胶束电动毛细管色谱法测定牡丹皮及六味地黄丸中丹皮酚的含量

目的用胶束电动毛细管色谱法分离测定中药材牡丹皮及中成药六味地黄丸中丹皮酚的含量。方法定量采用内标法 ,选取芦丁为内标。所用毛细管规格为 5 5cm(有效长度 5 0cm)× 75 μm,检测波长 2 74nm ,电压 1 5kV ,背景电解质分别为 30mmol/LSDS -30mmol/L硼砂 ,2 0mmol/LSDS -5 0mmol/L硼砂 ( pH 9 4 )。 结果线性分别为 6～ 4 2mg/L,1 8 2～ 91mg/L;相关系数分别为0 9995和 0 9997;RSD为 1 95 %和 3 6 %;加样回收率为 1 0 1 5 %～ 1 0 3 3%和 97 7%～1 0 1 9%。丹皮酚含量分别为 1 5 9%和 0 1 4 8%。结论胶束电动毛细管色谱法用于测定牡丹皮及六味地黄丸中丹皮酚的含量是可行的。     

苯磺酸氨氯地平对映体的高效毛细管电泳手性分离

目的：建立一种快速有效拆分苯磺酸氨氯地平对映体的分析方法。方法：采用高效毛细管电泳法。以羟乙基-β-环糊精为手性选择剂对苯磺酸氨氯地平对映体进行拆分,并考察了缓冲液的pH值、手性选择剂的浓度、缓冲液浓度、电压及柱温等对分离效果的影响。结果：确定了最佳分离条件：背景电解质为含30mmol·L^-1羟乙基-β-环糊精的100mmol·L^-1磷酸-三乙醇胺（pH4．0）体系,电压为28kV,柱温为20℃,进样压力为6kPa·s,检测波长为214nm。在此条件下,10分钟内完全分离了1．0g·L^-1苯磺酸氨氯地平外消旋体,分离度为4．5,并测得3批市售苯磺酸左旋氨氯地平片的光学纯度均不低于99．6％。结论：该法可快速有效地分离苯磺酸氨氯地平对映体,可用于其手性拆分及光学纯度测定。     

卡托普利致急性血尿1例

病例】　男 ,55y。高血压病史 2 0 a,脑出血病史 1 7a伴右上、下肢瘫痪 ,混合性失语 ,近 1 d因小便失禁 ,于 2 0 0 0年 3月 2 1日入院。查体 :BP2 2 .5/1 3.3k Pa(1 70 /1 0 0 mm Hg)。血常规 :RBC3.2×1 0 12 /L,Hb 95g/L,WBC 5.2× 1 0 9/L,N 0 .82 ,L0 .1 7。尿常规 :颜色黄 ,透明度清 ,反应碱 ,蛋白 (- ) ,白细胞 (- ) ,红细胞 (- ) ,上皮细胞 (- ) ,管型 (- )。电解质 :Na+1 32 .3mmol/L,K+3.36mmol/L,Cl-1 0 6.0 mmol/L,Ca++1 .8mmol/L,BUN 1 0 .76mmol/L,余查 (- )。入院后给予卡托普利 (常州制药厂 ,批号 991 0 2 2 - 2…     

毛细管电泳法分离硝基喜树碱的同分异构体

目的 :建立分离硝基喜树碱同分异构体的毛细管电泳分析法。方法 :用未涂渍熔融石英毛细管 ( 4 8.5 cm× 5 0 μm,有效长度 40 cm) ,以 40 mmol/L 硼砂 -4 0 mmol/L十二烷基硫酸钠、溶剂以水∶甲醇 =9∶ 1(磷酸调节 p H=8.0 )为缓冲液 ,运行电压 2 0 k V,温度 2 5℃ ,检测波长 2 40 nm。结果 :硝基喜树碱的一对同分异构体能够达到基线分离。 p H值和电压对其分离度影响较小 ;温度和 SDS的浓度对其分离度影响较大。 结论 :此方法可用于硝基喜树碱同分异构体的分离分析。     

MECC法测定玄参中哈帕酯苷和安格洛苷C的含量

用胶束电动毛细管色谱法以尼泊金丙酯为内标物测定玄参中哈帕酯苷和安格洛苷C的含量。色谱条件 :75 μm × 10 0cm毛细管柱 ;分离用缓冲液为 10 0mmol/L胆酸钠含 10 %乙腈和2 0mmol/L磷酸二氢钠 ,用 2 0mmol/L硼砂调节 pH 7 5 ;运行电压2 5kV ;温度 2 5℃ ;重力进样 ,时间5s ;检测波长 2 80nm。哈帕酯苷和安格洛苷C的平均回收率分别为 (10 2 5± 3 5 ) %和 (10 2 3±2 2 ) %。本法操作简便 ,结果准确     

