火绒草黄酮类成分的分离与鉴定(Ⅱ)

目的对火绒草的化学成分进行研究,为进一步开发利用该植物资源提供依据。方法采用反复正相硅胶、反相ODS、Sephadex LH-20等柱色谱以及高效液相色谱法等手段进行分离纯化,并通过理化性质与光谱分析鉴定化合物的结构。结果从火绒草体积分数为70%的乙醇溶液提取物中又分离鉴定了7个黄酮类化合物,分别为芹菜素(apigenin,1)、山柰酚-3-O-(6″-O-乙酰基)-β-D-吡喃葡萄糖苷[kaempferol-3-O-(6″-O-acetyl)-β-D-glucopyranoside,2]、山柰酚-3-O-(6″-O-反式对香豆酰基)-β-D-吡喃葡萄糖苷[kaempferol-3-O-(6″-O-trans-p-coumaroyl)-β-D-glucopyranoside,3]、山柰酚-3-O-(6″-O-顺式对香豆酰基)-β-D-吡喃葡萄糖苷[kaempferol-3-O-(6″-O-cis-p-coumaroyl)-β-D-glucopyranoside,4]、槲皮素-7-O-β-D-吡喃葡萄糖苷(quercetin-7-O-β-D-glucopyranoside,5)、槲皮素-3-甲氧基-7-O-β-D-吡喃葡萄糖苷(quercetin-3-me-thoxy-7-O-β-D-glucopyranoside,6)、槲皮万寿菊素-7-O-β-D-吡喃葡萄糖苷(quercetagetin-7-O-β-D-glucopyranoside,7)。结论化合物1为首次从火绒草植物中分离得到,化合物2～7为首次从火绒草属植物中分离得到。     

茶叶正丁醇萃取物化学成分的分离与鉴定

目的对茶叶正丁醇萃取物的化学成分进行研究,以进一步明确茶叶的化学成分。方法采用反复硅胶柱色谱、羟丙基葡聚糖凝胶柱色谱和重结晶等多种分离方法对茶叶体积分数70%乙醇回流提取物的正丁醇萃取物进行分离纯化,并根据理化性质和NMR谱数据对分离得到的化合物进行结构鉴定。结果分离得到10个化合物,分别鉴定为山柰酚(kaempferol,1)、槲皮素(quercetin,2)、山柰酚-3-O-β-D-吡喃葡萄糖苷(kaempferol-3-O-β-D-glucopyranoside,3)、槲皮素-3-O-β-D-吡喃葡萄糖苷(quercetin-3-O-β-D-glucopyranoside,4)、山柰酚-3-O-芸香糖苷(kaempferol-3-O-rutinoside,5)、芦丁(rutin,6)、槲皮素-3-O-α-L-呋喃阿拉伯糖苷(quercetin-3-O-α-L-arabinofuranoside,7)、正丁基-β-D-吡喃果糖苷(n-butyl-β-D-fructopyranoside,8)、绿原酸甲酯(methyl chlorogenate,9)、尿嘧啶(u-racil,10)。结论化合物8~10为首次从山茶属植物中分离得到;化合物7为首次从植物茶中分离得到。     

板栗花的化学成分

目的对板栗花的化学成分进行分离和结构鉴定。方法采用硅胶柱色谱、凝胶柱色谱和重结晶等分离方法对板栗花体积分数为90%的乙醇溶液提取物进行化学分离;通过谱学分析方法结合化合物理化性质对化合物结构进行鉴定。结果分离得到11个化合物,分别鉴定为2α,3β,23-三羟基齐墩果烷-12-烯-28-酸(2α,3β,23-trihydroxyolean-12-en-28-acid,1)、4-喹啉酮-2-羧酸-正丁基酯(4-quinolinone-carboxylic-2-acidn-butyl ester,2)、槲皮素-3-O-β-D-半乳糖苷(quercetin-3-O-β-D-ga-lactopyranoside,3)、山柰酚(kaempferol,4)、槲皮素(quercetin,5)、山柰酚-3-O[6″-O-反式-对-香豆酰基]-β-D-吡喃葡萄糖苷(kaempferol-3-O-[6″-O-(E)-p-coumaroyl]-β-D-glucopyranoside,6)、山柰酚-3-O-[2″,6″-O-双-反式-对-香豆酰基]-β-D-吡喃葡萄糖苷(kaempferol-3-O-[2″,6″-di-O-(E)-p-coumaroyl]-β-D-glucopyranoside,7)、没食子酸(gallic acid,8)、原儿茶酸(protocatechuic acid,9)、5-羟甲基糠醛(5-hydroxymethylfurfuraldehyde,10)、槲皮素3-O-β-D-葡萄糖醛酸甲酯(quercetin-3-O-β-D-glucuronide6″-methyl ester,11)。结论化合物1,2,11为从栗属植物中首次分离得到,化合物3为从该植物中首次分离得到。     

