龙牡壮骨颗粒对小鼠性激素水平的影响

目的：探讨龙牡壮骨颗粒对性激素水平的影响.方法：昆明小鼠雌雄各30只,以该制剂溶于水制成溶液剂为供试药,以双蒸水为空白对照.受试小鼠按性别随机分为龙牡壮骨颗粒雌性高、等效剂量组和龙牡壮骨颗粒雄性高、等效剂量组,给药14 d,观察对血清睾酮、雌二醇含量和骨指标的影响.结果：龙牡壮骨颗粒能显著提高小鼠骨干重、骨密度、骨量,等效剂量龙牡壮骨颗粒组还能明显提高雄性小鼠骨湿重（P=0.022）,等效剂量龙牡壮骨颗粒对小鼠性激素水平无影响（P=0.855）.高剂量龙牡壮骨颗粒显著降低雄性小鼠雌二醇水平（P=0.048）.结论：与临床剂量等效的龙牡壮骨颗粒对小鼠骨质有增强作用,同时对小鼠性激素水平无影响.     

白假丝酵母菌阴道炎小鼠模型的构建

摘 要 目的：构建白假丝酵母菌阴道炎小鼠模型,探索最佳成模条件,以提供经济实用的白假丝醇母菌性阴道炎动物模型。方法: 采用昆明雌性小鼠,预先连续灌胃给予低、中、高剂量（0.001 5,0.015,0.15 mg/10 g）的戊酸雌二醇7 d后接种白假丝酵母菌建立阴道炎模型,并进行阴道灌洗液真菌载量和阴道组织病理观察。结果: 戊酸雌二醇低、中、高剂量组阴道灌洗液的菌落计数分别为124.67±19.01、217.67±22.50、282.00±27.87,高剂量组与中、低剂量组比较差异有统计学意义（P<0.05或P<0.01）。HE染色和PAS染色结果显示,戊酸雌二醇高剂量组有较多多形核粒细胞（PMNs）浸润及紫红色线状菌丝。结论: 戊酸雌二醇高剂量组造模方式为昆明小鼠白假丝酵母菌阴道炎模型的最佳造模条件。     

芪防鼻敏颗粒抗炎、抗过敏作用研究

摘 要 目的：初步探讨中药复方芪防鼻敏颗粒的抗炎、抗过敏作用。方法: 采用二甲苯致小鼠耳廓肿胀法和大鼠棉球肉芽组织形成法观察芪防鼻敏颗粒的抗炎作用,采用大鼠同种被动皮肤过敏反应实验和小鼠耳异种被动皮肤过敏反应观察芪防鼻敏感颗粒的抗过敏作用。结果: 与空白组比较,芪防鼻敏颗粒各剂量组可显著降低二甲苯所致小鼠耳廓肿胀度（P<0.01或0.05）,对大鼠棉球肉芽组织增生无明显抑制作用。与空白组比较,芪防鼻敏颗粒各剂量组可明显降低卵蛋白所致大鼠皮肤蓝斑A值（P<0.01或0.05）,芪防鼻敏颗粒高剂量组可显著降低小鼠耳廓蓝染程度（P<0.05）。结论:芪防鼻敏颗粒具有一定抗炎、抗过敏作用。     

