桔梗乙酸乙酯部位的化学成分研究

目的:研究桔梗乙酸乙酯部位的化学成分.方法:采用多种色谱、核磁共振波谱方法对桔梗乙酸乙酯部位化学成分进行分离和结构鉴定.结果:分离得到9个化合物,分别为齐墩果酸 (1)、木栓醇 (2)、黄芩素-7-甲醚 (3)、胡萝卜苷(4)、α-菠菜甾醇 (5)、α-菠菜甾醇-3-O-β-D-吡喃葡萄糖苷 (6)、白桦脂醇 (7)、△7-豆甾烯醇 (8)、β-谷甾醇 (9).结论:化合物1,2,3,4为从该植物中首次分离得到.     

吉祥草甾体类化学成分研究

目的研究吉祥草甾体类化学成分。方法采用硅胶、Sephadex LH-20等色谱技术进行分离纯化,通过理化方法和波谱数据进行分析和结构鉴定。结果从吉祥草中分离鉴定了9个甾体类化合物,分别为薯蓣皂苷元(1)、奇梯皂苷元(2)、潘托落皂苷元(3)、β-豆甾醇(4)、β-豆甾醇-3-O-β-D-吡喃葡萄糖苷(5)、kitigenin 5-O-β-D-glucopyrannoside(6)、pentologenin 5-O-β-D-glucopyrannoside(7)、薯蓣皂苷元-3-O-β-D-吡喃葡萄糖苷(8)、25(S)-5β-1β-3β-diol(9)。结论化合物8和9为首次从该属植物中分离得到。     

新疆罗勒化学成分的分离鉴定

目的 研究新疆罗勒Ocimum bacilicum L.全草的化学成分. 方法用硅胶、凝胶柱色谱法分离化合物,用波谱法鉴定其结构. 结果从罗勒全草中分离鉴定了4个甾体类化合物即β-谷甾醇(Ⅰ)、胡萝卜苷(Ⅱ)、豆甾醇(Ⅲ)、豆甾醇-3-O-β-D-葡萄糖苷(Ⅳ)和3个黄酮类化合物即芦丁(Ⅴ)、槲皮素-3-O-β-D-葡萄糖苷(Ⅵ)、山奈酚-3-O-β-D-葡萄糖苷(Ⅶ).结论 化合物Ⅰ～Ⅶ均为首次从该植物中分得.     

工业大麻研究．I．甲醇提取物的石油醚萃取和正丁醇萃取部分的化学成分

从工业大麻甲醇提取物的石油醚萃取部分分离鉴定了14个化合物，分别为β-谷甾醇（1）、豆甾醇（2）、二十二烷酸甲酯（3）、△^5。22．豆甾醇乙酸酯（4）、α-菠菜甾醇（5）、表无羁萜醇（6）、无羁萜酮（7）、四氢大麻酚（8）、大麻二酚（9）、大麻二酚酸（10）、cannabielsoicacidA（11）、大麻酚（12）、催叶萝芙叶醇（13）和去氢催叶萝芙叶醇（14）。从正丁醇萃取部分分离鉴定了15个化合物，分别为芦丁（15）、槲皮素-3-O—α—L-鼠李糖苷（16）、山奈酚-3．O—α—L-鼠李糖苷（17）、芹菜素-7-O-α-L-鼠李糖苷（18）、芹菜素-7-O—α-D-吡喃葡萄糖苷（19）、木犀草素-7-O—β—D-吡喃葡萄糖苷（20）、1，3,6，7-四羟基-2-C-β-D-吡喃葡萄糖口山酮（21）、牡荆素（22）、荭草素（23）、芹菜素-6，8-二-C—β—D-吡喃葡萄糖苷（24）、牡荆素-2”-O—α—L-鼠李糖苷（25）、荭草素．2”．O—β—D-吡喃葡萄糖苷（26）、肌醇甲醚（27）、肌醇（28）、尿嘧啶（29）。其中化合物3、4、5、21、24、27、29为首次报道从该属植物中得到。     

桐花树化学成分的研究

目的 研究桐花树的化学成分.方法 采用硅胶柱色谱法分离纯化,薄层色谱及波谱法鉴定结构.结果 从桐花树茎皮的乙醇提取物分离得9个化合物,结构鉴定为α-菠甾醇(Ⅰ)、豆甾醇(Ⅱ)、齐墩果酸(Ⅲ)、原报春花素A(Ⅳ)、没食子酸甲酯(Ⅴ、化合物Ⅵ可能为α-菠甾醇-3-O-β-D-吡喃葡萄糖苷(Ⅵ)和△5,22豆甾醇-3-O-β-D-吡喃葡萄糖苷(Ⅵb)的混合物、正三十四烷醇(Ⅶ)、正三十二烷醇(Ⅷ)、没食子酸(Ⅸ).结论 化合物Ⅴ、Ⅵ、Ⅶ、Ⅷ为首次从桐花树茎皮中分离得到.     

