HPLC法测定扶正平消胶囊中芍药苷的含量

目的 建立扶正平消胶囊中芍药苷含量的测定标准。方法 采用HPLC法进行含量测定,色谱柱为Agilent Zorbax SB-C₁₈柱（150 mm×4.6 mm,5 μm）,流动相：乙腈-5 mmol/L磷酸二氢钠水溶液（10：90）,流速：1.0 ml/min,柱温：25℃;检测波长：230 nm,进样量10 μl,运行时间25 min。结果 芍药苷在25.0~500.0 μg/ml范围内线性关系良好（r=0.999 9）,线性方程：Y=12.65X+43.54,平均加样回收率为92.69%,RSD为1.77%。结论 该方法操作易行、结果可靠、重复性好,可用于扶正平消胶囊中芍药苷的含量测定。     

应用高效液相色谱法测定消亢胶囊中迷迭香酸的含量

目的 建立测定消亢胶囊含量的方法。 方法 采用高效液相色谱(HPLC)法测定消亢胶囊中迷迭香酸的含量。色谱柱:Agilent C₁₈柱,流动相:甲醇-0.5% 甲酸(50:50),流速:1 ml/min,检测波长:330 nm,柱温:30 ℃,进样量:10 μl。 结果 消亢胶囊中夏枯草迷迭香酸的浓度在2.88~20.16 μg范围内与峰面积积分值呈良好的线性关系(r=0.999 8),平均回收率为99.54%,RSD为0.40%(n=9)。 结论 该方法操作简便、结果准确可靠,适用于消亢胶囊中迷迭香酸的含量测定。     

高效液相色谱法测定鼻炎灵胶囊中黄芩苷含量

目的 建立高效液相色谱法测定鼻炎灵胶囊中黄芩苷的含量。方法 色谱柱为Waters XBridge C₁₈柱（4.6 mm×250 mm,5 μm）,流动相为乙腈-0.8%甲酸（25：75）,检测波长276 nm,流速1.0 ml/min,柱温30℃,进样量10 μl。结果 黄芩苷在1.25~40 μg/ml范围内（r=0.999 9）呈良好的线性关系,精密度实验中RSD均小于2%,加样回收率在95%~100%之间。结论 该测定方法简便、准确,分离效果好,可用于鼻炎灵胶囊的质量控制。     

高效液相色谱法测定降脂护肝胶囊中葛根素的含量

目的 建立高效液相色谱法测定降脂护肝胶囊中葛根素的含量。方法 色谱柱为Waters Symmetry C₁₈柱（4.6 mm×250 mm,5 μm）,流动相为乙腈-1%甲酸（11：89）,检测波长250 nm,流速1.0 ml/min,柱温30 ℃,进样量10 μl。结果 葛根素在2~40 μg/ml范围内（r=0.999 8）呈良好的线性关系,精密度实验中RSD均小于2%,加样回收率在98%~103%。结论 该测定方法简便、准确,分离效果好,可用于降脂护肝胶囊的质量控制。     

HPLC测定安尔眠胶囊中2,3,5,4’-四羟基二苯乙烯-2-O-β-D-葡萄糖苷

目的 建立安尔眠胶囊中2,3,5,4’-四羟基二苯乙烯-2-O-β-D-葡萄糖苷（C₂₀H₂₂0₉）的含量测定方法。方法 采用高效液相色谱（HPLC）法,以Dionex Acclaim 120^® C₁₈色谱柱（150 mm×4.6 mm,5 μm）为分离柱,以乙腈-1%甲酸溶液（23：77）为流动相,体积流量1.0 mL/min,检测波长320 nm,柱温25 ℃。结果 2,3,5,4’-四羟基二苯乙烯-2-O-β-D-葡萄糖苷在0.010～0.200 μg呈现良好的线性关系（r=0.999 6）,平均回收率为97.35%,RSD为2.07%。结论 该方法<准确可靠,适用于安尔眠胶囊中2,3,5,4’-四羟基二苯乙烯-2-O-β-D-葡萄糖苷的含量测定。     

