软肝缩脾丸的质量标准研究

目的 建立并提升软肝缩脾丸的质量标准。方法 采用显微鉴别法、薄层色谱法对软肝缩脾丸中的黄芪、丹参、赤芍、鳖甲、大黄、五味子、桃仁、三七进行定性鉴别;采用HPLC测定芍药苷、丹酚酸B的含量。色谱柱为Wondasil C₁₈柱（250 mm×4.6 mm,5 μm）,流动相为乙腈-0.1%磷酸溶液,梯度洗脱,流速：1.0 mL·min^-1,检测波长230,286 nm,柱温：30 ℃,进样量：10 μL。结果 4味药材的显微特征明显;5味药材的薄层色谱斑点清晰,分离度良好,阴性无干扰;HPLC显示芍药苷在9.79~195.80 μg·mL^-1（r=0.999 9）、丹酚酸B在11.45~229.00 μg·mL^-1 （r=0.999 9）内线性关系良好,平均回收率分别为100.6%,101.9%,RSD分别为1.26%,1.05%。结论 本方法简便、快捷、结果准确、重复性好,可用于软肝缩脾丸的质量控制。     

荔枝草的质量标准建立与探讨

目的 完善中药材荔枝草的质量标准。方法 采用显微鉴别、薄层鉴别、水分、总灰分、浸出物、含量测定等项目对荔枝草的质量进行考察。结果 荔枝草显微鉴别特征明显;薄层鉴别斑点清晰,易于识别;质量标准为：水分≤12.0%,总灰分≤10.0%,醇溶性浸出物≥20.0%;含量测定原儿茶酸在1.068~106.8 μg·mL^-1内呈良好的线性关系(r=0.999 7),其含量≥70 μg·g^-1。结论 荔枝草药材的显微鉴别、薄层鉴别、水分、总灰分、浸出物、含量测定研究可为该药材质量标准的修订、提高提供参考依据。     

红旱莲药材的质量标准研究

目的 完善红旱莲药材的质量标准。方法 采用显微鉴别法、薄层色谱（TLC）法鉴别红旱莲;按《中华人民共和国药典》（2015年版）规定方法考察水分、总灰分、酸不溶性灰分和醇溶性浸出物;用HPLC法测定金丝桃苷的含量。结果 建立了红旱莲显微鉴别法和TLC法鉴别,HPLC法含量测定;确定了水分、灰分、醇溶性浸出物的限度。结论 本实验为红旱莲药材的质量标准提高提供了依据。     

珍母丸质量标准研究

目的 建立珍母丸的质量标准。方法 采用显微鉴别方法对枸杞子、珍珠母的显微鉴别进行描述，采用薄层色谱法对香附、山茱萸、赤芍进行定性鉴别；采用HPLC测定赤芍中芍药苷的含量，色谱柱为Accurasil C₁₈（250 mm×4.6 mm，5 μm），以乙腈-0.2%磷酸溶液（15∶85）为流动相，流速为1.0 mL·min^-1，检测波长为230 nm，进样量为10 μL。结果 显微、薄层色谱有较强的专属性，赤芍中芍药苷在0.193~2.415 μg内线性关系良好（r=0.999 5），平均回收率为101.56%，RSD为1.45%（n=6）。结论 本方法操作简便，重复性好，可作为珍母丸的质量控制方法。     

米炒红娘子炮制工艺优化及其质量标准建立

目的 优化红娘子炮制工艺，建立米炒红娘子质量标准。方法 以浸出物、气味、色泽、破碎度及蛋白质含量为评价指标，结合熵权法-层次分析法建立综合评价方法，考察炒制时间、炒制温度及药材与辅料比例对米炒红娘子质量的影响，通过正交试验优选最佳炮制工艺。对米炒红娘子进行显微鉴别、薄层鉴别，测定其水分、灰分、浸出物及重金属含量，建立质量标准。结果 红娘子最佳炮制工艺为将2倍量大米投入炒药锅炒至冒烟时投入净制红娘子，140 ℃翻炒6 min。测得炮制品浸出物含量199 mg·g^-1，气味、色泽、破碎度分值均为5，蛋白质含量为136 mg·g^-1。米炒红娘子水分含量为2.97%，总灰分及酸不溶性灰分含量分别为3.79%，0.33%，重金属铅、镉、砷、汞、铜含量分别为2.26，1.91，0.06，0.13，38.14 mg·kg^-1，黄曲霉毒素B₁、B₂、G₁、G₂均低于检出限0.1 μg·kg^-1，浸出物含量为20.10%。结论 红娘子炮制工艺可靠、稳定，为规范红娘子饮片的炮制工艺和质量标准提供科学依据。建议米炒红娘子水分含量<3.56%，总灰分及酸不溶性灰分分别<4.55%、0.40%，重金属铅含量<2.71 mg·kg^-1、镉<2.29 mg·kg^-1、砷<0.07 mg·kg^-1、汞< 0.16 mg·kg^-1、铜<45.77 mg·kg^-1，浸出物含量>16.08%，黄曲霉毒素B₁、B₂、G₁、G₂<0.1 μg·kg^-1。     

