不同产地和品种天麻的HPLC指纹图谱研究

目的 研究不同产地和不同品种天麻的HPLC指纹图谱.方法 色谱柱为Diamonil C18柱(250mm×4.6 mm,5μm),流动相为甲醇-0.1％磷酸水溶液,梯度洗脱,检测波长220 nm,流速1 mL·min-1,柱温35℃.对20批天麻样品的HPLC指纹图谱进行相似度评价和聚类分析.结果 确立了13个共有峰,建立了天麻药材HPLC指纹图谱共有峰模式.20批不同产地和品种天麻的相似度为0.829 ～1.000,综合评判得分为-0.77～1.07.结论 建立的HPLC指纹图谱反映了天麻药材中的化学成分信息,同一产地天麻的化学成分趋同,而不同产地的天麻差异较大,表明产地因素对其化学成分的影响较大.     

广西产赪桐的HPLC指纹图谱研究

目的 研究广西产赪桐的HPLC指纹图谱.方法 采用Hypersil C18色谱柱(250 mm ×4.6 mm,5μm),流动相为0.1％磷酸-甲醇,梯度洗脱,检测波长320 nm,柱温25℃,流速1.0 mL· min-1;将色谱图导入《中药色谱指纹图谱相似度评价系统(2004A版)》软件中,生成对照图谱,并进行相似度评价和聚类分析.结果 建立了含12个共有峰的赪桐特征指纹图谱,不同产地赪桐特征图谱的相似度均＞0.9.结论 所建指纹图谱反映了同一产地赪桐中化学成分的趋同,可用于赪桐药材的质量控制.     

龙眼叶乙酸乙酯部位的HPLC指纹图谱研究

目的建立不同产地龙眼叶药材乙酸乙酯部位的HPLC指纹图谱,并进行聚类分析和主成分分析。方法采用Thermo C18(4. 6 mm×150 mm,5μm)色谱柱,甲醇-0. 2%磷酸水溶液为流动相梯度洗脱,流速1. 0 mL·min-1,柱温30℃,检测波长280 nm。结果提取12个色谱峰为药材指纹图谱共有峰,采用对照品指认了3个主要色谱峰,其中以对照品没食子酸乙酯为参照峰,运用相似度评价软件、聚类分析和主成分分析对所收集的10个不同产地龙眼叶药材乙酸乙酯部位进行系统比较与归类,10个产地龙眼叶药材相似度均大于0. 9,分别聚为4类。结论建立的指纹图谱方法重复性好,简便可靠,为不同产地地龙眼叶药材质量控制和评价提供依据。     

鸦胆子药材水溶性成分的HPLC指纹图谱检测方法

目的建立鸦胆子药材水溶性成分指纹图谱检测方法。方法采用汉邦BDS-C18色谱柱(250 mm×4.6 mm,5μm),用反相色谱法进行分离,以乙腈-磷酸水溶液(pH 3.0)进行线性梯度洗脱,检测波长:280 nm,柱温:40℃,进样量:10μL。以没食子酸峰作为内参照峰。结果测定20批不同产地的鸦胆子药材,共标定11个共有峰。通过中药色谱指纹图谱相似度评价系统(2009年版)进行评价,20批鸦胆子药材水溶性指纹图谱之间相似度均在0.95以上。易伪品女贞子水溶性成分与鸦胆子水溶性成分共有模式相似度为0.562。结论建立的指纹图谱检测方法可为鉴别鸦胆子药材真伪和药材质量控制提供试验依据。     

黔产钩藤HPLC指纹图谱的研究

目的收集贵州十个不同产地的钩藤药材为样品,建立钩藤药材高效液相色谱(HPLC)指纹图谱,以便更全面地评价黔产钩藤药材的内在品质,为黔产钩藤药材的质量控制提供客观依据。方法色谱柱为Kamsial C18色谱柱(4.6×250mm,5μm),流动相为甲醇-0.05%氨水的梯度洗脱,流速为1.0mL/min,紫外检测波长为245nm。结果将16个样品色谱峰作为钩藤特征色谱峰,运用中国药典委员会推荐使用的"中药色谱指纹图谱相似度评价软件"对指纹图谱的相似度进行评价,十批样品的相似度在0.880~0.9960之间。结论 90%药材指纹图谱与共有模式相似度在0.9以上,所建立的HPLC指纹图谱共有模式可作为钩藤药材质量综合评价的参考方法。     

