贯叶金丝桃止痛酊的制备及质量控制

目的：研制贯叶金丝桃止痛酊，并建立其质量标准。方法：用70％乙醇提取贯叶金丝桃，配以丁香油、薄荷油及氮酮制成酊剂，测定pH值及鉴别，并用可见紫外分光光度法测定含量。结果：该制剂1mL含总金丝桃素0．27mg，平均加样回收率100．06％。结论：本制剂制备工艺简单，质量控制方法简便、可靠。     

反相高效液相色谱法测定元宝草中金丝桃素和金丝桃苷的含量

目的 采用反相高效液相色谱(RP-HPLC)法对元宝草中金丝桃素和金丝桃苷含量进行测定. 方法 DiamonsilTM C₁₈色谱柱(200 mm×4.6 mm,5 μm),加装Phenomenex保护柱. 流动相分别是甲醇-乙腈-1.0%磷酸二氢钠溶液(340：15：5)和甲醇-0.025 mol.L^-1磷酸溶液(50：50);检测波长分别是588,360 nm. 结果金丝桃素和金丝桃苷分别在0.02～0.18 μg(r＝0.999 9,n＝6)和0.05～0.80 μg(r＝0.999 7,n＝6)范围内呈良好线性关系,回收率分别为98.08%和97.58%,RSD分别为1.05%和0.89%. 结论 该方法检测结果准确,重复性好,可用于元宝草的质量控制.     

黑龙江省两种金丝桃属植物理化鉴别特征

目的：为了探讨黑龙江省两种金丝桃属植物长柱金丝桃(Hypericum ascyron L．)、乌腺金丝桃(H．attenuatum Choisy．)理化鉴别特征。方法：分别采用黄酮、皂苷、鞣质及金丝桃素的鉴别试验。结果：黄酮定性反应均为阳性；皂苷定性反应表明均含三萜皂苷；鞣质的定性反应表明它们所含鞣质为缩合鞣质；金丝桃素的定性反应表明乌腺金丝桃含金丝桃素。结论：二者理化鉴别特征有一定差别．能通过化学鉴别方法予以鉴别。     

高效液相色谱法测定山楂叶中金丝桃苷的含量

目的：用高效液相色谱法(HPLC法)测定山楂叶中金丝桃苷的含量。方法：采用C18柱，以四氢呋喃-甲醇-乙腈-0．5％冰醋酸(19．4：1：1：78．6)为流动相，流速为1．0mL／min，检测波长为363nm。结果：金丝桃苷浓度在0．02278—0.94900μg／mL范围内与峰面积线性关系良好，相关系数为1．0000，平均回收率为97．47％，RSD为1、4％(n=6)。结论：HPLC法操作简便、准确，可作为山楂叶的定量分析方法。     

高效液相色谱—荧光检测法测定贯叶连翘中金丝桃素的含量

目的：建立高效液相色谱－荧光检测法测定贯叶翘中金丝桃素的含量。方法：色谱柱为18柱（5μm,4．6mmx200mm),流动相为甲醇－pH6．5的磷酸盐缓冲液（55：45）,流速为1．0mL.min^-1,柱温为30℃,荧光检测波长λEX＝580nm,λEM＝600nm。结果：该方法的线性范围为2．55－102ng(r=0.9999)。平均加样回收率为101．1％,RSD为1．4％（n =5)。最低检测限为80pg。结论：本方法快速,简单,灵敏度极高。     

HPLC法测定红旱莲中金丝桃苷的含量

目的建立红旱莲中金丝桃苷含量的测定方法。方法采用高效液相色谱法,分析柱为C18色谱柱,进行梯度洗脱,流速1．0ml·min^-1,检测波长：360nm,柱温为35℃。结果金丝桃苷浓度在5．8-58mg·L^-1范围内呈良好线形关系,平均回收率为98．38％,RSD=1．07％。结论该方法灵敏度高、准确、操作简便,可用于红旱莲药材及其制剂的含量测定。     

HPLC法测定不同产地黄蜀葵花中金丝桃苷含量

目的分析并比较了安徽四个不同产地黄蜀葵花药材中金丝桃苷的含量。方法高效液相色谱法,色谱柱Alltima C18（5μm,4．0mm×250mm）,流动相：乙腈-水-磷酸（175：825：1）,流速1．0ml·min^-1,检测波长：360nm,进样量：20μl,柱温为40℃。结果黄山黄蜀葵花中金丝桃苷含量1．18％,RSD为2．54％;合肥黄蜀葵花中金丝桃苷含量1．07％,RSD为1．62％;六安黄蜀葵花中金丝桃苷含量1．03％,RSD为1．94％;毫州黄蜀葵花中金丝桃苷含量0．92％,RSD为1.88％。结论HPLC法测得黄山黄蜀葵花中金丝桃苷含量最高,毫州黄蜀葵花中金丝桃苷含量最低,该方法简便准确,重现性好,为各地黄蜀葵花药材的进一步开发利用提供质量控制依据。     

不同方法除鞣质后贯叶金丝桃提取物中金丝桃素的含量变化

目的 考察用不同方法检测除鞣质后金丝桃素的含量变化和收率,建立贯叶金丝桃良好的除鞣质方法。方法采用明胶沉淀法、改良明胶沉淀法及碱性醇沉法除鞣质后,用高效液相色谱（HPLC）法测定贯叶金丝桃提取物中金丝桃素含量变化和收率;色谱柱为Phenomenex—C18柱（250mm×4．6mm,5μm）,流动相为甲醇-0．006mol／LNa214PO4（7：1V／V,H3P04调至pH=6．5）,流速为1．0mL／min,柱温30℃,检测波长590nm,外标法计算。结果金丝桃素的进样量线性范围为0．0194～0．7760μg（r=0．9999）,平均回收率为100．25％。RSD：1．29％（n=5）;明胶沉淀法、改良明胶沉淀法和碱性醇沉法除鞣质后金丝桃素含量分别为0．092％,0．098％和0．093％,收率分别为70．15％,85．21％和89．16％。结论改良明胶沉淀法具有鞣质去除完全、金丝桃素含量较高、损失较少的优点,且方法简便易行．可应用于贯叶金丝桃提取物除鞣质处理。     

黔产3种金丝桃属植物药中金丝桃苷的含量测定

目的:测定贵州地区3种金丝桃属植物药贯叶连翘、地耳草、贵州金丝桃中金丝桃苷的含量。方法:采用高效液相色谱法,选用岛津Shim-packVP-ODS(5μm,250mm×4.6mm)柱,流动相:甲醇-0.5％磷酸(45:55,用三乙胺调pH为3.0),流速1.1mL·min~(-1),检测波长为360 nm。结果:金丝桃苷在0.114～0.684μg范围内线性关系良好,r=0.999 9(n=6)。平均回收率为96.05％～103.3％,检测限为5 ng·mL~(-1)。结论:本方法便捷、灵敏、准确、重现性好。     

RP—HPLC法测定贯叶连翘片剂中有效成分金丝桃素和金丝桃苷的含量

采用ＲＰ－ＨＰＬＣ法测定贯叶连翘片剂中有效成分金丝桃素和金丝桃苷的含量。方法分别使用ＯＤＳ和ＯＤＳ－２色谱柱,流动相分别是１．５６％磷酸二氢钠－甲醇－醋酸乙酯（１：４：１）及甲醇－０．５％磷酸,检测波长分别为５９０ｎｍ,３６０ｎｍ。结论本方法有良好的重性及精密度。     

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.