利用响应面分析法优化金银花中的绿原酸的超声提取工艺

目的 优化金银花中绿原酸的超声提取工艺。方法 以绿原酸得率为指标,采用响应面分析法,考察料液比、提取时间、乙醇浓度等不同因素对提取条件的影响,优选最佳提取工艺。结果 超声提取法的最佳提取条件为：料液比为1∶14,乙醇浓度为58%,提取时间为27 min,绿原酸得率为1.39%。结论 该优化工艺简便稳定、重复性好,可用于金银花绿原酸的提取。     

利用响应面分析法优化金银花中的绿原酸的超声提取工艺

目的优化金银花中绿原酸的超声提取工艺。方法以绿原酸得率为指标,采用响应面分析法,考察料液比、提取时间、乙醇浓度等不同因素对提取条件的影响,优选最佳提取工艺。结果超声提取法的最佳提取条件为：料液比为1∶14,乙醇浓度为58%,提取时间为27 min,绿原酸得率为1.39%。结论该优化工艺简便稳定、重复性好,可用于金银花绿原酸的提取。     

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。     

正交试验法优化忍冬叶中总黄酮的提取工艺

目的：确定提取忍冬叶总黄酮的最佳工艺备件。方法：采用正交试验法，分别考察乙醇冷浸、回流和超声提取对提取率的影响，并与乙醇索氏提取以及水提取最佳工艺比较。用分光光度法测定总黄酮含量。结果：在不同的乙醇提取工艺中，总黄酮含量高低顺序为回流法≈索氏提取法＞超声法≈冷浸法。在不同的水提取工艺中，总黄酮含量高低顺序为回流法＞超声法≈碱水冷浸法＞冷浸法。结论：提取忍冬叶总黄酮的最佳备件为：12倍量60％乙醇，水浴回流提取2次，每次1．5h。     

正交实验法优选药用红树植物老鼠簕总黄酮提取工艺

目的以老鼠簕为对象,优选出两种黄酮提取工艺中的最佳提取条件。方法利用L_9(3~4)正交设计法优选药用红树植物老鼠簕总黄酮提取工艺,以老鼠簕总黄酮含量为指标,分别对索氏提取中的乙醇浓度、提取温度、提取时间和超声提取法中提取时间、乙醇浓度、液料比等因素进行考查,优选老鼠簕总黄酮的最佳提取条件。结果索氏提取法中,提取温度对总黄酮提取率影响最大,最佳提取条件为60%乙醇提取液,在85℃下提取2.5h。超声提取法中,乙醇浓度对提取率的影响最大,提取最佳条件为50%乙醇提取液,液料比为40:1,浸提50min,提取2次。结论超声提取方法优于索氏提取法,总黄酮提取量可达3.82%。     

药用菊花总黄酮提取方法的比较

目的 优化药用菊花总黄酮提取工艺.方法 通过对冷浸法、索提法、回流法、超声法等几种提取方法的研究和比较,采用正交试验设计优选药用菊花总黄酮的最佳提取工艺.结果 不同处理方法所得结果不同,李氏提取法(甲醇)所得浸膏重量及其得率均最高;超声法(70%乙醇)所得总黄酮含量及得率最高.结论 超声法为药用菊花总黄酮的最佳提取方法,其最佳提取条件是溶剂为70%乙醇,料液比为1:30,超声温度为60℃,超声时间为30min.     

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。     

超声提取麦冬总黄酮的工艺研究

目的 优化超声技术提取麦冬总黄酮的工艺条件.方法 采用L9(34)正交试验法,考察乙醇浓度、乙醇用量、提取时间、提取次数对超声提取的影响,以总黄酮含量为考核指标,确定最佳提取条件.结果 最佳提取工艺为加12倍生药量的60%乙醇,超声提取3 次,每次45min.结论 此方法 是一种简单、快捷、高效、可行的提取.     

复方槐花颗粒中槐花和侧柏叶总黄酮提取工艺的优化

目的 优选复方槐花颗粒中槐花和侧柏叶总黄酮最佳提取工艺。方法 采用超声浸提法对复方槐花颗粒中槐花和侧柏叶总黄酮进行提取,以乙醇体积分数、超声功率、超声时间和料液比为考察因素,通过单因素试验和正交优选,确定较优提取工艺,并与常规的热回流提取法进行比较研究。结果 超声浸提法最佳提取工艺条件为：用60%乙醇,在料液比1:10和超声功率40kHz条件下超声波辅助连续提取2次,每次15min,槐花和侧柏叶总黄酮提取率可达93.31%。结论 该工艺研究为复方槐花颗粒中槐花和侧柏叶总黄酮共提提供一种新方法和思路,具有耗时短、能耗低、溶剂用量少和提取效率高等优势。     

超声法与连续回流法提取黄芪总黄酮的工艺对比研究

目的:对比研究超声法和连续回流法提取黄芪总黄酮的工艺。方法:以乙醇浓度、提取时间、固液比、提取温度为考察因素,黄芪总黄酮提取率为考察指标,采用正交试验优选最佳提取工艺条件。结果:要获得相同的提取率,超声法效率更高,其最佳提取工艺为乙醇浓度75%,超声提取时间20min,固液比1∶10,超声提取温度25℃,提取率为0.325%。结论:与连续回流法比较,采用超声法提取黄芪总黄酮具有快速、节省溶剂、提取的有效成分含量高等优点。     

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.     

Nachweis einiger Heilmittel in der Kniegelenksynovialflüssigkeit

Zusammenfassung Mittels Gaschromatographie und Dünschichtchromatographie wiesen die Autoren 11 Substanzen nach, welche durch Injektion oder nach Verabreichung per os in die Kniegelenksynovialflüssigkeit eindrangen. In ihrer Aufstellung konnten sie eine direkte Beziehung zwischen Struktur sowie chemischphysikalischen Eigenschaften der Substanz und ihrer Fähigkeit, aus dem Blut in die Kniegelenksynovialflüssigkeit einzudringen, nicht nachweisen, außer der Tatsache, daß Substanzen mit starker Affinität zu Eiweißstoffen erst in höheren Dosen nachweisbar waren.     

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.