病毒合剂(Ⅱ)中黄芩苷、绿原酸和橙皮苷的含量测定

目的:建立HPLC法同时测定病毒合剂中黄芩苷、绿原酸和橙皮苷的含量。方法:色谱柱为Acclaim120 C18120A(150 mm×4.6 mm,5μm),流动相A为0.4%磷酸,流动相B为乙腈,梯度洗脱,流速1.0 ml/min,检测波长300 nm,进样量10μl。结果:黄芩苷、绿原酸和橙皮苷分别在29.16~121.50μg/ml(r=0.999 9)、3.23~13.44μg/ml(r=0.999 7)和6.55~27.30μg/ml(r=0.999 9)范围内与峰面积呈良好线性关系。平均回收率黄芩苷为102.6%(RSD为0.87%,n=6),绿原酸为100.1%(RSD为0.96%,n=6),橙皮苷为98.38%(RSD为0.38%,n=6)。结论:本方法简便、快速、结果准确、重现性好、灵敏度高,可用于病毒合剂的质量控制。     

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。     

高效液相色谱法测定强肝口服液中绿原酸含量

目的 建立测定强肝口服液中绿原酸含量的高效液相色谱(HPLC)法.方法 采用XBridgeTM C18色谱柱(150mm x4.6mm,5μm).流动相为甲醇-0.1%磷酸溶液(15:85),检测波长323 nm,柱温为室温,流速1.0 mL/min.结果绿原酸进样量在0.0258～0.4644μ范围内与峰面积线性关系良好(r=0.9998),平均加样回收率为97.66%,RSD=0.93%(n=6).结论该法简便、快速、灵敏、准确、专属、重现性好,为强肝口服液的绿原酸含量测定提供了可靠方法.     

高效液相色谱法测定妇科止痒胶囊中绿原酸含量

目的建立测定妇科止痒胶囊中绿原酸含量的高效液相色谱(HPLC)法。方法采用XBridgeTM-C18色谱柱(150 mm×4.6 mm,5μm),流动相为甲醇-0.1%磷酸溶液(15∶85),流速1.0mL/min,检测波长332nm。结果绿原酸进样量在0.0258～0.4644μg范围内与峰面积积分值线性关系良好,回归方程Y=2588978X-20732.66(r=0.9998),平均加样回收率为98.36%,RSD为1.29%(n=6)。结论该法简便、准确、重复性好,为测定妇科止痒胶囊的绿原酸含量提供了可靠的分析方法。     

HPLC法同步测定金银花中绿原酸和咖啡酸含量

目的同步测定河南产金银花中绿原酸和咖啡酸的含量。方法采用RP-HPLC方法测定,采用Kromasil-C18(4.6mm×250mm,5μm)色谱柱进行分离,流动采用甲醇-水(含0.2%醋酸)系统梯度洗脱,流速1.0ml/min,检测波长为280nm,柱温为30℃,进样体积10μL。结果绿原酸、咖啡酸分别在下列范围内有良好的线性和回收率:0.980～9.800μg(r=0.9999),99.85%(n=6,RSD=2.0%);0.00432～0.432μg(r=0.9992),98.7%(n=6,RSD=1.8%)。结论同步测定金银花中有机酸含量更加有利于金银花药材的质量控制。     

HPLC法测定珍杞降糖胶囊中绿原酸的含量

目的建立珍杞降糖胶囊中绿原酸的HPLC含量测定方法。方法采用HPLC法,色谱柱为AgilengtEclipsePlusC18柱(4.6mm×100mm);流动相:乙腈-0.4%磷酸(17︰83);流速:0.6mL/min;检测波长:327nm。结果绿原酸在0.0433～0.6938μg范围内线性关系良好(r=0.9999),平均加样回收率为98.39%,RSD=0.58%(n=6)。结论本方法简便快速、结果准确,可较好地控制该制剂的质量。     

