绿衣枳壳总黄酮提取工艺的研究

目的：研究绿衣枳壳中总黄酮的提取工艺.方法：采用正交试验法研究绿衣枳壳总黄酮的最佳提取工艺,考查了乙醇浓度、料液比、提取时间及提取次数对绿衣枳壳提取物中总黄酮量的影响.结果：确立了绿衣枳壳中总黄酮最佳提取条件为：90％的乙醇为溶剂、料液比为1∶10、提取时间为2h、提取2次.结论：在最佳提取工艺条件下,绿衣枳壳提取物中总黄酮含量分别为60.914、60.788和60.915 mg/g,表明本研究提取工艺稳定可行.     

不同产地不同品种柚皮中总黄酮和柚皮苷的含量比较

目的:测定不同产地柚皮中总黄酮和柚皮苷的含量,筛选各种不同柚皮作为柚皮苷提取原料的可行性.方法:以紫外分光光度法测定不同产地柚皮中总黄酮的含量,检测波长为 283 nm;用高效液相色谱法测定不同产地柚皮中柚皮苷的含量.流动相为甲醇-水-乙酸(v∶v∶v=35∶61∶4),柱温30℃,流速为 1.0 mL·min-1,检测波长为 283 nm.结果:化橘红中总黄酮和柚皮苷的含量最高,胡柚皮次之,普通柚皮中总黄酮和柚皮苷含量都较少.结论:化州橘红是最理想的提取柚皮苷的原料,胡柚皮也可做为提取柚皮苷的药材资源.     

枳壳不同炮制品中柚皮苷的含量测定

目的 对枳壳不同炮制品的柚皮苷含量进行测定,考察不同炮制方法对枳壳中柚皮苷含量的影响.方法 采用高效液相色谱法对枳壳不同炮制品的柚皮苷含量进行测定,色谱柱为Discovery C18(25 cm×4.6 mm,5 μm),流动相为乙腈-0.3%磷酸溶液(20∶80),检测波长283 nm,柱温35℃,流速1.0 ml/min.结果 广东常用品种制枳壳的含量最低,平均含量为3.72%,切薄片的枳壳柚皮苷含量最高,平均含量为5.17%,麸炒枳壳平均含量为4.16%.结论 不同炮制方法的枳壳柚皮苷含量有明显差异.     

正交实验法优化枳壳提取工艺的研究

目的研究枳壳中总黄酮提取工艺。方法以总黄酮含量为考察指标,以固液比、提取次数、提取时间、乙醇浓度为考察因素,采用正交试验法优选提取总黄酮的最佳工艺。结果最佳工艺为:用8倍量的50%乙醇,提取3次,每次2h,合并滤液,总黄酮的含量达到30%。结论本方法简单易行,适合于工业大生产。     

正交试验法优选绞股蓝软胶囊的提取工艺

目的优选绞股蓝软胶囊的最佳提取工艺。方法以总黄酮含量和浸膏得率为指标,用紫外分光光度法测定总黄酮含量,采用L9（34）正交试验法优化提取工艺条件。结果最佳提取工艺条件为用12倍量的70％乙醇、提取2次、每次提取1．5h。结论优选的提取工艺稳定,可为工业化生产提供依据。     

水芹总黄酮提取工艺正交试验研究

目的:为水芹总黄酮提取工艺提供依据。方法:采用正交设计法,因素为溶剂用量、浓度、提取时间和次数,以总黄酮及金丝桃苷含量为指标综合分析。结果与结论:水芹总黄酮最佳提取工艺为70%乙醇10倍量提取4h,共提取3次;水芹有效成分金丝桃苷最佳提取工艺为70%乙醇10倍量提取2h,共提取3次。     

泽漆中总黄酮超声提取工艺优化研究

目的研究泽漆总黄酮超声提取法的最佳提取工艺,在此基础上采用分光光度法测定不同部位总黄酮的含量。方法正交设计试验寻找超声提取法提取泽漆总黄酮的最佳工艺条件,以芦丁为考察指标,通过分光光度法对泽漆不同部位总黄酮含量进行精密测定。结果乙醇浓度50%,物料比1∶25,超声提取时间20 min,超声提取温度60℃为最佳提取工艺。泽漆叶中总黄酮含量最高,根次之,茎最低。结论优选的泽漆总黄酮提取工艺方法,简便易行,快速灵敏,实验结果准确可靠。     

桔梗中总黄酮的提取工艺优化

目的优选从桔梗根、茎、叶中提取总黄酮的最佳工艺,并在最佳提取条件下测定桔梗根、茎、叶中总黄酮的含量。方法以总黄酮含量为指标,采用正交实验,考察了乙醇体积分数、超声时间和超声次数对总黄酮得率的影响。结果提取总黄酮的最佳工艺为A3B3C3,即乙醇体积分数70%,超声时间50min,超声次数3次。在最佳实验条件下,分别测得桔梗根、茎及叶中总黄酮的含量分别为0.027%,0.039%和0.26%。结论该工艺简单可行,是提取桔梗中总黄酮的有效途径。     

正交法优选砂烫骨碎补的炮制工艺

目的:优选砂烫骨碎补的炮制工艺。方法:以柚皮苷、总黄酮和煎出物含量等多指标评价全概率综合评分法优选砂烫骨碎补的炮制工艺,高效液相色谱法测定柚皮苷含量,紫外法测定总黄酮含量。结果:砂烫骨碎补的最佳炮制工艺为210℃、加热炮制3min、用6倍量油砂。结论:该工艺炮制出的骨碎补质量好,工艺参数量化,可操作性强,为砂烫骨碎补炮制工艺规范化提供了可靠数据。     

榅桲子总黄酮提取工艺研究

目的 优选榅桲子中总黄酮的最佳提取工艺条件.方法 以芦丁为对照品,用分光光度法在506 nm波长处测定榅桲子总黄酮含量,优选总黄酮的提取工艺.结果 测得样品中总黄酮含量为13.60 mg•g-1,最佳提取工艺：乙醇浓度为75%,料液比1：10(倍)、回流时间 2.5 h,回流温度60 ℃,提取3次.结论 选用芦丁为对照品,用紫外分光光度法测定榅桲子总黄酮含量准确度较高,方法 简便,切实可行.     

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.