不同产地山楂叶HPLC指纹图谱比较分析

目的 建立不同产地的山楂叶50％乙醇提取物的HPLC指纹图谱,并对其中5种主要成分进行含量测定,结合聚类分析评价不同产地的山楂叶药材质量.方法 采用Diamonsil C18(4.6 mm×250 mm,5μm)色谱柱;以乙腈-0.1％冰醋酸-四氢呋喃体系梯度洗脱;检测波长320 nm;流速0.9 mL·min-1;柱温30℃;应用中药色谱指纹图谱相似度评价系统建立HPLC指纹图谱进行评价,用SPSS 19.0统计软件进行聚类分析.结果 标定出山楂叶HPLC指纹图谱共有峰7个,相似度0.09～0.90;聚类分析后,可以区分不同产地山楂叶,最终以19批主产地的山楂叶为样本,重新建立山楂叶50％乙醇提取物HPLC指纹图谱,标定出共有峰11个,相似度均大于0.85;对25批山楂叶提取物5种主要成分进行含量测定,结果显示主产区山楂叶的质量比较稳定.结论 建立的山楂叶HPLC指纹图谱重现性和特征性较好,能够快速鉴别山楂叶.应用SPSS 19.0聚类分析软件,可以较全面的反映不同产地山楂叶化学成分的差异,为其质量控制提供实验依据.     

高效液相色谱-二极管阵列检测法指纹图谱和聚类分析用于黄芪质量评价

目的 建立黄芪及相关药材的高效液相色谱-二极管阵列检测法(HPLC-DAD)色谱指纹图谱,采用相似度计算和聚类分析的方法评价药材质量.方法 色谱柱:Agilent Zorbax SB C18柱(4.6 mm×250.0 mm,5.0 μm);流动相为A相为乙腈-甲醇(体积比9∶1),B相为水,梯度洗脱,流速1.0 ml/min,柱温25℃,检测波长260 nm,进样量20 μl.进行方法学考察,并进行相似度计算和聚类分析.结果 黄芪药材HPLC-DAD色谱指纹图谱的稳定性、精密度和重复性良好,可以标定11个共有峰,黄芪药材相似度计算结果均大于0.85,聚类分析结果与其一致.结论 相似度计算和聚类分析方法均可以有效区分黄芪药材及其相关样品,使指纹图谱具有广泛的实用性和应用前景.     

秦皮药材HPLC指纹图谱研究

目的采用高效液相色谱法建立中药药材秦皮的指纹图谱,为秦皮药材科学的质量控制提供参考依据。方法采用Inertsil C_(18)色谱柱(250 mm×4.6 mm,5μm),以体积分数0.1%甲酸水-甲醇溶液为流动相进行梯度洗脱,流速为0.8 mL·min~(-1),检测波长为254 nm,柱温30℃;建立秦皮药材指纹图谱,运用中国药典委员会"中药色谱指纹图谱相似度评价系统软件"对10批秦皮药材进行相似度评价,并对其中四个色谱峰进行指认,对10批不同来源秦皮药材进行聚类分析。结果 10批秦皮药材指纹图谱中标定了18个共有色谱峰,相似度值均在0.9以上。结论该法所建立的指纹图谱方法精密、重复性好、稳定性强,对提高秦皮药材的整体质量控制提供参考依据。     

蒙药山川柳的HPLC指纹图谱建立、相似度评价和聚类分析

目的:建立蒙药山川柳的高效液相色谱(HPLC)指纹图谱,并进行相似度评价和聚类分析。方法:采用HPLC法,色谱柱为Agilent ODS C_(18),流速为1.0 m L/min,流动相为甲醇-水(梯度洗脱),检测波长为335 nm,柱温为30℃,进样量为10μL。以槲皮素峰为参照,生成10批药材样品的HPLC指纹图谱;采用《中药色谱指纹图谱相似度评价系统》(2004 A版)进行相似度评价,确定共有峰;采用SPSS 17.0软件对10批药材样品进行聚类分析。结果:10批药材样品的HPLC指纹图谱有13个共有峰,相似度大于0.95,并指认了槲皮素和山柰酚这2个共有峰。聚类分析结果显示,10批药材样品可聚为两类,S8聚为一类,其余批次聚为一类。结论:所建HPLC指纹图谱、相似度评价和聚类分析结果可为山川柳药材的质量控制提供依据。     

