贝那普利对原发性高血压患者血清细胞因子水平及内皮功能的影响

目的 探讨贝那普利对原发性高血压患者血清细胞因子水平及内皮功能的影响.方法 76例原发性高血压患者（治疗组）采用贝那普利治疗6个月,30例健康体检者作为对照组,采用酶联免疫吸附法检查两组治疗前后血清细胞因子肿瘤坏死因子-α（TNF-α）、白细胞介素-8（IL-8）、白细胞介素-10（IL-10）、及内皮功能指标血清一氧化氮（NO）和内皮素（ET）水平,并测定内皮依赖性舒张功能（EDD）.结果 治疗前血清IL-8、TNF-α水平明显高于对照组（均P＜0.01）,IL-10水平低于对照组（P＜0.05）.治疗组治疗后血清IL-8、TNF-α水平较治疗前明显下降（P＜0.05或P＜0.01）,IL-10水平明显升高（P＜0.05）;EDD及NO水平较治疗前均明显升高（均P＜0.01）、ET明显降低（P＜0.05）,EDD及NO水平与对照组差异均无统计学意义（均P＞0.05）、ET高于对照组（P＜0.05）.结论 贝那普利可明显改善原发性高血压患者的内皮功能,抑制炎性反应,是理想降压药物.     

贝那普利联合比索洛尔的降压效果与安全性分析

目的 探讨贝那普利联合比索洛尔的降压疗效与安全性.方法 选择原发性高血压患者174例,按随机数字表法分为观察组和对照组,每组87例.对照组给予贝那普利20 mg/次,2次/d.观察组给予贝那普利10 mg/次,1次/d;比索洛尔5 mg/次,1次/d.比较两组治疗前后偶测血压、24h动态血压变化及不良反应,并评价降压疗效.结果 治疗总有效率对照组为51.72％ (55/87),观察组为86.21％(75/87),差异有统计学意义(x2=11.32,P＜0.05).治疗后两组偶测血压、24h动态血压较治疗前均有明显下降(t=6.67、6.30、4.11、4.22,均P＜0.05),观察组较对照组下降更为显著(t=4.92、4.61,均P＜0.05).不良反应发生率对照组为11.49％(10/87),观察组为3.45％(3/87),差异有统计学意义(x2=4.76,P＜0.05).结论 小剂量贝那普利联合比索洛尔可优势互补,既增强降压效果,又减少不良反应,不失为一种理想组合,值得临床推广应用.     

缬沙坦与贝那普利治疗原发性高血压效果比较

目的观察缬沙坦和贝那普利对原发性高血压的降压效果。方法选择本院103例轻中度原发性高血压患者,随机分为缬沙坦组（53例）和贝那普利组（50例）,缬沙坦组每日晨服缬沙坦80mg;贝那普利组每日晨服10mg,均连续服用12周。实验结束后测定患者的舒张压和收缩压,并检查患者血糖、血脂以及肝肾功能的变化。结果用药12周后,缬沙坦组的收缩压与舒张压均明显低于用药前（t=2.73,P=0.0081;t=2.61,P=0.0091）,收缩压变化值为（19.6±3.6）mm Hg,舒张压变化值为（13.5±0.7）mm Hg;贝那普利组的收缩压与舒张压也明显低于用药前（t=2.68,P=0.0089;t=2.57,P=0.0093）,收缩压变化值为（9.7±1.4）mm Hg,舒张压变化值为（9.0±1.0）mmHg。两药用药前后收缩压舒张压变化值比较缬沙坦组均高于贝那普利组（t=2.13,P=0.0280;t=2.14,P=0.0410）。两组总有效率、血糖、血脂及肝肾功能治疗前后比较差异均无统计学意义。贝那普利组出现轻微不良反应。结论缬沙坦和贝那普利均有良好的降压作用和使用安全性,但缬沙坦的降压效果优于贝那普利,为一种安全有效的降压药物,可作为轻中度高血压一线降压药,且在同类产品中价格较低。     

替米沙坦对慢性心力衰竭患者神经内分泌激素的影响

目的 探讨替米沙坦对慢性心力衰竭患者神经内分泌激素的影响.方法 将96例慢性心力衰竭患者(心功能Ⅱ～Ⅳ级)随机分为两组,分别接受替米沙坦、贝那普利治疗.放射免疫法测定治疗前、治疗3个月后血浆去甲肾上腺素、肾素、血管紧张素Ⅱ、醛固酮及内皮素水平的变化.结果 替米沙坦、贝那普利治疗后血浆去甲肾上腺素、内皮素水平均有明显下降(P＜0.01);贝那普利组血浆肾素、血管紧张素Ⅱ、醛固酮水平无显著变化(P＞0.0 5);替米沙坦组血浆肾素、血管紧张素Ⅱ水平有显著下降(P＜0.01),但醛固酮水平无明显变化(P＞0.0 5).结论 替米沙坦对慢性心力衰竭患者神经内分泌激素只有部分改善作用.     

