反相高效液相色谱法测定Song木属植物中二萜酸,三萜酸和三萜皂苷的含量

为进一步探讨Ｓｏｎｇ木属草本自然群，木本自然群中植物的有效成分的差异，本首次建立了Ｓｏｎｇ木属植物中６种化学成分的反相高效液相色谱法，对本属１１种植物中该６种成分进行了定量分析。色谱柱为Ｓｕｐｅｌｃｏ ＳＩＬ－ＬＣ－１８，流动相为甲醇－１％乙酸－四氢呋喃（５００：１１０：１）；检测波长为２０５ｎｍ，流速１．２ｍｌ·ｍｉｎ＾－１，６种成分的线性范围分别为０．１３５￣２．１６０μｇ，０．１６３￣２．     

Antisense oligodeoxynucleotides downregulated c sis mRNA expression to inhibit proliferation of vascular smooth muscle cells 1

目的：研究ｃｓｉｓ反义寡脱氧核苷酸（ＯＤＮ）对ｃｓｉｓ表达及血管平滑肌细胞（ＶＳＭＣ）增殖抑制效应．方法：用合成ｃｓｉｓ正、反义ＯＤＮ培养ＶＳＭＣ;用液闪测定［３Ｈ］ＴｄＲ掺入并细胞计数,观察细胞增殖;用逆转录ＰＣＲ,评价ｃｓｉｓ表达．结果：ｃｓｉｓ反义ＯＤＮ２,４,６,８,１０μｍｏｌ·Ｌ－１抑制ＶＳＭＣ（１０３％±０７％,２２６％±０９％,３１０％±１１％,３５４％±０９％,４３３％±１２％）和降低［３Ｈ］ＴｄＲ掺入（６８％±０３％,９７％±０７％,２９０％±０６％,３２０％±０７％,５０６％±１３％）呈有剂量依赖性．反义ＯＤＮ１０μｍｏｌ·Ｌ－１培养细胞４ｄ,最大抑制率达６０３％±１０％,［３Ｈ］ＴｄＲ掺入降低５６３％±０９％,ｃｓｉｓｍＲＮＡ表达明显降低;而正义ｃｓｉｓＯＤＮ对ＶＳＭＣ无抑制,细胞数和［３Ｈ］ＴｄＲ掺入及ｃｓｉｓｍＲＮＡ水平与对照无差异．结论：ｃｓｉｓ反义ＯＤＮ明显下调ｃｓｉｓｍＲＮＡ表达,显著抑制ＶＳＭＣ增殖     

肉苁蓉类生药中苯乙醇甙类成分的 RP-HPLC 分析

采用反相高效液相色谱法，对４种及１变种肉苁蓉类生药和２５份商品药材所含的苯乙醇甙类成分进行了定性和定量分析，结果表明，荒漠肉苁蓉ＣｉｓｔａｎｃｈｅｄｅｓｅｒｔｉｃｏｌａＭａ，盐生肉苁蓉Ｃ．ｓａｌｓａ（Ｃ．Ａ．Ｍｅｙ）Ｇ．Ｂｅｃｋ，白花盐苁蓉Ｃ．ｓａｌｓａｖａｒ．ａｌｂｉｆｌｏｒａＰ．Ｆ．ＴｕｅｔＺ．Ｃ．Ｌｏｕ和管花肉苁蓉Ｃ．ｔｕｂｕｌｏｓａ（Ｓｃｈｅｎｋ）Ｗｉｇｈｔ所含成分相似，沙苁蓉Ｃ．ｓｉｎｅｎｓｉｓＧ．Ｂｅｃｋ区别较大；松果菊甙（ｅｃｈｉｎａｃｏｓｉｄｅ）和类叶升麻甙（ａｃｔｅｏｓｉｄｅ）的含量以盐生肉苁蓉最高，分别为２１３％和１５１％。采用ＡｌｔｉｍａＣ１８，５μｍ，２５０×４６ｍｍ色谱柱；乙腈─１５％乙酸水溶液，其中乙腈浓度从８％→２０％，０～６０ｍｉｎ线性梯度洗脱，作为定性分析流动相，乙腈浓度从１１５％→２０％，０～３５ｍｉｎ线性梯度洗脱，作为定量分析流动相；流速１２ｍｌ·ｍｉｎ－１，ＵＶ３３５ｎｍ检测。     

