板翘解毒颗粒质量标准研究

目的：研究板翘解毒颗粒的质量标准。方法：采用薄层色谱法（TLC）对板翘解毒颗粒中连翘、板蓝根及知母进行定性鉴别,并建立连翘苷的高效液相色谱法（HPLC）含量测定方法。结果：TLC检出连翘、板蓝根及知母的特征斑点;连翘苷在0.10～4.00μg范围内线性关系良好,平均回收率为99.84%,RSD为2.22%（n=6）。结论：该方法简便、专属性强,可用于该制剂的质量控制。     

苦牛止咳口服液质量标准的建立

摘 要 目的：建立苦牛止咳口服液的质量标准。方法: 采用TLC法对苦牛止咳口服液中的主要药味牛蒡子、前胡、桔梗、陈皮、甘草进行定性鉴别。采用HPLC测定苦牛止咳口服液中主要有效成分苦杏仁苷、牛蒡苷的含量。结果:TLC法可对牛蒡子、前胡、桔梗、陈皮、甘草进行鉴别,斑点清晰,专属性较强;HPLC测定结果显示,苦杏仁苷在25.26~151.6 μg·ml^-1,范围内线性关系良好（r=0.999 8）,牛蒡苷在22.98～137.9 μg·ml^-1,范围内线性关系良好（r=0.999 8,n=6）,平均回收率分别为99.96%（RSD=2.81%,n=9）、99.83%（RSD=2.82%,n=9）。结论:本方法重复性好、简便、快速,可作为有效控制苦牛止咳口服液质量标准的方法。     

藏药九味渣驯丸质量标准的建立

摘 要 目的：建立九味渣驯丸的质量标准。方法: 采用薄层色谱法对处方中的诃子、红花、异叶青兰进行定性鉴别,应用HPLC法对诃子中的没食子酸进行含量测定。结果:薄层色谱斑点清晰,且阴性对照无干扰;没食子酸在0.028 6～0.572 0 μg范围内线性关系良好（r=0.999 7）,平均加样回收率为97.74%,RSD为0.95%（n=6）。结论:本法专属性强、灵敏度高、重复性好,可用于九味渣驯丸的质量控制。     

连知解毒胶囊质量标准研究

目的：完善连知解毒胶囊的质量标准。方法：采用薄层色谱法对方中连翘、知母、广藿香进行定性鉴别;采用高效液相色谱法测定连翘中连翘酯苷A的含量,使用Hypersil BDS色谱柱(250 mm×4.6 mm,5 µm),以乙腈-0.1%磷酸溶液(14∶86)为流动相,流速1.0 mL·min^-1,检测波长330 nm,柱温35 ℃。结果：薄层色谱法中均检出连翘、知母和广藿香,阴性对照无干扰,斑点清晰,分离度较好; 连翘酯苷A进样量在0.0209~3.141 μg范围内具有良好的线性关系(r=0.9994),平均回收率为100.5%, RSD为1.42%。15批次样品中连翘酯苷A含量范围为5.4~12.6 mg·粒^-1。结论：该拟定的质量标准专属性强,重复性好,检测指标合理,可用于连知解毒胶囊的质量控制。     

参芪补血口服液质量标准的提高

摘 要 目的：提高并完善参芪补血口服液的质量标准。方法: 采用薄层色谱法对方中黄芪、何首乌、丹参、陈皮及柴胡进行定性鉴别,以高效液相色谱法对方中芍药苷进行含量测定。结果: TLC斑点清晰,分离良好,阴性无干扰;芍药苷在9.58～191.52 μg·ml^-1范围内呈良好线性关系（r=0.999 9）,平均加样回收率为99.48%,RSD为1.36%(n=9)。结论:本研究建立的质量标准准确、可靠、稳定、专属性强,可有效用于参芪补血口服液的质量控制。     

金黄连口服液质量标准的提高

摘 要 目的：建立金黄连口服液的质量提高标准。方法: 采用TLC法对金银花、黄芩、连翘中的绿原酸、黄芩苷、连翘苷进行定性鉴别;采用HPLC法定量测定金银花中绿原酸的含量,色谱柱：Promosil C18色谱柱(250 mm×4.6 mm,5 μm,Agela technologies公司);流动相：乙腈 0.4%磷酸（10∶90）;检测波长为327 nm;流速：1.0 ml·min^-1;进样量：10 μl,柱温：25℃。结果: 薄层鉴别斑点清晰,在与对照药材相同的位置上,显相同颜色的荧光斑点,阴性样品无干扰;绿原酸含量在5.325～170.400 μg·m-1之间,线性良好(r=0.999 8),平均回收率为97.95%,RSD为2.04%(n=6)。结论: 本方法结果可靠,操作简便,可作为金黄连口服液的质量控制方法。     