孟鲁司特对哮喘患者血浆炎症因子的影响及疗效观察

目的 探讨孟鲁司特对哮喘患者血浆炎症因子的影响及疗效观察.方法 对40例急性发作期的轻中度哮喘患者(哮喘组)予以孟鲁司特钠片10mg,口服,每晚1次,连用8周.在治疗前后检测血浆IL-6、IL-8和IL-10的水平,并观察肺功能和日夜间症状的变化.另取体检中心的健康体检者30例作为对照组.结果 哮喘组患者治疗前血浆IL-6和IL-8水平明显高于对照组,IL-10水平明显低于对照组(P＜0.01),经孟鲁司特治疗8周后患者血浆IL-6和IL-8水平均较治疗前明显下降,IL- 10水平较治疗前明显上升(均P＜0.01),且肺功能指标FEV1％、PEF％和日夜间症状均明显改善(均P＜0.01).结论 孟鲁司特治疗哮喘的疗效确切,能明显改善患者临床症状和肺功能,作用机制与调控血浆炎症因子的表达有关.     

原发性高血压病患者血清细胞因子水平变化及贝那普利对其影响的意义分析

目的探讨原发性高血压病患者细胞因子IL-8、TNF-α及IL-10的变化及临床意义。方法采用酶联免疫吸附法（ELISA法）检测52例原发性高血压病患者及30例正常人血清细胞因子水平并进行比较。结果与正常对照组相比,原发性高血压病患者血清IL-8及TNF-α水平明显升高（P〈0.01）,IL-10明显降低（P〈0.01）;贝那普利治疗后患者血清IL-8和TNF-α水平明显下降（P〈0.01）,血清IL-10明显升高（P〈0.01）。结论原发性高血压患者血清细胞因子水平出现明显变化,并在疾病的发生发展过程中起重要作用。     

卡维地洛对慢性充血性心力衰竭患者血浆炎性细胞因子及临床疗效的影响

目的 探讨卡维地洛对慢性充血性心力衰竭(CHF)患者血浆炎性细胞因子及临床疗效的影响.方法 选择住院治疗CHF患者72例,采用随机数字表将患者分为观察组与对照组.两组患者入院后予以强心、利尿和扩张血管等常规治疗.观察组患者在此基础上加用卡维地洛治疗,初始剂量3.125 ag,2次/d,逐渐递增加量,直至维持量25mg,2次/d,连用12周.观察比较两组治疗前后血浆肿瘤坏死因子-α(TNF-α)、白细胞介素-1(IL-1)和白细胞介素-6(IL-6)水平变化及临床治疗效果.结果 治疗12周后,两组血浆TNF-α、IL-1和IL-6均较前明显下降(t=3.02、3.17、2.97、2.26、2.25、2.21,均P＜0.05),且观察组下降幅度较对照组更显著(t =2.32、2.35、2.29,均P＜0.05);同时观察组的临床总有效率(94.44％)明显高于对照组(77.78％)(x2 =4.18,P＜0.05),两组患者治疗期间未见明显的药物不良反应.治疗后随访1年,观察组再次住院率(61.11％)明显低于对照组(36.11％)(x2=4.50,P＜0.05),但两组病死率差异无统计学意义(x2=0.26,P＞0.05).结论 卡维地洛治疗CHF安全有效,能降低血浆细胞因子TNF-α、IL-1和IL-6水平,减少患者的再次住院率,改善患者的预后.     

贝那普利联合黄芪注射液治疗肾实质性高血压临床观察

目的 观察贝那普利联合黄芪注射液治疗肾实质性高血压患者的疗效.方法 对42例肾实质性高血压患者应用贝那普利联合黄芪注射液治疗4周.于治疗前后测定收缩压、舒张压、24h尿蛋白定量、血浆白蛋白、血清肌酐、尿素氮水平.结果 收缩压由治疗前的(157.8±13.2)mm Hg降为治疗后的(129.0±14.2)mmHg(t =3.134,P＜0.001),DBP由治疗前的(100.7±11.6)mm Hg降为(88.0±9.3)mm Hg(t=4.237,P＜0.01).治疗后24h尿蛋白定量、血肌酐、尿素氮较治疗前明显下降(P＜0.05).结论 盐酸贝那普利联合黄芪注射液治疗肾实质性高血压在控制血压,减少尿蛋白,改善肾脏损害方面有可靠疗效.     

