苦楝皮化学成分的研究

目的研究苦楝皮的化学成分。方法在室温条件下,采用75%乙醇浸提,对得到的浸膏依次以石油醚和乙酸乙酯萃取。利用硅胶柱色谱、Spehadex LH-20凝胶柱色谱、ODS柱色谱及半制备高效液相色谱等分离方法,从乙酸乙酯萃取物中获得单体化合物,根据理化性质和波谱学特征鉴定其化学结构。结果分离得到5个单体化合物,其中4个为柠檬苦素类化合物:12-O-methyl-1-O-deacetylnimbolinin B(1)、12-O-methyl-1-O-tigloyl-1-O-deacetyl-nimbolinin B(2)、12-O-ethyl-1-deactylnimbolinin B(3)、6α,11β-diacetoxygedunin(4);1个为黄酮类化合物:3'-O-methylcatechin-7-O-β-D-glucopyranoside(5)。结论以上5个化合物均为首次从该植物中分离得到。     

玄参的化学成分研究

目的研究中药玄参(Scrophularia ninpoensis Hemsl.)的化学成分。方法利用乙酸乙酯萃取、硅胶柱色谱,Sephadex LH-20柱色谱,制备薄层色谱等方法对化合物进行分离和纯化,并通过波谱手段对分离得到的化合物进行鉴定。结果从玄参的乙酸乙酯萃取部位中分离得到6个化合物:eucalyptolic acid(Ⅰ),buergerisides A1(Ⅱ),原儿茶酸(Ⅲ),五-羟甲基糠醛(Ⅳ),肉桂酸(Ⅴ),β-谷甾醇(Ⅵ)。结论化合物Ⅰ,Ⅱ,Ⅲ为首次从该植物中分离得到。     

胀果甘草化学成分的分离与鉴定

目的研究胀果甘草乙醇提取物的乙酸乙酯萃取部分,对其中的化学成分进行分离鉴定。方法采用硅胶、Sephadex LH-20柱色谱以及半制备型高效液相色谱等手段进行分离纯化,通过理化性质和各种波谱技术对化合物进行结构鉴定。结果从胀果甘草的乙酸乙酯萃取部分分离得到5个化合物,分别鉴定为刺芒柄花素(Formononetin,1)、异甘草素(Isoliquiritigenin,2)、达维荚蒾苷元(Dihydroisoliquiritigenin,3)、α-甘草次酸(α-Glycyrrhetic acid,4)和β-甘草次酸(β-Glycyrrhetic acid,5)。结论化合物3为首次从胀果甘草中分离得到。     

酸浆宿萼的化学成分

目的研究茄科植物酸浆宿萼(Physalis alkekengiL.var.franchetii(Mast.)Makino)的化学成分。方法用体积分数为80%的乙醇溶液对酸浆宿萼进行加热回流提取,回收乙醇,浓缩后用水混悬,依次用环己烷、乙酸乙酯萃取,取乙酸乙酯层经硅胶柱色谱,CHCl3MeOH混合溶剂做梯度洗脱;CHCl3MeOH体积比为100∶2、100∶6,洗脱部分以及萃取后的水层再次经硅胶柱色谱、Sephadex LH 20柱色谱、反相ODS开放柱色谱及RP HPLC等,共得到7个化合物;利用其理化性质和波谱学分析数据,鉴定化学结构。结果分离得到了7个化合物中4个为酸浆苦素类化合物,分别鉴定为酸浆苦素D(Ⅰ)、酸浆苦素L(Ⅱ)、酸浆苦素O(Ⅲ)、4,7二脱氢新酸浆苦素B(Ⅳ);3个黄酮类化合物,分别鉴定为木犀草素(Ⅴ)、商陆素(Ⅵ)、木犀草素7,4′二OβD葡萄糖苷(Ⅶ)。结论商陆素(Ⅵ)、木犀草素7,4′二OβD葡萄糖苷(Ⅶ)为首次从该植物中分离得到的2个已知化合物。     

椒目的化学成分

目的对椒目(Zanthoxylum bungeanumMaxim.)质量分数为95%的乙醇提取物的化学成分进行研究。方法椒目用质量分数为95%的乙醇溶液回流提取,减压回收溶剂后,得浸膏加适量水混悬,依次用石油醚、氯仿、乙酸乙酯、正丁醇萃取,回收溶剂。所得各部分浸膏综合利用硅胶柱色谱S、ephadex LH 20凝胶柱色谱、薄层色谱、重结晶等各种方法进行分离纯化,根据化合物的理化性质和波谱数据分析进行结构鉴定。结果从椒目的乙酸乙酯萃取物中分离得到4个化合物,分别鉴定为:表儿茶素(Ⅰ)、槲皮素(Ⅱ)、24烯环阿尔廷酮(Ⅲ)、辛二酸(Ⅳ)。结论化合物Ⅰ~Ⅳ均为首次从该属植物中分离得到。     

