新的苄胺类化合物的合成及其体外抗真菌活性

目的：研究在萘环侧链α位引入大基团（三唑甲基）对苄胺类化合物抗真菌活性的影响。方法：设计合成了９个新的苄胺类化合物。选择６种临床致病真菌为试验菌株,观察本类化合物对它们的体外抑制活性。结果：新化合物的抗真菌活性低于对照药物布替萘芬。结论：在萘环侧链α位引入大基团（三唑甲基）降低了苄胺类化合物的抗真菌活性。     

1-(1H-1,2,4-三唑-1-基)-2-(2,4-二氟苯基)-3-芳氧基-2-丙醇的合成及抗真菌活性

目的:寻找高效抗真菌化合物,探讨三唑醇类化合物的构效关系.方法:根据三氮唑类抗真菌药物的构效关系和作用机制,设计合成了14个1-(1H-1,2,4-三唑-1-基)-2-(2,4-二氟苯基)-3-芳氧基-2-丙醇类化合物,用微量液基稀释法测定化合物对白念珠菌、新生隐球菌、近平滑念珠菌、热带念珠菌、红色毛癣菌、羊毛状小孢子菌、薰烟曲霉菌和紧密着色真菌8种临床常见致病真菌的体外抑菌活性(MIC80).结果:以氧原子替代侧链中的硫原子后,侧链中含有邻位取代苯基的化合物的总体抗真菌活性不高,而侧链含有间位或对位苯基的化合物表现了很好的体外抗真菌活性.结论:间位或对位取代苯基的引入有利于此类化合物的抗真菌活性.     

新的三唑类化合物体外抗真菌活性及构效关系

目的：研究１－［２－（取代苯基）－２－（取代苯基甲硫基）乙基］－１Ｈ－１，２，４－三唑类化合物体外抗真菌活性，并初步探讨其构效关系。方法：选择８种临床致病真菌为试验菌，观察本类化合物对它们的体外抑菌活性。结果：所有化合物对８种试验菌的抑菌活性均优于或相当于氟康唑，大部分化合物的抑菌活性与硫康唑相当或更优。结论：本类化合物具有较强的广谱抗真菌活性，为深入开展广谱抗真菌药研究提供一条途径。     

三氮唑醇苄胺类化合物的合成及其抗真菌活性

依据三氮唑醇类和烯丙胺类化合物的构效关系,合成高效、低毒,广谱的新型抗真菌化合物。方法：设计合成方法并对所合成的化合物用沙氏液法测定其体外最低抑菌浓度。结果：合成了８个新的三氮唑醇苄胺类化合物,８个目标化合物对选用７种病真菌都显示不同程度的抗 力活性,抗深部真菌效果均较好。     

2-\[(1-取代苯基-1H-1,2,3-三唑-4-基)甲硫基\]-5-(3,4,5-三甲氧基苯基)-1,3,4-二唑化合物的合成及抗真菌活性

[摘要] 目的：寻找高效抗真菌化合物,探讨2-[(1-取代苯基-1H-1,2,3-三唑-4-基)甲硫基]-5-(3,4,5-三甲氧基苯基)-1,3,4-噁二唑化合物的构效关系。方法：设计合成了20个2-[(1-取代苯基-1H-1,2,3-三唑-4-基)甲硫基]-5-(3,4,5-三甲氧基苯基)-1,3,4-噁二唑化合物,用微量液基稀释法测定化合物对6种临床常见致病真菌:白念珠菌、新生隐球菌、热带念珠菌(Candida tropicalis)、近平滑念珠菌、红色毛癣菌、克鲁氏假丝酵母的体外抑菌活性。结果：体外抗真菌活性测试结果表明,所合成的目标化合物对所测菌株均具有一定的体外抗真菌活性。其中化合物8m, 8o对白色念珠菌的抑制活性约为氟康唑,酮康唑的3倍;化合物8a, 8e, 8k, 8l, 8n 和 8p对白色念珠菌的抑制活性也较氟康唑,酮康唑强。结论：所合成的化合物中,苯环上连有体积较小取代基的化合物抗真菌活性较好。 [关键词] 合成;噁二唑;抗真菌活性     

20种四氢萘类抗真菌化合物体外抑菌活性测定

目的:考察20种四氢萘类化合物体外抗真菌活性.方法:采用NCCLS的M27-A方案,以不同氟康唑敏感性的念珠菌及非念珠菌为供试菌进行体外药敏试验.对化合物22-1、31-1及其盐酸盐22、31,还有化合物34-1、26-1及其溴酸盐34、26进行时间生长曲线实验以及与其他结构抗真菌药进行体外联合药敏试验.结果:该类化合物均具一定抗真菌活性,尤其是化合物31-1对氟康唑敏感白念珠菌的抑菌活性明显强于氟康唑,持续抑菌时间超过54 h;化合物22和22-1对氟康唑耐药白念珠菌及近平滑念珠菌和红色毛癣菌作用强大,MIC50值均＜0.125 μg/ml,对于氟康唑耐药的白念珠菌抑菌活性强于酮康唑.此类药物与小檗碱或特比萘芬联用可产生协同作用.结论:四氢萘类化合物结构新颖,体外抗真菌活性显著,值得进一步研究开发.     

