灵芝孢子油指纹图谱研究及其混淆品鉴别

目的 建立灵芝孢子油HPLC指纹图谱并鉴别其油类混淆品。方法 采用ACCHROM Unitary-C18(250mm×4.6mm,5μm)色谱柱,乙腈-异丙醇(51：49)为流动相,流速为1.0 mL.min-1,柱温为30℃,蒸发光散射检测器的HPLC方法。结果 建立了灵芝孢子油脂肪酸酯类成分HPLC指纹图谱,确定了8个共有峰,分别为三亚油酸甘油酯、1,2-二亚油酸-3-油酸甘油酯、1,2-二亚油酸-3-棕榈酸甘油酯、1,2-二油酸-3-亚油酸甘油酯、1-棕榈酸-2-油酸-3-亚油酸甘油酯、三油酸甘油酯、1,2-二油酸-3-棕榈酸甘油酯、1,2-二油酸-3-硬脂酸甘油酯。灵芝孢子油混淆品的图谱与灵芝孢子油指纹图谱有明显区别。结论 建立的灵芝孢子油脂肪酸酯类成分指纹图谱能很好地区别灵芝孢子油和其混淆品。     

灵芝孢子粉质量标准提高研究

目的 建立灵芝孢子粉的HPLC特征图谱及三油酸甘油酯的含量测定方法。方法 采用ACCHROM Unitary-C₁₈(250 mm×4.6 mm,5 μm)色谱柱,流动相为乙腈-异丙醇(51∶49),流速为1.0 mL·min^-1,柱温为30 ℃,检测器为蒸发光散射检测器。结果 建立了灵芝孢子粉HPLC特征图谱,确定了10个共有峰,指认了其中8个共有峰的成分分别为三亚油酸甘油酯、二亚油酸油酸甘油酯、二亚油酸棕榈酸甘油酯、二油酸亚油酸甘油酯、棕榈酸油酸亚油酸甘油酯、三油酸甘油酯、二油酸棕榈酸甘油酯和二油酸硬脂酸甘油酯。三油酸甘油酯进样量在0.613 2~18.40 μg(r=0.998 9)内与峰面积线性关系良好,平均加样回收率为104.1%(RSD=1.8%)。结论 特征图谱结合三油酸甘油酯的含量测定,能更好地控制灵芝孢子粉的质量。     

一测多评法同时测定薏苡仁油中4种甘油三酯类抗肿瘤成分的含量

目的:建立同时测定薏苡仁油中4种甘油三酯类抗肿瘤成分含量的方法。方法:采用高效液相色谱-蒸发光散射检测器法(HPLC-ELSD)。色谱柱为Inertsil ODS-3 C_(18),流动相为乙腈-异丙醇(57∶43,V/V),流速为1.0 mL/min,柱温为30℃,进样量为10μL;蒸发光散射检测器漂移管温度为70℃,气体流速为2 L/min。以甘油三油酸酯为内标,分别计算其与甘油三亚油酸酯、1,2-亚油酸-3-棕榈酸甘油酯、1-棕榈酸-2-油酸-3-亚油酸甘油酯的相对校正因子(RCF),通过RCF计算薏苡仁油中上述3种成分的含量,同时采用外标法测定薏苡仁油中这4种成分的含量,比较一测多评法和外标法的含量测定结果。结果:甘油三亚油酸酯、1,2-亚油酸-3-棕榈酸甘油酯、1-棕榈酸-2-油酸-3-亚油酸甘油酯、甘油三油酸酯进样量检测线性范围分别为0.15～4.50、0.15～4.50、0.35～10.50、0.35～10.50μg(r≥0.999 5);定量限分别为0.13、0.06、0.07、0.12μg,检测限分别为0.04、0.02、0.02、0.03μg;精密度、稳定性、重复性试验的RSD<2.0%(n=6);加样回收率为95.43%～102.67%(RSD<2.0%,n=6)。甘油三亚油酸酯、1,2-亚油酸-3-棕榈酸甘油酯、1-棕榈酸-2-油酸-3-亚油酸甘油酯的平均RCF分别为0.31、0.88、1.21。在不同试验条件下,RCF重现性良好。一测多评法和外标法的含量测定结果比较,差异无统计学意义(P>0.05)。结论:该方法操作简单快捷、结果准确可靠,可用于薏苡仁油中甘油三亚油酸酯、1,2-亚油酸-3-棕榈酸甘油酯、1-棕榈酸-2-油酸-3-亚油酸甘油酯、甘油三油酸酯4种抗肿瘤成分含量的同时测定。     

HPLC-ELSD法测定鸦胆子油中四种甘油三酯的含量

目的：建立鸦胆子油中1,2--二亚油酸-3-油酸甘油酯、1,3--二油酸-2-亚油酸甘油酯、三油酸甘油酯、1,3---油酸-2-棕榈甘油酯的含量测定方法.方法：运用岛津2010C高效液相色谱仪和奥泰2000蒸发光检测器,采用Waters C18色谱柱（250 mm×4.6mm,5μm）;流动相为乙腈-二氯甲烷（65∶35）,流速1.0 ml·min-1;检测温度：70℃.结果：四种甘油三酯分别在0.184～2.763 μg、0.382～5.724μg、0.406 ～6.084 μg和0.204～3.066 μg之间线性关系良好,r值分别为0.999 0、0.999 2、0.999 1和0.999 0,回收率分别为99.01％、98.70％、98.92％和98.46％,RSD分别为0.7％、0.5％、0.8％和0.9％.结论：该方法操作简单,分离效果好,灵敏度高,可更好的控制鸦胆子油的质量.     