维药蜀葵花化学成分的分离与鉴定(Ⅱ)

目的对维药蜀葵花(Althaea rosea(Linn.)Cavan.)的化学成分进行进一步的研究。方法采用正相硅胶、反相ODS、Sephadex LH-20等柱色谱及高效液相色谱手段进行分离纯化,并通过理化性质与波谱分析方法鉴定化合物的化学结构。结果从蜀葵花体积分数为95%的乙醇提取物中分离得到9个黄酮类单体成分,分别鉴定为槲皮素(quercetin,1)、槲皮素-3-O-β-D-吡喃葡萄糖苷(quercetin-3-O-β-D-glucopyranoside,2)、槲皮素-3-O-(6″-O-反式对香豆酰基)-β-D-吡喃葡萄糖苷(quercetin-3-O-(6″-O-trans-p-coumaroyl)-β-D-glucopyranoside,3)、槲皮素-3-O-芸香糖苷(quercetin 3-O-rutinoside,4)、槲皮素-7-O-β-D-吡喃葡萄糖苷(quercetin-7-O-β-D-glucopyranoside,5)、槲皮素-4'-O-β-D-吡喃葡萄糖苷(quercetin 4'-O-β-D-glucopyranoside,6)、槲皮素-3'-甲氧基-3-O-芸香糖苷(quercetin 3'-methoxy-3-O-β-D-rutinoside,7)、杨梅素-3-O-β-D-吡喃葡萄糖苷(myricetin-3-O-β-D-glucopyranoside,8)和芹菜素-4'-O-β-D-吡喃葡萄糖苷(apigenin-4'-O-β-D-glucopyranoside,9)。结论化合物3、7、9为首次从蜀葵属中分离得到,化合物6为首次从蜀葵花中分离得到。     

火绒草黄酮类成分的分离与结构鉴定

目的对火绒草的化学成分进行研究,为进一步开发利用该植物资源提供依据。方法采用反复正相硅胶、反相ODS、Sephadex LH-20等柱色谱以及高效液相色谱法等手段进行分离纯化,并通过理化性质与光谱分析鉴定化合物的结构。结果从火绒草体积分数为70%的乙醇溶液提取物中分离鉴定了9个黄酮类化合物,分别为槲皮素-3-O-β-D-吡喃葡萄糖苷(quercetin-3'-O-β-D-gluco-pyranoside,1)、槲皮素-3'-O-β-D-葡萄糖苷(quercetin-3'-O-β-D-glucopyranoside,2)、5,7,3',4'-tetra-hydroxy-3-methoxyflavone(3)、5,7,3',4'-tetrahydroxy-3-methoxyflavonol-3'-O-β-D-glucopyranoside(4)、山柰酚(kaempferol5,)、山柰酚-3-O-β-D-吡喃葡萄糖苷(kaempferol-3-O-β-D-glucopyranoside6,)、3-甲基-山柰酚(3-methyl-kaempferol,7)、3-甲醚-山柰黄素-7-O-β-D-吡喃葡萄糖苷(3-methylether-kaempferol-7-O-β-D-glucoside,8)、木犀草素-3'-O-β-D-葡萄糖苷(luteolin-3'-O-β-D-glucoside9,)。结论化合物2-57、8、为首次从火绒草属植物中分离得到。     

