HPLC法测定地黄及增液口服液中梓醇的含量

目的测定地黄药材及成药增液口服液中梓醇的含量。方法地黄药材用甲醇加热回流1h提取；成药增液口服液正丁醇萃取。采用反相液相色谱法测定，流动相为乙腈-0.1％磷酸(1：99)，检测波长为210nm。结果可测出地黄药材中梓醇的含量，回收率为98.3％，RSD小于2％。并可测出增液口服液是否含有梓醇。结论本方法简便可靠，可用作地黄药材和增液口服液的质量控制。     

高效液相色谱法测定增液口服液的梓醇含量

本文报道采用RP－HPLC法测定增液口服液的梓醇含量。以外标峰面积定量，标准曲线方程为X＝（Y＋54．24）／1998，r＝0．9999，回收率为100．2％，RSD＜2％。为控制含地黄制剂的内在质量提供了可靠的方法。     

神衰Ⅲ号口服液中有效组分梓醇的分析研究

目的:通过对本院自制纯中药制剂神衰Ⅲ号口服液中有效组分之一梓醇的分析研究,探索神衰Ⅲ号口服液的稳定性。方法:用HPLC法,对神衰Ⅲ号口服液中梓醇进行定性及定量试验。结果:在对照空白液中未测得梓醇;在生地液及神衰Ⅲ号口服液中可明显测得梓醇组分;梓醇的含量与峰面积呈线性关系;在不同批号的神衰Ⅲ号口服液中梓醇含量稳定。结论:本丈所建立的梓醇测定方法可作为神衰Ⅲ号口服液的质量控制指标之一。     

HPLC法测定不同来源地黄中梓醇的含量

目的建立地黄中有效成分梓醇的HPLC测定方法,测定不同来源地黄药材中的梓醇含量。方法采用高效液相色谱法,选用C18柱,流动相为甲醇-0.1%磷酸溶液(1∶99),流速1.0 ml.min-1,检测波长为210 nm,柱温为35℃。结果梓醇在25～250 mg.L-1范围内具有良好的线性关系(r=0.999 6),平均加样回收率95.66%,RSD为1.52%(n=9)。结论不同来源地黄中有效成分梓醇的含量差异较大,生地黄中的梓醇含量高于熟地黄中梓醇含量。     

不同品种地黄干茎中梓醇含量比较

目的:研究地黄6个品种地黄的干茎中梓醇含量的差异。方法:梓醇含量测定采用HPLC法。结果:北京Ⅰ号茎中梓醇含量最高。结论:不同品种地黄叶中梓醇含量有明显差异。     

HPLC法测定牛黄解毒片中黄芩苷的含量

目的 建立测定牛黄解毒片中黄芩苷的含量。方法 成药制剂牛黄毒片用70％乙醇溶液超声中提取黄芩苷。采用反相液相色谱法测定，流动相为甲醇-0．1％磷酸(55／45)，检测波长为274nm。结果 可测出牛黄解毒片中黄芩苷的含量，回收率为101．6％，RSD小于1．3％。结论 本方法简便可靠，可用作牛黄解毒片中的质量控制。     

TLC法和HPLC法对养阴清肺合剂的质量控制

目的建立养阴清肺合剂中地黄、麦冬的定性鉴别方法和梓醇的含量测定。方法用薄层色谱法鉴别合剂中的地黄、麦冬;用高效液相色谱法测定梓醇含量。结果在薄层色谱中可以检出地黄、麦冬;梓醇在进样量为0.1692~8.46μg(r=0.9999)范围内线性关系良好,平均加样回收率为100.67%,RSD为0.72%(n=6)。结论方法简便,准确,专属性强,可以更有效地控制养阴清肺合剂的质量。     

HPLC法测定地黄不同炮制品中梓醇的含量

目的测定地黄不同炮制品中梓醇的含量。方法高效液相色谱法测定,流动相为乙腈-0.1%磷酸(1∶99),检测波长为210nm,流速为1.0mL·min-1,柱温为25℃。结果地黄经炮制后,梓醇含量差异较大,含量由高到低依次为生地、熟地、生地炭、熟地炭。结论该法简便、准确,可用于地黄的质量控制。     

HPLC法测定滋肾健脾液中梓醇和大黄素含量

目的建立滋肾健脾液（生地、枸杞、制首乌等）中梓醇及大黄素含量测定的HPLC方法。方法采用ZORBAX SB-Aq Agdem 1100（150mm×4．6mm,5μm）色谱柱。梓醇含量测定色谱条件为：以乙腈-水（0．6：99．4,V/V）为流动相,流速1mL·min^-1,检测波长210nm,柱温25℃。大黄素含量测定色谱条件为：以甲醇-0．1％磷酸（80：20,V／V）为流动相,流速1mL·min^-1,检测波长290nm,柱温25℃。结果梓醇质量浓度在0．02408-0．2408g·L^-1内与峰面积呈良好的线性关系（r=0．9999,n=6）,低、中、高浓度的对照品溶液的加样回收率分别为97,54％、99．46％、101．35％;大黄素质量浓度在0．81—8．10mg·L^-1内与峰面积呈良好的线性关系（r=0．9999,n=6）,低、中、高浓度的对照品溶液的加样回收率分别为97．74％、100．18％、100．66％。结论本法简便、准确、专属性强,可用于该制剂中梓醇及大黄素含量测定。     

高效液相色谱法测定地黄干茎中梓醇的含量

目的：测定地黄干茎中梓醇的含量。方法：采用高效液相色谱（HPLC）法，色谱柱为Diamond C18（150mm×4.6mm,5μm），流动相写乙腈-水（0．5：99．5），流速1．0mL／min，柱温25℃，检测波长210nm，进样量5μL。结果：地黄干茎中梓醇含量为8．5％。结论：地黄中茎中梓醇含量较高，建议对地黄干茎进行研究，以便开发利用。     

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.