高效液相色谱法测定醒脑益智颗粒中淫羊藿苷的含量

目的:建立醒脑益智颗粒中淫羊藿苷含量的测定方法。方法:采用高效液相色谱法测定醒脑益智颗粒中淫羊藿苷的含量。色谱柱为ZORBAX SB-C18(150 mm×4．6 mm,5μm);流动相:甲醇-水(55∶45);柱温:35℃;流速:1．0 ml·min-1;检测波长:270 nm。结果:淫羊藿苷浓度在1．13～27．12μg·ml-1范围内与峰面积呈良好的线性关系(r=0．999 9)。平均加样回收率为101．5％,RSD为1．53％(n=7)。结论:本法简便、灵敏、准确,可用于醒脑益智颗粒中淫羊藿苷的含量测定。     

HPLC法测定补肾强身片中淫羊藿苷的含量

目的建立补肾强身片中淫羊藿苷的含量测定方法。方法采用高效液相色谱法。色谱条件:色谱柱为Diamonsil(钻石)C18(5μm,250×4.6mm);流动相:乙睛-水(30∶70);检测波长:270nm;柱温:室温;流速:1.0mL/min;理论板数按淫羊藿苷峰计算不低于3000。结果淫羊藿苷在0.0832～0.3328μg之间线性关系良好,r=0.9999。淫羊藿苷平均回收率为98.49%,RSD=0.62%。结论该方法准确,重复性好,可用于补肾强身片的质量控制。     

HPLC同时测定21种淫羊藿中朝藿定C和淫羊藿苷的含量

目的:建立同时测定淫羊藿药材中朝藿定C和淫羊藿苷含量的高效液相色谱方法。方法:采用Elite SinoChrom ODS-AP(250 mm×4.6 mm,5μm)色谱柱,流动相为乙腈(A)-水(B),梯度洗脱(0~8 min,27%A;8~30 min,27%A→29%A),流速1 mL.min-1,检测波长270 nm。结果:朝藿定C进样量在0.130~3.89μg,淫羊藿苷在0.0294~1.47μg范围内呈良好线性关系(r=0.9999);朝藿定C和淫羊藿苷平均回收率(n=9)分别为103.9%,100.0%;淫羊藿药材中朝藿定C和淫羊藿苷的含量分别为0.02%~7.80%,0.01%~1.74%。结论:该方法简便、快速、准确,重复性好,可作为淫羊藿药材中朝霍定C和淫羊藿苷的含量测定方法。     

HPLC法测定藿精片中淫羊藿苷含量

目的：拟定藿精片中淫羊藿苷的含量测定方法。方法：采用高效液相色谱法测定藿精片中淫羊藿苷的含量。选用Hypersil C18柱（4.6 mm×250 mm1,0μm）;以甲醇-水系统为流动相;检测波长为270 nm;进样量为20μl。结果：被测物淫羊藿苷进样浓度在19.8～198μg/ml范围内与峰面积线性关系良好,平均回收率为99.94%,RSD为0.30%（n=6）。结论：建立了藿精片中淫羊藿苷的含量测定方法,该方法操作简便,准确可靠,可用于藿精片中淫羊藿苷的含量测定。     

高效液相色谱法测定骨疏灵颗粒中淫羊藿苷含量

目的建立HPLC法测定骨疏灵颗粒中淫羊藿苷的含量。方法采用Cosmosil C18(250 mm×4.6 mm,5μm)为色谱柱,流动相:乙腈-水(30∶70),流速:1.0 m L/min,检测波长:270 nm。结果淫羊藿苷在0.01~0.25 mg/m L范围内呈良好的线性关系(r=0.999 9),回收率为99.99%(RSD=0.75%,n=6)。结论本方法简单、准确,灵敏度高,重现性好,可用于骨疏灵颗粒中淫羊藿有效成分淫羊藿苷的含量测定。     

高效液相色谱法测定藿蓉补肾颗粒中淫羊藿苷的含量

建立藿蓉补肾颗粒中淫羊藿苷含量的HPLC测定方法.色谱柱为YWG C18柱(4.6mm×150mm);流动相为乙腈-水(30∶70),流速为0.8ml·min-1,检测波长为270nm.线性范围:0.0104～0.0520mg·ml-1,r=0.9997,平均回收率为96.1%,RSD为1.5%.方法准确可靠,适用于藿蓉补肾颗粒中淫羊藿苷的含量测定.     

