野菊花化学成分研究

目的研究野菊花的化学成分。方法用80%乙醇提取野菊花化学成分,通过硅胶反复柱层析、纯化,用各种波谱数据分析鉴定化合物的结构。结果从野菊花头状花序中的乙酸乙酯提取物、氯仿提取物及正丁醇提取物中分离得到11个化合物,分别鉴定为香叶木素(Ⅰ),木犀草素(Ⅱ),木犀草素-7-O-β-D-葡萄糖苷(Ⅲ),芹菜素(Ⅳ),β-谷甾醇(Ⅴ),山奈酚(Ⅵ),大黄酚(Ⅶ),蒙花苷(Ⅷ),金合欢素(Ⅸ),金合欢素-7-O-(6″-O-乙酰基)-β-D-葡萄糖苷(Ⅹ)和金合欢素-7-O-β-D-芦丁糖苷(Ⅺ)。结论其中化合物Ⅹ～Ⅺ为首次从野菊花中分离得到。     

女贞花的化学成分研究

目的 研究女贞花蕾中的化学成分.方法 提取和分离纯化女贞花的化学成分,并通过波谱分析鉴定化合物的结构.结果 从女贞花的丙酮提物中分离出12个化合物,分别是:β-谷甾醇(Ⅰ)、胡萝卜苷(Ⅱ)、麦角甾-7,22-二烯-3β,5α,6β-三醇(Ⅲ)、柚皮素(Ⅳ)、木犀草素(Ⅴ)、芹菜素(Ⅵ)、槲皮素(Ⅶ)、芹菜素7-O-β-...     

水椰的化学成分研究

目的 研究水椰的化学成分,方法利用硅胶柱层析进行分离和纯化,通过渡谱分析鉴定其化学结构.结果 分离到7个甾体及其苷类化合物,鉴定为豆甾醇(stigmasterol,Ⅰ)、谷甾醇(sitosterol,Ⅱ)、β-谷甾酮(β-sitostenone,Ⅲ)、豆甾-4,22-二烯-3-酮(stigmasta-4,22-dien-3-one,Ⅳ)、胡萝卜苷(daucosterol,Ⅴ)、薯蓣皂苷元(diosgenin,Ⅵ)、薯蓣皂苷(diosein,Ⅶ).结论 7个化舍物均为首次从该植物中分离得到.     

藏药多舌飞蓬乙酸乙酯部位的化学成分

目的研究多舌飞蓬Erigeron multiradiatus(W all.)Benth.全草的化学成分。方法运用多种层析分离法分离纯化,采用化学及光谱法进行结构鉴定。结果分离并鉴定的10个化合物分别为β-谷甾醇(Ⅰ)、山奈素(Ⅱ)、芹菜素(Ⅲ)、异鼠李素(Ⅳ)、对羟基苯甲酸(Ⅴ)、1-羟基-2,3,5-三甲氧基酮(Ⅵ)、汉黄芩素(Ⅶ)、槲皮素(Ⅷ)、大黄素(Ⅸ)、3,5-二甲氧基-3,’4:’2,"3"-二氢呋喃并查尔酮(Ⅹ)。结论化合物Ⅰ、Ⅳ、Ⅵ、Ⅶ、Ⅸ、Ⅹ为首次从此种植物中分离得到。     

