黄麦合剂中淫羊藿苷、二苯乙烯苷、金丝桃苷的稳定性考察

摘 要 目的：考察黄麦合剂中淫羊藿苷、二苯乙烯苷、金丝桃苷的稳定性。方法: 以黄芪甲苷、巴戟天药材的TLC鉴别试验,以及淫羊藿苷、二苯乙烯苷、金丝桃苷的HPLC色谱法含量测定为指标,考察黄麦合剂在加速试验及长期试验条件下的稳定性。结果: 在加速试验及长期试验条件下,黄芪甲苷、巴戟天药材以及淫羊藿苷具有良好的稳定性;二苯乙烯苷、金丝桃苷在加速试验、长期试验条件下稳定性差。结论:黄麦合剂各成分中二苯乙烯苷、金丝桃苷稳定性不佳,应尝试改造成固体剂型,以保证稳定性。     

天地精丸质量标准的建立

摘 要 目的：建立天地精丸的质量标准。方法: 显微鉴别天地精丸中的粉碎药材,采用TLC 法对天地精丸中的黄精和女贞子进行薄层鉴别;采用HPLC法测定天麻素的含量。结果: 显微方法能鉴别地龙、石菖蒲特征片断;薄层鉴别分离度好,易于识别。天麻素在19.80～158.40 μg·mL^-1浓度范围内,线性关系良好（r=1.000 0）,平均加样回收率为98.33%,RSD为0.45%（n＝6）。结论:本方法简便、重复性好,可用于天地精丸的质量控制。     

扶正抗瘤丸的质量标准

摘 要 目的： 为提高扶正抗瘤丸的质量,现进一步完善其质量控制标准。方法: 对方中虎杖、丹参、黄芪、当归和川芎5味药进行薄层色谱鉴别,同时采用高效液相色谱法对方中黄芩苷进行含量测定。结果: 薄层色谱中斑点清晰,专属性强;黄芩苷在31~310 μg·mL^-1范围内成良好的线性关系,平均回收率为101.11%（RSD=1.26%,n=9）。结论:本方法简便、准确、可靠、重现性好,可用于扶正抗瘤丸的质量控制。     

Box-Behnken响应面法优化高压蒸法炮制何首乌工艺

摘 要 目的：通过Box-Behnken响应面法优化高压蒸法炮制何首乌工艺,并与传统炮制工艺进行比较。方法: 以蒸制温度、蒸制时间和干燥温度作为考察因素,以多糖含量、二苯乙烯苷含量和两指标归一化值作为评价指标,采用Box-Behnken响应面法考察了各个因素对高压法炮制工艺何首乌中多糖和二苯乙烯苷含量的影响,并比较高压蒸法炮制品与传统炮制品中多糖和二苯乙烯苷含量的差异。结果:高压蒸法炮制何首乌的最佳工艺为：蒸制温度为125.4 ℃、蒸制时间为3.1 h、干燥温度为52 ℃。优化的高压蒸法炮制的何首乌中多糖和二苯乙烯苷含量分别为传统炮制法的1.24和5.26倍。结论:利用Box-Behnken响应面法优化高压法炮制何首乌,方法简便,预测性良好。     

正交试验法优选芪葛颗粒的提取工艺

摘 要 目的：优化芪葛颗粒的提取工艺。方法: 建立芪葛颗粒中黄芪甲苷、葛根素2 种成分测定的HPLC 方法。采用 L9(34)正交设计,以黄芪甲苷、葛根素 2 种成分含量综合评分法进行数据分析,对芪葛颗粒的加水量、提取时间和提取次数3个因素进行优化。结果: 最佳提取工艺为：加入 12倍水,提取3次,每次 30 min。结论: 优选芪葛颗粒提取工艺能较好地保证制剂的质量。     