紫伪翼手参中4个甾醇苷的分离鉴定

目的研究中国南海紫伪黑手参的化学成分。方法应用多种色谱技术分离，运用波谱分析和化学方法鉴定化合物的结构。结果分离得到4个甾醇苷单体并分别鉴定为：24-甲基-5α-胆甾烷-7，22Z-二烯-3β-O-β-吡喃木糖苷（Ⅰ），24-甲基-5α-胆甾烷-7，24（28）-二烯-3β-O-β-D-吡喃木糖苷（Ⅱ），24-甲基-5α-胆甾烷-7-烯-3β-O-β-D-吡喃木糖苷（Ⅲ）和24-乙基-5α-胆甾烷-7-烯-3β-O-D-吡喃木糖苷（Ⅳ）。结论4个化合物均为首次从海参中获得单体。     

瓜蒌皮脂溶性化学成分的研究

从葫芦科植物瓜蒌果皮的脂溶性部位分得晶Ⅰ～Ⅵ,其中Ⅰ～Ⅴ经 IR,GC-MS,MS,~1H 和~(13)C-NMR 等方法鉴定,分别为饱和脂肪醇混合物、饱和脂肪酸混合物、Δ~7-豆甾烯醇、β-菠菜甾醇和Δ~7-豆甾烯醇-β-D-葡萄糖甙。     

金腰箭化学成分的研究

从菊科植物金腰箭全草的８５％乙醇提取物中，分离鉴定了２个三萜皂苷、３个甾体化合物和１个甾体皂苷，分别为齐墩果酸－３－Ｏ－β－Ｄ－吡喃葡萄糖醛酸甲酯（Ⅰ）、金腰箭苷甲（Ⅱ）、β－谷甾醇（Ⅲ）、豆甾醇（Ⅳ）、扶桑甾醇（Ⅴ）和豆甾醇－３－Ｏ－β－Ｄ－吡喃萄萄糖苷（Ⅵ）。其中金腰箭苷甲为新化合物，其余均是首次从该植物中发现。     

三叶悬钩子的化学成分研究北大核心CSCD

目的：研究三叶悬钩子的化学成分。方法：采用甲醇对药材进行提取得到浸膏,利用硅胶、Sephadex LH-20凝胶、RP-18等柱层析色谱分离纯化,根据理化性质、波谱学数据（1HNMR和13CNMR数据）以及和文献数据比较进行结构鉴定。结果：从三叶悬钩子的甲醇提取物中分离出11个化合物,分别鉴定为3β,16α,17-三羟基贝壳杉烷（Ⅰ）、16α,17,19-三羟基贝壳杉烷（Ⅱ）、委陵菜酸（Ⅲ）、蔷薇酸（Ⅳ）、2α,3α-二羟基-12-烯-28-齐墩果酸（Ⅴ）、齐墩果酸（Ⅵ）、槲皮素-3-O-β-D-吡喃葡萄糖苷（Ⅶ）、山柰酚-3-O-β-D-（6″-O-对香豆酸酯）吡喃葡萄糖苷（Ⅷ）、山柰酚3-O-β-D-吡喃葡萄糖苷（Ⅸ）、山柰酚（Ⅹ）和胡萝卜苷（Ⅺ）。结论：化合物Ⅰ~Ⅺ均为首次从该植物中分离得到。     

维药两色金鸡菊花化学成分的分离与鉴定

目的研究维药两色金鸡菊花的化学成分,以期更好地开发利用金鸡菊。方法采用聚酰胺、Sephadex LH-20和ODS柱色谱等分离手段进行化学成分的分离纯化,根据理化性质及波谱数据鉴定其化学结构。结果从两色金鸡菊花醇提取物的乙酸乙酯萃取部分中分离得到8个化合物,分别鉴定为山柰酚-7-O-β-D-吡喃葡萄糖苷(kaempferol-7-O-β-D-glucopyranoside,1)、3',4',7-三羟基黄酮-7-O-β-D-吡喃葡萄糖苷(3',4',7-trihydroxyflavone-7-O-β-D-glucopyranoside,2)、槲皮素-7-O-β-D-吡喃葡萄糖苷(quercetin-7-O-β-D-glucopyranoside,3)、6,7,3',4'-四羟基橙酮(6,7,3',4'-tetrahydroxyaurone,4)、3',5',5-三羟基二氢黄酮-7-O-β-D-吡喃葡萄糖苷(3',5',5-trihydroxyflavanone-7-O-β-D-glucopyranoside,5)、紫铆花素-4'-O-β-D-吡喃葡萄糖苷(butein-4'-O-β-D-glucopyranoside,6)、奥卡宁(okanin,7)、马里苷(marein,8)。结论化合物1~5为首次从金鸡菊属植物中分离得到,化合物6为首次从该两色金鸡菊花中分离得到。     

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.     

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.     

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.     

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.