首乌藤的化学成分

目的分离和鉴定首乌藤中的化学成分。方法利用硅胶柱色谱、Sephadex LH-20柱色谱法等进行分离纯化,并通过理化常数测定和光谱分析鉴定了其化学结构。结果分离得到9个化合物,分别鉴定为:大黄素甲醚(physcion,1)、大黄素-8-甲醚(questin,2)、2,5-二甲基-7-羟基色原酮(2,5-dimethyl-7-hydroxychromone,3)、大黄素(emodin,4)、儿茶素(catechin,5)、大黄素甲醚-8-O-β-D-葡萄糖苷(physcion-8-O-β-D-glucopyranoside,6)、决明蒽酮-8-O-β-D-葡糖苷(torachrysone-8-O-β-D-glucopyranoside,7)、大黄素甲醚-8-O-β-D-葡萄糖苷(emodin-8-O-β-D-glucopyranoside,8)、2,3,5,4′-四羟基二苯乙烯-2-O-β-D-葡萄糖苷(2,3,5,4′-tetrahydroxystil-bene-2-O-β-D-glucopyranoside,9)。结论化合物3、7为该种植物中首次分离得到的化合物。     

益肾乌发口服液中二苯乙烯苷、大黄素、大黄素甲醚的含量测定

目的 建立益肾乌发口服液中2,3,5,4'-四羟基二苯乙烯-2-O-β-D-葡萄糖苷、大黄素、大黄素甲醚含量的测定方法,从指标成分角度来探讨益肾乌发口服液毒性与何首乌的关系,并为益肾乌发口服液的质量控制提供方法.方法 采用HPLC法,C18柱(4.6mm×250mm,5μm);测定二苯乙烯苷的流动相为乙腈-水(25:75),检测波长为320hm,流速为1.0 mL·min-1,柱温:25℃;测定大黄素大黄素甲醚的流动相为甲醇-0.1%磷酸溶液(80:20),检测波长为254nm,流速为1.0 mL·min-1,柱温:25℃.结果 二苯乙烯苷在0.1μg～10μg、大黄素在0.0168μg～1.68μg、大黄素甲醚在0.0208～1.04μg范围内呈良好的线性关系,r分别为0.9989(n=8)、0.9984(n=8)、0.9966(n=8);平均回收率:二苯乙烯苷为99.33%,大黄素为99.998%,大黄素甲醚为99.576%;RSD:二苯乙烯苷为0.68%,大黄素为1.11%,大黄素为1.29%.结论 高效液相色谱法测定益肾乌发口服液中二苯乙烯苷、大黄素、大黄素甲醚的含量方法操作简单、灵敏度高、干扰少、重现性好、回收率高,可用于益肾乌发口服液的含量测定.初步证实益肾乌发口服液的毒性可能与君药制何首乌中二苯乙烯苷、大黄素、大黄素甲醚的含量有关,应控制其剂量范围,避免不良反应的发生.     

