圆滑番荔枝树皮中的化学成分

目的对番荔枝科植物圆滑番荔枝(Annona glabraLinn.)树皮的化学成分进行分离、鉴定。方法采用硅胶柱、色谱等分离手段;利用理化性质与波谱技术对化合物进行鉴定。结果分得7个化合物,经鉴定为:ent-kauran-16α,17-diol(1),16-αH-ent-kauran-17-oic acid(2),19-hydroxy-16-α(-)-kauran-17-oic acid(3),16-αhydro-19-acetoxy-ent-kauran-17-oic acid(4),liriodenine(5),β-谷甾醇(-βsitosterol,6)和胡萝卜苷(daucosterol,7)。结论化合物26、、7为首次从该植物中分离得到。     

1株红树来源真菌Daldinia eschscholtzii HJ001 的活性次级代谢产物研究

目的 研究1株红树尖瓣海莲来源内生真菌Daldinia eschscholtzii HJ001的次级代谢产物及其生物活性。方法 综合运用硅胶柱层析、Sephadex LH-20凝胶柱层析、半制备HPLC等色谱分离技术对菌株的发酵产物进行分离纯化,通过NMR、MS、旋光等多种现代波谱技术以及与文献数据对照,确定化合物的结构,对化合物进行抗氧化活性和α-葡萄糖苷酶测试。结果 从红树来源内生真菌D. eschscholtzii HJ001中分离得到8个化合物（1~8）,结构分别确定为sulochrin（1）、(4R)-O-methylsclerone（2）、(R)-(-)-mellein methyl ether（3）、helicascolide A（4）、kojic acid（5）、uracil（6）、cyclo（L-4-Hyp-L-pro）（7）、?ethyl β-D-xylopyranoside（8）,除化合物4外,其余化合物均首次从Daldinia属中分离得到。?结论 化合物5显示强的抗氧化活性,IC50值为11.9 μmol·L?1,强于阳性对照Trolox（IC50 = 26.6 μmol·L?1）。     

长柱金丝桃的化学成分研究

目的研究长柱金丝桃的化学成分。方法利用硅胶柱色谱、高效液相色谱等技术对长柱金丝桃甲醇提取物进行分离纯化,通过波谱数据分析鉴定其化学结构,利用噻唑蓝(MTT)法测试化合物抗肿瘤活性。结果从长柱金丝桃中共分离出10个化合物,均无抗肿瘤活性,分别鉴定为:isodauc-6-ene-10β,14-diol(1)、10-oxoisodauc-3-en-15-al(2)、10β-hydroxyisodauc-6-en-14-al(3)、artabotrol(4)、saniculamoid B(5)、1β-6α-dihydroxy-4(15)endesmene(6)、5-epi-eudesm-4(15)-eno-1β,6β-diol(7)、15-hydroxu-T-muurolol(8)、oplopanone(9)、larixol(10)。结论化合物1~10均为首次从该属植物中分离得到。     

一株红树内生真菌Phomopsis sp. MGF222次级代谢产物及其活性研究

目的 研究一株红树植物木果楝（Xylocarpus granatum Koenig）来源内生真菌Phomopsis sp. MGF222的次级代谢产物及其生物活性。方法 利用硅胶柱层析、Sephadex LH-20凝胶柱层析、半制备HPLC等色谱分离方法，对该菌发酵产物的乙酸乙酯浸膏的次级代谢产物进行分离纯化；综合利用NMR、MS等波谱解析方法以及与文献数据对照，鉴定化合物的结构；并对化合物进行抗菌和α-葡萄糖苷酶抑制活性评价。结果 从内生真菌Phomopsis sp. MGF222中分离鉴定9个化合物(1~9)，结构分别为12-epicitreoisocoumarinol (1)，5-hydroxy-7methoxy-4methylphthalide (2)，5-hydroxy-7-methoxy-4,6-dimethylphthalide (3)，(2-(2"-hydroxypropyl)-5-methyl-7-hydroxychromone (4)，tyrosol (5)，2-hydroxy-benzaldehyde (6)，5-hydroxymethyl-pyrrole-2-carbaldehyde (7)，(2S,2"R,3R,4E,8E,3"E)-2-(2"-hydroxy-3"-octadecenoylamino)-9-methyl-4,8-octadecadiene-l,3-diol (8)，(22E,24S)-5,8-epidioxy-24-methyl-cholesta-6,9(11),22-trien-3-ol (9)；其中化合物9对白色念珠菌Canidia albicans显示抗菌活性；化合物2, 5和8具有α-葡萄糖苷酶抑制活性。结论 发现1个具有抗菌活性和3个具有α-葡萄糖苷酶抑制活性的化合物，具有重要的研究和应用价值。     

圆滑番荔枝的化学成分研究

目的从番荔枝科植物圆滑番荔枝(annona glabra linn)树皮中分离其化学成分并进行成分分析.方法采用柱层析和红外、核磁共振、质谱仪等进行结构分析.结果分离到6个化合物,其中5个为贝壳杉烷型二萜,1个为生物碱.根据理化性质和波谱特征鉴定其为萜Ⅰ、Ⅱ分别为ent-19-carbomethoxykauran-17-oic acid、19-hydroxy-16α-(-)-kauran-17-oic acid,生物碱Ⅰ、Ⅱ分别为liriodenine、oxoglaucine.结论其中萜Ⅰ ent-19-carbomethoxykauran-17-oic acid、萜Ⅱ19-hydroxy-16α-(一)-kauran-17-oic acid和生物碱Ⅱoxoglaucine为首次从该植物中分得.     