口腔念珠菌感染患者口内菌株检出情况和药敏性观察

目的探讨口腔念珠菌病患者口内念珠菌珠菌种的分布和体外药物敏感性。方法收集患者标本采用念珠菌显色培养基对其进行分离鉴定,采用NCCLS M27-A2微量稀释法测定念珠菌株对特比萘芬、氟康唑、伊曲康唑、制霉菌素四种抗真菌药物以及联合用药的体外药敏情况。结果试验组和对照组口腔念珠菌检出率分别为74.65%%和35.42%,其中白色念珠菌分别占62.26%和58.82%。特比萘芬、氟康唑、伊曲康唑、制霉菌素对口腔念珠菌的体外试验敏感性总有效率分别为57.89%、86.84%、84.21%和100.00%。特比萘芬与氟康唑联用时,念珠菌对药物敏感性增高。结论口腔念珠菌病仍以白色念珠菌为主,治疗时应进行真菌常规菌种鉴定及药敏试验。对耐药菌株的治疗,联合用药也是重要方法。     

盐酸布替萘芬乳膏治疗体癣和足癣的疗效观察

盐酸布替萘芬是一种苄胺类化合物,其体外抗真菌的活性很高,尤其在抗浅部真菌感染时其疗效要优于咪唑类的抗真菌药物.我科对临床的240例体癣和足癣患者进行了临床观察.     

3-取代三唑类抗真菌化合物的设计、合成及体外抗真菌活性

目的合成1,2,3-三唑侧链取代三唑醇类化合物并考察其体外抗真菌活性。方法设计合成了21个三唑醇类新化合物,所得化合物结构都经过1HNMR、MS确证;选择8种真菌为实验菌株,进行体外抗真菌活性测试。结果所合成的化合物均具有一定的体外抗真菌活性,其中化合物7{1-(1H-1,2,4-三唑-1-基)-2-(2,4二氟苯基)-3-[N,N-(4-亚甲基-1-取代苄基-1H-1,2,3三唑)]-2-丙醇}对白色念珠菌的MIC80值为0.25μg/ml,是氟康唑活性的4倍,化合物Ⅵ{1-(1H-1,2,4-三唑-1-基)-2-(2,4二氟苯基)-3-(N,N-二炔丙基)-2-丙醇}对白色念珠菌的MIC80值为0.0156μg/ml,是氟康唑活性的64倍,是伊曲康唑的4倍。结论利用13偶极加成反应可以方便地在化合物中引入1,2,3-三唑基;较大的侧链结构可能不利于目标化合物活性的提高。     

105例念珠菌性包皮龟头炎菌种分析及药敏试验

目的了解念珠菌性包皮龟头炎的菌种分布及菌株对三种常用抗真菌药物的敏感性。方法对所有拟诊患者进行直接镜检和真菌培养。并根据美国国家临床实验室标准化委员会（CLSI）推荐的M27—A液基微量稀释法对部分分离株作伊曲康唑、特比萘芬和氟康唑3种抗真菌药物敏感性测定。结果共分离培养出115株念珠菌,其中单纯感染95例,混合感染10例,所分离的念珠菌中,白念珠菌79株,光滑念珠菌25株,热带念珠菌8株,克柔念珠菌3株。药敏试验显示：40株白念珠菌对伊曲康唑、特比萘芬和氟康唑的平均MIC（最低抑菌浓度）值分别是：0.85μg/ml,1.68μg/ml,4.42μg/ml;而20株光滑念珠菌对伊曲康唑、特比萘芬和氟康唑的平均MIC值分别是：2.34μg/ml,1.73μg/ml,32.32μ/ml。结论白念珠菌仍是念珠菌性包皮龟头炎的首要病原菌,体外药敏试验显示伊曲康唑和氟康唑对白念珠菌引起的念珠菌性包皮龟头炎有很好的敏感性,而特比萘芬对光滑念珠菌引起的念珠菌性包皮龟头炎的敏感性优于伊曲康唑和氟康唑。     