广西地不容药材的HPLC指纹图谱研究

目的:建立广西地不容药材的高效液相色谱(HPLC)指纹图谱。方法:采用HPLC法。色谱柱为Hypersil ODS2,流动相为乙腈-0.5%磷酸溶液(梯度洗脱),流速为1.0 m L/min,检测波长为282 nm,柱温为30℃,进样量为10μL。以延胡索乙素为参照,测定10批药材样品的HPLC图谱,采用《中药色谱指纹图谱相似度评价系统》(2012版)进行共有峰指认和相似度评价。结果:10批广西地不容的HPLC图谱有17个共有峰,10批药材样品中有8个产地药材指纹图谱与对照图谱比较相似度>0.900,2个产地药材相似度<0.900。结论:该研究所建HPLC指纹图谱可为广西地不容的鉴别和质量评价提供参考;广西区内多数产地的地不容药材所含生物碱类成分相似,少数存在差异。     

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.     

Nachweis einiger Heilmittel in der Kniegelenksynovialflüssigkeit

Zusammenfassung Mittels Gaschromatographie und Dünschichtchromatographie wiesen die Autoren 11 Substanzen nach, welche durch Injektion oder nach Verabreichung per os in die Kniegelenksynovialflüssigkeit eindrangen. In ihrer Aufstellung konnten sie eine direkte Beziehung zwischen Struktur sowie chemischphysikalischen Eigenschaften der Substanz und ihrer Fähigkeit, aus dem Blut in die Kniegelenksynovialflüssigkeit einzudringen, nicht nachweisen, außer der Tatsache, daß Substanzen mit starker Affinität zu Eiweißstoffen erst in höheren Dosen nachweisbar waren.     

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.     

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.     

Biochemical and molecular characterisation of cubozoan protein toxins

Class Cubozoa includes several species of box jellyfish that are harmful to humans. The venoms of box jellyfish are stored and discharged by nematocysts and contain a variety of bioactive proteins that are cytolytic, cytotoxic, inflammatory or lethal. Although cubozoan venoms generally share similar biological activities, the diverse range and severity of effects caused by different species indicate that their venoms vary in protein composition, activity and potency. To date, few individual venom proteins have been thoroughly characterised, however, accumulating evidence suggests that cubozoan jellyfish produce at least one group of homologous bioactive proteins that are labile, basic, haemolytic and similar in molecular mass (42-46 kDa). The novel box jellyfish toxins are also potentially lethal and the cause of cutaneous pain, inflammation and necrosis, similar to that observed in envenomed humans. Secondary structure analysis and remote protein homology predictions suggest that the box jellyfish toxins may act as α-pore-forming toxins. However, more research is required to elucidate their structures and investigate their mechanism(s) of action. The biological, biochemical and molecular characteristics of cubozoan venoms and their bioactive protein components are reviewed, with particular focus on cubozoan cytolysins and the newly emerging family of box jellyfish toxins.     

Dose tolerability of chronically inhaled voriconazole solution in rodents

Invasive pulmonary aspergillosis (IPA) is a fungal disease of the lung associated with high mortality rates in immunosuppressed patients despite treatment. Targeted drug delivery of aqueous voriconazole solutions has been shown in previous studies to produce high tissue and plasma drug concentrations as well as improved survival in a murine model of IPA. In the present study, rats were exposed to 20 min nebulizations of normal saline (control group) or aerosolized aqueous solutions of voriconazole at 15.625 mg (low dose group) or 31.25 mg (high dose group). Peak voriconazole concentrations in rat lung tissue and plasma after 3 days of twice daily dosing in the high dose group were 0.85 ± 0.63 μg/g wet lung weight and 0.58 ± 0.30 μg/mL, with low dose group lung and plasma concentrations of 0.38 ± 0.01 μg/g wet lung weight and 0.09 ± 0.06 μg/mL, respectively. Trough plasma concentrations were low but demonstrated some drug accumulation over 21 days of inhaled voriconazole administered twice daily. Following multiple inhaled doses, statistically significant but clinically irrelevant abnormalities in laboratory values were observed. Histopathology also revealed an increase in the number of alveolar macrophages but without inflammation or ulceration of the airway, interstitial changes, or edema. Inhaled voriconazole was well tolerated in a rat model of drug inhalation.