牛大力的化学成分研究

目的 研究牛大力Millettia speciosa Champ.的化学成分.方法 对牛大力的乙醇提取物进行色谱分离,用波谱方法和理化性质鉴定各化合物的结构.结果 分离得到14个化合物,分别鉴定为3β,11α-二羟基-6(7),12(13)-二烯-乌苏烷(Ⅰ)、3β,11α-二羟基-12(13)-烯-乌苏烷(Ⅱ)、异甘草素(Ⅲ)、美迪紫檀素(Ⅳ)、2',4,4',α-四羟基二氢查耳酮(Ⅴ)、2',4-二羟基-4'-甲氧基查耳酮(Ⅵ)、高丽槐素(Ⅶ)、3',4'-二羟基-7-甲氧基异黄酮(Ⅷ)、4-羟基-2',4-二甲氧基查耳酮(Ⅸ)、2',4',α-三羟基-4-甲氧基二氢查耳酮(Ⅹ)、毛蕊异黄酮(Ⅺ)、8-hydroxypinoresinol(Ⅻ)、甘草异黄醇(Ⅻ)、3',4',7-三羟基异黄酮(ⅩⅣ).结论 除化合物Ⅲ、Ⅳ、Ⅶ外,其余11个均为首次从该植物中分离得到.     

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.     

美洲凌霄花的化学成分研究

目的 研究美洲凌霄花的化学成分.方法 利用硅胶柱色谱、Sephadex LH-20凝胶柱色谱、反相柱色谱等手段对美洲凌霄花70％乙醇提物进行分离纯化,并通过理化性质和光谱数据鉴定其结构.结果 从美洲凌霄花中分离得到11个化合物,分别为棕榈酸(Ⅰ)、十九烷酸(Ⅱ)、β-谷甾醇(Ⅲ)、鼠李柠檬素(Ⅳ)、芹菜素(Ⅴ)、柯伊利素(Ⅵ)、反式对羟基桂皮酸(Ⅶ)、咖啡酸(Ⅷ)、3-羟基-4-甲氧基-苯甲酸(Ⅸ)、原儿茶酸(Ⅹ)、胡萝卜苷(Ⅺ).结论 化合物Ⅰ～Ⅺ均首次从该植物分离得到,化合物Ⅰ、Ⅱ、Ⅳ、Ⅵ～Ⅹ为首次从该属植物中分离得到.     

大花红景天的化学成分研究

目的研究景天科大花红景天的根和根茎中的化学成分。方法采用柱色谱法分离纯化,通过光谱数据鉴定其结构。结果从大花红景天的根和根茎乙醇提取物的石油醚部位、乙酸乙酯部位和正丁醇部位中分离得到12个化合物,分别鉴定为大花红天素(Ⅰ)、胡萝卜甾醇(Ⅱ)、草质素-7-氧-α-L-吡喃鼠李糖苷(Ⅲ)、阿魏酸二十八烷醇酯(Ⅳ)、酪醇(Ⅴ)、红景天苷(Ⅵ)、没食子酸(Ⅶ)、β-谷甾醇(Ⅷ)、正二十六烷酸(Ⅸ)、正二十六烷醇(Ⅹ)、正十八烷酸(Ⅺ)和十九烷(Ⅻ)。结论化合物Ⅱ、Ⅳ、Ⅸ、Ⅹ、Ⅺ、Ⅻ为首次从该植物中分离得到。     

蒙古黄芪化学成分的分离鉴定

从蒙古黄芪(Astragalus membranaceus Bge.var.mongholicus(Bge.)Hsiao)乙醇提取物中分离得到10个单体,分别鉴定为棕榈酸(Ⅰ),羽扇醇(Ⅱ),β-谷留醇(Ⅲ),黄芪皂甙Ⅳ(astragaloside Ⅳ,Ⅳ),黄芪异黄烷甙(3S-(—)mucronulatol-7-D-glucopyranoside,Ⅴ),胡萝卜甙(Ⅳ),α-联苯双酯(dimethyl 4,4-dimethoxy-5,6,5′,6′-dimethylenedioxybiphenyl-2,2-dicarboxylate,(Ⅶ),天冬酰胺(Ⅷ),γ-氨基丁酸(Ⅸ),蔗糖(Ⅹ)。其中Ⅰ,Ⅱ和Ⅸ首次由蒙古黄芪巾分得,联苯双酯(Ⅶ)为已知合成物,但在天然药物黄芪中属首次分出,黄芪异黄烷甙(Ⅴ)未见报道。     

鬼箭羽化学成分的研究(Ⅰ)

