯-28,29-双羧酸-28-O-[α-L-吡喃鼠李糖(1→6)-β-D-吡喃葡萄糖(1→4)-β-D-吡喃葡萄糖]酯甙(Ⅱ)和3-O-α-(3′-O-乙酰基)-L-吡喃阿拉伯糖-3β-羟齐墩果-12-烯-28,29-双羧酸甙(Ⅱ),前者命名为异叶梁王茶甙Ⅰ,后者命名为异叶梁王茶甙Ⅱ。这两个皂甙均系新化合物。     

异叶梁王茶甙Ⅲ和Ⅳ的结构

继前报后,又从异叶梁王茶[Nothopanax davidii(France)Harms]树皮中分离得到两种五环三萜皂甙。经化学和波谱(IR,¹HNMR,~(13)CHMR,¹H-¹HCOSY,¹³C-¹H COSY,MS)分析,分别鉴定为3-O-α-(2’,4’-O-二乙酰基)-L-吡喃阿拉伯糖-3β-羟基齐墩果-12-烯-28,29-双羧酸-28-O-[α-L-吡喃鼠李糖(1-4)-β-D-吡喃葡萄糖(1—6)-β-D-吡喃葡萄糖]酯甙(Ⅲ),命名为异叶梁王茶甙Ⅲ和3-O-β-(2-O-乙酰基)-D-吡喃木糖-3β-羟齐墩果-12-烯-28,29-双羧酸甙(Ⅳ),命名为异叶梁王茶甙Ⅳ。这两种皂甙均系首次从植物中分出的新化合物。     

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)。     

合欢皮中一个新的三萜皂甙

从合欢皮的乙醇提取物中用色谱法分离得到1个三糖链三萜皂甙（1）,其21位侧链含有较为少见的木糖。经化学和波谱分析,将皂甙1的结构鉴定为3－O－[β-D-吡喃木糖基-(1→2)-β-D-吡喃呋糖基－（1→6)-β-D-吡喃葡萄糖基]-21-O-{(6S)-2-反式－2－羟甲基－6－甲基－6－O－[4-O-(6R)-2-反式－2,6－二甲基－6－O－β-D-吡喃木糖基）－2,7－辛二烯酰基]－β-D-吡喃鸡纳糖基]-2,7-辛二烯酰基}-金合欢酸－28－O－β－D－吡喃葡萄糖基－（1→3)-[α-L-呋喃阿拉伯糖基－（1→4)]-α-L-吡喃鼠李糖基－（1→2)-β-D-吡喃葡萄糖基酯,为一新化合物,命名为合欢皂甙J23（1）。     

南柴胡中的新皂甙

从南柴胡（Bupleurum scorzonerifolium Willd）中分离出一个新柴胡皂甙。通过波谱分析，其结构定为3β,16α,23,28,30－五羟基－齐墩果烷－11，13（18）－二烯－3－O－β-D-吡喃葡萄糖－（1→2)-β-D-吡喃葡萄糖－（1→3)-β－D－吡喃呋糖甙，命名为柴胡皂甙r。     

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）。     

异丙基—1—硫—β—D—吡喃型葡萄糖苷的合成

介绍了黑曲霉菌β－葡萄糖苷酶诱导剂异丙基－1－硫－β－D－D吡喃型葡萄糖苷（1）的合成路线。以葡萄糖为起始原料,合成β－D1,2,3,4,6－五－O－乙酰基吡喃葡萄糖（2）,再与2－丙硫醇作用得到异丙基－2,3,4,6－四－O－乙酰基－1－1硫－β－D吡喃型葡萄糖苷（3）,再经醇解得到1。     

野木瓜甙YM10和YM12的结构

从野木瓜(Stauntonia chinensis DC.)中分离得到二个去甲五环三萜皂甙化合物,经化学和光谱分析,分别鉴定为3-O-α-L-吡喃鼠李糖-(1→2)-α-L-吡喃阿拉伯糖-30去甲齐墩果-12,20(29)-二烯-28-羧酸-28-O-α-L-呲喃鼠李糖-(1→4-β-D-吡喃葡萄糖-(1→6)-β-D-吡喃葡萄糖酯,命名为野术瓜甙YM10(Ⅰ)和3-O-α-L-呲喃鼠李糖-(1→2)-α-L-吡喃阿拉伯糖-30-去甲齐墩果-12,20(29)-二烯-28-羧酸-28-O-β-D-吡喃葡萄糖-(1→6)-β-D-吡喃葡萄糖酯,命名为野木瓜甙YM₁₂(Ⅱ)。Ⅰ和Ⅱ均系首次从植物中得到的新化合物。     

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.