高效液相色谱法测定复方亚油酸乙酯胶丸中橙皮苷的含量

目的建立复方亚油酸乙酯胶丸中橙皮苷的含量测定方法。方法液相色谱法。色谱柱:Kromasil C18柱(4.6mm×250mm,5μm);流动相:甲醇-0.5%冰醋酸溶液(40∶60);流速1.0mL.min-1;柱温:40℃;检测波长:283nm。结果橙皮苷在0.07505～0.3752μg范围内呈线性关系(r=0.9997,n=5),平均加样回收率为99.16%,RSD为1.7%(n=6)。结论该方法操作简便,结果可靠,可用于复方亚油酸乙酯胶丸中橙皮苷的含量测定。     

高效液相色谱法测定木香分气丸中橙皮苷含量

目的建立测定木香分气丸中橙皮苷含量的高效液相色谱法。方法采用Agela Promosil C18柱(100 mm×4.6 mm,5μm),流动相为甲醇-水-冰醋酸(32∶63∶5),流速为1.0 mL/min,检测波长为283 nm。结果橙皮苷检测进样量在0.102 0～1.02μg范围内与峰面积积分值呈良好线性关系(r=0.999 8),平均加样回收率为98.21%,RSD=0.90%(n=6)。结论该法简便、准确、可靠,可用于产品的质量控制。     

RP-HPLC法测定清热祛湿冲剂中橙皮苷的含量

目的:建立反相高效液相色谱法测定清热祛湿冲剂中橙皮苷的含量。方法:以Alltima-C18(250 mm×4.6mm,5μm)为分析柱,甲醇-醋酸-水(35∶4∶61)为流动相,流速0.6 ml/min,检测波长283 nm。结果:橙皮苷在7.2~144.0μg/ml的范围内与峰面积呈良好的线性关系(r=0.999 9);平均回收率为100.06%,RSD为0.74%(n=9)。结论:该方法简便,灵敏度高,结果准确,可用于清热祛湿冲剂的质量控制。     

HPLC法测定通舒口爽胶囊中3种成分的含量

目的建立测定通舒口爽胶囊中柚皮苷,橙皮苷和新橙皮苷含量的HPLC方法。方法采用Diamonsil C18(200 mm×4.6 mm,5μm)色谱柱,流动相:甲醇-乙腈-体积分数为0.05%的磷酸水溶液(体积比为20∶10∶65),流速:1.0 mL.min-1,柱温:30℃,检测波长:280 nm。结果柚皮苷在8.88~88.8 mg.L-1内呈线性关系(r=0.999 7),平均回收率为100.5%;橙皮苷在7.60~76.0 mg.L-1内呈线性关系(r=0.999 6),平均回收率为100.5%;新橙皮苷在10.56~105.6 mg.L-1内呈线性关系(r=0.999 9),平均回收率为100.5%。结论本实验建立的方法可作为通舒口爽胶囊质量控制方法之一。     

HPLC法测定芙扑感冒颗粒中橙皮苷的含量

目的:建立了测定芙朴感冒颗粒中橙皮苷的HPLC测定方法。方法:采用C18柱(250mm×4.6mm,5μm),甲醇-水-冰醋酸(30∶65∶5)为流动相,检测波长为280nm。结果:橙皮苷在10～100μg/mL浓度范围内呈良好的线性关系,r=0.9999。平均回收率为98.62%,RSD为1.72%。结论:本法简便、快速,可用于该制剂的质量控制。     

高效液相色谱法测定康儿灵颗粒中橙皮苷的含量

目的建立高效液相色谱法(HPLC)测定康儿灵颗粒中橙皮苷的含量。方法用C18柱(250mm×4.6mm,5μm),流动相为甲醇-水-冰醋酸(35∶61∶4),流速1.0mL·min-1,柱温25℃,检测波长284nm。结果橙皮苷在0.08～0.90μg范围内呈良好的线性关系,r=0.9999,平均回收率为98.8%,RSD为4.8%。结论方法简单,结果准确,可靠。     

HPLC法测定参苏丸中橙皮苷的含量

目的:建立以HPLC法测定参苏丸中橙皮苷含量的方法。方法:色谱柱为Microsorb C18(250mm×4.6mm,5μm),流动相为乙腈-甲醇-0.2mol·L-1醋酸铵-冰醋酸(65∶11∶23∶1),柱温为23℃,检测波长为283nm,流速为0.8mL·min-1。结果:橙皮苷在10~50μg·mL-1浓度范围内与峰面积积分值呈良好线性关系(r=0.9996);平均回收率为99.37%,RSD=1.63%。结论:本法快速、简便、回收率高、重现性好。     

HPLC测定维尔康胶囊中甲基橙皮苷的含量

目的建立高效液相色谱法测定维尔康胶囊中甲基橙皮苷的含量。方法采用C18(150mm×4.6mm,5μm)柱,冰醋酸-甲醇-水(5∶25∶70)为流动相,流速为1.0mL·min-1,检测波长为283nm。结果甲基橙皮苷质量浓度在29.1~291mg·L-1范围内呈良好的线性关系(r=0.9999);平均回收率为99.3%,RSD为1.8%(n=6)。结论该方法操作简便准确,重现性好,可用于维尔康胶囊中甲基橙皮苷的质量控制。     

HPLC同时测定理气舒心片中3种活性成分

目的利用HPLC同时测定理气舒心片中柚皮苷、橙皮苷和新橙皮苷。方法 Thermo SCIENTIFIC Syncronis C18色谱柱(4.6mm×250mm,5μm);流动相为乙腈-0.1%磷酸溶液(25∶75);流速1.0m L/min;柱温30℃;检测波长284nm。结果 3种成分均达到基线分离,柚皮苷、橙皮苷和新橙皮苷的质量浓度与峰面积,分别在1.92~102.28μg/m L(r=0.9996),1.73~92.25μg/m L(r=0.9995),2.10~111.86μg/m L(r=0.9996)范围呈良好的线性关系;平均加样回收率分别为102.05%、99.53%、100.62%,RSD分别为0.89%、1.17%、2.02%。结论本研究建立的方法符合方法学验证要求,适用于同时测定理气舒心片中柚皮苷、橙皮苷和新橙皮苷的含量。     

HPLC法测定乳癖康片中橙皮苷的量

目的:探讨乳癖康片中橙皮苷的定量方法,以控制其质量。方法:采用HPLC法,色谱柱为MerkLichrospher RP-18(250mm×4.6mm,5μm)柱,流动相为甲醇-水(35∶65),检测波长为284nm。结果:橙皮苷质量浓度在25.12~125.60μg/mL具有良好的线性关系(r=0.9999),平均回收率为99.81%,RSD=0.72%。结论:该方法能满足乳癖康片中橙皮苷的测定要求,可以用于该制剂的质量控制。     

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.