非离子表面活性剂逆转肿瘤细胞多药耐药性的机制

目的探讨非离子表面活性剂聚氧乙烯醚﹑聚乙二醇300﹑曲拉通X100对肺癌耐药细胞A549/DDP(耐顺铂)多药耐药性的逆转及其机制。方法用四氮唑盐(MTT)法进行体外耐药逆转实验,Westernblot检测P-gp(P-糖蛋白)蛋白的表达。结果①合用非离子型表活剂前后,A549/DDP对化疗药物阿霉素、顺铂、丝裂霉素、5-氟尿嘧啶、依托泊甙和长春新碱的敏感性显著增加(各组都为P<0.01);②三种非离子型表面活性剂能抑制P-gp蛋白的表达。结论三种非离子表面活性剂具有逆转A549/DDP耐药性的作用,逆转机制与其抑制P-gp蛋白的表达有关。     

毒蕈胆碱M_1受体激动剂的高通量筛选模型

目的　建立毒蕈碱样胆碱M1 受体激动剂的高通量筛选模型 ,以此模型进行M1 受体激动剂筛选。方法　将M1 受体基因质粒 (M1 /pCDNA3 1 )与报告基因质粒 (3×CRE/ 3×MRE/SRE LUC)按 1∶5的比例共转染HEK2 93 ,建立了一个稳定的M1 受体激动剂报告基因筛选细胞株。配体与细胞表面M1 受体结合后 ,激活相应的信号通路 ,调节报告基因的表达 ,通过测定荧光酶素报告基因表达水平的变化 ,评估配体激活M1 受体的生物活性。结果　通过对筛选条件 ,如细胞数目、荧光素酶表达时间、底物浓度的优化 ,建立了可靠的筛选方法 ,并对多种抗衰老中药水提物进行了筛选 ,找到 3种对M1 受体有活性的中药。结论　该系统能准确、稳定、有效地应用于M1 受体激动剂的高通量筛选     

某院儿科门诊抗菌药物使用合理性分析

目的：了解某院儿科门诊抗菌药物使用情况,为临床合理用药提供参考。方法：对某院儿科门诊某月某一工作周5个工作日的处方进行统计,选择使用抗菌药物的处方进行分析。结果：共抽查处方2 336张,使用抗菌药物处方为1 018张,占43.58%,使用注射用抗菌药物处方数占总处方数的26.54%（620/2 336）,抗菌药物联合用药处方数占总处方数的3.42%（80/2 336）。儿科抗菌药物使用基本合理,但存在给药方案不当、联合用药不合理、给药时间不合理等一些问题。结论：应加强抗菌药物合理使用的培训及管理,提高儿科抗菌药物合理应用水平。     

我院二类精神药品处方调查与分析

目的：了解我院二类精神药品的使用情况，促进合理用药。方法：采用限定日剂量（DDD）和药物利用指数（DUI）为指标对我院2005年1月～2006年12月门急诊32553张二类精神药品处方进行调查和分析。结果：8种二类精神药品中，7种药品的DUI〈1．00．1种药品的DUI〉1．00。结论：我院二类精神药品使用基本合理，但合并用药频度较高，需引起重视。     

疑难性下腔静脉滤器取出的技巧及策略

目的探讨疑难性下腔静脉滤器取出的策略及操作技巧。方法 2005年11月至2010年10月我院收治的采用常规圈套技术无法成功取出的下腔静脉滤器置入术后患者11例,采用导管辅助法、异物钳法及股静脉剖开等方法行下腔静脉滤器取出术,其中男性8例,女性3例,年龄22～71岁。术后给予抗凝、抗炎治疗3～5d。随访4～12个月复查血管超声。结果 10例患者成功回收下腔静脉滤器,成功率91%。导管辅助法取出7例;异物钳法取出2例;1例因滤器无法进入鞘中,股总静脉剖开后取出滤器。1例因滤器与血管壁粘连紧密,回拉捕捉器时,回收钩断裂,最后家属放弃,取出失败。回收过程平均透视时间57.2min(17～115min)。滤器平均体内留置时间为37.8d(0～80d)。术后5d内全部患者顺利出院。随访期间,复查血管超声未出现下肢静脉血栓形成。结论采用多种辅助性圈套技术回收疑难性下腔静脉滤器的成功率较高,可有效提高下腔静脉滤器回收率,有一定临床应用价值。     

