黄芪中重金属超临界CO_2净化技术研究

目的利用超临界CO2 萃取技术净化黄芪中重金属。方法a 以二乙基二硫代氨基甲酸钠(DDTC)为金属络合剂 ,用超临界流体萃取技术净化药材中的重金属 ,并对萃取方案进行最优化。b 选择不同的混酸消化液完全消解药材后 ,以空气 乙炔火焰AAS法和氢化物发生AAS法分别测定其中的铅 (Pb)、镉 (Cd) ,以及砷 (As)、汞 (Hg)。c 采用UCTRONVX -ODS(2 5 0mm×4 6mm ,5 μm)色谱柱 ,以乙腈 水 (V∶V =30∶70 )为流动相 ,检测波长为 2 0 3nm ,卡马西平为内标 ,测定黄芪中黄芪甲苷的含量。结果与结论a 确定了药材中重金属的最佳萃取条件。在最佳萃取条件下 ,重金属净化率达到 85 %以上 ;同时 ,中药材中的有效成分损失低于 5 %。b 建立了药材中金属元素和有效成分的含量测定方法 ,为正确评价中药材的质量奠定了基础 ,可用于正确评价净化前后药材的质量变化     

RP-HPLC法同时测定不同品种淫羊藿药材中5种主要黄酮类成分的含量

目的:建立以反相高效液相色谱法测定不同品种淫羊藿药材中5种主要黄酮类成分含量的方法。方法:色谱柱为Zorbax SB-C18(250mm×4.6mm,5μm),流动相为乙腈-水(梯度洗脱),检测波长为270nm,柱温为30℃,同时测定淫羊藿药材中淫羊藿苷、朝藿定A、朝藿定B、朝藿定C、宝藿苷Ⅰ的含量。结果:5种成分均能达到基线分离,线性良好。不同品种淫羊藿药材中5种主要黄酮类成分的含量差别较大。结论:建议在考察淫羊藿药材的质量时,不能只考察淫羊藿苷,应建立多种黄酮类成分测定指标,以全面控制淫羊藿药材的质量。     

HPLC同时测定21种淫羊藿中朝藿定C和淫羊藿苷的含量

目的:建立同时测定淫羊藿药材中朝藿定C和淫羊藿苷含量的高效液相色谱方法。方法:采用Elite SinoChrom ODS-AP(250 mm×4.6 mm,5μm)色谱柱,流动相为乙腈(A)-水(B),梯度洗脱(0~8 min,27%A;8~30 min,27%A→29%A),流速1 mL.min-1,检测波长270 nm。结果:朝藿定C进样量在0.130~3.89μg,淫羊藿苷在0.0294~1.47μg范围内呈良好线性关系(r=0.9999);朝藿定C和淫羊藿苷平均回收率(n=9)分别为103.9%,100.0%;淫羊藿药材中朝藿定C和淫羊藿苷的含量分别为0.02%~7.80%,0.01%~1.74%。结论:该方法简便、快速、准确,重复性好,可作为淫羊藿药材中朝霍定C和淫羊藿苷的含量测定方法。     

响应面法优化超临界CO_2萃取淫羊藿苷的工艺研究(英文)

利用星点设计-响应面法对淫羊藿中淫羊藿苷的超临界萃取工艺进行优化。根据星点设计原理采用3因素5水平的响应面分析法,以提取温度、提取压力、夹带剂流速为自变量,淫羊藿苷得率为因变量,通过对自变量各水平的多元线性回归及二项式拟合,选取超临界CO_2提取淫羊藿苷最优工艺为超临界提取温度46.5℃、提取压力30.6 MPa、夹带剂流速3.3 mL/min。星点设计-响应面法优选淫羊藿中的淫羊藿苷提取工艺,方法简便,预测性良好。     