一株红树内生真菌Penicillium sp. JY246次级代谢产物及其活性研究

目的 研究一株红树角果木来源内生真菌Penicillium sp. JY246的次级代谢产物及其生物活性。方法 利用硅胶柱层析、Sephadex LH-20凝胶柱层析、半制备HPLC等方法,对该菌发酵产物的乙酸乙酯浸膏进行分离纯化;利用NMR、MS等波谱解析方法以及与文献数据对照,鉴定化合物的结构;通过抗菌和抗虫活性模型对化合物的生物活性进行评价。结果 从内生真菌Penicillium sp. JY246中分离得到12个化合物,分别为7-hydroxy-2-(2-hydroxypropyl)-5-methylchromone (1),(2′S)-2-(propan-2′-ol)-5-hydroxy-benzopyran-4-one (2),2, 3-dihydro-5-hydroxy-2(S)-methyl-4H-1-benzopyran-4-one (3),(11S)-diaprothin (4),questin (5),4-hydroxy-3-prenylbenzoic acid (6),4-methoxy-6-styryl-pyran-2-one (7),(R) 4-hydroxy-2-oxo-1-pyrrolidineacetamide (8),p-hydroxy-benzaldehyde (9),4-hydroxyacetophenone (10),apocynin (11)和1-(2,6-dihydroxyphenyl) ethan-1-one (12)。结论 从内生真菌Penicillium sp. JY246的次级代谢产物中分离得到12个单体化合物,并对所有化合物进行抗菌和抗虫活性测试。结果表明,化合物1, 2, 4和5显示抗细菌活性;化合物4, 5和8对棉铃虫幼虫显示了生长抑制活性。     

紫丁香叶三萜类化学成分研究

目的研究木犀科丁香属植物紫丁香(Syringa oblata Lindl.)叶的化学成分。方法利用硅胶柱色谱法、Sephadex LH-20凝胶柱色谱法、中压柱层析及半制备高效液相色谱等方法分离纯化;通过核磁共振谱、质谱等光谱数据鉴定化合物结构。结果分离得到8个三萜类化合物,分别鉴定为Maslinic acid(1),3β-O-trans-p-coumaroyl maslinic acid(2),3β-O-cis-p-coumaroyl maslinic acid(3),2α-Hydroxy ursolic acid(4),3β-O-trans-p-coumaroyloxy-2α-hydroxyurs-12-en-28-oic acid(5),3β-O-cis-p-coumaroyloxy-2α-hydroxyurs-12-en-28-oic acid(6),3β-O-trans-p-coumaroyl tormentic acid(7),3β-O-cis-p-coumaroyl tormentic acid(8)。结论化合物1～8均为首次从丁香属植物中分离得到。     

中国南海侧扁软柳珊瑚Subergorgia suberosa次级代谢产物

目的研究中国南海侧扁软柳珊瑚Subergorgia suberosa的次级代谢产物。方法利用硅胶柱层析、Sephadex LH-20凝胶柱层析、HPLC等方法对化合物进行分离纯化;利用NMR,MS等波谱方法,并与文献对照,鉴定化合物的结构;利用抗菌活性模型和卤虫致死活性模型评价化合物的生物活性。结果从侧扁软柳珊瑚中分离鉴定了6个单体化合物,分别为:倍半萜化合物subergorgic acid(1),2-β-hydroxysubergorgic acid(2)和2-β-acetoxysubergorgic acid(3);甾体化合物3β-hydroxy-5α-pregnan-20-one(4),5α-pregnane-3,20-di-one(5)和胆甾醇(6)。结论化合物1～3对白色葡萄球菌Staphylococcus albus均显示出较强的抑制活性,化合物4对蜡状芽孢杆菌Bacillus cereus显示出较强的抑制活性,而化合物4和5显示出较强的卤虫致死活性。     

红树植物拟海桑(Sonneratia paracaseolaris)化学成分研究

目的研究红树植物拟海桑Sonneratia paracaseolaris的化学成分。方法利用硅胶柱层析、凝胶Sephadex LH-20柱层析、HPLC等手段对化学成分进行了分离纯化;通过理化性质,结合波谱数据分析并与文献对照,鉴定化合物的结构,分别以MTT和SRB法评价化合物的抗肿瘤活性。结果从红树植物拟海桑Sonneratia paracaseolaris的甲醇提取物中,分离鉴定了9个单体化合物:9-氧橙花叔酮(1),3,7,11-三甲基-1,7(E),10-十二碳三烯-3-羟基-9-酮(2),(22E,24R)-5α,8α-过氧化麦角甾-23-甲基-6,22-二烯-3β-醇(3),(22...     

绿舒筋化学成分研究

目的 分离、鉴定绿舒筋活性化学成分。方法 采用反复硅胶柱色谱和Sephadex LH 20凝胶柱色谱对绿舒筋中化合物进行分离得到单体,应用理化常数测定和现代波谱方法鉴定其化学结构。结果 从绿舒筋中分离并鉴定了6个化合物：雷公藤内酯甲（wilforlide A , I）,雷公藤内酯乙（wilforlide B, II）, 齐墩果-12-烯-3,29-二醇(olean-12-en-3,29-diol, III),3-羟基-2-氧代-无羁萜烯-29-酸(3-hydroxy-2-oxo-3-fridelen-20α-carboxylic acid, IV),3β,22α-二羟基-△12-齐墩果烯-29-羧酸(3β,22α-dihydroxy-olean-12-en-29-oic-acid, V),β-谷甾醇 (β-sitosterol, VI)。结论化合物V为首次从该植物中分离得到。     

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.     

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.