In vitro activity of SK&F 104662, a new glycopeptide antibiotic.

The in vitro activity of SK&F 104662, a new glycopeptide antibiotic, against gram-positive bacteria was evaluated. Activity was comparable to those of teicoplanin and vancomycin against most organisms. SK&F 104662 inhibited diphtheroids at concentrations of less than or equal to 0.5 microgram/ml. Addition of human serum to the test medium lowered the inhibitory activity of this glycopeptide against some organisms by as much as eightfold.     

输尿管镜下输尿管会师术治疗医源性输尿管损伤的临床效果分析

目的探讨经皮输尿管镜技术在医源性输尿管损伤中的应用价值。方法 2009年2月至2012年12月吉林大学中日联谊医院泌尿外科收治因腹腔镜手术导致输尿管部分或完全断裂患者12例,平均年龄41(23⁵2)岁,男性1例,女性11例;右侧9例,左侧3例;12例合并输尿管瘘,其中输尿管部分断裂8例,完全断裂4例。腹腔镜术后发现输尿管损伤中位之间6(252)岁,男性1例,女性11例;右侧9例,左侧3例;12例合并输尿管瘘,其中输尿管部分断裂8例,完全断裂4例。腹腔镜术后发现输尿管损伤中位之间6(2¹8)d。4例尿瘘患者引流液或阴道溢出液测得肌酐平均值1567(42518)d。4例尿瘘患者引流液或阴道溢出液测得肌酐平均值1567(425²856)μmol/L。12例行经皮穿刺于近端输尿管内置入导丝,后行经尿道输尿管镜输尿管梗阻段内切开术,找到导丝并钳入远端输尿管,将输尿管断端拉近、会师,留置输尿管内支架管。术后复查超声、肾盂分泌造影并定期复查。结果12例手术均成功置入输尿管支架管。术中腹平片证实输尿管支架管位置良好,肾盂分泌造影显示积水减轻或消失,支架管保留8.2(62856)μmol/L。12例行经皮穿刺于近端输尿管内置入导丝,后行经尿道输尿管镜输尿管梗阻段内切开术,找到导丝并钳入远端输尿管,将输尿管断端拉近、会师,留置输尿管内支架管。术后复查超声、肾盂分泌造影并定期复查。结果12例手术均成功置入输尿管支架管。术中腹平片证实输尿管支架管位置良好,肾盂分泌造影显示积水减轻或消失,支架管保留8.2(6³6)周。平均随访时间352(4236)周。平均随访时间352(42⁹12)d。结论熟练掌握经皮肾穿刺和输尿管镜技术的医师可以完成输尿管镜下输尿管会师术,对于医源性输尿管损伤的病例,这种治疗方式微创、有效,可以避免二次开放手术。     

左支气管内径值对双腔支气管导管型号选择的指导作用

目的探讨左支气管内径值在双腔支气管导管（DLT）型号选择中的指导作用。方法将300例使用左DLT进行单肺通气的择期胸外科手术患者,随机数字表法分为两组,即：A组（传统方法组：根据患者身高、体质量选择左支气管导管型号）、B组（左支气管内径值组：根据螺旋CT测量患者的左支气管内径值选择合适导管）,每组150例。记录每位患者的年龄、性别、身高、体质量、疾病种类、使用的左DLT型号、导管合适度评价指标、肺萎陷质量、术后24h并发症的发生情况,对记录指标进行统计学分析。结果两组年龄、性别、身高、体质量及病种构成差异均无统计学意义（均P〉0．05）;与A组比较,B组使用的左DLT的型号大（0=8．650,P〈0．05）,导管的适合度高（P〈0．01）,肺萎陷质量高（X^2=6．549,P〈0．05）,并且术后24h并发症的发生率低（X^2=3．991,P〈0．05）。结论根据螺旋cT测量左支气管内径值能较准确选择合适的导管型号,在DLT使用中具有指导作用。     

