Anisomycin induces glioma cell death via down-regulation of PP2A catalytic subunit in vitro

Aim:

To examine the effects of anisomycin on glioma cells and the related mechanisms in vitro.

Methods:

The U251 and U87 human glioblastoma cell lines were tested. The growth of the cells was analyzed using a CCK-8 cell viability assay. Apoptosis was detected using a flow cytometry assay. The expression of proteins and phosphorylated kinases was detected using Western blotting.

Results:

Treatment of U251 and U87 cells with anisomycin (0.01–8 μmol/L) inhibited the cell growth in time- and concentration-dependent manners (the IC₅₀ values at 48 h were 0.233±0.021 and 0.192±0.018 μmol/L, respectively). Anisomycin (4 μmol/L) caused 21.5%±2.2% and 25.3%±3.1% of apoptosis proportion, respectively, in U251 and U87 cells. In the two cell lines, anisomycin (4 μmol/L) activated p38 MAPK and JNK, and inactivated ERK1/2. However, neither the p38 MAPK inhibitor SB203580 (10 μmol/L) nor the JNK inhibitor SP600125 (10 μmol/L) prevented anisomycin-induced cell death. On the other hand, anisomycin (4 μmol/L) reduced the level of PP2A/C subunit (catalytic subunit) in a time-dependent manner in the two cell lines. Treatment of the two cell lines with the PP2A inhibitor okadaic acid (100 nmol/L) caused marked cell death.

Conclusion:

Anisomycin induces glioma cell death via down-regulation of PP2A catalytic subunit. The regulation of PP2A/C exression by anisomycin provides a clue to further study on its role in glioma therapy.     

羟丙基-β-环糊精用于静脉给药的研究概况

羟丙基-β-环糊精是β-环糊精的一种化学修饰性衍生物，对于水难溶性药物具有良好的包合增溶效果。现对其理化性质、静脉给药后的毒性、药动学和组织分布的研究概况进行综述，并简要介绍其在国内外制剂中的使用情况，同时围绕静脉给药，对实际应用泾丙基-β-环糊精时需考虑的一些问题进行较详细的概述。     

麦冬消渴胶囊和糖淤消胶囊微生物限度检查方法研究

目的：建立中成药麦冬消渴胶囊和糖淤消胶囊的微生物限度检查方法。方法：对5种阳性对照菌进行回收率试验以确定其检验方法。结果：回收率试验表明,麦冬消渴胶囊5种试验茵的回收率均高于70％,证明无抑菌现象;糖淤消胶囊对枯草芽孢杆菌有一定的抑菌作用,可用培养基稀释法消除其抑菌作用。结论：麦冬消渴胶囊可按常规方法进行微生物限度检查;糖淤消胶囊可按培养基稀释法进行微生物限度检查。     

4-(4-甲氧基苄基氧基)苯丙二酸-4-甲氧基苄基单酯的工艺改进

目的 4-(4-甲氧基苄基氧基)苯丙二酸-4-甲氧基苄基单酯的合成工艺改进。方法 以对甲氧基苄醇与盐酸反应后生成的对甲氧基苄氯和对羟基苯乙酸为原料,经过酯化和醚化反应及羧基的α位发生羧基化反应得到4-(4-甲氧基苄基氧基)苯丙二酸-4-甲氧基苄基单酯。结果 目标产物的结构经过熔点,1H-NMR确认。结论 与原工艺相比,改进后的工艺减少了碘化钠的用量,提高了溶剂利用率,收率高,成本低,操作简单。     

RP-HPLC-DAD法同时测定吴茱萸汤中7个生物碱和2个黄酮苷含量(英文)

建立反相高效液相色谱-二极管阵列检测 (RP-HPLC-DAD) 法同时测定经典名方吴茱萸汤中7个生物碱 (去氢吴茱萸碱、10-羟基吴茱萸次碱、吴茱萸碱、吴茱萸次碱、1-甲基-2-正壬基-4(1H)喹诺酮、吴茱萸卡品碱和二氢吴茱萸卡品碱) 和2个黄酮苷 (异鼠李素-7-O-芸香糖苷和香叶木素-7-O-β-D-吡喃葡萄糖苷)的含量。RP-HPLC分离应用反相C18 色谱柱, 甲醇-1%醋酸水溶液梯度洗脱, 流速为1.0 mL/min, 检测波长为300 nm。上述9个分析物达到基线分离, 标准曲线线性关系良好(r2>0.9941), 日内和日间精密度和准确度符合分析方法学要求, 加样回收率为90.13%-102.48% (RSDs<3.6%)。经方法学验证, 所建立的方法适用于吴茱萸汤物质基础的质量控制。     