二丁二仙合剂质量标准的建立

摘 要 目的：建立二丁二仙合剂质量标准。方法: 采用TLC法对二丁二仙合剂中紫花地丁、黄柏进行定性鉴别;用HPLC法对制剂中淫羊藿苷、仙茅苷进行含量测定。结果:定性鉴别分离度较好,专属性强;淫羊藿苷的含量测定线性范围为5.77～184.50 μg·m^-1 （r=0.999 9）,平均回收率为96.55%（RSD=1.14%,n=9）;仙茅苷的含量测定线性范围为12.36～395.50 μg·m^-1 （r=1.000 0）,平均回收率为100.58%（RSD=2.92%,n=9）。结论:所建立方法准确可靠、灵敏度高、专属性强,可用于二丁二仙合剂的质量控制。     

柴芩清热胶囊质量控制研究

目的 建立柴芩清热胶囊的质量控制方法。方法 采用薄层色谱(TLC)法对组方中柴胡、连翘、诃子、大黄进行定性鉴别,采用高效液相色谱(HPLC)法测定黄芩苷。结果 薄层色谱清晰,分离良好,阴性无干扰。黄芩苷定量测定的平均回收率为98.39%,RSD为0.81%。结论 该方法简便易行、灵敏准确、专属性强,可用于柴芩清热胶囊的质量控制。     

滋肾健脑口服液质量标准的提高

摘 要 目的：提高滋肾健脑口服液的质量标准。 方法: 通过简化前处理及调整色谱条件优化何首乌、白芍、黄芪及甘草的TLC鉴别方法;采用HPLC法对制剂中女贞子所含的特女贞苷含量进行测定以完善其质量标准,色谱柱为Wondasil C18 WR(250 mm×4.6 mm,5 μm）,流动相为甲醇 水（35∶65）,流速为1.0 ml·min-1,检测波长为224 nm,柱温为35℃,进样量为10 μl。 结果: 优化后的TLC法,供试品制备方法简单,薄层色谱斑点清晰,阴性无干扰。特女贞苷在11.462～1 194.0 μg·ml-1范围内线性关系良好(r=0.999 9),平均回收率为99.89%(RSD=0.50%,n=6)。 结论: 提高后的质量标准方法简便可行,专属性强,重复性好,能更加有效地控制滋肾健脑口服液的质量。     

肾复康胶囊的质量标准研究

摘 要 目的： 建立肾复康胶囊的质量标准。方法: 采用显微鉴别法对肾复康胶囊中大黄、当归和全蝎进行定性鉴别;采用TLC法对肾复康胶囊中的大黄、何首乌、山茱萸、丹参、川牛膝、黄芪进行定性鉴别;采用HPLC法对制剂中大黄酚的含量。结果: 大黄、何首乌、山茱萸、丹参、川牛膝、黄芪薄层色谱斑点清晰、重现性好、专属性强、阴性对照无干扰。含量测定中大黄酚在1.712~17.120  μg·ml^-1范围内线性关系良好（r=0.999 9）,平均回收率为101.2%,RSD=0.34%（n=6）。结论:所建立的定性、定量方法简便易行,重复性好,为肾复康胶囊提供了质量控制方法。     

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.     

In vitro studies on sterically stabilized liposomes (SL) as enzyme carriers in organophosphorus (OP) antagonism

This study describes a new approach for organophosphorous (OP) antidotal treatment by encapsulating an OP hydrolyzing enzyme, OPA anhydrolase (OPAA), within sterically stabilized liposomes. The recombinant OPAA enzyme was derived from Alteromonas strain JD6. It has broad substrate specificity to a wide range of OP compounds: DFP and the nerve agents, soman and sarin. Liposomes encapsulating OPAA (SL)* were made by mechanical dispersion method. Hydrolysis of DFP by (SL)* was measured by following an increase of fluoride ion concentration using a fluoride ion selective electrode. OPAA entrapped in the carrier liposomes rapidly hydrolyze DFP, with the rate of DFP hydrolysis directly proportional to the amount of (SL)* added to the solution. Liposomal carriers containing no enzyme did not hydrolyze DFP. The reaction was linear and the rate of hydrolysis was first order in the substrate. This enzyme carrier system serves as a biodegradable protective environment for the recombinant OP-metabolizing enzyme, OPAA, resulting in prolongation of enzymatic concentration in the body. These studies suggest that the protection of OP intoxication can be strikingly enhanced by adding OPAA encapsulated within (SL)* to pralidoxime and atropine.     

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.     

Steroidal sapogenin contents in some domestic plants

In order to find out the values of the steroid resources for the future use. the compositions and contents of steroidal sapogenins from 13 domestic plants have been investigated. As a result,Dioscorea nipponica, D. quinqueloba andSmilax china were found to have large amount of diosgenin. And pennogenin inTrillium kamtschaticum andParis verticillata, yuccagenin inAllium fistulosum, hecogenin inAgave americana and neochlorogenin inSolanum nigum were appeared to be major steroidal sapogenins.