芪防鼻敏颗粒对变应性鼻炎大鼠炎性因子表达的影响研究

摘 要 目的：观察芪防鼻敏颗粒对变应性鼻炎（AR）大鼠血清白介素 4(IL 4),白介素 17(IL 17）,肿瘤坏死因子（TNF α）及鼻黏膜γ干扰素（IFN γ）、白介素 6（IL 6）、TNF α表达的影响。方法: SD大鼠随机分为正常组,模型组,氯雷他定组（1.17 mg·kg^-1）,鼻炎康组（0.6 g·kg^-1）,芪防鼻敏颗粒高（26.48 g·kg^-1）、中（13.24 g·kg^-1）、低（6.62 g·kg^-1）剂量组。采用卵蛋白（OVA）建立AR大鼠模型。造模成功后分别灌胃给药,连续14 d。酶联免疫吸附法（ELISA）检测AR大鼠血清IL 4、IL 17、TNF α水平,免疫组化染色法（IHC）检测鼻黏膜IFN γ、IL 6、TNF α表达。结果:与正常组相比,模型组大鼠血清IL 4、IL 17水平明显上升（P<0.01）;鼻黏膜IFN γ阳性表达明显降低（P<0.05）,IL 6、TNF α阳性表达显著升高（P<0.01）。与模型组相比,氯雷他定组、芪防鼻敏颗粒中剂量组大鼠血清IL 4水平显著下降（P<0.05）,芪防鼻敏颗粒低剂量组大鼠血清IL 17水平明显下降（P<0.05）,氯雷他定组、鼻炎康组、芪防鼻敏颗粒高、中剂量组大鼠血清TNF α水平显著下降（P<0.05或P<0.01）;高、低剂量组大鼠鼻黏膜IFN γ阳性表达显著升高（P<0.05或P<0.01）,高、中剂量组IL 6阳性表达显著降低（P<0.01）,高剂量组TNF α阳性表达显著降低（P<0.01）。与氯雷他定组相比,鼻炎康组、芪防鼻敏颗粒高剂量组大鼠血清IL 17水平明显上升（P<0.05）,鼻炎康组、芪防鼻敏颗粒低剂量组大鼠血清IL 4水平明显上升（P<0.05）,芪防鼻敏颗粒高、中、低剂量组TNF α阳性表达显著升高（P<0.05）;与鼻炎康组比较,芪防鼻敏颗粒中剂量组大鼠血清IL 4水平明显下降（P<0.05）;与芪防鼻敏颗粒低剂量组相比,芪防鼻敏颗粒高剂量组大鼠血清IL 17水平明显上升（P<0.05）,芪防鼻敏颗粒中剂量组大鼠血清IL 4水平明显下降（P<0.05）。结论:芪防鼻敏颗粒可增加AR鼻黏膜IFN γ表达,降低血清IL 4、TNF α、IL 17水平及鼻黏膜TNF α、IL 6表达。     

乳癖消颗粒不同提取物对小鼠原发性痛经模型的影响

摘 要 目的： 研究乳癖消颗粒各提取部位的抗痛经作用。方法: 采用缩宫素致小鼠扭体实验观察乳癖消颗粒各提取部位的抗痛经作用。结果: 与模型组相比,乳癖消颗粒的各提取部位均能显著减少缩宫素引起的小鼠扭体反应次数（P <0.05,P<0.01或P<0.001）;其中,水溶性部位效果最好（P<0.001）,且与阳性对照组相比差异无统计学意义（P＞0.05）。结论:乳癖消颗粒的水溶性部位具有显著抗痛经作用。     

阿那曲唑对绝经后乳腺癌患者性激素水平的影响及人乳腺癌细胞的抑制作用

摘 要 目的：探讨阿那曲唑对绝经后乳腺癌患者性激素水平的影响及对人乳腺癌细胞（MCF 7）的抑制作用。方法: 收集80例女性乳腺癌病例,将接受常规管理与他莫昔芬治疗的40例患者纳入对照组;将接受常规管理与阿那曲唑治疗的40例患者纳入观察组。比较两组患者治疗前、治疗3个月后性激素水平变化、疗效及药品不良反应发生率,以及两种药物对MCF 7细胞的抑制作用。结果: 治疗后,两组患者雌二醇、孕酮、黄体生成素水平均较治疗前降低,睾酮水平则较治疗前升高（P＜0.01）;且他莫昔芬组患者雌二醇、孕酮、黄体生成素水平均高于阿那曲唑组,睾酮水平低于阿那曲唑组（P＜0.01）。两种药物作用72 h的MCF 7细胞抑制率均高于作用48 h（P＜0.05）;阿那曲唑不同时点的MCF 7细胞抑制率均优于他莫昔芬（P＜0.05）。对照组患者治疗总有效率（45.0%）低于观察组（70.0%）（P＜0.05）;两组药品不良反应总发生率比较,差异无统计学意义（P＞0.05）。结论: 给予绝经后乳腺癌患者阿那曲唑疗效显著,安全性高,对MCF 7细胞有较强的抑制作用,能有效调节患者性激素水平,减少乳腺癌复发及转移风险。     

晕吐宁颗粒抗眩晕作用研究

摘 要 目的： 晕吐宁颗粒对小鼠及豚鼠抗眩晕作用及初步机制探讨,为该药临床应用提供实验支持。方法: 机械旋转使小鼠产生眩晕后,通过迷宫实验与跳台实验测定正常组,模型组,阳性对照组(盐酸地芬尼多片,10 mg·kg^-1·d^{-1),晕吐宁颗粒低、中、高剂量三组 (3,6,12 g·kg-1·d-1)小鼠逃避电击所用时间,并观察各组眩晕小鼠的进食量;观察外耳道注入三氯甲烷的眩晕模型豚鼠摇头和眼球震颤次数,观察晕吐宁颗粒的抗眩晕作用。结果: 晕吐宁颗粒各剂量组能够显著缩短眩晕小鼠逃避电击所用时间(P＜0.01或0.05),增加眩晕小鼠进食量;降低眩晕豚鼠的摆头和眼球震颤次数(P＜0.01, P＜0.05)。结论: 晕吐宁颗粒对眩晕具有显著的治疗效果。}     