目的 研究鬼箭羽的化学成分.方法 采用溶剂法和色谱法进行分离纯化,通过理化性质、光谱数据的解析进行结构鉴定.结果 分离并鉴定的9个化合物分别为β-谷甾醇(Ⅰ)、木栓醇(Ⅱ)、木栓酮(Ⅲ)、松萝酸(Ⅳ)、羽扇豆酮(Ⅴ)、白桦脂醇(Ⅵ)、齐墩果酸(Ⅶ)、正二十六烷酸(Ⅷ)和正二十八烷醇(Ⅸ).结论 化合物Ⅴ～Ⅷ均为首次从鬼箭羽中分离获得.     

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.     

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.

     

Lung disease and PKCs

The lung offers a rich opportunity for development of therapeutic strategies focused on isozymes of protein kinase C (PKCs). PKCs are important in many cellular responses in the lung, and existing therapies for pulmonary disorders are inadequate. The lung poses unique challenges as it interfaces with air and blood, contains a pulmonary and systemic circulation, and consists of many cell types. Key structures are bronchial and pulmonary vessels, branching airways, and distal air sacs defined by alveolar walls containing capillaries and interstitial space. The cellular composition of each vessel, airway, and alveolar wall is heterogeneous. Injurious environmental stimuli signal through PKCs and cause a variety of disorders. Edema formation and pulmonary hypertension (PHTN) result from derangements in endothelial, smooth muscle (SM), and/or adventitial fibroblast cell phenotype. Asthma, chronic obstructive pulmonary disease (COPD), and lung cancer are characterized by distinctive pathological changes in airway epithelial, SM, and mucous-generating cells. Acute and chronic pneumonitis and fibrosis occur in the alveolar space and interstitium with type 2 pneumocytes and interstitial fibroblasts/myofibroblasts playing a prominent role. At each site, inflammatory, immune, and vascular progenitor cells contribute to the injury and repair process. Many strategies have been used to investigate PKCs in lung injury. Isolated organ preparations and whole animal studies are powerful approaches especially when genetically engineered mice are used. More analysis of PKC isozymes in normal and diseased human lung tissue and cells is needed to complement this work. Since opposing or counter-regulatory effects of selected PKCs in the same cell or tissue have been found, it may be desirable to target more than one PKC isozyme and potentially in different directions. Because multiple signaling pathways contribute to the key cellular responses important in lung biology, therapeutic strategies targeting PKCs may be more effective if combined with inhibitors of other pathways for additive or synergistic effect. Mechanisms that regulate PKC activity, including phosphorylation and interaction with isozyme-specific binding proteins, are also potential therapeutic targets. Key isotypes of PKC involved in lung pathophysiology are summarized and current and evolving therapeutic approaches to target them are identified.     

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.     

Gender-related symptoms and correlates of alcohol dependence among men and women with a lifetime diagnosis of alcohol use disorders

This study explored gender-related symptoms and correlates of alcohol dependence in a crosssectional study of 150 men and 150 women with a lifetime diagnosis of alcohol use disorders (AUD). Participants were recruited in equal numbers from treatment settings, correctional centres and the general community. Standardized measures were used to determine participants' use of substances, history of psychiatric disorders and psychosocial stress, their sensation seeking and family history of substance use and mental health disorders. Multivariate analyses were used to detect patterns of variables associated with gender and the lifetime severity of AUD. Men had a longer history of severe AUD than women. Women had similar levels of alcohol dependence and medical and psychological sequelae as men, despite 6 fewer years of AUD. More women than men had a history of severe psychosocial stress, severe dependence on other substances and antecedent mental health problems, especially mood and anxiety disorders. There were differences in family history of alcohol-related problems approximating same-gender aggregation. The severity of a lifetime AUD was predicted by its earlier age at onset and the occurrence of other disorders, especially anxiety, among both men and women. The limitations in the generalizability of these findings due to sample idiosyncrasies are discussed.