膜荚黄芪毛状根中异黄酮成分的反相高效液相色谱分析

对膜荚黄芪毛状根中６种异黄酮成分进行了反相高效液相色谱法测定。色谱柱为ＮｕｃｌｅｏｓｉｌＣ１８柱，流动相为甲醇—水（３∶２和３∶１，ｖ／ｖ），检测波长为２５４ｎｍ和２８０ｎｍ。６种异黄酮成分为：１０羟基３，９二甲氧基紫檀烷，（３Ｒ）８，２’二羟基７，４’二甲氧基异黄烷，芒柄花素（７羟基４’甲氧基异黄酮），８，３’二羟基７，４’二甲氧基异黄酮，２’羟基３’，４’二甲氧基异黄烷７Ｏ葡萄吡喃糖甙，毛蕊异黄酮（７，３’二羟基４’甲氧基异黄酮）。异黄酮浓度在２５～１２５μｇ范围内与峰面积有良好的线性关系；加样回收率为９６４７％～１０３３３％；精密度试验相对标准偏差为２５７％～６５２％；测得黄芪毛状根中６种异黄酮成分的含量在００００５％～０００６５％之间。     

高效液相色谱法测定双扑伪麻片中扑热息痛、盐酸伪麻黄碱、扑尔敏的含量

用高效液相色谱法,同时分离测定双扑伪麻片中扑热息痛、盐酸伪麻黄碱和扑尔敏的含量．线性范围：扑热息痛０２０～０８０ｇ／Ｌ,ｒ＝０９９９５;盐酸伪麻黄碱００１２～００４８ｇ／Ｌ,ｒ＝０９９９６;扑尔敏００００７２～０００２８８ｇ／Ｌ,ｒ＝０９９９２．平均回收率（ｘ±ｒｓｄ）％分别为：扑热息痛（１００２±１７）％;盐酸伪麻黄碱（９９６±１４）％;扑尔敏（９８４±２６）％．     

莶脂溶性成分的研究

从莶（ＳｉｅｇｅｓｂｅｃｋｉａｏｒｉｅｎｔａｌｉｓＬ）的地上部分，分离出八个化合物，其中Ｉ和Ｉ根据理化性质和光谱数据确定其结构为ｅｎｔ１７ａｃｅｔｏｘｙ１８ｉｓｏｂｕｔｙｒｙｌｏｘｙ１６（α）ｋａｕｒａｎ１９ｏｉｃａｃｉｄ（Ｉ）和ｅｎｔ１７ｅｔｈｏｘｙ１６（α）ｋａｕｒａｎ１９ｏｉｃａｃｉｄ（ＩＩ），均为新化合物，分别被命名为莶酯酸（ｓｉｅｇｅｓｅｓｔｅｒｉｃａｃｉｄ，Ｉ）和莶醚酸（ｓｉｅｇｅｓｅｔｈｅｒｉｃａｃｉｄ，Ｉ）。其余化合物分别鉴定为腺梗莶萜醇酸（ｅｎｔ１６β，１７ｄｉｈｙｄｒｏｘｙｋａｕｒａｎ１９ｏｉｃａｃｉｄ，ＩＩ），奇任醇（ｋｉｒｅｎｏｌ，ＩＶ，β谷甾醇葡萄糖甙（βｓｉｔｏｓｔｅｒｏｌｇｌｕｃｏｓｉｄｅ，Ｖ），二十一醇（ｈｅｎｅｉｃｏｓａｎｏｌ，ＶＩ），花生酸甲酯（ｍｅｔｈｙｌａｒａｃｈｉｄａｔｅ，ＶＩＩ）和β谷甾醇（βｓｉｔｏｓｔｅｒｏｌ，ＶＩＩ）。除奇任醇和β谷甾醇外，均为首次从该植物中分得。     