Value of D-Dimers in patients with acute aortic dissection

Objective: To evaluatel the value of D-dimers in patients with acute aortic dissection (AAD). Methods: This study consisted of 16 patients with AAD and 27 non-AAD patients. Serum D-dimets were measured by Sta-Liatest D-DI immunoturbidimetric assay. Results: D-dimer level was higher (P ＜ 0.001) in patients with AAD(7.91 ± 5.52 μg/ml) than that in non- AAD group(1.57±1.24 μg/ml). D-dimer was positive (＞0.4 μg/ml) in all patients with AAD and in 10 control group patients (37%). Among patients with acute AAD, D-dimers tended to be higher in Stanford A than in Stanford B (8.67 ± 4.31 μg/ml vs. 3.24±1.27 μg/ml, P ＜0.01). D-dimer values tended to be higher in more extended disease(3.84 ± 1.65 μg/ml, 8.57 ± 3.58 μg/ml and 11.87 ± 5.69 μg/ml in thoracic aorta, thoracic and abdominal aorta, thoracic and abdominal aorta and iliacal arteries, respectively, P ＜ 0.05 for both 8.57 ± 3.58 and 11.87 ± 5.69 vs. 3.84 ± 1.65 ). Including the control group into the analysis, we found a sensitivity of 100%, a negative predictive value of 100%, and a specificity of 66% and a positive predictive value of 64% for D-dimer in diagnosis of AAD in our patients with suspected AAD. Conclusion: D-dimer was elevated in patients with AAD. A negative D-dimer test result could be useful in excluding AAD.     

Research of combined liver-kidney transplantation model in rats

Objective： To set up a simple and reliable rat model of combined liver-kidney transplantation. Methods： SD rats served as both donors and recipients. 4℃ sodium lactate Ringer＇s was infused from portal veins to donated livers,and from abdominal aorta to donated kidneys, respectively. Anastomosis of the portal vein and the inferior vena cava （IVC） inferior to the right kidney between the graft and the recipient was performed by a double cuff method, then the superior hepatic vena cava with suture. A patch of donated renal artery was anastomosed to the recipient abdominal aorta. The urethra and bile duct were reconstructed with a simple inside bracket. Results： Among 65 cases of combined liver-kidney transplantation, the success rate in the late 40 cases was 77.5%. The function of the grafted liver and kidney remained normal. Conclusion： This rat model of combined liver-kidney transplantation can be established in common laboratory conditions with high success rate and meet the needs of renal transplantation experiment.     

Development on Adjustable Calibration Marker for Shock Wave Focus

Shock wave lithotripsy （SWL） is a treatment of choice for upper urinary stones. However, this procedure is inappropriate for obese patients because the focus is often unable to reach the target owing to the limited focal distance in shock wave source. Although treating such patients in a blast path may increase the application length of shock wave source, it＇s difficult to find this path on the lithotripter monitor. For this reason, we invented an adjustable calibration marker in order to set an effective focus in the shock wave hath.     

Study on the TCM Pathogenesis of Angiopathic Complications of Type II Diabetes

Excess production of reactive oxygen species(ROS)of mitochondrion mediated by hyperglycemia is the common pathogenesis of angiopathic complications of diabetes.TCM holds that the damp from the dysfunction of spleen.kidney and liver is the causative factor of complications of diabetes.This is similar to the mechanism of Ros resulting in angiopathic complications of diabetes.When the angiopathic complications of type II diabetes mellitus(T2DM)are difierentiated as caused by turbid damp in TCM can be explained as ROS.Since the obstruction of pathogenic damp in channels and collaterals is said to be the main pathogenesis,the treating principle should be dissolving the damp to remove the obstruction.     

Leptin, Ghrelin and TNF-α before and after Hypo-caloric Traditional Chinese Diet and Auricular Acupuncture

INTRODUCTION Obesity is a complex emergent problem, which can be possibly solved not only by the diet but also by the life style and promotion of a constant physical exercise. 1, 2 No doubt careful attentions must be given to the nutritional condition of obese people, the dietary habits, the somatic build (i.e. distribution of fat mass) and the organic functions linked to formation of the fat mass. All the parameters should be constantly monitored before, during and after a diet treatment. 3, 4, 5     

BLOOD PRESSURE CHANGE WITH AGE IN SALT-SENSITIVE TEENAGERS

Objective To observe blood pressure change with age in salt-sensitive teenagers whose salt sensitivity were determined by repeated testing.Methods Salt sensitivity was determined through intravenous infusion of normal saline combined with volume-depletion by oral diuretic furosemide in 55 teenagers. After five years, salt sensitivity was re-examined and subject blood pressure was followed up. Blood pressure changes in salt-sensitive teenagers were compared to that of non-salt sensitive teenagers over five years.Results After 5 years, the repetition rate of salt sensitivity determined by intravenous saline loading is 92.7%. In teenagers with salt sensitivity on the baseline, both the systolic blood pressure increments and increment rates were much higher than non-salt sensitive teenagers (12.7±12.1 mmHg vs. 2.8±5.2 mmHg, P＜ 0.01; 12.2%± 12.0% vs. 2.5% ±4.4%, P＜ 0.001,respectively). There was a similar trend for diastolic blood pressure (8.4 ± 6.4 mmHg vs. 3.7 ± 6.4 mmHg, P = 0.052; 13.2% ±10.6 % vs. 6.8%± 10.1%, P = 0.053, respectively).Conclusions Salt sensitivity determined by intravenous saline loading showed good reproducibility. Blood pressure increments with age were much higher in salt-sensitive teenagers than non-salt sensitive teenagers, especially in terms of systolic blood pressure.     

