城南细辛化学成分研究(Ⅰ)

目的研究城南细辛的活性化学成分.方法利用柱层析方法分离化合物,理化性质以及光谱方法(UV、IR、NMR、MS)鉴定化合物.结果从城南细辛中离分得3个化合物,鉴定为1-细辛脂素(Ⅰ),1-芝麻脂素(Ⅱ)和β-谷甾醇(Ⅲ).结论化合物Ⅰ、Ⅱ、Ⅲ均为首次从该植物中分离得到.     

假地枫皮中黄酮类化合物研究

目的对假地枫皮进行化学成分研究。方法采用色谱和光谱法分离鉴定假地枫皮的化学成分。结果分离得到三个化合物,分别鉴定为槲皮苷(querc itrin,Ⅰ)、槲皮素(quercetin,Ⅱ)、未知化合物(Ⅲ)。结论Ⅰ、Ⅱ均为首次从该植物中分离得到。     

南葶苈子的化学成分

目的对十字花科植物播娘蒿(Descurainiasophia(L )WebbexPrantl)的种子南葶苈子提取物的化学成分进行分离鉴定。方法南葶苈子的乙醇提取物经D10 1大孔树脂用水及不同体积分数的乙醇洗脱,硅胶柱色谱分离,通过波谱( 1H NMR ,13 C NMR)分析和化学方法鉴定其结构。结果所得到的2个化合物分别被鉴定为4 戊烯酰胺( 4 pentenamide ,Ⅰ)、5 羟甲基糠醛( 5 hydrox ymethylfurfural,Ⅱ)。结论化合物Ⅰ为一个新天然产物;化合物Ⅱ为首次从播娘蒿属植物中分离得到。     

楤木化学成分的研究

目的 研究楤木的化学成分.方法 采用硅胶柱层析、Sephadex LH-20、ODS柱层析、半制备型高效液相色谱等分离方法进行分离纯化,经理化性质和波谱数据分析鉴定化合物结构.结果 分离鉴定了4个三萜皂苷类化合物,分别鉴定为elatoside K methyl ester(Ⅰ)、araloside Amethyl ester(Ⅱ)、pseudoginsenoside RTl butyl ester (Ⅲ)和太白楤木皂苷Ⅰ(Ⅳ).结论 化合物Ⅰ为新化合物,化合物Ⅱ～Ⅳ均为首次从该植物中分离得到.     

桑椹的化学成分

目的对桑科植物桑 (MorusalbaL .)的果实桑椹醇提取物中的化学成分进行提取分离和结构鉴定。方法色谱技术进行分离 ,MS、NMR和IR光谱解析及与对照品比较鉴定化合物。结果共分离得到 7个化合物 ,根据理化性质和谱学分析鉴定了其中的 5个化合物 ,分别为 3 ,4 丙叉基苯甲酸 (2 ,2 dimethyl 1 ,3 dioxa benzo[d]pentane 6 carboxylicacid,Ⅰ )、水杨酸 (salicylicacid ,Ⅱ )、琥珀酸 (succinicacid ,Ⅲ )、胡萝卜苷 (daucosterol,Ⅳ )和己六醇 (1 ,2 ,3 ,4,5 ,6 hexanehexanol,Ⅴ )。结论化合物Ⅰ、Ⅱ、Ⅴ为首次从本属中分离得到的化合物     

黄心卫矛的化学成分研究

目的 研究黄心卫矛Euonymus macropterus Rupr.的化学成分.方法 采用色谱技术分离纯化,并通过波谱技术及理化性质鉴定化合物结构.结果 从黄心卫矛根部的乙醇提取物中分离得到6个化合物,分别鉴定为2-hydroxy hexacosanoicacid,ethyl ester(Ⅰ)、9,12-eicosadienoic acid(9Z,12Z)-,2-hydroxy-3-[[(9Z)-1-oxo-9-oetadecen-1-y1]oxy]pro-pyl ester(Ⅱ)、表木栓醇(Ⅲ)、羽扇豆醇(Ⅳ)、二十烷醇(Ⅴ)、硬脂酸(Ⅵ).结论 以上化合物均首次从黄心卫矛中分离得到,其中,化合物Ⅰ、Ⅱ、Ⅴ、Ⅵ为首次从卫矛属植物中分离得到,化合物Ⅰ首次作为天然产物分离得到.     

刺五加种子的化学成分

目的分离鉴定五加科五加属植物刺五加(Acanthopanaxsenticosus(Rupr .etMaxim .)Har rms)种子的75 % ( φ)乙醇提取物中的化学成分。方法用硅胶柱色谱进行分离纯化,根据理化性质和波谱数据进行结构鉴定。结果得到4个化合物,分别鉴定为:3 Оrhamnopyranosyl ( 1 2 ) ara binopyranosyloleanolicacid(化合物Ⅰ)、hederagenin 3 O βglucuronopyranoside(化合物Ⅱ)、oleanolicacid 3 O βglucuronopyranoside(化合物Ⅲ)和齐墩果酸(化合物Ⅳ)。结论化合物Ⅱ、Ⅲ为首次从该属植物中分得     

板蓝根化学成分研究

目的从板蓝根中分离化学成分。方法板蓝根95%乙醇提取物经硅胶吸附,不同溶剂洗脱部分经硅胶柱层析反复分离纯化,测定所得化合物的理化常数和波谱数据,鉴定其化学结构。结果从氯仿及正丁醇部位分离得5个化合物,分别鉴定为4—(1,2,3—三羟基丙基)—2,6—二甲氧基苯—1—O—β—D—葡萄糖苷(Ⅰ)、香草醛(Ⅱ)、甘露醇(Ⅲ)、琥珀酸(Ⅳ)、苯甲酸(Ⅴ)。结论化合物Ⅰ、Ⅱ、Ⅲ为首次从板蓝根药材中分离,具有一定的参考价值。     

南海海绵Hyrtios erectus的肿瘤细胞毒活性成分研究

目的对中国南海海绵Hyrtios erectus的细胞毒活性化学成分进行研究。方法采用多种色谱技术对化合物进行分离纯化,应用光谱技术和理化性质,结合文献对照,鉴定化合物的结构。并用MTT法测定化合物的细胞毒活性。结果从海绵Hyrtios erectus的脂溶性部分共分离得到5个化合物,其结构鉴定为:Hyr-tiosal(Ⅰ),12-βHydroxy-16-scalaren-24,25-olide(Ⅱ),5-Hydroxy-1H-indole-3-ethanol(Ⅲ),胆甾醇(Ⅳ),邻苯二甲酸二丁酯(V)。结论化合物为首次从海绵Hyrtios erectus中分离得到,化合物Ⅰ和Ⅱ显示了较强的细胞毒活性。     

苦味西葫芦果实的三萜类化学成分

目的对苦味西葫芦(Cucurbita pepocv.Dayangua)果实的抗炎活性部位的化学成分进行分离、鉴定。方法采用各种色谱技术进行分离,应用1H NMR1、3C NMR谱学技术确定化合物的结构。结果从抗炎活性部位分离得到4个化合物,分别鉴定为:乙酸蛇麻脂醇酯(lupeol acetate,Ⅰ)、β乙酸香树脂醇酯(βamyrin acetate,Ⅱ)i、somultiflorenol(Ⅲ)i、somultiflorenone(Ⅳ)。结论其中化合物Ⅰ、Ⅱ、Ⅲ为首次从南瓜属植物中分离得到,Ⅳ为首次从本植物中分离得到。     

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.     

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.     

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.