西沙短指软珊瑚Sinularia sp.化学成分研究△

目的研究中国南海西沙群岛短指软珊瑚Sinularia sp.的化学成分。方法 利用薄层色谱,凝胶柱层析,Sephadex LH-20柱层析, MHPLC, HPLC等常规化学分离手段对该属化学成分进行分离纯化;借助NMR、MS等方法,并对照文献,鉴定其次级代谢产物的结构。结果 从短指软珊瑚的甲醇氯仿提取物中,分离鉴定了5个甾醇类化合物：Subergorgol I (1)、9,11-开环-24-亚甲基-5-胆甾-7-烯-3β,6α,11-三羟基-9酮 (2)、7α-hydroxy-crassarosterol A (3)、(22E)-胆甾-7,22-二烯-3β,5α,6β-三醇 (4)、24-亚甲基胆甾醇 (5)。4个环戊烯酮衍生物：Suberosanone B (6)、Suberosanone A (7)、Hydroxydihydrobovolide (8)、Sinularone C (9)。     

西沙短指软珊瑚Sinularia cf. molesta化学成分研究△

目的 研究西沙短指软珊瑚Sinularia cf. molesta的化学成分。方法 利用薄层色谱、硅胶色谱、Sephadex LH-20凝胶色谱、MPLC、HPLC等方法对化学成分进行分离纯化;通过NMR、MS等方法,并结合文献,鉴定化合物的结构。结果 从短指软珊瑚的甲醇粗提物中,分离鉴定了8个单体化合物：(5"Z)-5-(2", 6"-二甲基癸烷-5", 7"-二烯)呋喃-3-羧酸 (1), Norcembrene (2), Norcembrene E (3),(1R, 3S, 4S, 7E, 11E)-3, 4-环氧西松烷-7, 11, 15-三烯 (4), (3E, 7Z, 11Z)-西松烷-2-羰基-3, 7, 11, 15-四烯 (5), clavirolides D (6),β-谷甾醇 (7), 3β-羟基-24-亚甲基胆甾-5-烯-7-酮 (8)。结论 所有化合物(1-8)均为首次从该种分离得到,化合物(5, 6)为第一次从Sinularia属中分离得到。     

西沙短指软珊瑚Sinularia notanda化学成分研究△

目的 研究西沙短指软珊瑚Sinularia notanda的化学成分。方法 利用薄层色谱,硅胶柱色谱、凝胶(Sephadex LH-20)柱色谱、MPLC、HPLC、GC-MS等分析分离方法对Sinularia notanda中的化学成分进行分离纯化,并进一步对NMR、MS等其数据进行分析,同时对照文献鉴定所得化合物的结构。结果 从短指软珊瑚的甲醇提取物中,分离鉴定了11个化合物：顺-5,8,11,14,17-二十碳五烯酸甲酯(1),顺-4,7,10,13,16,19-二十二碳六烯酸甲酯(2),顺-5,8,11,14-二十四碳烯酸甲酯(3),顺-9,12-十八碳二烯酸甲酯(4),laurenisol(5),2,4-二乙基-5-羟基-2-辛烯醛(6),麦角甾-5,24(28)-二烯-3β-醇(7),3β-羟基-麦角甾-5,24(28) –二烯-7-酮(8),(+)-3,4-二甲基-5-羟基-5-戊基呋喃-2(5H)-酮(9),尿嘧啶(10),胸腺嘧啶(11)。     

西瑁岛软珊瑚Dendronephthya sp.的化学成分和生物活性研究

目的 对采自中国南海西瑁岛海域的软珊瑚Dendronephthya sp.的化学成分和抗炎活性研究。方法 综合利用薄层色谱、硅胶柱色谱和凝胶柱层析等分离手段,对纯化的单体成分采用核磁波谱(NMR)和质谱(MS)等方法进行鉴定,结合文献数据比对确定化合物结构;并对化合物进行了抗炎活性测试和细胞毒性实验。结果 从软珊瑚Dendronephthya sp.中共分离鉴定了11个化合物,包括6个甾体化合物,4个嘧啶类化合物及1个醇类化合物：胆固醇(1),胆固醇乙酸脂(2),胆固醇-5α,6α-环氧化物(3),鲨肝醇(4),11-acetoxy-3β,6α-dihydroxy-9,11-seco-5α-cholest-7-en-9-one(5),啤酒甾醇(6),3β,5α,6β-三羟基胆甾烷醇(7),胸腺嘧啶(8),脲嘧啶(9),胸苷(10),脲苷(11)。结论 化合物5和6是首次从该种属中分离得到,其中化合物5对脂多糖诱导的BV-2细胞的炎症反应具有抑制作用。     