用HPLC法测定人凝血酶制品中甘氨酸的含量

目的 建立一种测定人凝血酶制品中甘氨酸含量的HPLC方法。方法 以2、4-二硝基氟苯（DNFB）为柱前衍生剂,采用ODS-C₁₈色谱柱,流动相为50%乙腈溶液-0.05 mol/L醋酸钠缓冲液（35︰65）,流速1.0 ml/min,检测波长360 nm。结果 甘氨酸的线性范围为0.006~0.030 mg/ml（r=0.999 6）,平均回收率为100.4%,RSD为0.44%（n=9）。结论 该方法简便、准确、专属性好,可用于人凝血酶制品中甘氨酸的含量测定。     

甘地胶囊中马钱苷含量测定方法的优化

目的 建立HPLC法测定甘地胶囊中马钱苷的含量。方法 色谱柱为Waters Symmtry C₁₈柱（4.6 mm×150 mm,5 μm）;流动相为乙腈-水（13∶87）;流速1.0 ml/min;检测波长240 nm。结果 马钱苷对照品在0.030 1~3.01 μg范围内呈良好的线性关系（r=0.999 9）,平均加样回收率为99.62%,RSD为0.86%。结论 本方法简便、准确,重复性好,可用于甘地胶囊中马钱苷的含量测定。     

高效液相色谱法测定康得灵胶囊中黄芩苷的含量

目的 建立康得灵胶囊中黄芩苷的HPLC测定方法。方法 色谱柱为Agilent Tc-C₁₈色谱柱（4.6 mm×250 mm,5 μm）,柱温为30 ℃;流动相为乙腈-0.5‰磷酸溶液（26：74）,流速为1.0 ml/min,检测波长265 nm。结果 黄芩苷保留时间约为16 min。以峰面积（Y）对进样浓度（X, μg/ml）线性回归,得回归方程：Y=22 114.67 X－112 836.7,r=0.998 8,线性范围5.410~108.2 μg/ml。平均加样回收率为98.78%,RSD为0.74%。结论 本方法操作简便,测定结果准确可靠,可用于康得灵胶囊中黄芩苷的含量测定。     

用HPLC法测定丹参素棕榈醇酯脂质体药物含量

目的 建立HPLC法测定丹参素棕榈醇酯脂质体中药物含量的方法。方法 采用Agilent ZORBAX Eclipse Plus C₁₈柱（4.6 mm×200 mm,5 μm）;以乙腈-水（50∶50）含0.02%甲酸和0.02%三乙胺水、以pH 6~7的溶液为流动相,流速为1 ml/min,检测波长为280 nm,柱温为室温。结果 本色谱条件下丹参素棕榈醇酯与辅料及溶剂分离度符合要求,在0.05~0.45 mg/ml范围内线性关系良好（r=0.999 5,n=5）,回收率在96%~102%之间,日内及日间RSD均小于2%（n=5）。3批样品的含量分别为97.81%、101.20%、98.53%。结论 该方法准确可靠、简单快速,可用于丹参素棕榈醇酯脂质体含量的测定。     

啤酒花中黄酮类成分的含量分析

目的 建立啤酒花中总黄酮和黄腐酚含量测定方法,对来自不同产地和品种的29个啤酒花样品中的总黄酮和黄腐酚进行测定。方法 用芦丁-AlCl₃分光光度法测定总黄酮的含量;用HPLC-UV法测定黄腐酚的含量。色谱条件：色谱柱为Dikma Technologies Diamonsil C₁₈柱（250 mm×4.6 mm,5 μm）;流动相为乙腈-1%冰醋酸梯度洗脱,流速为1.0 ml/min;柱温为25℃;检测波长为370 nm。结果 总黄酮回归方程为A=30.345C+0.016 8,r=0.999 9;黄腐酚回归方程为A=55 446C+9 040.5,r=0.999 9,表明总黄酮在20.2~404.0 μg/ml,黄腐酚在2.152~43.040 μg/ml范围内,线性关系良好,两者精密度和重复性RSD均<2%,平均加样回收率分别为102.71%和100.21%。结论 不同种类的啤酒花之间,总黄酮和黄腐酚含量存在巨大差异,进口啤酒花优于国产。     

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.