急性心肌梗塞静脉溶栓治疗的临床观察

本文对５２例急性心肌梗塞（ＡＭＩ）６小时内入院患者进行静脉给药溶解血栓治疗，其溶栓药物为尿激酶（ＵＫ）、去纤酶，其中６例并用前列腺素Ｅ１（ＰＧＥ１）联合溶栓。其结果显示：５２例中再通２９例再通率５５．７７％。其中ＵＫ组３６例再通２０例，再通率５５．５６％；ＵＫ＋ＰＧＥ１组６例，４例再通，再通率６６．６７％；去纤酶组１０例，再通５例，再通率５０．０％。再通表现：梗塞性胸痛明显缓解；抬高ＳＴ段明显下降，平均最大下降率７２．２５±１９．２５％；ＣＫ峰值时间１５．１±３．１小时，ＣＫ一ＭＢ峰值１４．８±２．６小时；再灌注心律改变２１例，占７２．４％。再阻塞９例，占３１．０３％。住院死亡５例，占９．６％。     

尿激酶联合阿斯区林治疗急性心肌梗塞临床观察

对５５例急性心肌梗塞（ＡＭＩ）患者行尿激酶（ＵＫ）＋阿斯区林治疗（联合用药组）和单用ＵＫ组（对照组）Ｐ，以单盲法观察联合用药对ＡＭＩ的溶栓效果：结果：（１）联合用药组冠脉再通率显著高于对照组。（２）冠脉再闭塞率，４周内死亡率、磷酸肌酸激酶（ＣＰＫ）峰值显著低于对照组。（３）联合用药组胸痛缓解时间、心电图（ＥＣＧ）心肌受损抬高的ＳＴ段回降〉５０％。再灌注性心律失常（ＡＲ）发生的时间，ＣＰＫ峰值时间和     

抗血小板药物与溶栓剂联合溶栓治疗深静脉栓塞治疗机制的研究

抗血小板药物与溶栓剂联合溶栓治疗深静脉栓塞治疗机制的研究山西医学院第一附属医院（０３０００１）李正中，贺抗，温柱德，李思晋我们联合应用尿激酶（ＵＫ）、前列腺素Ｅ１（ＰＧＥｌ）和中药，对５６例深静脉栓塞（ＤＶＴ）病人进行治疗并检测凝血及纤溶指标，以探讨治疗机制及监测指标。材料与方法一、材料：ＵＫ：２万单位／Ａｍｐｌｅ，南京大学制药厂提供。１０万单位／Ａｍｐｌｅ，太原生化制药厂。ＰＧＥ１：白求恩医科大学制药厂。６０％泛影葡胺，上海信谊药厂。二、病例选择：７１例深静脉栓塞（ＤＶＴ）病人。随机分为二组进行治疗。治疗前均经９９ｍＴｃ－ＲＢＣ，ＥＣＴ血管显像及静脉造影确诊。①ＵＫ治疗组：５４例５６肢体，男２６例，女２８例；年龄２２～７８岁（４８．５±１５．９２）。病程２天～３年。５０例左下肢栓塞，２例左上肢，２例双下肢栓塞。②对照组：１５例。男７例，女８例。年龄２９～６８岁（４１．３±２０．６）。病程６月～１０年。三、治疗方案：①治疗组：ＵＫ２０００００Ｕ／日。静脉滴注，３小时滴完，每日一次，同时滴注ＰＧＥ１２００ｎｇ／日及中药通脉汤口服，１０天为一疗程。根据病情治疗２～３疗程。两疗程间休息３～５大。②对照组：１０例静     

急性心肌梗塞溶栓疗效与心脏舒张功能关系

目的 观察急性心肌梗塞（ＡＭＩ）患者静脉溶栓的临床疗效与心脏舒张功能关系。方法 选择接受静脉溶栓治疗的ＡＭＩ患者５０例，用ＨＰ２５００彩色多普勒超声心动图测定二尖瓣血流Ａ峰／Ｅ峰面积（ＶＡ／ＶＥ）、左室射血分数（ＬＶＥＦ）、短轴缩短率（ＦＳ），以及应用ＫｉｌｌｉＰ分级判定心功能。结果①３６例血管再通组与１４例未溶通组之间，在年龄、性别、ＡＭＩ部位、临床心功能、ＬＶＥＦ、ＦＳ以及高血压、糖尿病。陈旧心肌梗塞病史等方面均无显著差异（Ｐ＞ ０．０５）。②溶通组与未通组相比，ＶＡ／ＶＥ比值明显低于未通组（１．０１２９±０．３４２７比１．３３３５± ０．４０７７，Ｐ＜０．０１）；ＶＡ／ＶＥ＞１出现率少于未通组（４７．２％比８５．７％，Ｐ ＜ ０．０５）。结论 静脉溶栓治疗 ＡＭＩ使梗塞相关血管再灌注后，对左室舒张功能的保护作用可能会更大些。     

