高效液相色谱法测定丹栀逍遥丸中栀子苷的含量

目的采用高效液相色谱法测定丹栀逍遥丸中栀子苷的含量。方法色谱柱为K rom asil C18柱(150×4.6mm,5μm),流动相为:乙腈∶水(15∶85);流速:1.0m l.m in-1,检测波长为238nm。结果栀子苷的进样量在0.30~3.00μg范围内与峰面积呈良好线形(r=0.9994);平均回收率为98.96%,RSD为1.32%(n=5)。结论该法简便,结果可靠,可有效地用于丹栀逍遥丸的质量控制。     

不同采收时期及干燥方法对栀子中栀子苷含量的影响

目的:评价不同采收期以及不同干燥方法对栀子苷的影响.方法:应用高效液相色谱法测定,色谱柱为Agilent Zorbax XDB-C18色谱柱(150 mm×4.6 mm,5 μm);流动相为乙腈-水(15:85),流速1.0 ml·min-1;柱温:30℃;检测波长238 nm.结果:栀子苷的线性范围为0.31～155.76 μg·ml-1(r=0.999 9),加样回收率为100.9%(RSD=1.2%);定量分析了6个采收时间、12种干燥方法的栀子中栀子苷含量.结论:不同采收时期、不同干燥方法对栀子中栀子苷的含量有一定的影响.     

HPLC法测定丹栀逍遥丸中栀子苷和芍药苷的含量

建立HPLC法同时测定丹栀逍遥丸中栀子苷和芍药苷的含量。采用Hypersil BDS C18色谱柱,流动相:乙腈-1%醋酸溶液(13∶87);流速:1.0mL.min-1,检测波长:238nm,柱温:30℃。栀子苷的线性范围0.48~3.20μg,r=0.9990;芍药苷线性范围0.45~3.00μg,r=0.9992;平均回收率栀子苷为100.08%,RSD为0.79%;芍药苷为99.75%,RSD为1.10%。该法简便,结果可靠,可有效地用于丹栀逍遥丸的质量控制。     

双波长RP-HPLC法同时测定黄连上清丸中栀子苷和黄芩苷的含量

目的 建立RP-HPLC同时测定黄连上清丸中栀子苷和黄芩苷含量的方法.方法 色谱柱:Hibor C18柱,流动相:乙腈-0.2％磷酸水溶液,梯度洗脱;检测波长分别为240 nm(栀子苷),278 nm(黄芩苷);柱温:30℃.结果 栀子苷、黄芩苷进样量分别在0.16～0.8 μg、0.24～1.2 μg范围内线性关系良好;平均回收率分别为96.8％、98.8％,RSD分别为1.83％、2.32％.结论 该方法简便、快速、准确,适用于黄连上清丸中栀子苷和黄芩苷的含量测定.     

RP-HPLC法测定复方丹栀逍遥丸中栀子苷的含量

目的:建立以反相高效液相色谱法测定复方丹栀逍遥丸中栀子苷含量的方法。方法:色谱柱为Shim-pack-vp-ODS(150mm×4.6mm,5μm),流动相为乙腈-水(15∶85),流速为1.0mL·min-1,检测波长为240nm。结果:栀子苷的进样量在0.11～0.67μg范围内与峰面积积分值呈良好的线性关系(r=0.9992);平均回收率为96.7%,RSD=1.2%(n=6)。结论:本方法简单、准确、快速,可用于复方丹栀逍遥丸的质量控制。     

丹栀逍遥胶囊质量标准研究

目的建立丹栀逍遥胶囊的质控标准。方法用TLC法对丹栀逍遥胶囊中的当归、白术、牡丹皮、甘草进行鉴别;用HPLC法对丹栀逍遥胶囊中栀子苷、芍药苷的含量进行测定。采用C18(SYNCRONIS AQ 250mm×4.6mm,5μm)色谱柱,流动相为乙腈-水(15:85),检测波长为238nm,流速:1.0mL.min-1。结果当归、白术、牡丹皮、甘草的薄层色谱鉴别效果好、专属性强,分离度高,且阴性样品无干扰;栀子苷在0.117～0.780μg范围内线性关系良好,R2=0.9996,平均回收率97.63%,RSD=0.93%(n=6)。结论本文建立的方法不仅操作简便、结果准确、重现性好,而且能够对丹栀逍遥胶囊进行定性和定量质控,符合中成药的质控要求。     

HPLC法同时测定精制冠心颗粒中芍药苷与丹酚酸B含量

目的:建立HPLC法同时测定精制冠心颗粒中芍药苷、丹酚酸B含量,为质量控制提供技术支持.方法:采用WondasilTM C18色谱柱(150 mm ×4.6 mm,5μm);流动相为0.1％磷酸溶液-乙腈体系,线性梯度洗脱,流速0.8 ml·min-1,柱温30℃,检测波长芍药苷(230 nm)、丹酚酸B(286 nm).结果:芍药苷、丹酚酸B进样量分别在0.430～5.375 μg、0.416～4.160 μg范围内线性关系良好(R2 ≥0.9996),加样回收率分别为100.61％和101.17％,RSD分别为1.12％和1.65％.结论:本法简便可靠,重复性好,可用于该制剂的含量测定.     

HPLC法测定丹栀逍遥散中栀子苷的含量

目的:建立测定丹栀逍遥散中栀子苷含量的方法。方法:采用高效液相色谱法。色谱柱为Agilent TC-C18,流动相为乙腈-水(15∶85,V/V),检测波长为238 nm,流速为1.0 ml/min,柱温为30Ⅴ,进样量为10μl。结果:栀子苷检测质量浓度在0.51¹6.32μg/ml范围内与峰面积积分值呈良好的线性关系(r=0.999 5);精密度、稳定性、重复性试验的RSD≤2.30%;平均加样回收率为99.40%,RSD=1.99%(n=9)。结论:该方法简单、准确、重复性好,可用于丹栀逍遥散中栀子苷的含量测定。     

HPLC法测定热毒平颗粒中栀子苷的含量

目的 建立热毒平颗粒中栀子苷含量的高效液相色谱法.方法 采用C18(250 mm×4.6 mm,5 μm)色谱柱,流动相为乙腈-水(12∶88);流速为1.0 ml·min-1;检测波长为238 nm.结果 栀子苷在0.128～6.416 μg范围内呈线性关系,r=0.999 9.平均加样回收率为99.04%.结论 用该法测定热毒平颗粒中栀子苷的含量,操作简便、结果准确、重复性好,可以用于热毒平颗粒的质量控制.     

高效液相色谱法测定解郁安神饮中栀子苷含量

目的 建立测定解郁安神饮中栀子苷含量的高效液相色谱法.方法 采用C18柱(200 mm×4.6mm,5μm),流动相为乙腈-水(15:85),流速为1.0mL/min,检测波长为238 nm.结果 栀子苷进样量线性范围为0.18～0.42 μg(r=0.999 9),平均回收率为99.10％,RSD=1.03％(n=9).结论 所用方法简单、结果准确、灵敏度高,能有效控制解郁安神饮的质量.     

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.