中国南海短指软珊瑚Sinularia acuta化学成分研究△

目的 研究短指软珊瑚Sinularia acuta的化学成分。方法 利用薄层色谱、硅胶色谱、Sephadex LH-20凝胶色谱、ODS中低压色谱、半制备HPLC等方法对化学成分进行了分离纯化;通过NMR、MS等方法,并结合文献对照,鉴定化合物的结构。结果 从短指软珊瑚的甲醇提取物中,分离鉴定了13个单体化合物：麦角甾-5, 22, 24(28)-三烯-3β-醇(1)、麦角甾-5, 24(28)-二烯-3β-醇(2)、胆甾-5-烯-3β-醇(3)、(22E)-胆甾-5, 22(23)-二烯-3β-醇(4)、(22E)-3β-羟基胆甾-5, 22(23)-二烯-7-酮(5)、3β-羟基麦角甾-5, 24(28)-二烯-7-酮(6)、(22E)-3β-羟基麦角甾-5, 22(23)-二烯-7-酮(7)、3β-羟基麦角甾-5-烯-7-酮(8)、3β-羟基胆甾-5-烯-7-酮(9)、尿嘧啶(10)、胸腺嘧啶(11)、脱氧胸腺嘧啶核苷(12)、脱氧腺嘌呤核苷(13)。结论 化合物(1-13)均为首次从该种软珊瑚中分离得到。     

西瑁岛软珊瑚Sinularia sp. 的化学成分和生物活性研究

摘要：目的 对采自中国南海西瑁岛的软珊瑚Sinularia sp.的化学成分和生物活性进行研究。方法 综合利用薄层色谱、硅胶柱色谱、凝胶柱层析、半制备HPLC等分离手段,结合NMR和MS等波谱数据分析并对比文献数据,对化合物进行分离鉴定;选用A549和HL-60细胞株,采用CCK-8筛选方法,对化合物进行体外细胞毒活性测试。结果 从软珊瑚Sinularia sp.中共分离鉴定了10个甾体化合物,包括8个孕甾烷及其苷类化合物：3β-羟基-5,20-二烯孕甾烷乙酸酯（1）,20-烯-3-酮孕甾烷（2）,1,20-二烯-3-酮孕甾烷（3）,1,4,20-三烯-3-酮孕甾烷（4）,3β-羟基-20-烯孕甾烷（5）,3β-羟基-5,20-二烯孕甾烷（6）,1,4-二烯-3-酮-20α-羟基孕甾烷乙酸酯（7）,3β-羟基-5,20-二烯孕甾烷吡喃岩藻糖苷（8）;1个麦角甾烷类化合物：(22E,24R)-3β,5α,6β-三羟基-7,22-二烯麦角甾烷（9）和1个胆甾烷类化合物：(20S)-1,4-二烯-3,16-二酮-20β-羟基胆甾烷（10）。结论 化合物1～10对A549细胞株均未表现明显的细胞毒活性,但化合物4和7对HL-60细胞株具有中等的细胞毒活性,其IC50值分别为1.61 和 3.26 μmol/L。     

南海小月柳珊瑚中倍半萜类化学成分研究(英文)

对南海小月柳珊瑚Menellasp.的化学成分进行研究。应用反复硅胶柱层析、Sephadex LH-20柱色谱和制备薄层等多种色谱方法进行分离和纯化。从中分离得到3个subergorane倍半萜和1个suberosane倍半萜化合物,利用波谱分析技术和文献比对等方法确定化合物的结构,分别为柳珊瑚酸(1),柳珊瑚酸甲酯(2),2β-羟基柳珊瑚酸甲酯(3)和suberosenol A(4)。以上化合物均为首次从小月柳珊瑚属(Menella)中分离得到。     

