炮制方法对巴戟天糖类成分影响的研究

目的:比较不同炮制方法对巴戟天各糖类成分的含量及指纹图谱的影响。方法:采用紫外-可见分光光度法测定巴戟天各炮制品中醇溶性糖和水溶性糖的含量;采用高效液相色谱-蒸发光散射检测(HPLC-ELSD)法建立巴戟天糖类成分指纹图谱。结果:巴戟天不同炮制品中糖类成分含量与生品比较有差异;HPLC-ELSD法共确定14个主要共有峰,不同炮制品糖类组分相同,但相对含量有差异。结论:炮制方法对巴戟天糖类成分的溶出有影响。     

不同炮制方法对藤茶中双氢杨梅素含量的影响

目的:通过测定不同炮制方法制备的藤茶中双氢杨梅素的含量,探讨不同炮制方法对藤茶主要活性成分的影响。方法:分别采用微波炮制、传统炒制、水煮法对采自3个不同产地的新鲜藤茶进行加工炮制处理,制得藤茶不同炮制品;用自然晾干法处理得藤茶生品。采用高效液相色谱法测定不同藤茶炮制品和藤茶生品中双氢杨梅素的含量。结果:不同炮制方法对藤茶中主要活性成分含量有较大影响,其中微波炮制法所制备的藤茶中双氢杨梅素含量最高,传统炒制法含量与其相近;其次为水煮法;藤茶生品中双氢杨梅素的含量最低。结论:炮制可提高藤茶叶中双氢杨梅素含量,且以微波法炮制为佳。     

茯苓及其不同炮制品中总糖及多糖的含量分析

目的:考察茯苓生品及不同炮制品中总糖及多糖含量的变化,以确定不同炮制方法对总糖及多糖含量的影响。方法:硫酸-苯酚显色后用分光光度计测定吸收度,测定波长491nm。按照回归方程计算含量。结果:茯苓的不同炮制品中,总糖及多糖含量从高到低顺序依次为米汤制>明矾米汤制>土炒>朱砂制1>朱砂制2>生品。结论:不同的炮制方法对茯苓总糖及多糖的含量较生品有显著性增加。     

几种常见中药炮制工艺的摸索

目的探究几种常见有毒中药不同炮制方法对有毒成分含量的影响。方法分别采用蒸制、清炒、酒炙和醋炙这四种炮制方法对雷公藤、川乌以及麻黄三种常见的有毒中药进行炮制,并测定其不同炮制品的有毒成分生物碱的含量,比较该三种炮制方法对其有毒成分生物碱含量影响。结果雷公藤的各炮制品的生物碱的含量从高到低:醋炙>酒制>清炒>蒸制;川乌的各炮制品的生物碱的含量从高到低:醋炙>清炒>酒制>蒸制;麻黄的各炮制品的生物碱的含量从高到低:清炒>醋炙>酒制>蒸制。雷公藤及川乌:与生品的生物碱含量比较,醋炙炮制品的生物碱含量无统计学差异(P>0.05),三种炮制品的生物碱含量均有明显差异(P<0.05);麻黄:与生品的生物碱含量比较,三种炮制品的生物碱含量均有明显差异(P<0.05)。结论蒸制炮制在降低药物的毒性效果优于清炒炮制法、酒炙炮制法及醋炙炮制法。     

地黄不同炮制品中梓醇含量比较

目的 :探讨不同炮制方法对地黄中梓醇含量的影响。方法 :用双波长薄层扫描法对不同地黄炮制品中梓醇含量进行检测。结果 :地黄不同炮制品与生品中梓醇的含量有显著性差异。结论 :不同的炮制方法及辅料可使地黄炮制前、后梓醇的含量发生变化。     

不同炮制方法对木香中有效成分含量的影响

目的 探讨不同炮制方法对木香炮制品的影响.方法 通过HPLC法测定6种炮制方法(纸煨、滑石粉煨、麦麸煨、清炒、麦麸炒、酒制)的木香中有效成分,以木香烃内酯、去氢木香内酯的含量为评价指标,比较不同炮制方法对木香中有效成分的影响.结果 炮制品与生品比较,各指标性成分都有所降低.结论 不同炮制方法制得的木香炮制品在有效成分含...     

何首乌炮制工艺的研究

目的:优化何首乌高压炮制工艺,比较其与传统炮制工艺的差异。方法:采用正交设计,以水浸出物、二苯乙烯苷、水溶性糖含量为指标优化何首乌高压炮制工艺;比较高压炮制品与传统炮制品各指标含量、高效液相指纹图谱、不同分子量糖百分含量比的差异。结果:高压炮制何首乌影响因素大小依次为蒸制温度>蒸制时间>干燥温度;高压炮制法和传统炮制法热动力过程不同,所炮制的何首乌无论是醇溶性成分变化还是多糖分子量变化都存在差异。结论:高压炮制法能否代替传统炮制法,需药效学的进一步验证。     

电子鼻区分牛膝及其不同炮制品气味的初步研究

目的:建立区分牛膝及其不同炮制品气味的方法。方法:制备牛膝生品、黄酒炙牛膝、白酒炙牛膝、盐水炙牛膝、清水炙牛膝,并按相应炮制方法制成泛糖牛膝炮制品。采用电子鼻分析上述牛膝及其炮制品气味:数据获取持续时间为200 s,获取周期为1 s,延滞时间为1 080 s,空气流速为150 mL/min,进样体积为2.5 mL,进样速度为500μL/s,孵化时间为300 s,孵化温度为40℃,冲洗时间为120 s,进样器温度为50℃,搅动速度为500 r/min。结果:与牛膝生品比较,4种炮制品的气味存在显著差异;盐水炙牛膝与牛膝生品气味的相对距离最近,白酒炙牛膝与牛膝生品气味的相对距离最远。可根据气味的相对距离判断(泛糖)牛膝炮制品的工艺是否相同。结论:电子鼻能够快速区分牛膝及其不同炮制品的气味。     

金樱根不同炮制品中总黄酮的含量测定

目的考察金樱根生品及其不同炮制品中总黄酮含量的变化,以确定不同炮制方法对总黄酮含量的影响。方法采用紫外-可见分光光度法测定金樱根不同炮制品的总黄酮含量。结果总黄酮含量为:醋制品(7.83%),盐制品(6.63%),黑豆汁制品(6.01%),生品(5.88%)。结论不同炮制方法对金樱根中总黄酮含量的影响较大。     

不同炮制方法对黄芪化学成分的影响

目的探讨不同炮制方法对于黄芪制品中黄酮类及糖类成分的影响。方法将统一产地及批次的黄芪通过不同的炮制方式转变为酒黄芪、米黄芪、炒黄芪、盐黄芪及蜜黄芪,分析不同方式炮制的黄芪中含有的糖类及黄酮类成分的变化情况。结果黄酮类:酒黄芪中毛蕊异黄酮的含量相对于生黄芪明显增加;蜜黄芪中黄酮类成分含量明显下降,而盐黄芪、米黄芪对黄酮类成分的影响不明显。糖类:水溶性糖在不同炮制方式中的含量由高到低依次为生黄芪米黄芪酒黄芪盐黄芪炒黄芪;还原性糖:生黄芪米黄芪酒黄芪盐黄芪炒黄芪;多糖:酒黄芪盐黄芪炒黄芪米黄芪生黄芪,以酒炙黄芪最高。结论不同的炮制方式会对黄芪中的有效成分含量产生明显的影响,黄酮类以酒制增加最为明显,蜜制则下降明显;多糖类也亦酒制增加明显,而水溶性糖及还原性糖则通过炮制后含量下降,以盐黄芪下降最明显。     

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.