Perspectives on developing small molecule inhibitors targeting HIV-1 integrase

HIV-1 integrase (IN) is a crucial enzyme in the life cycle of HIV-1 and also a validated target for developing anti-HIV inhibitors. Recent progress in drug design has significantly accelerated the development of anti-AIDS IN inhibitors. A large amount of novel inhibitors that interact specifically with IN were developed along with the expanding and application of methods to drug design. This article reviewed the anti-HIV IN inhibitors discovered by the rational drug design approaches in the recent 5-year.     

Binding and Anticancer Properties of Plumbagin with Human Serum Albumin

Plumbagin has received extensive attention as a promising anticancer drug. Therefore, we investigated the binding and anticancer properties of plumbagin with human serum albumin. Fluorescence results demonstrated that plumbagin interacts with human serum albumin, although its binding affinity may be affected to various extents by different compounds. The human serum albumin–plumbagin complex structure revealed that plumbagin binds to the hydrophobic cavity in the IIA subdomain of human serum albumin through hydrogen bonding and hydrophobic interactions. The plumbagin–human serum albumin complex enhances cytotoxicity by 2‐ to 3‐fold particularly in cancer cells but has no effect on normal cells in vitro. Compared with the unbound drug, the human serum albumin–plumbagin complex promotes HeLa cell apoptosis and has a stronger capacity for cell cycle arrest at the G2/M phase of HeLa cells. In conclusion, this study contributes to the rational design and development of plumbagin‐based drugs and a drug–human serum albumin delivery system.     

氯氟乙酯(21例)和地西泮(22例)治疗焦虑障碍的疗效和安全性比较

目的评价氯氟     

妊娠期高血压疾病胎盘组织中白血病抑制因子与基质金属蛋白酶-9表达水平与子痫前期病情的关系研究

目的 探讨妊娠期高血压疾病(HDCP)孕妇胎盘组织中白血病抑制因子(LIF)与基质金属蛋白酶-9(MMP-9)表达水平与子痫前期病情的关系.方法 选取2013年3月—2017年2月陕西省榆林市第二医院收治的HDCP子痫前期患者76例,按照疾病严重程度分为轻度子痫前期组与重度子痫前期组,每组38例,选取同期36例正常孕妇作为对照组,比较分析3组胎盘组织中LIF与MMP-9表达水平与子痫前期病情的关系.结果 轻度子痫前期组与重度子痫前期组LIF与MMP-9阳性表达率均低于对照组,且重度子痫前期组低于轻度子痫前期组,差异有统计学意义(P<0.05).重度子痫前期组LIF与MMP-9表达水平呈正相关(r=0.413,P=0.031).结论 正常孕妇与HDCP子痫前期患者的胎盘组织中均有LIF与MMP-9的表达,子痫前期患者LIF与MMP-9的表达水平明显下降,且与病情严重程度有关.     

Analysis of The Working Performance of Large Curvature Prestressed Concrete Box Girder Bridges

Based on numerical shape functions and the structural stressing state theory, the mechanical properties of the curved prestressed concrete box girder (CPCBG) bridge model under different loading cases are presented. First, the generalized strain energy density (GSED) obtained from the measured strain data is used to represent the stressing state pattern of the structure; then, the stressing state of the concrete section is analyzed by plotting the strain and stress fields of the bridge model. The stressing state pattern and strain fields of the CPCBG are shown to reveal its mechanical properties. In addition, the measured concrete strain data are interpolated by the non-sample point interpolation (NPI) method. The strain and stress fields of the bridge model have been plotted to analyze the stressing state of the concrete cross-section. The internal forces in the concrete sections are calculated by using interpolated strains. Finally, the torsional effects are simulated by measuring the displacements to show the torsional behavior of the cross-section. The analysis and comparison of the internal force and strain fields reveal the common and different mechanical properties of the bridge model. The results of the analysis of the curved bridge model provide a reference for the future rational design of bridge projects.