肾康注射液联合贝那普利对特发性膜性肾病患者蛋白尿的影响

目的观察肾康注射液对特发性膜性肾病患者蛋白尿的影响。方法将78例特发性膜性肾病患者随机分为4组,对照组18例,给予常规降压、调脂、双嘧达莫片抗凝治疗。贝那普利片组20例,常规治疗基础上加用贝那普利片治疗;肾康注射液组19例,常规治疗基础上加用肾康注射液治疗;联合治疗组21例,常规治疗基础上加用肾康注射液联合贝那普利片治疗。4组疗程均为4周。观察治疗前后24h尿蛋白定量、血浆白蛋白、血肌酐变化。结果肾康注射液组、贝那普利片治疗组治疗后24h尿蛋白定量较对照组下降（P〈0.05）,血浆白蛋白升高（P〈0.05）,血肌酐未见明显变化（P〉0.05）。肾康注射液组24h尿蛋白定量较贝那普利片组下降明显（P〈0.05）,血浆白蛋白升高明显（P〈0.05）。联合治疗组治疗后24h尿蛋白定量较其余3组显著下降（P〈0.05）,血浆白蛋白较其余3组显著升高（P〈0.05）。结论肾康注射液联合贝那普利片治疗原发性膜性肾病蛋白尿有明显疗效,且未出现明显的不良反应。     

培哚普利联合美托洛尔治疗老年人慢性心力衰竭

目的 观察培哚普利联合美托洛尔治疗老年人慢性心力衰竭的疗效.方法 136例60岁以上慢性心力衰竭患者随机分为两组,对照组(68例)采用洋地黄、利尿剂和硝酸酯类药物等治疗,治疗组(68例)在对照组治疗基础上加服培哚普利和美托洛尔.4～8周为1个疗程.观察两组治疗前后心功能、左室射血分数、六分钟步行试验和血浆脑利钠肽(BNP)改变等.结果 治疗后,治疗组总有效率94.1％,明显高于对照组的70.6％(x2=5.96,P＜0.05);两组治疗后慢性心力衰竭评价指标均较治疗前明显改善(t=2.56、3.23、2.48、2.53、2.79、3.31,均P＜0.05),治疗组较对照组改善更明显(t=2.87、3.12、2.59,均P＜0.05),两组治疗过程中均未发生严重不良反应.结论 培哚普利联合美托洛尔治疗慢性心力衰竭可改善心室重构,提高治疗效果.     

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.     

Aquatic Insects and Trace Metals: Bioavailability,Bioaccumulation, and Toxicity

Abstract

The uptake of metals from food and water sources by insects is thought to be additive. For a given metal, the proportions taken up from water and food will depend both on the bioavailable concentration of the metal associated with each source and the mechanism and rate by which the metal enters the insect. Attempts to correlate insect trace metal concentrations with the trophic level of insects should be made with a knowledge of the feeding relationships of the individual taxa concerned. Pathways for the uptake of essential metals, such as copper and zinc, exist at the cellular level, and other nonessential metals, such as cadmium, also appear to enter via these routes. Within cells, trace metals can be bound to proteins or stored in granules. The internal distribution of metals among body tissues is very heterogeneous, and distribution patterns tend to be both metal and taxon specific. Trace metals associated with insects can be both bound on the surface of their chitinous exoskeleton and incorporated into body tissues. The quantities of trace meals accumulated by an individual reflect the net balance between the rate of metal influx from both dissolved and particulate sources and the rate of metal efflux from the organism. The toxicity of metals has been demonstrated at all levels of biological organization: cell, tissue, individual, population, and community. Much of the literature pertaining to the toxic effects of metals on aquatic insects is based on laboratory observations and, as such, it is difficult to extrapolate the data to insects in nature. The few experimental studies in nature suggest that trace metal contaminants can affect both the distribution and the abundance of aquatic insects. Insects have a largely unexploited potential as biomonitors of metal contamination in nature. A better understanding of the physico-chemical and biological mechanisms mediating trace metal bioavailability and exchange will facilitate the development of general predictive models relating trace metal concentrations in insects to those in their environment. Such models will facilitate the use of insects as contaminant biomonitors.     

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.     

Alzheimer’s disease – current trends in basic and clinical research. Highlights from the 16th ECNP

Advances in the molecular biological knowledge of neuronal nicotinic acetylcholine receptors (nAChRs) have led to a growing interest by the pharmaceutical industry in the development of novel compounds that selectively modulate nAChR function. The ability of (-)-nicotine, an activator of nAChRs, to enhance attentional aspects of cognition in animals and humans, to exert neuroprotective and anxiolytic-like effects, and presumably to mediate the negative correlation between smoking and Alzheimer's (and Parkinson's) Disease, has focused interest on the potential therapeutic utility of modulators of nAChR function for treatment of some of the deficits associated with these progressive, neurodegenerative conditions. Numerous compounds are known which activate nAChRs and which might serve as lead compounds toward the development of such agents. The pharmacologic diversity of neuronal nAChR subtypes suggests the possibility of developing selective compounds which would have more favourable side-effect profiles than existing agents. This broader class of agents, collectively called cholinergic channel modulators (ChCMs), is anticipated to encompass compounds which would have more favourable side-effect profiles than existing agents, which generally exhibit low selectivity. This selectivity may be achieved by preferentially activating some subtypes of nAChRs (i.e., Cholinergic Channel Activators, ChCAs) or inhibiting the function of other subtypes (Cholinergic Channel Inhibitors, ChCIs). An overview of the biology of nAChRs and the rationale for the use of ChCMs for the treatment of dementia related to neurodegenerative diseases are presented, followed by a discussion of lead compounds and compounds under consideration for clinical evaluation.