落花生茎叶醋酸乙酯部位化学成分研究

目的 研究落花生Arachis hypogaea茎叶的化学成分.方法 采用硅胶柱色谱、凝胶柱色谱和ODS柱色谱进行分离纯化,通过理化方法和波谱数据进行结构鉴定.结果 从落花生茎叶70％乙醇提取液的醋酸乙酯萃取部位分离得到8个化合物,经波谱分析鉴定其结构,分别为肉豆蔻酸(1)、十五碳酸(2)、汉黄芩素(3)、美迪紫檀素(4)、邻苯二甲酸二丁酯(5)、异香草酸(6)、芒柄花素(7)、β-谷甾醇(8).结论 化合物2、3、4、5、7为首次从该植物中分离得到.     

海洋真菌Y26-02的灰黄霉素类化学成分

目的研究海洋真菌Y26-02发酵液的乙酸乙酯萃取部分,对其中的化学成分进行分离鉴定。方法采用硅胶、Sephadex LH-20柱色谱以及制备型高效液相色谱等手段进行分离纯化,通过理化性质和各种波谱数据对这些化合物进行结构鉴定。结果从海洋真菌Y26-02菌液的乙酸乙酯萃取部分分离得到7个化合物,分别鉴定为灰黄霉素(griseofulvin,1)、表灰黄霉素(epigriseofulvin,2)、异灰黄霉素(isogriseofulvin,3)、脱氯表灰黄霉素(dechloroepigriseofulvin,4)、脱氢灰黄霉素(de-hydrogriseofulvin,5)、4′-丁氧基异灰黄霉素(4′-butoxyisogriseofulvin,6)、2′-丁氧基表灰黄霉素(2′-butoxyepigriseofulvin,7)。结论这7个化合物均为首次从该真菌的代谢产物中分离得到,其中化合物6、7是新天然产物。     

分蘖葱头中含氮化合物的分离与鉴定

目的 研究分蘖葱头中的非挥发性成分。方法 用硅胶和凝胶柱色谱进行分离,根据理化性质和波谱特征鉴定结构。 结果 从分蘖葱头的乙酸乙酯和正丁醇萃取部分中分离得到两个含氮化合物,分别鉴定为N-反式-对羟基苯乙基香豆酰胺（I）和1,6-己内酰胺（II）。结论 化合物I和II均为首次从分蘖葱头中分离得到的单体,其中化合物II为首次从植物中分离得到的天然产物。     

广东石豆兰的化学成分研究

目的:对广东石豆兰(Bulbophyllum kwangtungense Schltr)60%乙醇提取物乙酸乙酯萃取层中的化学成分进行分离鉴定.方法:采用硅胶、ODS等多种柱色谱方法,对广东石豆兰的60%乙醇提取物的乙酸乙酯萃取层进行分离,以反相HPLC进行纯化.根据化合物的理化常数、波谱学特征并参考文献,鉴定了化合物的结构.结果:从广东石豆兰的60%乙醇提取物的乙酸乙酯层中,分离得到了3个菲类化合物和2个9,10二氢菲类化合物,利用理化常数和波谱学分析鉴定为Bulbophyllanthrin(Ⅰ)、2,3,4-三甲氧基-5-羟基菲(Ⅱ)、2,3,4,5-四甲氧基菲(Ⅲ)、Coelonin(Ⅳ)和2,4,7-三甲氧基-9,10-二氢菲(Ⅴ).结论:化合化Ⅴ为首次从该属植物中分离得到,其余4个化合物均为首次从该种植物中分离得到.     

中药异叶爬山虎抗氧化活性部位化学成分研究

目的对中药异叶爬山虎Parthenocissus heterophylla(BI.)Merr.抗氧化活性部位——乙酸乙酯萃取部位进行化学成分研究。方法采用硅胶、Sephadex LH-20柱色谱等方法进行分离纯化,根据理化性质及波谱数据鉴定化合物的结构。结果从异叶爬山虎乙酸乙酯萃取部位分离并鉴定了6个化合物,分别为豆甾-4-烯-3-酮(1)、胡萝卜苷(2)、芹菜素(3)、木犀草素(4)、槲皮素(5)、槲皮素3-O-β-D-葡萄糖苷(6)。结论化合物1~6为首次从该植物中分离得到。     

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.