正交实验优选栀子苷的提取工艺

目的:优选栀子中栀子苷的最佳提取工艺。方法:采用正交实验法对栀子苷的提取工艺进行研究,采用高效液相色谱法测定提取物中栀子苷的含量,采用方差分析确定栀子的最佳提取工艺。结果:栀子的最佳提取工艺为乙醇的浓度为80%,加醇量为10倍,提取时间1.5h,提取次数为2次,在此工艺下验证测得栀子苷平均含量为6.1854%。结论:栀子的提取方法简便易行,质量控制方法可靠。     

正交试验法优选复方黄芩喷雾剂的提取工艺

目的:优选出复方黄芩喷雾剂的乙醇渗漉最佳提取工艺。方法:以黄芩苷为检测指标,高效液相色谱法测定黄芩苷,采用正交试验考察各因素对黄芩苷含量的影响。结果:影响因素为:饮片粒度>乙醇浓度>乙醇量>浸泡时间。结论:复方黄芩喷雾剂乙醇渗漉最佳提取工艺为70%乙醇10倍量、粗粉药材、浸泡24h渗漉。     

比较和优化党参炔苷的提取工艺

目的优选党参炔苷的提取工艺。方法比较煎煮法、乙醇回流法、渗滤法,应用正交试验筛选党参炔苷的提取工艺,以提取液中党参炔苷的含量作为评价指标。结果最佳提取方法为渗漉法,加100 ml 65%乙醇浸泡48 h后渗滤,流速为9 m.lmin-1。结论优选得到的工艺简便易行,稳定性好。     

正交试验法优选扶正防喘颗粒的提取工艺

目的优选扶正防喘颗粒剂的最佳提取工艺.方法采用L9(34)正交试验,以丹参酮ⅡA、补骨脂素及异补骨脂素的含量为指标,以乙醇浓度、用量、浸润时间及渗漉速度为考察因素,筛选扶正防喘颗粒剂最佳醇提取工艺;以出膏率为指标,以加溶媒用量、提取次数和提取时间为考察因素,筛选扶正防喘颗粒剂的最佳水提取工艺条件.结果扶正防喘颗粒剂脂溶性成分的提取优选渗漉法,渗漉法提取的最佳工艺条件为加95%乙醇、6倍药材的渗漉收集液、浸润时间为48 h、渗漉速度为2 mL·min-1;最佳水提取工艺条件为加12倍药材量水,煎煮3次,每次2 h.结论优选提取得到的提取工艺稳定、可行.     

正交试验优化补肾健骨片中青风藤的提取工艺

目的:研究补肾健骨片中青风藤乙醇提取的最佳工艺。方法:以乙醇为溶剂采用浸渍法、连续渗漉法、回流法对药材进行提取工艺优选;以青藤碱含量为指标,以乙醇浓度、乙醇用量、药材粒度、pH值为考察因素,优选提取工艺。结果:最佳提取工艺为采用连续渗漉法,药材粉碎过10目筛,氨水调节pH8～9的12倍量75%乙醇提取。结论:本工艺稳定、操作简便、质量可控,可用于工业化大生产。     

淫羊藿中淫羊藿苷提取工艺研究

目的:优选淫羊藿中淫羊藿苷的提取工艺。方法:以淫羊藿苷提取转移率为考察指标,对不同提取方法和提取条件进行考察。结果:最佳提取工艺为采用渗漉法,用60%～75%乙醇作溶媒,收集渗漉液的量为药材的8倍。此时,淫羊藿苷提取转移率为90%。结论:该提取工艺效率高、节约能源,方法可行。     

复方六月雪颗粒提取工艺研究

目的 :优选复方六月雪颗粒提取工艺的最佳条件。方法 :先对处方中的药材用乙醇渗漉提取 ,药渣再用水煎煮提取。以齐墩果酸、总黄酮含量为评价指标 ,用正交设计法对两步提取工艺条件进行考察。结果 :以80 %的乙醇为渗漉溶媒 ,溶媒用量为药材量的8倍 ,浸渍时间24h作为乙醇渗漉提取的最佳工艺条件 ;以加水量为药材量的12倍 ,每次煎煮1 5h ,共煎煮3次作为水煎煮提取的最佳工艺条件。结论 :优选出的最佳工艺条件经验证其结果稳定 ,指标性成分含量高 ,可以用于投入生产。     

渗漉法提取祖师麻叶有效成分

目的:优选祖师麻叶有效成分的最佳渗漉提取工艺.方法:以总黄酮和祖师麻甲素提取率为评价指标,用综合评分法进行数据处理,采用正交试验考察乙醇体积分数、乙醇用量、浸泡时间、滴速对提取效果的影响.结果:祖师麻叶有效成分最佳渗漉提取工艺为:加12倍量的60%乙醇,浸泡36 h,流速3 ml·min-1.结论:该渗漉工艺参数合理,结果可靠,提取效果较好.     

中药栀子提取工艺的实验研究

目的:优选栀子药材的提取工艺.方法:采用直接比较法、正交试验设计法,以HPLC法测定各样品中栀子苷的含量为指标,比较了提取方法和提取溶媒种类、溶媒用量、提取时间、提取次数对栀子苷含量的影响,并比较不同条件下的醇沉工艺.结果:以10倍量水,提取3次,每次提取1.5h为最优工艺,醇沉条件为提取液浓缩至相对密度为1.12(60℃),醇沉浓度为60%.结论:该工艺稳定、可行.     

正交设计法优选骨痛贴膏乙醇渗漉提取工艺

目的:优选骨痛贴膏的乙醇渗漉提取工艺条件.方法:以欧前胡素提取量为考察指标,用高效液相色谱法测定欧前胡素含量,以乙醇浓度、乙醇用量、浸泡时间、渗漉速度为影响因素,选用L9(34)表进行正交试验.结果:优选工艺为:药材用10倍量的90%乙醇浸泡12 h,以7 ml·min-1·kg-1速度渗漉提取.结论:优选工艺提取的欧前胡素含量较高,而浸膏量较低.     

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.     

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.     

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.