太白木忽木根皮中三萜皂甙成分研究

从太白木忽木（ＡｒａｌｉａｔａｉｂａｉｅｎｓｉｓＺ．Ｚ．ＷａｎｇｅｔＨ．Ｃ．Ｚｈｅｎｇ）根皮中首次分离到四个三萜皂甙，根据理化性质和光谱数据，分别鉴定为齐墩果酸３Ｏ［βＤ吡喃木糖（１→２）］［βＤ吡喃葡萄糖（１→３）］βＤ吡喃葡萄糖醛酸甙（１），ｔａｒａｓａｐｏｎｉｎＶ（２），３Ｏ｛βＤ吡喃木糖（１→２）［βＤ吡喃葡萄糖（１→３）］βＤ吡喃葡萄糖醛酸乙酯｝齐墩果酸２８ＯβＤ吡喃葡萄糖甙（３）和３Ｏ｛βＤ吡喃木糖（１→２）［βＤ吡喃葡萄糖（１→３）］βＤ吡喃葡萄糖醛酸丁酯｝齐墩果酸２８ＯβＤ吡喃葡萄糖甙（４）。１为新天然产物，３和４为新化合物，分别命名为太白木忽木皂甙ＶＩ（ｔａｉｂａｉｅｎｏｓｉｄｅＶＩ）、太白木忽木皂甙ＶＩＩ（ｔａｉｂａｉｅｎｏｓｉｄｅＶＩＩ）和太白木忽木皂甙ＶＩＩ（ｔａｉｂａｉｅｎｏｓｉｄｅＶＩＩ）。     

Triterpenoid Saponins from the Root Bark of Araliataibaiensis

从太白木（ＡｒａｌｉａｔａｉｂａｉｅｎｓｉｓＺ．Ｚ．ＷａｎｇｅｔＨ．Ｃ．Ｚｈｅｎｇ）根皮中首次分离得到四个三萜皂甙，根据理化性质和光谱数据，分别鉴定为齐墩果酸３Ｏ［βＤ吡喃木糖（１→２）］［βＤ吡喃葡萄糖（１→３）］βＤ吡喃葡萄糖醛酸甙（１），ｔａｒａｓａｐｏｎｉｎⅤ（２），３Ｏ｛［βＤ吡喃木糖（１→２）］［βＤ吡喃葡萄糖（１→３）］βＤ吡喃葡萄糖醛酸乙酯｝齐墩果酸２８ＯβＤ吡喃葡萄糖甙（３）和３Ｏ｛［βＤ吡喃木糖（１→２）］［βＤ吡喃葡萄糖（１→３）］βＤ吡喃葡萄糖醛酸丁酯｝齐墩果酸２８ＯβＤ吡喃葡萄糖甙（４）。１为新天然产物，３和４为新化合物，分别命名为太白木皂甙Ⅵ（ｔａｉｂａｉｅｎｏｓｉｄｅⅥ）、太白木皂甙Ⅶ（ｔａｉｂａｉｅｎｏｓｉｄｅⅦ）和太白木皂甙Ⅷ（ｔａｉｂａｉｅｎｏｓｉｄｅⅧ）。     

离子对反相高效液相色谱法测定头孢三嗪、7-氨基头孢菌烷酸及7-氨基头孢烯三嗪酸的含量

用四丁基溴化铵离子对试剂，在Ｃ１８色谱柱上同时测定头孢三嗪产品，７氨基头孢菌烷酸原料及７氨基头孢烯三嗪酸中间体的含量。流动相为乙腈—四丁基溴化铵—ｐＨ７０磷酸盐缓冲液—水（３２∶０３２∶４４∶６３６），检测波长２７０ｎｍ。结果表明：７氨基头孢菌烷酸浓度在９３６～２３４μｇ／ｍＬ，７氨基头孢烯三嗪酸浓度在１０４～２６０μｇ／ｍＬ，头孢三嗪浓度在１２９２～３２３μｇ／ｍＬ的范围均存在良好的线性关系，回收率分别在９９７％～９９９％，９９５％～９８％，１０００％～１００４％。     

Enantioselective Determination of R-(-)-and S-( )-Mexiletine in Microsomal Incubates by Capillary gas Chromatography

本文建立了同时测定大鼠肝微粒体孵育液中Ｒ（）和Ｓ（＋）美西律的气相色谱／火焰离子化检测方法。首先，将美西律从微粒体孵育液中提取出来；然后，与手性试剂Ｓ（）Ｎ三氟乙酰基脯氨酰氯反应形成酰胺类非对映体衍生物；最后，采用高分辨毛细管气相色谱分离测定。分析方法的线性范围为５０～５０００μｇ／ｍｌ；平均回收率Ｒ（）美西律是９３３１±５５９％，Ｓ（＋）美西律是９３１０±５１１％（ｎ＝１０）；检测限是１０μｇ／ｍｌ，定量限是５０μｇ／ｍｌ（ＲＳＤ＜１６５％）。该法已用于Ｒ（）和Ｓ（＋）美西律在大鼠肝微粒体中的氧化代谢研究     

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.