胃复春片联合化疗治疗晚期非小细胞肺癌的临床观察

目的观察胃复春片联合化疗治疗晚期非小细胞肺癌（NSCLC）的临床疗效及毒副反应。方法68例晚期NSCLC患者随机数字表法分为两组,每组各34例,对照组采用单纯化疗（吉西他滨＋顺铂）,观察组采用胃复春片（1．436g／次,2次／d）联合化疗,完成2个周期治疗后进行疗效及毒副反应评价。结果对照组有效率为41．18％（14／34）,观察组有效率为52．94％（18／34）,两组差异无统计学意义（χ2=0．94,P〉0．05）。但观察组改善生活质量效果明显优于对照组（χ2=4．12,P〈0．05）,并且发生血小板、白细胞、血红蛋白减少及恶心呕吐等毒副反应明显低于对照组（χ2=4．66、5．96、4．12、5．90,均P〈0．05）。结论胃复春片联合化疗治疗晚期NSCLC有较好疗效,能有效减轻化疗毒副反应,提高了患者生活质量,值得临床推广。     

冠心病与雄性激素的相关性

目的 探讨老年男性冠心病与内生性血浆睾酮及其它相关因素的关系.方法 选择ACS男性患者28例、稳定型心绞痛（SAP）男性患者28例、男性健康体检者28例为对照组.分别对三组人员进行颈动脉多普勒检查,并检查外周血睾酮（T）浓度及血脂（TC、LDL-C）、血糖（Glu）、CRP等相关指标,计算BMI.结果 ACS组、SAP组外周血T、TC、LDL-C、Glu等均显著高于对照组（P＜0.05）,冠心病患者（包括ACS、SAP）较对照组颈动脉中内膜厚度（IMT）、斑块个数等差异有统计学意义（P＜0.05）.ACS组与SAP组比较：外周血T、Tc、LDL-C、CRP的浓度及BMI、IMT、不稳定斑块差异均有统计学意义（P＜0.05）.ACS组与SAP组比较外周血Glu及硬斑例数差异无统计学意义（P＞0.05）.结论 老年男性冠心病患者T浓度与动脉粥样硬化、不稳定斑块、Tc、LDL-C、BMI呈负相关.     

布洛芬缓释胶囊单剂量与多剂量给药的人体药动学及生物等效性研究

目的：建立高效液相色谱法测定人血浆中布洛芬浓度,并应用于两种布洛芬缓释制剂的人体生物等效性研究。方法：采用双周期自身随机交叉试验设计,24名男性健康志愿者分别单剂量、多剂量口服布洛芬缓释胶囊受试制剂和参比制剂300mg,采用高效液相色谱法测定人血浆中布洛芬浓度,利用DAS 2.0程序计算主要药动学参数,并对两种制剂进行生物等效性评价。结果：单剂量口服受试制剂和参比制剂后血浆中布洛芬的Cmax分别为（12.7±5.4）和（13.5±5.9）μg/mL,tmax分别为（5.5±1.4）和（5.1±1.0）h,AUC0→24分别为（96.8±50.2）和（95.7±45.4）μg·h·mL^-1。多剂量口服受试制剂和参比制剂后血浆中布洛芬的Cmax分别为（14.1±5.3）和（14.9±6.4）μg/mL,tmax分别为（4.8±1.0）和（4.6±0.9）h,Cav分别为（8.3±3.4）和（8.6±4.3）μg/mL,DF值分别为（117.2±35.3）%和（131.7±35.1）%。经统计学检验,两种制剂主要药动学参数间无统计学差异（P〉0.05）。结论：所建立的高效液相色谱法适合用于人体血浆中布洛芬测定。布洛芬受试制剂和参比制剂具有生物等效性。     

