复方矮地茶片定性定量方法研究

目的建立复方矮地茶片的定性定量方法。方法采用高效液相色谱法对制剂中矮地茶药材中的岩白菜素进行定量分析,同时对矮地茶进行显微鉴定,对矮地茶、野菊花、甘草进行薄层色谱鉴别。结果岩白菜素的平均回收率在96.2%~99.1%,RSD均<1.5%(n=3)。显微鉴别特征明显,薄层图谱斑点清晰,阴性样品无干扰。结论结果准确,方法重复性好,可做为该制剂的质量控制方法。     

柴芩菊感冒软胶囊质量标准研究

目的:建立柴芩菊感冒软胶囊的质量标准.方法:采用薄层色谱法鉴别柴芩菊感冒软胶囊中柴胡、青蒿、野菊花及石膏;用高效液相色谱法对制剂中黄芩苷进行定量分析.结果:平均回收率为98.6%,RSD=1.9%(n=6).结论:所建立之方法可靠、准确、专属性强,可有效控制柴芩菊感冒软胶囊的质量.     

感冒灵颗粒薄层鉴别和含量测定方法的研究

目的:为完善感冒灵颗粒的质量控制方法.方法:采用薄层鉴别和高效液相色谱法,增订了咖啡因、野菊花的薄层鉴别,修订了对乙酰氨基酚的含量测定.结果:通过方法学考察,对乙酰氨基酚的进样量在0.1441μg～1.1532μg范围内,呈良好的线性关系.对乙酰氨基酚的平均回收率(n=5)为99.80%,RSD为0.25%.结论:薄层鉴别,方法专属、斑点清晰;含量测定方法,简便、灵敏、重现性好、精密度高.可有效控制感冒灵颗粒剂的质量.     

消疝合剂质量标准研究

目的 建立中药制剂消疝合剂的质量标准.方法 采用薄层色谱法对消疝合剂中苦参、当归、延胡索、野菊花等进行定性鉴别;采用高效液相色谱法测定苦参碱的含量.色谱柱:NUCLEOSIL-NH2柱;流动相:乙腈-无水乙醇-3%磷酸溶液(82∶10∶8);检测波长为220 nm;流速:1.0 ml/min;柱温:30℃.结果 定性鉴别薄层色谱斑点清晰,阴性对照均无干扰;苦参碱在0.080 4～0.804 0 μg范围内呈良好的线性关系,r=0.999 2,平均加样回收率为97.76%,RSD为1.45%(n=6).结论 该方法简便、准确、可靠,可作为消疝合剂的质量控制方法.     

苦参洗液的薄层色谱鉴别

目的 探讨苦参洗液的薄层色谱鉴别方法,建立苦参洗液的质量标准.方法 采用薄层色谱法对苦参洗液中苦参、野菊花、大黄3味药材进行鉴别.结果 苦参、野菊花、大黄3味药材薄层色谱斑点清晰、Rf值适宜、分离度好、专属性强.结论 试验建立的薄层鉴别方法简便可行、重复性好,为苦参洗液的院内生产质量控制奠定基础.     

蓝菊抗病毒口服液的质量标准研究

目的 建立蓝菊抗病毒口服液的质量控制方法.方法 分别采用聚酰胺薄膜板对野菊花、硅胶G板对板蓝根、大青叶、重楼进行薄层鉴别;含量测定采用HPLC法,色谱柱:戴安Dionex Acclaim 120 C18柱(4.6 mm×150 mm,5μm);流动相:甲醇-水-冰醋酸(26∶23∶1);柱温:25℃;检测波长为334 nm;流速为1.0 ml·min-1.结果 蓝菊抗病毒口服液中的野菊花、板蓝根、大青叶、重楼的薄层色谱特征明显,阴性对照无干扰;蒙花苷在0.025～ 0.25μg之间线性关系良好,R2=0.9999,平均加样回收率为102.41％(RSD=1.5％,n=6).结论 本鉴别方法具有良好的专属性,重现性,含量测定方法准确,重复性好,可用于该制剂的质量控制.     

防芷鼻炎片的质量标准提高研究

目的建立防芷鼻炎片的质量标准,为2015年版中国药典修订提供数据资料。方法采用薄层色谱法对方中野菊花、防风、苍耳子、白芍进行定性鉴别,建立防芷鼻炎片中蒙花苷含量的HPLC测定方法。结果薄层色谱鉴别专属性强,斑点清晰,蒙花苷与其他成分能达到良好的分离,在0.040 99~0.614 9μg内与峰面积线性关系良好(r=0.999 9,n=5),平均回收率在101.7%~103.5%(n=3)。结论建立的方法简便,所得结果可靠,适用于防芷鼻炎片的质量控制。     

乳泰胶囊质量标准研究

目的研究乳泰胶囊的薄层色谱鉴别和含量测定方法。方法分别采用野黄芩苷、α-香附酮、野菊花为对照鉴别制剂中的半枝莲、香附、野菊花。采用高效液相色谱法测定陈皮、青皮中的有效成分橙皮苷的含量,色谱柱为AgilentTc-C18色谱柱(4.6mm×250mm,5μm),流动相为甲醇-0.025mol/L磷酸溶液(20:80),流速为1.0mL/min,检测波长为283nm,柱温为30℃。结果薄层色谱方法专属性强。橙皮苷线性范围为1.00～8.02μg(r=0.9996),平均回收率为99.06%,RSD为1.15%(n=9)。结论所建立的方法准确,能科学评价乳泰胶囊的质量。     

三黄软膏质量标准研究

目的 建立三黄软膏质量控制方法.方法 用薄层色谱法对其中黄柏进行定性鉴别,用高效液相色谱法测定其中姜黄的含量.结果 薄层色谱鉴别方法有良好的重现性、专属性,姜黄在浓度线性范围是7.5～120μg/mL,r=0.999 6,平均回收率为96.10%,RSD=1.67%（n=5）.结论 该方法简便、准确,可作为该制剂的质量控制方法.     

HPLC法测定野菊花注射液中绿原酸的含量

目的建立野菊花注射液中绿原酸的含量测定方法。方法用HPLC法,分析色谱柱为ODS(150mm×4.6mm,5μm),流动相为甲醇-0.1mol/L磷酸二氢钠溶液(23:77)为流动相;检测波长327nm。结果精密度试验(n=6)RSD为0.55%,重现性实验(n=6)RSD为2.12%;平均回收率(n=6)为:92.23%,RSD=1.54%。三批野菊花注射液中绿原酸的含量为175.02￣188.58μg.ml-1。结论该法简单,可靠,可用来测定野菊花注射液中绿原酸的含量。     

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.     

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.