乳康舒胶囊中活性物质的测定

目的:研究乳康舒胶囊中活性物质淫羊藿苷、芍药苷及原儿茶醛的测定.方法:采用薄层色谱法对该复方中的淫羊藿、白芍、丹参药材进行色谱鉴别,HPLC法测定乳康舒胶囊中淫羊藿苷和芍药苷的含量.结果:该制剂中,淫羊藿、白芍、丹参有良好的展开系统,不存在阴性干扰.淫羊藿苷在92.4～3 326.4ng范围内呈良好的线性关系,r=0.999 9,回收率为100.4%,RSD为1.84%;芍药苷在93.0～3 348.0ng范围内有良好的线性关系,r=0.999 7,回收率为100.3%,RSD为1.46%.结论:本质量标准可有效地控制乳康舒胶囊的质量.     

复方淫羊藿胶囊质量标准的研究

目的建立复方淫羊藿胶囊的质量控制方法。方法用薄层色谱法对复方淫羊藿胶囊制剂中的淫羊藿、女贞子进行定性鉴别,HPLC法测定淫羊藿苷的含量。结果鉴别方法专属性好,测定淫羊藿苷的线性范围为4.096μg·mL-1～24.576μg·mL-1,r=0.9995,平均加样回收率99.43%,RSD=0.62%(n=6)。结论方法专属性好,稳定,可用于复方淫羊藿胶囊的质量控制。     

穿龙骨刺胶囊质量标准研究

目的建立穿龙骨刺胶囊的质量标准控制方法。方法采用薄层色谱法对本品中的穿山龙、枸杞子、淫羊藿进行薄层鉴别;采用高效液相色谱法对本品中的淫羊藿苷进行含量测定。结果在薄层色谱图中可检出穿山龙、枸杞子、淫羊藿;淫羊藿苷在进样量0.2236~4.472μg范围内,与峰面积呈良好的线性关系(r=0.999 9),平均回收率为100.79%(RSD=1.49%)。结论所建立的方法可靠、准确、专属性强,可有效控制穿龙骨刺胶囊的质量。     

HPLC-DAD法同时测定龙胆舒肝胶囊中6种活性成分的含量

目的：建立HPLC-DAD法同时测定龙胆舒肝胶囊中天麻素、龙胆苦苷、芍药苷、毛蕊花糖苷、迷迭香酸和丹酚酸B含量的方法。方法：采用液相色谱法,色谱柱为Waters Symmetry ShieldTM RP18,流动相为乙腈（A）和0.1%的磷酸水溶液（B）,梯度洗脱;流速：1.0 mL·min-1;柱温：35 ℃;检测波长：天麻素、毛蕊花糖苷、迷迭香酸和丹酚酸B为220 nm,芍药苷230 nm,龙胆苦苷为275 nm。结果：天麻素、龙胆苦苷、芍药苷、毛蕊花糖苷、迷迭香酸和丹酚酸B的线性范围分别为3.13～62.6 μg·mL-1(r=0.999 5),4.12～82.4 μg·mL-1(r=0.999 9),6.60～132.0 μg·mL-1(r=0.999 7),1.66～33.2 μg·mL-1(r=0.999 5),3.54～70.8 μg·mL-1(r=0.999 8)和4.65～93.0 μg·mL-1(r=0.999 6),6种成分的平均加样回收率（n=6）分别为97.8%、98.0%、98.6%、98.1%、98.7%和98.1%,RSD分别为1.9%、1.3%、1.6%、1.0%、1.3%和1.0%。结论：本法操作简便,结果准确,重现性好,可用于龙胆舒肝胶囊的质量控制。     

乳痛宁糖浆的制备及质量标准研究

目的制备乳痛宁糖浆并建立其质量标准。方法以薄层色谱法鉴别乳痛宁糖浆中的淫羊藿、首乌藤;采用RP-HPLC法测定淫羊藿有效成分淫羊藿苷的含量,检测波长为270nm。结果淫羊藿、首乌藤的薄层斑点清晰,分离良好。淫羊藿苷检测质量浓度在2.97～107.10mg·L-1范围内与峰面积积分值呈良好线性关系(r=0.9997);平均加样回收率为101.33%,RSD为1.75%(n=9)。结论制备方法简便,可行;所建立的标准可用于该制剂的质量控制。     

心痛康胶囊质量标准研究

目的　建立心痛康胶囊质量标准。方法　对红参进行显微鉴别 ,白芍和淫羊藿进行薄层鉴别 ,并用HPLC法测定制剂中芍药苷和淫羊藿苷的含量。结果　显微鉴别特征明显 ,薄层图谱斑点清晰 ,阴性对照无干扰 ,芍药苷在 2 5 34～ 12 6 70 μg间、淫羊藿苷在 1 96～ 17 6 6 μg间呈现良好的线性关系 ;芍药苷回收率为 99 5 1% ,RSD为 1 2 9% ,淫羊藿苷回收率为 99 11% ,RSD为 1 6 2 %。结论　结果准确 ,重复性好 ,可用于该制剂的质量控制。     

乳痛宁颗粒的质量标准研究

目的：建立乳痛宁颗粒的质量标准。方法：用薄层色谱法对乳痛宁颗粒中的淫羊藿和柴胡进行鉴别；用高效液相色谱法测定制剂中芍药苷含量。结果：在薄层色谱中均能鉴别出制剂中的淫羊藿和柴胡；芍药苷进样量在0．212—0．636μg范围内呈良好线性关系（r=0．9997）；平均回收率分别为100．5％，100．0％和99．8％，RSD分别为0．55％，0．20％和0．85％（n=3）。结论：本方法可用于乳痛宁颗粒的质量控制。     

淫羊藿总黄酮胶囊质量标准的研究

目的:研究淫羊藿总黄酮胶囊的质量控制标准。方法:采用薄层色谱法和紫外分光光度法,对制剂中的淫羊藿苷进行定性和定量测量。结果:淫羊藿苷在3.9～19.2μg·ml~(-1)范围内线性关系良好,r=0.999 8,平均回收率为97.1％,胶囊剂中含总黄酮以淫羊藿苷计不低于80mg/粒。结论:本研究为淫羊囊胶囊提供了准确、简便的质量控制方法。     

麟生颗粒的制备及质量控制

目的 制备麟生颗粒并建立质量控制标准.方法 对麟生颗粒中的主要成分淫羊藿、仙茅进行了薄层色谱定性鉴别;用高效液相色谱法对淫羊藿苷进行含量测定.结果 薄层鉴别方法专属性强.淫羊藿苷在1.1～20.9 μg·mL-1内有良好的线性关系,回归方程Y=43 857X-5 324.2(r=0.999 9),平均回收率为98.28%,RSD为2.39%.结论 本法操作简便、准确、分离效率高、稳定性好、分析速度快,为本制剂的质量控制提供了可靠的方法.     

更安颗粒的质量标准研究

目的建立更安颗粒的质量控制方法。方法采用薄层色谱法（TLC）对更安颗粒中的淫羊藿、丹参、首乌藤、黄芩进行定性鉴别;采用高效液相色谱法测定淫羊藿苷的含量。结果 TLC可鉴别出上述各组分与对照品相应的斑点,且阴性对照无干扰。淫羊藿苷在0.0116～1.0300mg·mL-1线性关系良好（r2=0.9997）,平均加样回收率为：98.35%,RSD=1.23%（n=6）。结论该方法操作简便,方法稳定,可作为该制剂的质量控制方法。     

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.     

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.