淮海经济区城市居民生命质量与健康影响因素的研究

目的了解淮海经济区城市居民生命质量状况受到哪些因素的影响,以期提高该地区城市居民健康水平。方法采用世界卫生组织编写的生存质量测定简表（即WHOQOL-BREF）为主要内容的调查问卷对淮海经济区经济水平较好的2个城市（徐州和淮安）和经济水平较差的3个城市（连云港、宿迁和枣庄）1 000名居民（每城市随机调查200名居民）进行调查。结果不同经济水平城市的居民生命质量得分比较,差异均无统计学意义（P〉0.05）;对居民生命质量产生影响的因素主要为学历、婚姻、有无慢性病、吸烟、饮酒和体育运动。在生理、心理、社会关系、环境领域中生理领域受到最广泛的因素影响。结论体育运动是最重要的促进健康的手段,学历和婚姻是健康的重要保护因素,吸烟、饮酒等行为仅影响生理健康。     

益生菌肠内营养治疗重症急性胰腺炎临床效果分析

目的探讨添加益生菌肠内营养治疗重症急性胰腺炎的临床效果。方法将2012年5月至2013年7月新疆维吾尔自治区人民医院收治的104例重症急性胰腺炎患者分为益生菌肠内营养组（观察组）和常规肠内营养组（对照组）,每组52例。比较两组患者住院时间、腹痛消失时间、感染率以及肠内菌群变化情况。结果治疗后观察组与对照组比较,患者腹痛消失时间、平均住院时间均缩短,且感染发生率降低,差异有统计学意义（P〈0．05）。观察组患者肠道双歧杆菌、乳杆菌的总数较治疗前显著提高,差异有统计学意义（P〈0．05）。结论添加益生菌的肠内营养治疗可有效调节肠道菌群微生态平衡,降低重症急性胰腺炎肠黏膜损伤,保护肠屏障功能。     

Synthesis and antitumor properties of novel alizarin analogs

Series of novel hybrids of alizarin and diamide scaffold (3a–3h, 7a–7h) were designed and synthesized. In vitro antitumor activities of all compounds against HepG-2, CNE, Spca-2, Hct-116, and MGC-803 cell lines were evaluated, and employing standard MTT assay compared with commercial anticancer drug 5-fluorouracil (5-FU). Compounds 7b, 7c, 7d, and 7e showed relatively high cytotoxicity. Especially, compound 7c exhibited the best cytotoxicity against CNE cells with IC₅₀ 9.08 µM, which was even stronger than that of 5-FU. All the synthesized compounds exhibited low cytotoxicity against HUVEC cells. The action mechanism of representative compound 7c was preliminarily investigated by flow cytometry, which indicated that the compound can induce cell apoptosis in CNE cells. Cell cycle analysis showed that compound 7c mainly arrested CNE cells in G1 stage. In addition, the binding properties of a model analog 7c to DNA were investigated by different methods (fluorescence, CD spectroscopy), and the results indicated that 7c showed a moderate preference for binding ct-DNA.     

Synthesis and structure–activity relationship of nuciferine derivatives as potential acetylcholinesterase inhibitors

Acetylcholinesterase inhibitors (AChEIs) are currently the best available pharmacotherapy for Alzheimer patients, but because of bioavailability issues, there is still great interest in discovering better AChEIs. The aporphine alkaloid is an important class of natural products, which shows diverse biological activity, such as acetylcholinesterase inhibitory activity. To find new lead AChEIs compounds, eight aporphine alkaloids were synthesized by O-dealkylation, N-dealkylation, and ring aromatization reactions using nuciferine as raw material. The anti-acetylcholinesterase activity of synthesized compounds was measured using modified Ellman’s method. The results showed that some synthesized compounds exhibited higher affinity to AChE than the parent compound nuciferine. Among these compounds, 1,2-dihydroxyaporphine (2) and dehydronuciferine (5) were the most active compounds (IC₅₀ = 28 and 25 μg/mL, respectively). Preliminary analysis of structure–activity relationships suggested that aromatization of the C ring, the presence of the alkoxyl group at C1 and the hydroxy group at C2 position as well as the alkyl substituent at the N atom were favorable to the acetylcholinesterase inhibition. Molecular docking was also applied to predict the binding modes of compounds 1, 2, and 9 into the huperzine A binding site of AChE.