复方双黄连分散片的质量标准研究

目的建立复方双黄连分散片（金银花、黄芩、连翘、蒲公英等）的质量标准。方法采用TLC法对蒲公英、黄芩苷和绿原酸进行鉴别。用HPLC法测定黄芩苷的含量。结果TLC鉴别方法专属性强。黄芩苷在1．6μg～4．0μg范围内呈良好的线性关系，r=0．9998，加样回收率为99．69％，RSD为0．4％。含量限度黄芩苷为不少于80mg／片。本方法操作简单，结果准确，灵敏度高，重复性好。结论本质量标准可有效地控制复方双黄连分散片的质量。     

高效液相色谱法测定复方鱼腥草口服液中黄芩苷和绿原酸含量

目的建立复方鱼腥草口服液中黄芩苷和绿原酸的含量测定方法。方法采用Shimadzu C18柱（250mm×4．6mm,5μm）,黄芩苷测定以甲醇-水-磷酸（45：55：0．2）为流动相,检测波长为315nm;绿原酸测定以乙腈-0．4％磷酸溶液（13：87）为流动相,检测波长为327nm。结果黄芩苷进样量在0．2654—1．3270μg范围内与峰面积线性关系良好,r=0．99996（n=5）,平均回收率为100．5％,RSD=1．08％（n=6）;绿原酸进样量在0．1072～0．5360μg范围内与峰面积线性关系良好,r=0．99998（n=5）,平均回收率为97．26％,RSD=1．41％（n=6）。结论该方法快速准确、结果可靠。     

高效液相色谱法测定银黄软胶囊中绿原酸和黄芩苷的含量

目的：建立银黄软肢囊含量测定方法。方法：采用HPLC法测定。色谱柱：KromasilC1。柱，流动相：乙腈-0．1％磷酸溶液（梯度洗脱），检测波长：318nm，柱温：35℃。结果：绿原酸在进样量为9．89～988．8I）ng范围内呈良好的线性关系（r=0．999 9）；平均加样回收率为102．38％，RSD为1．82％（n=6）；黄芩苷在进样量为0．04～3．99μg范围内呈良好的线性关系（r=0．9995）；平均加样回收率为97．90％，RSD为1．79％（n=6）。结论：该法操作简便易行、准确可靠，可用于银黄软胶囊的质量控制。     

RP-HPLC法测定银黄胶囊中绿原酸和黄芩苷的含量

目的：测定银黄胶囊中绿原酸和黄芩苷的含量。方法：采用RP-HPLC法，色谱柱为Agilent Extend-C18柱（250mm×4．6mm，5μm），样品用45％甲醇溶解，乙腈-水-磷酸（28：72：0．4）（用三乙胺调pH为2．7±0.1）为流动相，检测波长为280nm测定黄芩苷含量；样品用50％甲醇溶解，0．2mol·L^-1磷酸二氢钠-甲醇（75：25，磷酸调节pH为3．2）为流动相；检测波长为327nm测定绿原酸含量。结果：黄芩苷在0．0392-0．784μg范围内，线性关系良好（r=1．0000），平均回收率为99．5％。方法精密度RSD=0．61％（n=5）；绿原酸在0．0429～0．858μg范围内，线性关系良好（r=1．0000），平均回收率为99．8％；方法精密度RSD=0．71％（n=5）。结论：该方法可用于银黄胶囊质量控制。     

HPLC法测定妇炎康复胶囊中橙皮苷和黄芩苷的含量

目的：建立测定妇炎康复胶囊中橙皮苷和黄芩苷含量的HPLC测定方法。方法：采用Shim—pack VP-ODS柱,乙腈-0．5％磷酸（25：75）为流动相,检测波长为283nm,流速1．0ml·min^-1。结果：橙皮苷在0．13～0．38μg范围内与峰面积呈良好线性关系,r=1．0000,平均加样回收率为99．53％,RSD为1．1％（n=6）;黄芩苷在0．59—1．76μg范围内与峰面积呈良好线性关系,r=1．0000,平均加样回收率为99．55％,RSD为1．3％（n=6）。结论：该方法简便、准确,专属性强,重现性好,可用于妇炎康复胶囊的质量控制。     