中国南海扁小尖柳珊瑚Muricella sibogae化学成分研究△

目的 研究扁小尖柳珊瑚Muricella sibogae的化学成分。方法 利用硅胶薄层色谱、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;结合化合物理化性质和波谱数据分析,通过文献对照,鉴定化合物的结构。结果 从扁小尖柳珊瑚Muricella sibogae的甲醇提取物中,分离并鉴定了9个单体化合物：(22E)-3β-羟基胆甾-5,22-二烯-7-酮 (1),3β-羟基胆甾-5-烯-7-酮(2),胆甾-5-烯-3β,7α-醇 (3),(22E, 24S)-麦角甾-5, 22-二烯-3β-醇(4),(22E, 24R)-麦角甾-5, 22-二烯-3β-醇 (5),次黄嘌呤核苷 (6),尿嘧啶核苷 (7),顺-5, 8, 11, 14-二十碳四烯酸甲酯 (8),顺-9, 12-十八碳二烯酸甲酯 (9)。其中化合物1-3、6-9为首次从该物种中分离得到。     

中国南海鳞指形软珊瑚的化学成分和生物活性研究

目的 对采自中国南海的鳞指形软珊瑚化学成分和生物活性进行研究。方法 综合利用薄层色谱、硅胶柱色谱、凝胶柱层析、半制备高效液相色谱（HPLC）等分离手段进行纯化,结合核磁共振（NMR）和质谱（MS）等波谱数据分析及比对文献数据,开展化合物的结构鉴定。结果 从鳞指形软珊瑚中共分离鉴定了18个化合物,包括2个倍半萜：(E)-β-金合欢烯（1）和β-榄香烯（2）;6个二萜：xiguscabrate A（3）、19-hydroxylcembrene-C（4）、xiguscabrate B（5）、(11S,12S)-11,12-epoxycembrene-C（6）、sinulariol C（7）和isosarcophytoxide（8）;9个降二萜：10-epi-gyrosanolide E（9）、scabrolide D（10）、scabrolide G（11）、5-epi-sinuleptolide（12）、sinuleptolide（13）、gyrosanolide F（14）、ineleganolide（15）、scabrolide A（16）和scabrolide B（17）;1个甾醇：crassarosterol A（18）。结论 化合物1为首次从软珊瑚科软珊瑚中分离得到,2、9、12、13、15和18为首次从该种软珊瑚中分离得到。抗炎活性测试时,化合物8对脂多糖（LPS）诱导的B淋巴细胞的增殖具有显著的抑制作用（IC50 = 4.4 μmol/L）。     

中国南海软珊瑚Sinularia dissecta的化学成分研究

目的研究中国南海软珊瑚Sinularia dissecta的化学成分。方法运用色谱方法进行化学成分的分离和纯化,运用现代波谱技术鉴定各化学成分的结构,并用MTT法和SRB法测定部分化学成分对6种肿瘤细胞株的细胞毒活性。结果与结论共分离鉴定了11个化学成分,分别为:(1S,4R,2E,7E,11E)-西松烷-2,7,11-三烯-4-醇(1)(、1S,2E,4E,7E,11E)-西松烷-2,4,7,11-四烯(2)、(1R,3S,4S,7E,11E)-3,4-环氧西松烷-7,11,15-三烯(3)、4α-甲基-麦角甾-24-烯-3β-醇(4)、26-甲基-麦角甾-5-烯-3β-醇(5)、麦角甾-5,24-二烯-3β-醇(6)、胆甾-5-烯-3β-醇(7)、鲨肝醇(8)、对羟基苯甲醛(9)、尿嘧啶(10)、胸腺嘧啶脱氧核苷(11)。化合物1对PC-3MIE8人前列腺癌细胞的IC50为2.54μg.mL-1。所有化合物都是首次从该种软珊瑚中分离得到。通过2D-NMR首次对化合物1和4进行了全归属,并论证了其立体构型。     

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.