HPLC-DAD法同时测定肝八味胶囊中4种成分的含量

目的 用高效液相色谱(HPLC)法同时测定肝八味胶囊中4种成分的含量。方法 采用HPLC法,色谱柱为C18柱(250mm×4.6mm,5μm),以乙腈为流动相A,以水为流动相B,梯度洗脱;检测波长为240nm;流速1.0ml/min。结果 丹酚酸B对照品在15.026~100.17μg/ml范围内呈良好线性关系,平均加样回收率为96.6%(n=6),RSD=1.8%(n=6);芍药苷对照品在14.335~95.564μg/ml范围内呈良好线性关系,平均加样回收率为97.0%(n=6),RSD=1.7%(n=6);虎杖苷对照品在8.235~54.90μg/ml范围内呈良好线性关系,平均加样回收率为97.2%(n=6),RSD=1.8%(n=6);大黄素对照品在1.582 5~10.55μg/ml范围内呈良好线性关系,平均加样回收率为98.1%(n=6),RSD=1.7%(n=6)。结论 此法简单准确、重现性好、专属性强、阴性对照无干扰,适用于肝八味胶囊的质量控制。     

两种不同方法测定注射用阿魏酸钠的含量

目的比较注射用阿魏酸钠含量的两种不同测定方法。方法分别采用紫外分光光度(UV)法及高效液相色谱(HPLC)测定。UV法采用纯化水为溶剂,310nm为测定波长;HPLC法采用Wa-tersXTerraRP18(4.6mm×250mm,5μm)色谱柱,流动相为甲醇-水(62∶38),流速为1ml/min,检测波长为310nm。结果 UV法中阿魏酸钠在6.216～14.504μg/ml范围内,浓度与吸光度呈良好线性关系(r=0.9999),平均回收率99.71%,相对标准偏差(RSD)为0.92%。HPLC法中阿魏酸钠在44.08～220.4μg/min范围内线性关系良好(r=0.9997),平均回收率98.79%,相对标准偏差(RSD)为1.61%。结论两种方法含量测定结果无明显差异,均可作为注射用阿魏酸钠含量测定的方法,可将UV法用于制剂半成品含量控制,而将HPLC法用于成品的含量控制,可缩短检验时间,保证制剂质量。     

银翘解毒丸(大蜜丸)中绿原酸含量测定方法研究

目的探讨银翘解毒丸(大蜜丸)质量标准。采用HPLC法对银翘解毒丸(大蜜丸)中的绿原酸进行含量测定。方法色谱柱为Kromasil C18色谱柱(4.6×250mm,5μm),以乙腈-0.3%磷酸(10∶90)为流动相;流速:1.0mL.min-1,检测波长327nm。结果绿原酸的进样量在0.03～0.15mg范围内呈良好的线性关系(r=0.9995),平均加样回收率为100.6%,RSD为1.57%(n=6)。结论方法简便、准确,可用于银翘解毒丸(大蜜丸)中绿原酸的含量测定。     

毒热清颗粒的质量标准研究

目的为新制剂毒热清颗粒建立质量标准。方法对制剂中连翘、紫花地丁、甘草采用薄层色谱(TLC)法进行定性鉴别;采用高效液相色谱法(HPLC)测定毒热清颗粒中黄芩苷、绿原酸的含量。色谱柱为Agilent ZORBAX XDB-C18柱(4.6mm×150mm,5μm),流动相甲醇-0.4%磷酸(梯度洗脱),流速1.0m L/min,检测波长为316nm,柱温25℃。结果连翘、紫花地丁、甘草的TLC图斑点清晰,分离度好。黄芩苷、绿原酸检测进样量线性范围分别为0.4764~2.382μg(r=0.9999),0.4216~2.108μg(r=0.9999),加样回收率分别为98.8%(RSD=1.5%),99.1%(RSD=1.1%),精密度、重复性、稳定性实验的RSD2%,n均为6。结论所建质量控制方法科学合理,可作为毒热清颗粒的质量标准。     

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.