UPLC-ELSD法同时测定鸦胆子中两种脂溶性成分的含量

目的建立同时测定鸦胆子药材中1,2-油酸-3-亚油酸甘油酯和甘油三油酸酯两种脂溶性成分含量的方法。方法采用UPLC-ELSD法,色谱柱为Thermo Accucore XL C18柱(250 mm×2.1 mm,4μm);流动相为乙腈-二氯甲烷(体积比70∶30);流速为0.4 m L·min-1;柱温为30℃;进样量为4μL;漂移管温度为45℃;雾化器载气压为0.276 MPa。结果 1,2-油酸-3-亚油酸甘油酯和甘油三油酸酯进样量分别在0.509~2.55μg(r=0.999 6)和0.685~3.42μg(r=0.999 1)内线性关系良好,平均加样回收率分别为97.5%和99.5%,RSD分别为1.7%和2.3%(n=9)。结论建立的方法可用于同时测定鸦胆子中1,2-油酸-3-亚油酸甘油酯和甘油三油酸酯的含量,为控制鸦胆子药材质量提供试验依据。     

HPLC法测定灵芝孢子油中甘油三油酸酯含量

目的:建立高效液相色谱法(HPLC)测定灵芝孢子油中甘油三油酸酯含量的方法。方法:色谱柱为Kromasil100-5C18,流动相为乙腈-异丙醇(53∶47),流速为1.0mL/min,蒸发光散射检测器检测。结果:甘油三油酸酯在2.290~13.740μg范围内线性关系良好,r=0.9996,平均回收率为99.10%,RSD为1.65%。结论:该方法准确可行、重复性好,可作为灵芝孢子油及其制剂质量评价的方法之一。     

HPLC指纹图谱结合系统聚类分析法对灵芝孢子油质量的研究

目的:建立灵芝孢子油的高效液相色谱指纹图谱,并结合聚类分析法初步考察不同采收时间、产地及破壁工艺对灵芝孢子油质量的影响。方法:采用反相高效液相色谱法测定灵芝孢子油中甘油三油酸酯的含量,色谱柱为LiChrospher RP-18e(250mm×4.6mm,5μm),流动相为甲醇-异丙醇(梯度洗脱),蒸发光散射检测器检测。采用系统聚类法对灵芝孢子油样品色谱中各特征峰的相对峰面积进行分析。结果:系统聚类法将供试品分成两大类,其中采收时间及破壁工艺对灵芝孢子油的质量影响明显,产地影响则不明显。结论:该方法能较好地为灵芝孢子油的质量评估提供有益的信息。     

植物油或脂肪合剂治疗炎症、免疫疾病、糖尿病、酒精中毒或创伤

本合剂含有:A.选自以下各项一个或一个以上的组分:(1)植物油或植物脂肪;(2)油酸(或衍生物);(3)亚油酸(或衍生物);(4)甘油三酸酯-甘油三酸酯混合物;(5)磷脂与二个或二个以上酸,选自油酸、亚油酸和 n-3或     

GC法同时测定鸦胆子油中4种脂肪酸的含量

目的建立同时测定鸦胆子油中棕榈酸、硬脂酸、油酸和亚油酸4种成分含量的方法。方法采用毛细管气相色谱法,甲酯化后测定鸦胆子油中棕榈酸、硬脂酸、油酸和亚油酸的含量。色谱柱:DB-17弹性石英毛细管柱(30 m×0.25 mm×0.25μm),检测器:氢火焰离子化检测器(FID),柱温恒温:200℃(保持11 min),进样口温度:250℃,检测器温度:250℃,流速:1.0 mL.min-1,分流比:20∶1,内标物:苯甲酸苯酯。结果棕榈酸、硬脂酸、油酸和亚油酸的线性分别为74～738 mg.L-1(r=0.999 6)、51～509 mg.L-1(r=0.999 1)、741～7 410 mg.L-1(r=0.999 1)和265～2 650 mg.L-1(r=0.999 1);各成分的平均回收率(n=9)分别为94.6%、94.2%、94.2%和95.3%。结论此方法可为鸦胆子油的质量评价提供依据。     

凝胶渗透色谱法同时测定山嵛酸甘油酯中单、二、三甘油酯和游离甘油含量

目的:建立凝胶渗透色谱法同时测定山嵛酸甘油酯中单、二、三甘油酯和游离甘油含量。方法:采用两根苯乙烯-二乙烯基苯柱(5μm, 100?,300 mm×7.8 mm)串联;以四氢呋喃为流动相;示差折光检测器;进样器温度、柱温和检测器温度均为35℃。结果:3家企业9批山嵛酸甘油酯中的单、三甘油酯的含量会有差异,二甘油酯的含量基本一致,游离甘油含量均小于1.0%。结论:该方法可用于山嵛酸甘油酯的质量控制,同时对企业选用不同含量组分组成的山嵛酸甘油酯有一定的指导意义。     

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.     