HPLC法同时测定淫羊藿药材中8种黄酮类成分的含量

目的建立HPLC法同时测定淫羊藿药材中朝藿定A、朝藿定B、朝藿定C、淫羊藿苷、宝藿苷I等8种黄酮类成分含量的方法。方法色谱柱为Agilent Zorbax SB-C18柱(250 mm×4.6 mm,5μm),流动相为乙腈-水梯度洗脱,检测波长为270 nm,流速为1.0 m L·min-1,柱温为30℃。结果朝藿定A、朝藿定B、朝藿定C、淫羊藿苷、宝藿苷I、朝藿苷丙、epimedokoreanoside I、朝藿苷乙等8种黄酮类成分的线性关系良好,线性范围分别为2.0²0.2、1.020.2、1.0⁵7.2、3.057.2、3.0¹32.0、1.0132.0、1.0⁵0.0、1.050.0、1.0⁴5.2、0.445.2、0.4¹5.0、0.615.0、0.6²5.8、0.225.8、0.2⁵2.7 mg·L-1;平均回收率分别为98.3%、96.7%、97.2%、96.9%、95.5%、98.5%、98.2%、98.5%,RSD分别为1.0%、0.7%、0.9%、0.6%、0.2%、1.1%、1.4%、0.3%(n=6)。结论该方法可作为淫羊藿药材含量测定的方法。对收集的104批市售的淫羊藿药材中淫羊藿苷含量进行了测定,淫羊藿苷含量质量分数为0.01%52.7 mg·L-1;平均回收率分别为98.3%、96.7%、97.2%、96.9%、95.5%、98.5%、98.2%、98.5%,RSD分别为1.0%、0.7%、0.9%、0.6%、0.2%、1.1%、1.4%、0.3%(n=6)。结论该方法可作为淫羊藿药材含量测定的方法。对收集的104批市售的淫羊藿药材中淫羊藿苷含量进行了测定,淫羊藿苷含量质量分数为0.01%⁰.17%,大部分不符合《中华人民共和国药典》标准。     

参龙健脑胶囊质量标准的研究

目的:建立参龙健脑胶囊质量控制方法.方法:采用TLC方法对参龙健脑胶囊中的人参、地龙、淫羊藿药材进行定性鉴别;采用HPLC法对参龙健脑胶囊中的淫羊藿苷进行含量测定.色谱条件:Zorbax Eclipse XDB-C18柱(250 mm×4.6mm,5μm),以乙腈-水-磷酸(30:70:0.025)为流动相,柱温40℃,流速1 mL·min-1,检测波长270 nm.结果:采用TLC法能检出人参、地龙、淫羊藿;淫羊藿苷在10～160 μg.mL-1浓度范围内与峰面积呈良好的线性关系(r=1.000,n=5).淫羊藿苷的平均回收率为99.5％,RSD=0.96％.结论:本方法可准确地进行定性、定量,可用于控制参龙健脑胶囊的质量.     

RE-HPLC法测定仙灵脾颗粒中淫羊藿苷的含量

目的测定仙灵脾颗粒中淫羊藿苷的含量。方法采用RE-HPLC法。色谱柱为HYPERSIL C18柱(150mm×4.6mm,5μm);乙腈-水(30∶70)为流动相,流速:1.0mL/min;检测波长270nm。结果淫羊藿苷在0.02316～1.146μg范围内具有良好线性关系,平均回收率为100.80%,RSD为1.35%。结论该法可用于仙灵脾颗粒中淫羊藿苷的含量测定。     

不同产地的淫羊藿理化分析和有机氯类农药残留量比较

目的:了解淫羊藿中淫羊藿苷含量及在种植过程中有机氯类农药残留量.方法:采用2000年版<中国药典(一部)>中方法对不同产地的4批朝鲜淫羊藿药材进行理化分析,以高效液相色谱法分析淫羊藿苷含量,以气相色谱法测定有机氯类农药残留量.结果:不同产地的4批药材中总黄酮含量均在7.4%以上,淫羊藿苷含量在0.15%～0.28%之间.结论:淫羊藿苷的含量偏低.     

益肾强身片中淫羊藿苷的含量测定

目的:分离并测定益肾强身片剂中淫羊藿苷的含量.方法:采用HPLC法进行片剂中淫羊藿成分淫羊藿苷的含量测定,采用Diamonsil C18柱(250mm×4.6 mm,5 μm),流动相为甲醇-水(60:40),流速1 mL·min-1,检测波长为268 nm,柱温为室温.结果:淫羊藿苷的线性范围为0.201-4.020μg,r=0.999,平均回收率为97.92%,RSD=0.55%.结论:本方法简便、快速,灵敏度高,可用于益肾强身片生产的质量控制.     

SPE-HPLC测定乳增宁片中淫羊藿苷的含量

目的采用SPE-HPLC法测定乳增宁片中淫羊藿苷的含量. 方法以甲醇-水(55∶45)为流动相,Hypersil ODS(3)柱(250 mm×4.6 mm,5 μm)为固定相,流速1 ml/min,检测波长230 nm. 结果淫羊藿苷的测定在0.05733～1.911 mg范围内线性关系良好,平均回收率为100.4%,RSD为1.2%. 结论方法简单、灵敏度高,可用于乳增宁片中淫羊藿苷的含量测定.     

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.