女贞子中8个化合物对胰岛素抵抗HepG2细胞葡萄糖消耗的影响

目的探讨女贞子中乙酰齐墩果酸、齐墩果酸、19α-羟基-3-乙酰乌索酸、槲皮素、GI3、女贞苷、对羟基苯乙醇-O-β-D-葡萄糖苷、芹菜素-6＇＇-O-乙酰-7-O-β-D-葡萄糖苷对胰岛素抵抗HepG2细胞葡萄糖消耗的影响。方法采用高浓度胰岛素诱导培养HepG2细胞,建立胰岛素抵抗细胞模型,培养液中加入各化合物共同孵育,采用葡萄糖试剂盒检测培养液中的葡萄糖含量。探讨其对胰岛素抵抗HepG2细胞葡萄糖消耗的影响。结果齐墩果酸、19α-羟基-3-乙酰乌索酸、GI3、对羟基苯乙醇-O-β-D-葡萄糖苷、芹菜素-6＇＇-O-乙酰-7-O-β-D-葡萄糖苷在不合胰岛素条件下可使胰岛素抵抗HepG2细胞的葡萄糖消耗量增加11．62％、17．21％、10．54％、12．08％、11.85％,加入生理浓度胰岛素后,上述化合物可使细胞葡萄糖消耗量增加12．95％、13.83％、10．84％、14．26％、17．41％。槲皮素、女贞苷在不含胰岛素条件下不增加细胞的葡萄糖消耗量,加入生理浓度胰岛素后,可使细胞萄萄糖消耗量增加15．70％、17．04％,其中槲皮素促进细胞增殖。结论齐墩果酸、芹菜素-6＇＇-O-乙酰-7-O-β-D-葡萄糖苷等增加胰岛素抵抗HepG2细胞的葡萄糖消耗量呈非胰岛素依赖性,其中芹菜素-6＇＇-O-乙酰-7-O-β-D-葡萄糖苷与生理浓度胰岛素有协同增强作用;女贞苷、槲皮素增加细胞葡萄糖消耗量呈胰岛素依赖性,槲皮素能显著促进细胞增殖。     

HPLC法同时测定固肾安胎丸中7种成分含量

摘要：目的:建立HPLC梯度洗脱法同时测定固肾安胎丸中2,3,5,4’-四羟基二苯乙烯-2-O-β-D-葡萄糖苷、芍药内酯苷、芍药苷、苯甲酰芍药苷、川续断皂苷Ⅵ、续断苷A和续断苷B含量。方法:采用Diamonsil C18色谱柱（250 mm×4.6 mm,5μm）,流动相为乙腈-0.1%磷酸水溶液,梯度洗脱,流速为1.0 ml·min-1,柱温为25℃,检测波长分别为320 nm（2,3,5,4’-四羟基二苯乙烯-2-O-β-D-葡萄糖苷）、230 nm（芍药内酯苷、芍药苷、苯甲酰芍药苷）和212 nm（川续断皂苷Ⅵ、续断苷A和续断苷B）。结果:2,3,5,4’-四羟基二苯乙烯-2-O-β-D-葡萄糖苷、芍药内酯苷、芍药苷、苯甲酰芍药苷、川续断皂苷Ⅵ、续断苷A和续断苷B质量浓度分别在2.98～74.50,5.66～141.50,9.88～247.00,0.89～22.25,10.77～269.25,1.99～49.75,1.06～26.50μg·ml-1范围内线性关系良好（r≥0.999 3）,平均加样回收率分别为97.77%,98.03%,99.22%,98.49%,100.03%,97.86%,96.89%,RSD分别为1.51%,1.11%,0.86%,1.18%,0.67%,1.29%,1.08%（n=9）。结论:该方法操作简便、重复性好,可用于固肾安胎丸中多指标性成分的质量控制。     

益肾养元合剂质量标准研究

目的提高益肾养元合剂的质量标准。方法采用薄层色谱法鉴别金樱子、何首乌、狗脊,用高效液相法鉴定并测定2,3,5,4'-四羟基二苯乙烯-2-O-β-D-葡萄糖苷含量。结果益肾养元合剂采用薄层色谱法鉴别金樱子、何首乌、狗脊可行,高效液相法鉴定并测定2,3,5,4'-四羟基二苯乙烯-2-O-β-D-葡萄糖苷含量的专属性均符合要求,各阴性对照无干扰。结论改良后的检测方法可行。     