乳癖消颗粒对家兔乳腺增生的抑制作用

摘 要 目的：考察乳癖消颗粒对家兔乳腺增生的抑制作用,并探讨其抑制作用的可能机制,为该药临床应用提供理论依据。方法: 苯甲酸雌二醇联合黄体酮法构建家兔乳腺增生模型,以逍遥丸、三苯氧胺为阳性对照组,受试药乳癖消颗粒分为低、中、高（0.525,1.05,2.1 g·kg^-1）剂量组,按组别灌胃30 d,测定家兔血清中的雌二醇（E2）、孕酮（PROG）、催乳素（PRL）、促卵泡生成素（FSH）及促黄体生成素（LH）含量。并对乳腺组织进行病理组织学检查同时检测各组家兔乳腺组织中血管内皮增长因子（VEGF）的含量表达。结果: “保留卵巢 苯甲酸雌二醇联合黄体酮法” 可用于构建家兔乳腺增生模型。与模型组比较,乳癖消颗粒可使家兔血清E2及PRL含量明显下降（P<0.01）,PROG含量显著升高（P<0.01或P<0.001）。与模型组比较,乳癖消颗粒高剂量组可恢复到空白对照组家兔的乳腺结构的水平,抗乳腺增生作用优于逍遥丸和三苯氧胺。与模型组比较,各给药治疗组家兔乳腺组织中VEGF的表达均明显下降（P<0. 001）。结论: 乳癖消颗粒对家兔乳腺增生有较好的治疗作用。乳癖消颗粒对家兔乳腺增生的抑制作用可能与抑制家兔乳腺增生组织中VEGF的表达有关,其抑制水平与三苯氧胺和逍遥丸的抑制水平无差异。     

耳复康口服液对小鼠微循环障碍的影响

摘 要 目的：观察耳复康口服液对肾上腺素致急性血瘀症小鼠微循环障碍的影响。方法: 将小鼠随机分为模型组,脑得生片组（1.35 g·kg^-1）,高(30 ml·kg^-1)、中(15 ml·kg^-1)、低(7.5 ml·kg^-1)剂量耳复康口服液组,用微循环仪观察正常小鼠给药1 h后毛细血管开放数。尾静脉注射肾上腺素造成耳廓微循环障碍,观察造模后2 min小鼠的毛细血管开放数及血流情况。结果:和模型组相比,高、中、低剂量耳复康口服液对正常小鼠耳廓毛细血管开放数无明显影响(P＞0.05);与模型组相比,高、中剂量耳复康口服液可显著改善肾上腺素致小鼠耳壳微循环障碍模型微循环血流情况(P＜0.05或P<0.01),可明显对抗肾上腺素所致小鼠耳壳微循环障碍模型毛细血管网开放数的减少(P<0.05)。结论:耳复康口服液有改善微循环障碍的作用。     

健脾生血颗粒对气虚、脾虚型贫血模型小鼠的治疗效果

摘 要 目的： 探讨健脾生血颗粒对气虚、脾虚型贫血小鼠的治疗效果。方法: 昆明鼠（SPF级）随机分为模型对照组、正常对照组、健脾生血组、浸膏组、硫酸亚铁组等5组。除正常对照组外,其余受试动物均皮下注射利血平建立脾气虚症小鼠模型。分别考察健脾生血颗粒对小鼠单核吞噬细胞功能、小鼠血清溶血素的影响以及对小鼠疏肝和胃功效的影响。结果: 与其余各实验组相比,健脾生血组能显著提高小鼠的血清溶血素水平（P<0.05）;对廓清指数作用显著（P<0.05）,可提高吞噬活性（P<0.01）,显著改善疏肝和胃模型小鼠的体质量和进食量（P<0.01）。结论:健脾生血颗粒能提高免疫水平,对于气虚脾虚型贫血中医模型小鼠具有显著的治疗效果,这对于临床使用健脾生血颗粒具有一定的参考价值。     

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.

     

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.     

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.     

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.     

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.