RE-HPLC法测定仙灵脾颗粒中淫羊藿苷的含量

目的测定仙灵脾颗粒中淫羊藿苷的含量。方法采用RE-HPLC法。色谱柱为HYPERSIL C18柱(150mm×4.6mm,5μm);乙腈-水(30∶70)为流动相,流速:1.0mL/min;检测波长270nm。结果淫羊藿苷在0.02316～1.146μg范围内具有良好线性关系,平均回收率为100.80%,RSD为1.35%。结论该法可用于仙灵脾颗粒中淫羊藿苷的含量测定。     

HPLC法测定益肾灵颗粒中淫羊藿苷的含量

建立益肾灵颗粒中淫羊藿苷的含量测定方法。采用HPLC法,色谱柱:Diamonsil(C18,流动相:乙腈-水(20∶80,用磷酸调节pH为3.5),流速:1.0mL·min-1,检测波长:270nm,柱温:30℃。淫羊藿苷在0.06032～0.7540μg之间线性关系良好,r=1.000,回收率(n=6)为97.72%,RSD=0.64%。本法作为益肾灵颗粒的含量测定方法来控制制剂质量,方法简便,重现性好。     

紫外分光光度法和高效液相色谱法测定淫羊藿总黄酮含量的比较研究

目的:比较紫外分光光度法和高效液相色谱法测定淫羊藿总黄酮含量的差异,探讨淫羊藿总黄酮含量测定方法的可靠性。方法:紫外分光光度法以淫羊藿苷为指标性成分,在270 nm 波长处进行测定。高效液相色谱法以 ZORBAX SB-C_(18)柱(250mm×4.6 mm,5μm)为分析柱,乙腈-水梯度洗脱,流速1.0 mL·min~(-1),检测波长为270 nm。经紫外光谱识别的黄酮类成分(部分经 ESI-MS 确认),除朝藿定 C、淫羊藿苷、鼠李糖基淫羊藿次苷-Ⅱ和宝藿苷Ⅰ以自身对照外,其他黄酮类成分均以淫羊藿苷为参比进行定量,淫羊藿总黄酮含量等于朝藿定 C、淫羊藿苷、鼠李糖基淫羊藿次苷-Ⅱ、宝藿苷Ⅰ和其他黄酮成分含量之和。结果:紫外分光光度法,淫羊藿苷在2.45～24.50μg·mL~(-1)范围内线性关系良好(r=0.9996),测得淫羊藿总黄酮含量以淫羊藿苷计为56.6%。高效液相色谱法中,与淫羊藿苷紫外光谱相似的33个色谱峰,MS 归属了其中10个主要成分均为黄酮类成分。朝藿定 C、淫羊藿苷、鼠李糖基淫羊藿次苷-Ⅱ和宝藿苷Ⅰ分别在0.093～1.852μg(r=0.9998)、0.107～2.136μg(r=0.9997)、0.094～1.876μg(r=0.9998)、0.098～1.956μg(r=0.9998)线性关系良好,淫羊藿总黄酮含量为35.6%。结论:紫外分光光度法和高效液相色谱法测定的淫羊藿总黄酮含量差异显著,紫外分光光度法的准确性有待进一步考证。     

反相高效液相色谱法测定强筋健骨颗粒中淫羊藿苷的含量

目的建立复方制剂强筋健骨颗粒中的有效成分淫羊藿苷的含量测定方法。方法采用高效液相色谱法,色谱条件：色谱柱Kromasil Cus（4．6mm×250mm,5μml以乙腈-水（25：75）为流动相;检测波长：270nm;流速：1．Oml／min;柱温：25℃。结果本法可用来测定强筋健骨颗粒中淫羊藿苷的含量。淫羊藿苷在0．01949—0．3898μg范围内成良好线性关系,y=0．9998,平均回收率为99．90％,RSD为1．11％。结论本测定方法简便可行、重复性好,可用于本制剂中有效成分淫羊藿苷的含量测定。     

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.