地塞米松及甘草酸对小鼠肝细胞凋亡的影响

目的研究地塞米松（ＤＭ）及甘草酸（ＧＬ）对小鼠肝细胞凋亡的影响。方法以肝／体重比、肝组织ＤＮＡ含量、组织学改变及原位凋亡细胞ＴＵＮＥＬ反应为指标,观察ＤＭ（９ｍｇ·ｋｇ－１）及ＧＬ（５０ｍｇ·ｋｇ－１）,ｉｐ,每８ｈ１次,对撤除苯巴比妥（ＰＢ）后引起的小鼠肝细胞凋亡的影响。结果与ＰＢ不撤除对照组相比,ＤＭ组小鼠肝／体重比及肝ＤＮＡ含量无明显回落,组织学检查未见明显凋亡改变,ＴＵＮＥＬ反应阴性。ＧＬ组小鼠肝／体重比及ＤＮＡ含量分别回落１２０％和１３６％,肝细胞出现典型凋亡改变,ＴＵＮＥＬ反应阳性。结论ＤＭ能阻断撤除ＰＢ诱导的小鼠肝细胞凋亡,甘草酸对其无影响。     

正交试验法优选大黄醇回流提取工艺

观察２６例肺心病呼衰并肺动脉高压患者应用前列腺素Ｅ１（ＰＧＥ１）栓剂治疗前后血浆ＴＸＢ２、６Ｋ－ＰＧＥ１ａ及ＰＡｍＰ的变化。结果发现，血浆ＴＸＢ２及ＰＡｍＰ治疗后均明显低于治疗前（Ｐ＜０．０１及Ｐ＜０．００１），血浆６－Ｋ－ＰＧＦ１ａ治疗后则明显高于治疗前（Ｐ＜０．００１）。提示ＰＧＥ１栓剂治疗肺心病呼衰患者肺动脉高压的近期疗效是显著的，可能通过调节ＴＸＢ２──６－Ｋ－ＰＧＦ１ａ平衡失调，间接发挥扩张血管的作用，并克服了静脉应用ＰＧＥ１及其他扩血管药物引起的体循环低血压等副作用。     

前列腺素E1治疗原发性肾病综合征蛋白尿的临床研究

为探讨前列腺素Ｅ４（ＰＧＥ４）对原发性肾病综合征（ＰＮＳ）病人蛋白尿的影响，对１０６例ＰＮＳ病人分组观察，ＰＧＥ４组４８例，用２００μｇ的ＰＧＥ１每日１次静滴，连用１５天为１疗程，共用２个疗程，强的松组４０例，给强的松每日１ｍｇ／ｋｇ连用４周，联合治疗组已用强的松４周以上尿蛋白消退下明显者，继续强的松应用的同时联用ＰＧＥ４，结果发现，ＰＧＥ４强的松对ＰＮＳ单纯型有效率分别为３０．５％，８１．８％，     

氯化钾泡腾颗粒的药代动力学研究

２０名健康自愿受试者分别于规定时间口服氟化钾泡腾颗粒（ＴＰＥＧ）和１０％氯化钾（ＫＣｌ）液，用原子吸收分光光度法测定血清Ｋ＋浓度，以二室模型拟合，在ＴＢＭ机上计算药动学参数。结果表明：实验组与对照组氯化钾的Ｋａ、ｔ（１／２）Ｋａ、α、ｔ（１／２）α、ＡＵＣ（０－∞）很接近，两者的Ｋ（２１）／Ｋ（１２）之比值分别为４．８５９和１．２２２，ＡＵＣ（０－∞）分别为１９７．１９０ｍｇ／ｍｌ·ｈ和２００．５８５ｍｇ／ｍｌ·ｈ，经ＳｔｕｄｅｎｔＴ检验无显著差异（ｐ＞０．０５），Ｆ＝９８．３％，证明ＴＰＥＧ有较好的补血钾效果。     

前列腺素 E_1 治疗原发性肾病综合征蛋白尿的临床研究

为探讨前列腺素Ｅ１（ＰＧＥ１）对原发性肾病综合征（ＰＮＳ）病人蛋白尿的影响，对１０６例ＰＮＳ病人分组观察。ＰＧＥ１组４８例，用２００μｇ的ＰＧＥ１每日１次静滴，连用１５天为１疗程，共用２个疗程；强的松组４０例，给强的松每日１ｍｇ／ｋｇ连用４周；联合治疗组为已用强的松４周以上尿蛋白消退不明显者，继续强的松应用的同时联用ＰＧＥ１。结果发现，ＰＧＥ１、强的松对ＰＮＳ单纯型有效率分别为３０．５％、８１．８％，两者间有非常显著性差异；对肾炎型有效率分别为８８０％和５５．６％，两者间有显著性差异，而两者的疗效与单纯型相反；联合应用时降尿蛋白作用加强。说明ＰＧＥ１比强的松对ＰＮＳ肾炎型患者的降尿蛋白作用更有效。     

前列腺素E1对慢性阻塞性肺疾病的疗效

目的：观察前列腺素Ｅ１（ＰＧＥ１）对慢性阻塞性肺疾病（ＣＯＰＤ）急性加重期患者的疗效。方法：对２５例ＣＯＰＤ的患者在常规治疗的基础上加用ＰＧＥ１ １００￣２００μｇ／ｄ,对照组仅接受常规治疗。结果：ＰＧＥ１治疗组患者临床症状和体征改善的有效率明显高于对照组;治疗组治疗后肺功能（ＦＥＶ１．０）有明显改善（Ｐ〈０．０１）,但对照组改善不明显（Ｐ〉０．０５）;２组患者治疗后血气分析各项指标（ｐＨ,ＰａＯ     

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.