红松松针中黄酮类成分的分离与鉴定

目的研究红松松针中的黄酮类成分,为松属植物的化学分类学研究提供依据。方法采用反复硅胶、聚酰胺、ODS、Sephadex LH-20柱色谱等方法进行分离纯化,根据理化性质和1H-NMR、13C-NMR等技术对分离得到的化合物进行结构鉴定。结果从红松松针中分离得到7个化合物,分别鉴定为蛇葡萄素4′-O-β-D-吡喃葡萄糖苷[ampelopsin 4′-O-β-D-glucopyranoside,1]、槲皮素3-O-α-L-呋喃阿拉伯糖苷[quercetin3-O-α-L-arabinofuranoside,2]、山柰酚3-O-α-L-呋喃阿拉伯糖苷[kaempferol3-O-α-L-arabinofuranoside,3]、山柰酚3-O-β-D-吡喃葡萄糖苷[kaempferol3-O-β-D-glu-copyranoside,4]、5,7,8,4′-四羟基-3-甲氧基-6-甲基黄酮8-O-β-D-吡喃葡萄糖苷[5,7,8,4′-tetra-hydroxy-3-methoxy-6-methylfavone8-O-β-D-glucopyranoside,5]、山柰酚3-O-(5″-O-反式-阿魏酰基)-α-L-呋喃阿拉伯糖苷[kaempferol3-O-(5″-O-E-feruloyl)-α-L-arabinofuranoside,6]、山柰酚3-O-(5″-O-反式-对-香豆酰基)-α-L-呋喃阿拉伯糖苷[kaempferol3-O-(5″-O-E-p-coumaroyl)-α-L-arabi-nofuranoside,7]。结论化合物1-3为首次从松属植物中分离得到,4-7为首次从该种植物中分离得到。     

油松松针中黄酮类成分的分离与鉴定

目的研究油松松针中的黄酮类成分,为松属植物的化学分类学研究提供科学依据。方法采用反复硅胶、聚酰胺、ODS、Sephadex LH-20柱色谱等方法进行分离纯化,根据理化性质和1H-NMR、13C-NMR、质谱等技术对分离得到的化合物进行结构鉴定。结果从油松松针中分离得到4个化合物,分别鉴定为山柰酚-3-O-(3″-O-反式-对-肉桂酰基)-(6″-O-反式-阿魏酰基)-β-D-吡喃葡萄糖苷[kaempferol 3-O-(3″-O-E-p-coumaroyl)-(6″-O-E-feruloyl)-β-D-glucopyranoside,1]、山柰酚-3-O-(3″,6″-二-反式-对-肉桂酰基)-β-D-吡喃葡萄糖苷[kaempferol3-O-(3″,6″-di-O-E-p-coumaroyl)-β-D-glucopyranoside,2]、山柰酚-3-O-(3″-反式-对-肉桂酰基)-β-D-吡喃葡萄糖苷[kaempferol3-O-(3″-O-E-p-coumaroyl)-β-D-glucopyranoside,3]、异鼠李素-3-O-β-D-吡喃葡萄糖苷[isorhamnetin3-O-β-D-glucopyranoside,4]。结论化合物1、3为首次从松属植物中分离得到,化合物2、4为首次从该种植物中分离得到。     

桃儿七中黄酮类成分的分离与鉴定

目的对桃儿七的95%(φ)乙醇提取物的化学成分进行研究。方法利用反复硅胶、SephadexLH-20、开放ODS柱色谱等方法进行分离纯化;根据理化性质及波谱分析对分离得到的化合物进行结构鉴定。结果分离得到8个黄酮类化合物,分别鉴定为山柰酚(kaempferol,1)、槲皮素(querce-tin,2)、杨梅素-3',4'-二甲醚(myricetin-3',4'-dimethyl ether,3)、3-O-甲基-槲皮素(3-O-methyl-quercetin,4)、山柰酚-3-O-β-D-葡萄糖苷(kaempferol-3-O-β-D-glucopyranoside,5)、槲皮素-3-O-β-D-葡萄糖苷(quercetin-3-O-β-D-glucopyranoside,6)、芦丁(rutin,7)、山柰酚-3-O-芸香糖苷(kaempfer-ol-3-O-rutinoside,8)。结论化合物3、4、8为首次从该属植物中分离得到。     

