毛叶假鹰爪根化学成分的研究

目的：寻找番荔枝科假鹰爪属植物毛叶假鹰爪［Desmos dumosus (Roxb.) Saff］根抗肿瘤活性成分。方法：用硅胶柱色谱分离化学成分;UV,IR,EI-MS,¹HNMR,¹³CNMR,¹H-¹H COSY,HMQC,HMBC,NOESY等方法鉴定结构。结果：从氯仿萃取物中分离鉴定了6个化合物,分别为2-甲氧基-3-甲基-4,6-二羟基-5-(3′-羟基)肉桂酰基苯甲醛(I),5-羟基-7-甲氧基-8-甲酰基-3-苯甲酰基-2,6-二甲基-2S,3R-二氢色原酮(II),豆甾-4-烯-3,6-二酮(III),豆甾烷-3,6-二酮(IV),荠宁黄酮(V),黄芩素-7-甲醚(VI)。结论：化合物II为新化合物,命名为毛叶假鹰爪素A。I,III和IV为首次从本种植物中得到。III有细胞毒活性。     

假鹰爪属植物化学成分和药理活性

假鹰爪属的假鹰爪、毛叶假鹰爪、大叶假鹰爪和云南假鹰爪等植物中含黄酮类、生物碱类、挥发油、有机酸、三萜和植物甾醇等化学成分,并具有抗肿瘤、抗病毒、强心、抑菌等药理活性。总结了近30年来对该属植物的研究概况,为进一步研究提供参考。     

鹰爪叶化学成分研究

从鹰爪 Artabotrys hexapetalus 叶分得5种黄酮:鹰爪甙-A(1),鹰爪甙-B(2),黄杉素(3),木犀草素-7-O-葡萄糖甙(4),芹菜素-7-O-芹糖(1→2)葡萄糖甙(5),以及琥珀酸(6)和富马酸(7)。其中1和2是新的黄酮甙,其他5种成分为第一次从本植物分得。经光谱解析测定了1和2化学结构。     

鹰爪种子的木脂素和半萜化学成分

从药用植物鹰爪种子分得4个木脂素：异洋商陆素A（soamericanin A,1)，异洋商陆醇A（isoamericanol A,2)，洋商陆素B（americainin,B,3),鹰爪木脂醇（atabotrycinol,4)和一个半萜 ：（R）－鹰爪三醇[(R)-arttaboriol,5],以及棕榈酸（6），β谷甾醇（7）和胡萝卜苷（8），根据光谱数据（IR，UV，MS，1D，2D－NMR）分析，确定它们的化学结构，其中，鹰爪木脂醇（4）是一个新木脂素，（R）－鹰爪三醇（5）是一个新半萜醇，木脂素化合物1，2和3是首次从该植物分得。     

鹰爪种子化学成分的研究

目的研究药用植物鹰爪Artabotrys hexapetalus (L.f.)Bhandari的化学成分。方法利用各种色谱技术进行分离纯化,根据化合物的理化性质和光谱数据进行结构鉴定。结果从鹰爪种子分得4种木脂素:异洋商陆素A(isoamericaninA,1)、异洋商陆醇A(isoamericaninolA,2)、洋商陆素B(americaninB,3)、鹰爪木脂醇(artabotrycinol,4),以及(R)-鹰爪三醇［(R)-artabotriol,5］、棕榈酸(6)、β-谷甾醇(7)和胡萝卜苷(8)等。结论鹰爪木脂醇(4)和鹰爪三醇(5)为新化合物,其余3种木脂素为首次从该植物分得。     

假鹰爪根中黄酮成分的分离鉴定

假鹰爪根中黄酮成分的分离鉴定吴久鸿，廖时萱，梁华清，毛士龙（上海第二军医大学药学院植化教研室２００４３３）继前报（１）从假鹰爪（ＤｅｓｍｏｓｃｏｃｈｉｎｃｈｉｎｅｎｓｉｓＬｏｕｒ．）根中分得ｌａｗｉｎａｌ，ｉｓｏｕｎｏｎａｌ和４，７－二羟基－５－甲氧...     

假鹰爪双氢黄酮素Ⅱ：从假鹰爪中获得的新双氢黄酮

从假鹰爪根中分离得到一个新双氢黄酮，根据波谱分析确定其化学结构为7－羟基－5－甲氧基－8－甲酰基－6－甲基双氢黄酮，命名为假鹰爪双氢黄酮素Ⅱ。     

假鹰爪根化学成分的研究

假鹰爪(Desmos cochinensis Lour.)根的石油醚提取物中分得三个黄酮类化合物。其中化合物Ⅰ和Ⅱ分别鉴定为5,7-二羟基-6-甲酰基-8-甲基双氢黄酮(lawinal)和5,7-二羟基-6-甲酰基-8-甲基黄酮(isounonal)。Ⅲ为一含醛基的新化合物。根据光谱分析(紫外、红外、质谱、氢谱、碳谱、二维核磁共振异核位移相关谱及X-单晶衍射)证明其结构为4,7-二羟基-5-甲氧基-6-甲基-8-甲酰基黄烷。化合物Ⅰ和Ⅱ均属首次从该植物中分得。     

鹰爪花属植物化学成分研究进展

本文就鹰爪花属植物的化学成分及相关的药理活性研究进展作一概述。     

Desmosflavanone Ⅱ: A New Flavanone from Desmos cochinchinensis Lour

从假鹰爪根中分离得到一个新双氢黄酮，根据波谱分析确定其化学结构为７羟基５甲氧基８甲酰基６甲基双氢黄酮，命名为假鹰爪双氢黄酮素Ⅱ。     

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.

     

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.     

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.     

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.     

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.