RP-HPLC法测定脉舒胶囊中木犀草素的含量

目的建立脉舒胶囊中木犀草素的含量测定方法并确定其限度。方法以木犀草素为对照品，以ODS-C18柱为分析柱，以甲醇-0．4％磷酸溶液为流动相，紫外检测波长为350nm的反相高效液相色谱法测定木犀草素含量。结果木犀草素进样量在0．033～1．04μg范围内线性良好，r=0．9998；平均加样回收率为100．5％，RSD为1．2％；每粒脉舒胶囊的木犀草素含量在4．37～4．93mg之间。结论本研究提出的含量测定方法准确稳定、简便易行，经方法学验证符合要求。木犀草素含量限度确定为不得少于4．0mg每粒胶囊。     

HPLC法测定苦碟子注射液中木犀草素的含量

目的：采用HPLC法测定苦碟子注射液中木犀草素的含量。方法：采用Kromasil—c18（250mm×4．6mm,5μm）色谱柱,乙腈-0．4％磷酸水溶液（25：75）为流动相,流速为0．8ml·min-1,柱温：30℃,检测波长为350nm。结果：木犀草素在1．1～13．2μg·ml-1浓度范围内线性关系良好（r=0．9998）,平均加样回收率为98．76％,RSD为0．98％。结论：本方法简便准确,重复性好,可用于苦碟子注射液中木犀草素的含量测定。     

银黄胶囊中木犀草苷的含量测定

目的建立银黄胶囊中木犀草苷的含量测定方法。方法以PhenomenexC18（250nm×4．6mm,5μm）为色谱柱,乙腈-0．5％冰醋酸为流动相,进行梯度洗脱,流速为1．0ml·min-1,检测波长为315nm,柱温为30％。结果木犀草苷在0．20～1．23μg范围内线性关系良好（r=-0．9999）,方法回收率为98．56％,RSD=1．22％．结论方法简便、准确,可用于银黄胶囊中木犀草苷的含量测定。     

高效液相色谱法测定北刘寄奴中木犀草素的含量

目的建立测定不同产地北刘寄奴中木犀草素的HPLC方法。方法Shim-pack CLC-ODS C18柱（200mm×4．6mm,5μm）,流动相：甲醇-0．4％磷酸溶液（50：50）;流速：1．0mL·min^-1;检测波长：350nm;柱温：35℃。结果北刘寄奴中木犀草素的回收率为99．8％,木犀草素含量在2．02-20．17μg·mL^-1与峰面积呈良好的线性关系。结论该方法简便、灵敏,可作为北刘寄奴中木犀草素的定量分析方法。     

高效液相色谱法测定金银花中绿原酸和木犀草苷的含量

目的：建立高效液相色谱（HPLC）法测定金银花中绿原酸和木犀草苷的含量。方法：流动相：0．5％冰乙酸-乙腈,线性梯度洗脱：0—20min（90：10—78：22）,20～35min（78：22～76：24）,35—37min（76：24～65：35）,37—40min（65：35—90：10）;流速：1．0ml／min;检测波长：绿原酸为326nm,木犀草苷为350nm;柱温：30℃;色谱柱：依利特HypersilODS2（4．6mm×250mm,5μm）;进样量：10μl。结果：绿原酸的质量浓度在0．0216～0．1080mg／ml内与峰面积具有良好的线性关系,回归方程为Y=26347606．4815X-76704．9000（R^2=0．9990）。木犀草苷的质量浓度在0．000416—0．002080mg／ml内与峰面积具有良好的线性关系,回归方程为Y=28566947．1154X＋22．1500（R^2=0．9991）。70％甲醇超声提取方法较好,金银花提取物中绿原酸和木犀草苷的含量分别为3．416％和0．124％,这2种成分在24h内稳定性良好。结论：该方法简便、准确、快速易行,且该色谱条件可测定金银花中2种成分的含量。     

HPLC法测定夜香牛中木犀草素的含量

目的：建立夜香牛中木犀草素的含量测定HPLC方法。方法：色谱柱为Agilent C18（150mm×4．6mm,5μm）,甲醇-0．2％磷酸溶液（44：56）为流动相,流速1．0ml·min^-1,检测波长350m。结果：木犀草素在0．93～9．27μg·ml^-1（r=0．9998）范围内呈良好线性关系,平均回收率为99．2％,RSD=1．7％（n=6）。结论：方法简便,准确,重复性好。可有效地控制夜香牛的质量。     

金银花中木犀草苷的含量测定

目的：建立测定金银花中木犀草苷含量的HPLC法。方法：采用Phenomenex Luna C8色谱柱（250mm×4．6mm，5μm），以0．4％磷酸溶液-四氢呋喃-甲醇（79：11：10）为流动相；流速：1mL·min^-1；检测波长为350nm。结果：木犀草苷进样量在0．86—427．4μg的范围内线性良好，r=0．9999；供试品溶液在24h内稳定，日内精密度良好（RSD=1．2％）；平均回收率（n=9）为100．1％。结论：所建立的方法专属性强，精密度好，结果准确。     

裸花紫珠总黄酮中槲皮素、木犀草素和阿亚黄素含量测定

目的：建立裸花紫珠总黄酮中木犀草素、槲皮素和阿亚黄素的含量测定方法。方法：色谱柱：DIONEX Acclaim 120 C18柱（250mm×4．6mm,5μm）;以甲醇-水-冰醋酸（68：32：0．8）为流动相A;以甲醇-水-冰醋酸（100：2：0．8）为流动相B,线性梯度洗脱;流速：1．0ml·min^-1,检测波长为356nm。结果：木犀草素、槲皮素和阿亚黄素分别在19．2～96．0、22．3～111．6和24．8～124．0 μg·ml^-1的范围内线性关系良好（r=1．0000）;回收率分别为98．5％,98．8％和98．0％。结论：本方法简便,快捷,准确,可用于裸花紫珠总黄酮中木犀草素、槲皮素和阿亚黄素的含量测定。     

RP-HPLC同时测定神农香菊中绿原酸和木犀草素的含量

目的：建立同时测定神农香菊中绿原酸和木犀草素含量的方法。方法：采用RP-HPLC法,色谱柱为Kromasil-C18（250mm×4．6mm,5μm）,流动相为甲醇（A）-乙腈（B）-0．8％磷酸溶液（C）,进行梯度洗脱,流速为0．5ml·min^-1,柱温30℃,检测波长为328nm。结果：绿原酸和木犀草素分别在4．5～90．0μg·ml^-1（r=0．9993）和10．5-210．0μg·ml^-1（r=0．9996）浓度范围内均有良好的线性关系,平均加样回收率分别为98．72％,97．77％。结论：本方法简便,快速,准确,重复性好,可用于神农香菊药材的质量控制。     

高效液相色谱-二极管阵列法测定鄂西北产白毛夏枯草中木犀草素的含量

目的：采用HPLC-DAD法测定白毛夏枯草中木犀草素的含量。方法：采用ZOBAXSB-C18（4．6mm×150mm，5μm），以甲醇-0．8%磷酸溶液（45：55）作为流动相，流速为0．8mL^-1·min，柱温：30℃，检测波长为350nm。结果：木犀草素在1．06～10．6mg·L^-1,范围内有良好的线性关系，平均加样回收率为98．44％，RSD为1．10％。结论：本方法简便准确，重复性好，可用于白毛夏枯草中木犀草素的含量测定。     

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.