Relationship between Dysglycemia and Carotid Atherosclerosis in Tibetan Population

People with dysglycemia are at high risk for atherosclerotic diseases. This study aims at investigating the atherosclerotic vascular damage in dysglycemia and its metabolic origin in Tibetan population.     

APPLICATION OF LORNOXICAM TO PATIENT-CONTROLLED ANALGESIA IN PATIENTS UNDERGOING ABDOMINAL SURGERIES

FOR anesthesiologis s ,treatingpostoperativepainhas alwaysbeen a problem.Althoughopioidshave been provedtobe effective,theirsideeffectscouldnotbeignored.With thedevelopmentofscienceand pharmacology,many drugs with aspectsof satisfactoryanalgesicefficacyand couldbe welltoleratedby patientshave been developed.And lornoxicamisone of them, which isa non-steroidalanti-inflammatorydrug (NSAID ), with analgesic, anti-infl-ammatory,andantipyreticproperties.Itseliminationhalf-time(3 to 5 hours) isle…     

安心颗粒对急诊经皮冠状动脉介入术后生活质量影响的研究

目的：评价使用安心颗粒对急诊经皮冠状动脉介入术（PPCI）术后生活质量的影响.方法：将160例接受PPCI的急性ST段抬高型心肌梗死患者随机分为安心颗粒组（术前顿服安心颗粒8.8g,术后安心颗粒4.4 g/次,每日2次）和对照组（仅接受基础药物治疗）.所有患者均服用阿司匹林、氯吡格雷和阿托伐他汀.分别在入院时、出院前1d、出院后180 d时,应用心肌梗死多维度量表（MIDAS）、中文版SF-36评价量表对患者生活质量评分.并观察术后30 d以内的出血并发症、血小板减少症发生情况.结果：入院时和出院前1d,两组患者的心肌梗死MIDAS、SF-36量表评分比较无差异（P＞0.05）;出院后180 d时,与对照组比较,安心颗粒组MIDAS、SF-36评分明显减低（P＜0.05）;组内与入院时比较,两组出院前1d、出院后180 d时,MIDAS、SF-36评分均降低（P＜0.05）.两组患者在随访期间均无大量出血、少量出血、重度和极重度血小板减少症发生,安心颗粒组有4例、对照组有7例发生不明显出血（P＞0.05）.两组发生轻度血小板减少症的患者数比较无差异（P＞0.05）.结论：PPCI使用安心颗粒,能改善急性ST段抬高型心肌梗死患者的生活质量,且不增加出血风险.     

CLINICAL SIGNIFICANCE OF SERUM CYTOKINES IL-1β,sIL-2R,IL-6,TNF-α,AND IFN-v IN ACUTE CORONARY SYNDROME

Objectives To explore serum cytokines levels (including IL-1 β, sIL-2R, IL-6, TNF-α, and IFN-v) and their significance in patients with acute coronary syndrome (ACS) and the subsequent follow-ups, with attempt to estimate the role of various serum inflammatory markers in the diagnosis and assessment of ACS.Methods The study population include 40 patients with acute myocardial infarction (AMI), 40 patients with unstable angina pectoris (UAP), and 40 controls. Among the 80 patients, 60 patients attended a follow up 4 months later. Serum inflammatory markers including IL-1 β, sIL-2R, IL-6, TNF-α, and IFN-v were measured by enzyme linked immunosorbent assay.Results Serum IL- 1 β, sIL-2R, IL-6, TNF-α were significantly higher in AMI group or UAP group compared to the control group and became significantly lower 4 months later in the follow-up patients. Serum levels of IFN-v shows no significant difference between AMI group or UAP group and controls, also showing no significant change when measured in follow up patients. There was no correlation between serum creatine kinase-MB isoenzyme levels and serum inflammatory markers either in UAP or AMI group. Furthermore, when divided into two subgroups using Wagner's QRS scoring system in the AMI group, there is no difference of each serum inflammatory marker between ≤ 6 scores group and ＞ 6 scores group.Conclusion Serum levels of certain inflammatory markers may have some diagnostic value for ACS, and can be a useful marker reflecting disease stability.