空心莲子草中三萜皂苷类化学成分的研究

为了研究苋科植物空心莲子草[Alternanthera philoxeroides(Mart.)Griseb]抗病毒活性的物质基础,对其化学成分进行了研究。本文主要报道从空心莲子草正丁醇部位分离得到的5个三萜皂苷类化合物,经图谱分析,结构分别鉴定为:3-O-β-D-吡喃葡萄糖(1→3)-O-[β-D-吡喃葡萄糖]-齐墩果酸-28-O-β-D-葡萄糖醛酸苷(1)、齐墩果酸-3-O-β-D-吡喃葡萄糖醛酸苷(2)、齐墩果酸-3-O-β-D-吡喃葡萄糖醛酸-28-O-β-D-吡喃葡萄糖苷(竹节参苷Ⅳa,3)、3-O-β-D-吡喃葡萄糖醛酸丁酯-齐墩果酸-28-O-β-D-吡喃葡萄糖苷(4)和3-O-β-D-吡喃葡萄糖醛酸-常春藤皂苷K(尼泊尔常春藤皂苷K,5),其中化合物1为新化合物,化合物4和5为首次从该植物中分离得到。     

超高效液相色谱法测定安乐片中甘草苷和2,3,5,4'-四羟基二苯乙烯-2-O-β-D-葡萄糖苷含量

目的 用UPLC法测定安乐片中甘草苷和2,3,5,4-四羟基二苯乙烯-2-O-β-D-葡萄糖苷含量.方法 色谱柱为Waters BEH C18 (50 mm×2.1 mm×1.7 μm),流动相为乙腈-水(10:90),流速为0.2 mL·min-1,检测波长为280 nm,柱温 20 ℃.结果 甘草苷在133.25～2665 ng与峰面积线性关系良好(r=0.9998),2,3,5,4'-四羟基二苯乙烯-2-O-β-D-葡萄糖苷在127.25～2545 ng与峰面积线性关系良好(r=0.9997),其平均回收率(n=6)分别为99.3% (RSD为1.6%)和96.6% (RSD为1.7%).结论 本法灵敏、准确、专属性强,能简便有效的控制安乐片中甘草苷和2,3,5,4'-四羟基二苯乙烯-2-O-β-D-葡萄糖苷的含量.     

HPLC法测定扶正颗粒中2,3,5,4′-四羟基二苯乙烯-2-O-β-D-葡萄糖苷的含量

目的对扶正颗粒中的主要有效成分2,3,5,4′-四羟基二苯乙烯-2-O-β-D-葡萄糖苷,建立含量测定方法。方法采用高效液相色谱法,测定本制剂中二苯乙烯苷的含量。结果 2,3,5,4′-四羟基二苯乙烯-2-O-β-D-葡萄糖苷的含量测定线性范围在0.026～0.130mg·mL~(-1),平均回收率为99.32%。结论建立的方法准确、稳定、重现性好,可用于该制剂的质量控制。     

牛膝中酸性三萜皂苷成分的分离与鉴定

目的研究中药牛膝中的三萜皂苷类成分.方法采用大孔树脂、硅胶、ODS柱色谱分离纯化,经理化常数、光谱学方法鉴定结构.结果分离得到了6个化合物,鉴定了其中的两个,结构分别为3-O-[2′-O-β-D-吡喃葡萄糖基-3′-O-(2″-羟基-1″-羧乙氧基羧丙基)]-β-D-葡萄糖醛酸基齐墩果酸-28-O-β-D-吡喃葡萄糖苷(牛膝皂苷Ⅰ)和齐墩果酸3-O-[3′-O-(2″-羟基-1″-羧乙氧基羧丙基)]-β-D-葡萄糖醛酸苷(牛膝皂苷Ⅱ).结论牛膝皂苷Ⅰ和Ⅱ均为首次从牛膝中得到.     

何首乌中芪合酶基因的克隆、鉴定及其功能分析

2,3,5,4’-四羟基二苯乙烯-2-O-β-D-葡萄糖苷(2,3,5,4’-tetrahydroxy-stilbene-2-O-β-D-glucoside,TSG),简称二苯乙烯苷,是我国传统大宗中药材何首乌特有的药效成分,具有抗氧化、清除自由基等功效。二苯乙烯苷属于芪类次生代谢     

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.