我院2004-2007年心血管中成药应用分析

目的评价医院心血管中成药的应用情况。方法对2004-2007年心血管中成药的种类、销售金额、用药频度等进行统计、分析。结果心血管中成药销售金额逐年上升,银杏、复方丹参制剂的用药金额和用药频度均排前列。结论心血管中成药应用基本合理,中药制剂应用前景广阔。     

血清高迁移率族蛋白 B1和糖类抗原72-4在早期胃癌患者检测中的价值

目的：探讨血清高迁移率族蛋白B1（HMGB1）和糖类抗原72-4（CA72-4）在早期胃癌患者检测中的价值。方法50例早期胃癌患者作为胃癌组,45例胃部良性病变患者作为胃部良性病变组,100例健康查体者作为健康组,测定并比较入选人群血清HMGB1和CA72-4。结果早期胃癌组血清HMGB1和CA72-4阳性率高于胃部良性病变组和健康体检组（χ^2＝33．69、82．95、51．41、104．74,均P＜0．01）,而胃部良性病变组的阳性率与健康体检组的差异无统计学意义（χ^2＝3．80、1．90,均P＞0．05）。 HMGB1诊断早期胃癌敏感度为70．0％,特异度为95．2％,准确度为88．7％;CA72-4诊断早期胃癌的敏感度为80．0％（40／50）,特异度为97．2％（141／145）,准确度为92．8％（181／195）。联合检测时,诊断早期胃癌的敏感度为94．0％（47／50）,而特异度为93．1％（135／145）,准确度为93．3％（182／195）,高于单项检测的敏感度与准确度。有淋巴结转移的早期胃癌患者血清HMGB1和CA72-4均明显高于无淋巴结转移的患者（ t＝2．927、4．096,均P ＜0．05）。结论联合检测血清HMGB1和CA72-4可以早期诊断胃癌,并对患者预后进行判断。     

气相色谱-质谱法分析矮地茶挥发油的化学成分

目的 分析矮地茶挥发油的化学成分.方法 采用水蒸气蒸馏法提取挥发油,用气相色谱-质谱法对其进行定性和定量分析.结果 共分离出62个峰,确认其中44个化合物,含量较多的有石竹烯(34.99%)、棕榈酸(20.44%)、α-芹子烯(6.69%).结论 首次分析了恩施地区矮地茶挥发油的化学成分组成,为其进一步开发利用提供了一定依据.     

An automated process for building reliable and optimal in vitro/in vivo correlation models based on Monte Carlo simulations

Many mathematical models have been proposed for establishing an in vitro/in vivo correlation (IVIVC). The traditional IVIVC model building process consists of 5 steps: deconvolution, model fitting, convolution, prediction error evaluation, and cross-validation. This is a time-consuming process and typically a few models at most are tested for any given data set. The objectives of this work were to (1) propose a statistical tool to screen models for further development of an IVIVC, (2) evaluate the performance of each model under different circumstances, and (3) investigate the effectiveness of common statistical model selection criteria for choosing IVIVC models. A computer program was developed to explore which model(s) would be most likely to work well with a random variation from the original formulation. The process used Monte Carlo simulation techniques to build IVIVC models. Data-based model selection criteria (Akaike Information Criteria [AIC], R2) and the probability of passing the Food and Drug Administration "prediction error" requirement was calculated. To illustrate this approach, several real data sets representing a broad range of release profiles are used to illustrate the process and to demonstrate the advantages of this automated process over the traditional approach. The Hixson-Crowell and Weibull models were often preferred over the linear. When evaluating whether a Level A IVIVC model was possible, the model selection criteria AIC generally selected the best model. We believe that the approach we proposed may be a rapid tool to determine which IVIVC model (if any) is the most applicable.     

稳心颗粒联合心理干预对心脏介入患者心理应激的影响

目的 探讨稳心颗粒联合心理干预对心脏介入患者心理应激的干预效果。方法 将186例拟行心脏介入手术的患者随机分为3组,各62例。对照组予单纯心理干预治疗,观察A组予心理干预联合坦度螺酮治疗,观察B组予心理干预联合稳心颗粒治疗。所有患者分别于术前及术后1周采用焦虑量表（SAS）进行评分,同时比较组间SAS评分、血压、心率、血糖及血皮质醇水平的变化,观察不良反应的发生情况。结果 各组患者术后SAS评分均较术前降低,观察B组下降程度最大（P〈0.05）;各组患者术后血压较术前均有升高,其中观察B组上升程度最小（P〈0.05）;各组患者手术前后心率变化无明显差异;各组患者术后血皮质醇水平均有上升,其中观察B组患者上升程度最小（P〈0.05）。各组患者干预后不良反应发生率无明显差异。结论 稳心颗粒联合心理干预能有效降低心脏介入患者的心理应激效应,作用明显,安全性好,值得临床推广。