HPLC法测定舒胆颗粒中橙皮苷的含量

目的:建立HPLC法测定舒胆颗粒中橙皮苷的含量.方法:色谱柱为Nova PAK C18 (150mm×3.9mm,4μm),流动相为16%的乙睛水溶液,检测波长为283nm.结果:线性范围为0.606～6.060μg(r=0.999 6),平均回收率为98.99%,RSD为1.80%(n=5).结论:本法简便、灵敏、快速、准确,可作为舒胆颗粒的质量控制方法.     

高效液相色谱法测定肾病Ⅰ号颗粒中牛蒡苷含量

目的:建立肾病Ⅰ号颗粒中牛蒡苷的含量测定方法.方法:采用高效液相色谱法,色谱柱为ProntosilEurobond C18柱(4.6mm×125mm,5μm)流动相为甲醇-水(1:1.1),检测波长为280 nm.结果:牛蒡苷线性范围为2.10～10.51μg(r=0.999 9),平均回收率为99.28%,RSD=0.32%(n=6).结论:高效液相色谱法简便、准确,重现性好,可用于肾病Ⅰ号颗粒的质量控制.     

HPLC测定鼻窦炎颗粒中的栀子苷

目的:采用HPLC法测定鼻窦炎颗粒中的栀子苷.方法:色谱柱为Agilent ZORBAX SB-C18(250 mm×4.6 mm,5μm),流动相为水.乙腈.磷酸(86:14:0.01),检测波长238 am,流速1.0 ml·min-1,柱温30℃.结果:栀子苷浓度3.36～126μg·ml-1,与峰面积的线性关系良好(r=0.999 9),平均加样回收率98.09%,RSD=1.69%.结论:所建方法准确、重复性好,可用于测定鼻窦炎颗粒中的栀子苷.     

HPLC-ELSD法测定盐酸金刚烷胺颗粒中盐酸金刚烷胺的含量

目的:建立HPLC-ELSD法测定盐酸金刚烷胺颗粒中盐酸金刚烷胺的含量。方法:采用C18(4.6 mm×250 mm,5μm)色谱柱,流动相为乙腈-0.06%三氟乙酸溶液(20︰80),流速1.0 mL.min-1,柱温30℃,进样量10μL;检测器为ELSD,漂移管温度55℃,雾化气体为空气,载气流速为2.0 L.min-1。结果:盐酸金刚烷胺的线性浓度范围为80.48～281.68μg.mL-1(r=0.9991);平均回收率(n=9)为100.3%(RSD=0.9%)。结论:本方法较标准方法简便、可靠、准确,适合盐酸金刚烷胺颗粒的质量控制。     

高效液相色谱法检测参鹿胶颗粒中绿原酸的含量

目的:建立高效液相色谱法测定参鹿胶颗粒中绿原酸含量的方法.方法:采用Shim-pack vp-ODS柱(4.6mm×250mm,5μm);流动相为乙腈-0.09%磷酸水溶液(13:87);检测波长327mm;结果:绿原酸在0.092 352～0.461 76μg范围内有良好的线性关系.平均回收率为99.2%(n=6),RSD为1.5%.结论:该方法简便、具有良好的准确性和精密性,重现性良好,结果可靠,可有效地控制参鹿胶颗粒的质量.     

HPLC法测定山茱萸配方颗粒中马钱苷的含量

目的:建立山茱萸配方颗粒中马钱苷的含量测定方法.方法:色谱柱为HangBang C18(200*4.6mm5μm):流动相为乙腈:水(15:85);检测波长240nm;流速1.0ml/min;柱温30℃.结果:马钱苷的检测浓度线性范围为0.005～0.025μg(r=0.9998),RSD=2.16%(n=5);平均加样回收率为98.79%,RSD=1.77%(n=6).结论:本法简便、快捷、准确,可用于山茱萸配方颗粒的含量测定.     

HPLC法测定通脉活络康颗粒中齐墩果酸的含量

目的:研究通脉活络康颗粒中齐墩果酸的HPLC定量分析方法.方法:色谱柱:Kromasil-C18(4.6 mm×150mm,5μm),流动相:甲醇-水(90:10);流速:1ml·min-1,检测波长:220 nm.结果:齐墩果酸在1.26～20.16μg(r=1.0000)呈良好的线性关系,平均回收率为97.6%,RSD为0.8%.结论:本法简便、灵敏、准确,可用于通脉活络康颗粒的质量控制.     

高效液相色谱法测定苦参配方颗粒中苦参碱含量

目的:建立苦参配方颗粒中苦参碱的含量测定方法.方法:色谱柱为HangBang C18柱(200mm×4.6 mm,5 μm),流动相为乙腈-0.5%三乙胺溶液(20:50),流速为1.0 mL/min,检测波长为270 nm.结果:苦参碱的检测浓度线性范围为0.5～14.3μg/mL, r=0.999 7(n=5),平均加样回收率为98.58%,RSD=1.77%(n=6).结论:高效液相色谱法简便、快捷、准确,可用于苦参配方颗粒的含量测定.     

高效液相色谱法测定妇乐颗粒中延胡索乙素的含量

目的:建立妇乐颗粒中延胡索乙素的含量检测方法.方法:高效液相色谱法(HPLC法),色谱柱为Diamonsi¨M C18柱(250 mm×4.6 mm,5μm),用三乙胺调pH=6.0的流动相为甲醇-0.1%磷酸溶液(60:40),检测波长为280 nm.结果:延胡索乙素的线性范围是0.102～1.632μg范围内线性良好,平均回收率为98.78%,RSD为2.75%.结论:HPLC法简便、可靠,可用于妇乐颗粒的质量控制.     

高效液相色谱法测定尼美舒利颗粒的含量

目的建立 HPLC法测定尼美舒利颗粒含量的方法.方法色谱柱为 KromasilC18柱(4.6mm×250mm,5μm);流动相:甲醇 乙腈 0.1%三氟乙酸溶液(20∶30∶50);流速1.0ml·min-1;柱温:30℃;检测波长298nm.结果尼美舒利在4.1254~82.5086mg·L-1范围内线性关系良好(r=1.0000,n=6),平均加样回收率为98.2%,RSD为1.1%(n=9).结论该方法简便快速,结果准确,可作为尼美舒利颗粒质量控制方法.     

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.