沙生蜡菊花中黄酮类成分的分离与鉴定

目的研究沙生蜡菊(Helichrysum arenarium(L.)Moench)花的化学成分。方法采用硅胶柱色谱?ODS柱色谱和HPLC柱色谱分离纯化,依据理化性质、波谱数据分析进行结构鉴定。结果从沙生蜡菊花的甲醇提取物中分离得到8个黄酮类化合物,分别鉴定为山奈酚3-O-β-D-吡喃葡萄糖苷(kaempferol 3-O-β-D-glucopyranoside,1)、木犀草素3′-O-β-D-吡喃葡萄糖苷(luteolin3′-O-β-D-glucopyranoside,2)、木犀草素7-O-β-D-吡喃葡萄糖苷(luteolin7-O-β-D-glucopyranoside,3)、木犀草素6-羟基-7-O-β-D-吡喃葡萄糖苷(luteolin6-hydroxy-7-O-β-D-glucopyranoside,4)、木犀草素3′-甲氧基-6-羟基-7-O-β-D-吡喃葡萄糖苷(luteolin3′-methoxyl-6-hydroxy-7-O-β-D-glucopyranoside,5)、黄芩素7-O-β-D-吡喃葡萄糖苷(scutellarein7-O-β-D-glucopyranoside,6)、山柰酚3-O-β-D-龙胆二糖苷(kaempferol3-gentiobioside,7)、山柰酚3-O-(3-β-D-吡喃葡萄糖基)-β-D-吡喃葡萄糖苷(kaempferol3-O-(3-β-D-glucopyranosyl)-β-D-glucopyranoside,8)。结论化合物2、4~8为首次从蜡菊属植物中分离得到。     

黄独的化学成分

目的研究中药黄独(Dioscorea bulbifera L.)乙醇提取物的乙酸乙酯萃取部分的化学成分。方法采用硅胶、Sephadex LH-20柱色谱等方法进行分离,利用理化性质和1H-NMR13C-NMR等谱学技术,对分离得到的化合物进行结构鉴定。结果从中分离得到6个化合物,其结构鉴定为(+)儿茶素(catechin,1)、3,5-二甲氧基山柰酚(3,5-dimethoxykaempferol,2)、山核桃素(caryatin,3)、山柰酚(kaempferol,4)、山柰酚-3-O-β-D-吡喃半乳糖苷(kaempferol-3-O-β-D-galactopyranoside,5)、山柰酚-3-O-β-D-吡喃葡萄糖苷(kaempferol-3-O-β-D-glucopyranoside,6)。结论化合物4、6为首次从薯蓣属植物中分离得到的已知化合物。     

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.     

Synthesis,Cytotoxicity and Antileishmanial Activity of Some N-(2-(indol-3-yl)ethyl)-7-chloroquinolin-4-amines

We report herein the condensation of 4,7-dichloroquinoline (1) with tryptamine (2) and D-tryptophan methyl ester (3) . Hydrolysis of the methyl ester adduct (5) yielded the free acid (6) . The compounds were evaluated in vitro for activity against four different species of Leishmania promastigote forms and for cytotoxic activity against Kb and Vero cells. Compound (5) showed good activity against the Leishmania species tested, while all three compounds displayed moderate activity in both Kb and Vero cells.     

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.     

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.     

Glycofection: The Ubiquitous Roles of Sugar Bound on Glycoplexes

Glycofection (transfection by using sugar-substituted polylysine) was assessed in order to provide an alternative to viral vectors for the transfer of genes into vascular smooth muscle cells. A rabbit vascular smooth muscle cell line (Rb-1 cells) was selectively transfected by using glycoplexes (glycosylated polylysine/pSV2LUC complexes) in the presence of 10 mu M of the fusogenic peptide GALA. A sugar-specific transfection was obtained when the glycofection was conducted for 1 h with glycoplexes containing either alpha Gal, alpha -Glc, alpha -GalNAc, beta -GlcNAc, or beta -GalNAc residues. The gene expression was high after transfection, with glycoplexes bearing alpha Gal, alpha -GalNAc, or beta -GalNAc residues that were weakly internalized, and low with glycoplexes carrying Lact or Rha residues that were well taken up by cells. These results suggest that 1) glycofection can be a good approach for a selective transfer of genes intovascular smooth muscle cells, 2) an efficient uptake of the glycoplexes is not the unique limiting step for an efficient transfection, and 3) the sugar-dependent trafficking of the glycoplexes inside the cells may account for the transfection efficiency.