高效液相色谱法测定复方银黄胶囊中黄芩苷含量

目的建立高效液相色谱法测定复方银黄胶囊中黄芩苷的含量。方法色谱柱为Diamonsil（钻石）C18（250×4．6mm,5μ）,流动相为甲醇-水-冰醋酸（50：50：1）,检测波长为280nm,流速为1．0ml／min,柱温为30℃。结果黄芩苷进样量在0．0997～1．994μg范围内与峰面积有良好的线性关系,r=0．9999;平均加样回收率为99．82％,RSD=1．13％（n=6）。结论该方法简便、灵敏、结果准确、重复性好,可用于复方银黄胶囊的质量控制。     

热炎清颗粒的质量标准

目的：建立热炎清颗粒的质量标准。方法：采用薄层色谱法（TLC）对本品的黄芩、金银花进行鉴别;采用HPLC法测定本品中黄芩苷的含量。结果：薄层色谱中阴性样品无干扰;黄芩苷在0．18～1．13g（r=0．9997）范围内呈良好线性关系。平均加样回收率为97．9％（RSD=1．87％）。结论：该法简便,准确可靠。     

HPLC法同时测定银翘解毒合剂中栀子苷与黄芩苷的含量

目的：建立银翘解毒合剂中同时测定栀子苷和黄芩苷的HPLC方法。方法：色谱柱：AgilentZORBAXSB—C18（150mm×4．6mm,5μm）,流动相：乙腈-0．5％冰醋酸梯度洗脱,流速：1．0ml·min^-1,检测波长：238nm,柱温：25℃。结果：栀子苷进样量在0．084-1．05μg范围内线性关系良好,回归方程Y=1422．6X＋3．377,r=0．9998（n=5）;黄芩苷进样量在0．23～4．56vg范围内线性关系良好,回归方程Y=1164X＋47．201,r=0．9998（n=5）。平均加样回收率栀子苷为99．65％,RSD=1．44％（n=6）;黄芩苷为100．01％,RSD=0．23％（n=6）。结论：该法快速简便,专属性强,重现性好,能用于银翘解毒合剂的质量控制。     

高效液相色谱法测定小儿清化丸中的绿原酸和芍药苷的含量

目的：测定小儿清降丸中的绿原酸和芍药苷的含量。方法：采用高效液相色谱法,色谱柱为：DiamondC18（250mm×4．6mm,5μm）,流动相均为乙腈-0．4％磷酸水溶液（15：85）;流速均为1．0ml／min。检测波长：绿原酸327nm;芍药苷230nm。柱温：35℃。结果：绿原酸进样量在0．0396-0．5940μg范围内线性关系良好（r=0．9999）,平均回收率为99．50％,RSD为0．68％（n=6）。芍药苷进样量在0．1646-2．4690μg范围内线性关系良好（r=0．9999）,平均回收率为99．32％,RSD为0．72％（n=6）。结论：该方法简便、准确、重复性好,适用于小儿清降丸的质量控制。     

高效液相色谱法测定病毒清颗粒中黄芩苷含量

目的建立测定病毒清颗粒中黄芩苷含量的高效液相色谱（HPLC）法。方法色谱柱为DiamonsilC18（250mm×4．6mm,5μm）,以甲醇-水-冰醋酸（50：50：1）为流动相,检测波长为274nm。结果黄芩苷进样量在0．1034—1．0340μg范围内与峰面积线性关系良好,r=0．9992（n=5）,平均加样回收率为99．30％,RSD为1．79％（n=6）。结论所用方法简便易行、准确、重现性好,可用于病毒清颗粒的质量控制。     

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.