西藏棱子芹的植物基原考证及生药学研究

目的：对西藏棱子芹进行基原考证和生药学鉴别研究。方法：利用生药学方法,对西藏棱子芹进行本草考证,对其植物形态特征、组织粉末显微特征和薄层色谱进行鉴别;同时还进行水分、总灰分、酸不溶性灰分和醇溶性浸出物的相关检查,以及挥发油的含量测定。结果：提供西藏棱子芹使用的历史依据,对其基原进行修正,薄层色谱鉴别的特征斑点清晰,相关检查数据符合《中华人民共和国药典》2015年版项下要求,6批西藏棱子芹挥发油平均含量不少于0.3%。结论：通过相关的试验研究,为西藏棱子芹的品种鉴别、生药学研究和质量标准制定以及药材的进一步开发和利用提供参考。     

HPLC同时测定双氯芬酸钠滴眼液中3种抑菌剂的含量

目的 建立HPLC同时测定双氯芬酸钠滴眼液中羟苯乙酯、硫柳汞和苯扎氯铵含量的方法。方法 用十八烷基键合硅胶为填充剂,以1%三乙胺溶液（磷酸调节pH值至3.0）为流动相A,以甲醇为流动相B,进行梯度洗脱;流速1.0 mL·min^-1,柱温40℃,检测波长254 nm。结果 羟苯乙酯在20.58~205.8 μg·mL^-1、硫柳汞在8.242~82.42 μg·mL^-1、苯扎氯铵n-C₁₂H₂₅取代物在12.88~128.8 μg·mL^-1、苯扎氯铵n-C₁₄H₂₉取代物在6.624~66.24 μg·mL^-1内线性良好（r≥0.999 8）,平均回收率为99.3%~102.5%（n=9）。结论 该方法简单、准确、重复性好,可用于控制双氯芬酸钠滴眼液中羟苯乙酯、硫柳汞和苯扎氯铵的含量。     

川菊止痛胶囊的质量标准研究

目的 建立川菊止痛胶囊质量标准。方法 采用薄层色谱法对复方中柴胡、菊花进行定性鉴别。HPLC同时测定制剂中黄芩苷、黄芩素、汉黄芩苷、汉黄芩素及甘草苷含量,色谱柱：Kromasil 100-5C₁₈（250 mm×4.6 mm,5 μm）;流动相：乙腈-0.05%磷酸溶液,梯度洗脱;检测波长为280 nm;流速：1.0 mL·min^-1;进样量：10 μL。结果 薄层色谱斑点清晰且阴性样品无干扰。甘草苷、黄芩苷、黄芩素、汉黄芩苷及汉黄芩素分别在10.7~107 μg·mL^-1、12.12~121.2 μg·mL^-1、11.2~112 μg·mL^-1、10.02~100.2 μg·mL^-1、10.32~103.2 μg·mL^-1内线性关系良好,精密度、重复性、稳定性试验RSD均<1.8%,加样回收率分别为98.34%~101.77%（RSD=1.28%,n=6）、98.69%~101.36%（RSD=1.01%,n=6）、98.46%~101.06%（RSD=0.92%,n=6）、98.67%~101.33%（RSD=1.17%,n=6）、98.43%~100.79%（RSD=0.92%,n=6）。结论 本研究建立的质量标准方法准确、简便,可用于川菊止痛胶囊的质量控制,且所建立的菊花、柴胡薄层鉴别方法可供其他含有二药的复方标准建立作参考。     

HPLC同时测定通脉颗粒中丹参素、原儿茶醛、丹酚酸B、阿魏酸和葛根素的含量

目的 建立通脉颗粒中丹参素、原儿茶醛、丹酚酸B、阿魏酸和葛根素的HPLC测定方法。方法 采用Welch Ultimate XD-C₁₈色谱柱（4.6 mm×250 mm,5 μm）,以乙腈-0.1%三氟乙酸为流动相,梯度洗脱,双波长检测（282,305 nm）,柱温35℃,流速1.0 mL·min^-1。结果 丹参素、丹酚酸B、原儿茶醛、葛根素和阿魏酸的线性范围分别为3.117~62.33 μg·mL^-1（r=0.998 7）,4.044~80.88 μg·mL^-1（r=0.9985）,1.280~25.60 μg·mL^-1（r=0.997 9）,7.964~159.3 μg·mL^-1（r=0.992 8）,1.980~39.60 μg·mL^-1（r=0.999 1）;平均回收率分别为101.6%（RSD=1.62%）,99.7%（RSD=1.76%）,97.4%（RSD=1.19%）,99.9%（RSD=1.52%）,102.2%（RSD=1.56%）。结论 该方法操作简便、快速,结果准确,可用于通脉颗粒的质量控制。     

CO2超临界流体色谱法同时测定莪术油中3个倍半萜类成分的含量

目的 建立CO₂超临界流体色谱法测定莪术油中呋喃二烯、牻牛儿酮和莪术二酮含量的方法。方法 采用ACQUITY UPC² HSS C₁₈ SB色谱柱（3.0 mm×150 mm,1.8 μm）,以CO₂-乙腈为流动相,梯度洗脱;流速为1.0 mL·min^-1;检测波长为216 nm,柱温为55℃,背压为2 000 psi。结果 呋喃二烯在2.67~1 337.26μg·mL^-1内线性关系良好（r=1.000）,加样回收率为97.94%（n=6,RSD=1.50%）。牻牛儿酮在2.77~1 386.00 μg·mL^-1内线性关系良好（r=1.000）,加样回收率为96.07%（n=6,RSD=1.68%）;莪术二酮在6.99~3 493.00 μg·mL^-1内线性关系良好（r=1.000）,加样回收率为99.33%（n=6,RSD=1.88%）。结论 本方法快捷准确、稳定且绿色环保,可用于莪术油中上述3个倍半萜类成分的质量控制。     

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.     

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.