野菊花膏粉质量标准研究

目的 建立野菊花膏粉的质量标准.方法 采用薄层色谱法定性鉴别,分光光度法测定总黄酮含量.结果 在薄层色谱法中检出野菊花,芦丁在8～48 mg·L-1范围内呈良好的线性关系,r=0.9997,平均回收率为98.6%,RSD=1.1%.结论 该方法结果准确、重现性好,可用于该制剂的质量控制.     

野菊花中总黄酮的提取

目的研究野菊花中总黄酮的最佳提取工艺。方法采用正交试验,以提取次数、提取时间、提取温度、溶剂用量4个因素研究水提野菊花的最佳工艺。结果最佳提取工艺为水提取野菊花2次,2次溶剂用量依次为8倍和6倍,提取温度100℃,提取时间都为40 min。结论本文所用工艺提取野菊花总黄酮工艺简单、提取率高、操作控制容易、稳定性好、适合于工业化生产。     

优化枳椇子的提取工艺

目的　确定枳椇子干浸膏的最佳提取工艺?椒ā∫愿山嗟寐屎透山嘀凶芑仆课副?,对索式提取器提取的方法、渗滤法和浸渍法进行筛选。结果　渗滤法出膏率和干浸膏中黄酮含量最高,索式提取次之,浸渍法出膏率和干浸膏中黄酮含量最低。结论　渗滤法提取干浸膏简单易行,成本低廉,适合批量生产。     

番石榴叶总黄酮提取工艺的优选

目的:用正交试验法优选番石榴叶中总黄酮的提取工艺。方法:以干浸膏中总黄酮的含量作为主要评价指标,以出膏率作为次要评价指标,选择醇沉浓度、提取时间、料液比、提取次数为考察因素,采用正交试验法确定了番石榴叶中总黄酮的最佳工艺,采用分光光度法对干浸膏中总黄酮的含量进行测定,检测波长502nm。结果:最佳提取工艺条件为醇沉浓度70%,提取时间2h,料液比1∶18,提取次数2次。芦丁在8.32~49.92mg.L-1浓度范围之内呈良好的线性关系。平均回收率为99.21%,RSD为1.04%。结论:总黄酮正交提取工艺的试验,结果比较可靠,含量测定方法简便、准确,可用于番石榴叶干浸膏中总黄酮的含量测定。     

正交试验优选野菊花中总黄酮的提取工艺

目的：优选野菊花中总黄酮的提取工艺。方法：以乙醇质量分数、加醇倍数、提取时间为考察因素,以野菊花总黄酮含量为评价指标,采用正交试验优选提取工艺。结果：最佳提取工艺为加12倍量50％乙醇,回流2次,每次1h。结论：所选工艺合理、可行,可用于野菊花中总黄酮的提取。     

降压益肾颗粒的提取工艺考察

目的：对降压益肾颗粒提取工艺进行优选。方法：采用正交试验法，以总黄酮含量和浸膏收率为指标，考察加水量、浸泡时间、煎煮时间和煎煮次数4因素及醇沉浓度对浸膏收率和有效成分的影响。结果：优化的提取工艺为用药材10倍量水，浸泡1h，每次煎煮1．5h，煎煮3次，醇沉浓度70％。结论：此工艺有效成分提取率高，重现性好，稳定可行。     

正交试验优选江南卷柏总黄酮提取工艺

目的:优选江南卷柏总黄酮的提取工艺。方法:以乙醇浓度、提取时间、提取次数、乙醇用量为考察因素,总黄酮含量、浸膏得率为指标,采用正交试验进行提取工艺优选。结果:江南卷柏总黄酮最佳提取工艺为乙醇浓度85%、提取时间1h、提取次数2次、9倍乙醇用量;总黄酮含量为0.1552g,浸膏得率为8.91%。结论:该方法简便、稳定,可用于江南卷柏总黄酮的提取。     

野菊花不同部位总黄酮含量的比较

目的测定野菊花不同部位中总黄酮的含量。方法选用山东蒙山产野菊花,采用比色法进行测定。结果叶中总黄酮含量最高。结论野菊花不同部位中总黄酮的含量有较明显的差异。     

正交试验优选独一味总黄酮的提取工艺

目的建立独一味黄酮类成分的提取工艺。方法采用L9(34)正交设计法,以独一味总黄酮含量、山栀苷甲酯和8-O-乙酰山栀苷甲酯含量以及出膏率为检测指标进行试验。结果优选的提取工艺为,70%乙醇,提取3次、每次1.5 h,溶剂用量10倍。结论优选的独一味总黄酮类成分提取工艺简便、省时、节约成本,适合工业化生产。     

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。     

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.