生化丸质量标准的提高和优化

摘 要 目的：优化生化丸的提取工艺并建立薄层鉴别和高效液相测定有效成分的最佳方法,为定量和定性分析生化丸的质量提供有效手段和可靠依据。方法: 采用TLC法对生化丸中主要药材当归、川芎、甘草进行鉴别;采用HPLC法测定生化丸中阿魏酸的含量,色谱柱：Agilent 5 TC C18(2)（250 mm×4.6 mm,5 μm）;流动相：甲醇 5.0%冰醋酸溶液（25∶75）;检测波长：322 nm;流速：1.0 ml·min-1;柱温：室温。结果: TLC 图谱中可检出当归、川芎、甘草的特征图谱,阿魏酸质量浓度在1.28~20.51 μg·ml-1内线性关系良好,r =0.999 9;平均回收率为98.47%,RSD=0.36% (n= 6)。结论: 采用此种方法,能高效提取生化丸中有效成分,方法可行、准确、重复性好,可用于生化丸的质量控制。     

清热安宫丸质量标准研究

摘 要 目的: 研究完善清热安宫丸的质量标准。方法: 薄层色谱法鉴别制剂中的黄连、黄芩,HPLC法测定制剂中黄芩苷的含量,采用Waters C₁₈色谱柱(250 mm×4.6 mm,5 μm);流动相为甲醇-0.2%磷酸(45∶55),流速为1.0 ml·min^-1;检测波长为315 nm,柱温为30℃,进样量为10 μl。用滴定法测定朱砂的含量。结果:鉴别阴性对照均无干扰;含量测定方法中黄芩苷的线性范围为0.029～0.870 μg（r=0.999 9）,回收率为99.2%（RSD=0.67%,n=6）,朱砂的含量测定平均回收率为100.5％（RSD=0.45%,n=6）。结论:所建方法简单、可靠,可作为清热安宫丸的质量控制标准。     

芪山无糖颗粒剂的提取工艺优化

摘 要 目的：研究芪山无糖颗粒的最佳提取工艺。方法: 应用L9（34）正交设计法对水提取工艺进行优选,以总黄酮、黄芩苷、盐酸小檗碱含量为指标,考察煎煮时间、煎煮次数、加水倍数对提取工艺的影响。结果: 最佳工艺条件为：加水量为10倍药材量,煎煮2次,每次1 h。结论: 优选出芪山无糖颗粒剂的最佳提取工艺,该工艺稳定可行,有效成分含量高。     

Box-Behnken 设计 效应面法优化益安宁丸中尿苷和腺苷的提取工艺

摘 要 目的：采用Box-Behnken 效应面法,优选益安宁丸中尿苷和腺苷的提取工艺。 方法: 以乙甲醇浓度、提取时间、料液比为自变量,以尿苷与腺苷含量的总评“归一值”为因变量,通过对自变量各水平进行多元线性回归及二项式拟合,采用响应面法优选提取工艺,并进行预测分析。 结果: 最佳提取工艺为甲醇浓度76%、提取时间45 min、料液比为2 ml∶43 ml;此条件下尿苷和腺苷含量理论值分别为0.309 0,0.833 0 mg·g-1。 结论: 模型预测值与实验观察值接近,表明采用Box-Behnken响应面法优化后得到的提取工艺参数可用于益安宁丸中尿苷与腺苷的提取。     

添子胶囊的质量标准的建立

摘 要 目的：建立添子胶囊的质量标准。方法: 采用薄层色谱法定性鉴别山茱萸、女贞子及何首乌;采用高效液相色谱法定量测定制剂中二苯乙烯苷的含量。色谱柱：Diamonsil Plus C18色谱柱(250 mm×4.6 mm,5 μm);流动相：乙腈 水（25 ∶〖KG-*2〗75）;检测波长为254 nm;流速：1.0 ml·min-1;进样量：10 μl,柱温：30℃。结果: 山茱萸、女贞子及何首乌与对照品及对照药材在相同位置显同样斑点,阴性对照品在相应位置不显斑点。二苯乙烯苷的线性范围21.12~105.60 μg·ml-1,r=0.999 8,平均回收率为97.95%,RSD=0.61%（n=6）。结论: 本方法简便可靠,可作为添子胶囊质量控制标准。     

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.