Efficacy of gut lavage,hemodialysis, and hemoperfusion in the therapy of paraquat or diquat intoxication

Clinical and in vitro investigations were carried out to test the efficacy of gut lavage, hemodialysis, and hemoperfusion in the treatment of poisoning with paraquat or diquat. In a patient suffering from diquat intoxication 130 times more diquat was removed by gut lavage 30 h after ingestion than was removed by complete aspiration of the gastric contents.Determination of in vitro clearances for paraquat and diquat by hemodialysis showed that, at serum concentrations of 1–2 ppm, such as are frequently encountered in poisoning in man, toxicologically relevant quantities of herbicide cannot be removed from the body. At a concentration of 20 ppm, on the other hand, hemodialysis proved to be effective, the clearance being 70 ml/min at a blood flow rate of 100 ml/min. The efficacy of hemoperfusion with coated activated charcoal was on the whole better. Especially at concentrations around 1–2 ppm, the clearance values for hemoperfusion were some 5–7 times higher than those for hemodialysis.In a patient suffering from paraquat poisoning, both hemodialysis as well as hemoperfusion were carried out. The in vitro results could be confirmed: At serum concentrations of paraquat less than 1 ppm no clearance could be obtained by hemodialysis while by hemoperfusion with activated charcoal quite high clearance values were measured and the serum level dropped down to zero.

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Zusammenfassung Klinische Untersuchungen und Laboratoriumsversuche wurden durchgeführt, um die Wirksamkeit von Darmspülung, Hämodialyse und Hämoperfusion bei Paraquat- und Deiquat-Vergiftungen zu prüfen.Bei einem Patienten wurde 30 Std nach Deiquat-Aufnahme durch Darmspülung 130mal mehr Deiquat entfernt als durch vollständige Aspiration des Mageninhaltes. In vitro-Versuche ergaben, daß bei Blutserumkonzentrationen von 1–2 ppm, die bei Vergiftungen oft gemessen werden, durch Hämodialyse keine toxikologisch relevanten Paraquat- oder Deiquat-Mengen entfernt werden können. Dagegen erwies sich die Hämodialyse bei 20 ppm und einer Blutumlaufgeschwindigkeit von 100 ml/min mit einer Clearance von 70 ml/min als wirksam. Die Hämoperfusion mit beschicheter Aktivkohle war in diesen Versuchen aber eindeutig überlegen, denn insbesondere bei Konzentrationen um 1–2 ppm waren die Clearance-Werte 5–7mal höher als bei der Hämodialyse.Die in vitro-Ergebnisse wurden bei einem Patienten mit einer Paraquat-Vergiftung bestätigt: Bei Konzentrationen unter 1 ppm war die Hämodialyse wirkungslos, während durch Hämoperfusion relativ hohe Clearance-Werte erreicht wurden, so daß der Serumspiegel rasch unter die Nachweisgrenze abfiel.

     

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.     

Aquatic Insects and Trace Metals: Bioavailability,Bioaccumulation, and Toxicity

Abstract

The uptake of metals from food and water sources by insects is thought to be additive. For a given metal, the proportions taken up from water and food will depend both on the bioavailable concentration of the metal associated with each source and the mechanism and rate by which the metal enters the insect. Attempts to correlate insect trace metal concentrations with the trophic level of insects should be made with a knowledge of the feeding relationships of the individual taxa concerned. Pathways for the uptake of essential metals, such as copper and zinc, exist at the cellular level, and other nonessential metals, such as cadmium, also appear to enter via these routes. Within cells, trace metals can be bound to proteins or stored in granules. The internal distribution of metals among body tissues is very heterogeneous, and distribution patterns tend to be both metal and taxon specific. Trace metals associated with insects can be both bound on the surface of their chitinous exoskeleton and incorporated into body tissues. The quantities of trace meals accumulated by an individual reflect the net balance between the rate of metal influx from both dissolved and particulate sources and the rate of metal efflux from the organism. The toxicity of metals has been demonstrated at all levels of biological organization: cell, tissue, individual, population, and community. Much of the literature pertaining to the toxic effects of metals on aquatic insects is based on laboratory observations and, as such, it is difficult to extrapolate the data to insects in nature. The few experimental studies in nature suggest that trace metal contaminants can affect both the distribution and the abundance of aquatic insects. Insects have a largely unexploited potential as biomonitors of metal contamination in nature. A better understanding of the physico-chemical and biological mechanisms mediating trace metal bioavailability and exchange will facilitate the development of general predictive models relating trace metal concentrations in insects to those in their environment. Such models will facilitate the use of insects as contaminant biomonitors.