人血高密度脂蛋白制备新工艺

以血浆制备白蛋白 (Cohn 6法 )后所产生的 F - 1沉淀为原料 ,采用低温乙醇工艺 ,经过 3步分离纯化 ,再用截留分子量 5 0 k D的超滤膜超滤脱醇浓缩后 ,加入 (10± 1) %(g/ m l)蔗糖作保护剂进行巴斯德病毒灭活 ,制得人血高密度脂蛋白。制品经 SDS- PAGE显示 ,纯度 85 %～ 95 %,载脂蛋白 A 分子量 2 7.3k D,活性 4.0× 10 6u/ g蛋白以上 ,载脂蛋白 A 回收率在 6 0 %以上。     

氧化型低密度脂蛋白和内皮素-1与肝病的关系

为探讨血浆氧化型低密度脂蛋白 (ox -LDL)和内皮素 -1 (CET -1 )与肝病的关系 ,采用单克隆抗体酶联免疫吸附双抗体夹心法和放射免疫分析均相竞争法分别检测不同型肝病患者和正常人血浆中的ox -LDL和ET -1含量。结果 ,ox -LDL急性肝炎组为 ( 0 .4 2± 0 .0 7)mg/L ,慢性肝炎组为( 0 .4 4± 0 .0 8)mg/L ,肝硬变组为 ( 0 .4 8± 0 .0 8)mg/L ,肝癌组为 ( 0 .4 6± 0 .0 9)mg/L ,均显著高于正常人的 ( 0 .3 2± 0 .0 7)mg/L(P <0 .0 5) ;ET -1急性肝炎组为 ( 6.9± 1 .7)ng/L ,慢性肝炎组 ( 1 2 .4± 2 .5)ng/L ,肝硬变组 ( 1 7.5± 3 .6)ng/L ,肝癌组 ( 1 8.1± 3 .4 )ng/L ,均高于正常人组的 ( 6.1± 1 .4 )ng/L( P <0 .0 5) ;ox -LDL及ET -1的含量在不同肝病患者间也存在差异 ,与病情的严重程度相平行 ,二者呈明显正相关 (r =0 .764 9,P <0 .0 5)。     

毛细管电泳-激光诱导荧光分离检测手性5-(2-氨基丙基)-2-甲氧基苯磺酰胺对映体

目的建立毛细管电泳——激光诱导荧光法分离测定(R/S)-5-(2-氨基丙基)-2-甲氧基苯磺酰胺对映体。方法用异硫氰酸荧光素衍生(R/S)-5-(2-氨基丙基)-2-甲氧基苯磺酰胺,衍生产物在70mmol/L的硼砂(pH=9.5)缓冲液中用毛细管电泳分离,激光诱导荧光方法测定。结果(R/S)-5-(2-氨基丙基)-2-甲氧基苯磺酰胺对映体得到了基线分离,线性范围均为8.20×10-8～9.02×10-7mol/L。结论本方法简单,精密度高,灵敏度高,可为盐酸坦索罗辛的质量控制提供方法。     

葡萄糖异黄酮致急性溶血1例

【病例】女 ,74y。因“反复头晕 4a,再发 2 d”而住院。查体 :体温 (t) 3 6 .2℃ ,脉搏 (P) 78beats/min,呼吸 (R) 1 8beats/min,血压 (BP) 1 3 5 /83mm Hg(1 8/1 1 k Pa) ,神清 ,全身皮肤无黄染 ,无皮疹及淤斑 ,心、肺、腹未见异常 ,病理反应未引出 ;查血常规 :WBC 6 .3× 1 0 9/L,N 0 .6 1 ,L 0 .3 9,RBC 4.42× 1 0 12 /L,PLT1 1 1× 1 0 9/L,Hb1 2 8g/L;肝功能 :D- Bil1 .0 ︼mol/L,T- Bil1 0 .2 ︼mol/L,A/G3 8/2 5g/L,ALT3 2 U/L,AST3 3 U/L,AKP5 4 U/L,GGT2 2 U/L;尿常规 :(- )。 TCD:脑动脉弹性减退。给予葡…     

大鼠体内硝基精氨酸的手性代谢动力学

目的　应用毛细管电色谱 (CEC)对大鼠体内的硝基精氨酸手性转化和代谢动力学进行研究。方法　采用手性配体交换法检测大鼠血浆中D型硝基精氨酸 (D NNA)和L型硝基精氨酸(L NNA)的浓度,应用非房室模型对所获得的血药浓度-时间数据进行拟合,计算药动学参数。结果　D NNA和L NNA在大鼠体内代谢具有明显的异构体选择性,清除率分别为(0 46±0 02)ml·h-1·kg-1和(0 17±0 03)ml·h-1·kg-1 (P<0 05 );T1 /2分别为 ( 1 44±0 28 )h和(3 48±0 41)h(P<0 05)。D NNA到L NNA的单项手性转化率为(50 03±8 5)%。结论　D NNA和L NNA在大鼠体内的代谢有明显的异构体选择性 (其差异可能主要源于D NNA到L NNA的单向手性转化)。     

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.