Influence of oil droplet surface charge on the performance of antibody--emulsion conjugates.

Targeted drug delivery requires binding of (and subsequent uptake by) the carrier to target cells. The purpose of our present study is to compare the binding and uptake of emulsions with different electric surface properties to SK-BR3 cell line, which over-expresses the HER2 receptor. Cationic emulsion was prepared by incorporating 0.25% w/w of the cationic lipid, stearylamine in the formulation while the anionic emulsion formulation was identical but lacking stearylamine. Immunoemulsions were prepared by conjugating the 2-iminothiolane derivative of the monoclonal antibody trastuzumab (Herceptin) through the reactive maleimide group of the octadecyl-4-(maleimidomethyl)cyclohexane-carboxylic amide linker which was incorporated in the oil phase of the anionic and cationic emulsions. Cationic emulsion exhibited a droplet size of approximately 130 nm and a zeta potential of +50 mV compared to anionic emulsion with a droplet size of approximately 140 nm and a zeta potential of -30 mV which decreased to -5 mV following antibody coupling. There was no significant difference in the coupling efficiency of trastuzumab to anionic and cationic emulsions which was in the range of 60-70%. The cationic emulsion and immunoemulsion appeared to be physically stable over a long period of time, as indicated by particle-size measurements while the droplets of the anionic immunoemulsion coalesced with time resulting in phase separation within 20 days storage at 4 degrees C. The results of binding and uptake to cells showed that both cationic and anionic immunoemulsions bind and internalized to cells much more than the respective blank emulsions. The enhanced penetration of the probe coumarin-6 with both immunoemulsions clearly indicated that the internalization process was mainly controlled by a cell-receptor endocytosis mechanism mediated by the binding affinity of trastuzumab to the cell surface receptor since the uptake of the cationic immunoemulsion was not significantly different from the uptake of the anionic immunoemulsion. However, only the cationic immunoemulsion might be considered for further investigation in view of its long standing physical stability.     

“活血降脂胶囊”治疗高脂血症疗效观察

目的：探讨“活血降脂胶囊”治疗高脂血症的疗效。方法：将２２０例高脂血症患者随机分为治疗组１４０例和对照组８０例；用酶法测定甘油三酯（ＴＧ）和胆固醇（ＴＣ），用沉淀法测定高密度脂蛋白胆固醇；治疗方法：治疗组口服自制“活血降脂胶囊”，每次５粒（含生药０．３ｇ），每日３次；对照组口服月见草油，每次５粒，每日３次。疗程为２个月，治疗期间患者均用低脂饮食。结果：治疗组显效率与总有效率均优于对照组，Ｐ值分别为＜０．０５和Ｐ＜０．０１；治疗后２组ＴＣ、ＴＧ和ＨＤＬＣｈ改善亦均有显著性差异（Ｐ值分别＜０．０１和＜０．００１）。结论：“活血降脂胶囊”治疗高脂血症疗效较好，对防治心脑血管疾病具有一定意义     

莪术油对HSC-T6细胞基因表达的影响

目的:研究莪术油对HSC-T6细胞基因表达的影响.方法:从基因库中查询50种肝纤维化相关基因的mRNA序列,用寡核苷酸探针设计软件设计探针,在PE8909DNA合成仪上合成寡核苷酸,用OGR-04点样仪及醛基化玻片制备成基因芯片.以莪术油不同浓度含药培养液培养HSC-T6细胞.根据细胞毒性实验,确定细胞存活率在50%以上的药物浓度作为实验所用浓度,每组设空白对照,分别按1小时、6小时、12小时、24小时4个时间段收集细胞,按操作步骤提取细胞总RNA,经反转录荧光标记,杂交和洗涤,用Genepix 4000B扫描仪扫描芯片,ImaGene 4.2软件进行数据分析和归一化处理,使用看家基因和阳性对照对Cy3和Cy5扫描结果进行校正.结果:莪术油78.125μg/ml作用HSC-T6细胞24小时,可使基因TIMP-2、IL-6表达分别下调2.3、2.2倍.结论:从分子水平揭示了莪术有效成分莪术油的抗肝纤维化机制.     

Nutritional impact on the plasma metabolome of rats

Metabolite profiling (metabolomics) elucidates changes in biochemical pathways under various conditions, e.g., different nutrition scenarios or compound administration. BASF and metanomics have obtained plasma metabolic profiles of approximately 500 compounds (agrochemicals, chemicals and pharmaceuticals) from 28-day rat studies. With these profiles the establishment of a database (MetaMap^®Tox) containing specific metabolic patterns associated with many toxicological modes of action was achieved. To evaluate confounding factors influencing metabolome patterns, the effect of fasting vs. non-fasting prior to blood sampling, the influence of high caloric diet and caloric restriction as well as the administration of corn oil and olive oil was studied for its influence on the metabolome. All mentioned treatments had distinct effects: triacylglycerol, phospholipids and their degradation product levels (fatty acids, glycerol, lysophosphatidylcholine) were often altered depending on the nutritional status. Also some amino acid and related compounds were changed. Some metabolites derived from food (e.g. alpha-tocopherol, ascorbic acid, beta-sitosterol, campesterol) were biomarkers related to food consumption, whereas others indicated a changed energy metabolism (e.g. hydroxybutyrate, pyruvate). Strikingly, there was a profound difference in the metabolite responses to diet restriction in male and female rats. Consequently, when evaluating the metabolic profile of a compound, the effect of nutritional status should be taken into account.     

四氧化三铁微粒与碘化油混悬液栓塞肝癌血管的疗效

目的:研究四氧化三铁微粒与碘化油混悬液对原发性肝癌供瘤血管的影响。方法:对98例经导管肝动脉化疗栓塞术(TACE)治疗的原发性肝癌患者进行回顾性的研究。栓塞方法分为3组:A组(碘化油+化疗药物的混悬液),B组(碘化油+化疗药物的混悬液+明胶海绵)和C组(碘化油+化疗药物+四氧化三铁微粒的混悬液)。比较栓塞后供瘤血管再通情况。结果:B组与C组的血管未再通率明显高于A组(P<0.01),而部分再通率及完全再通率明显低于A组(P<0.01);B组与C组的血管再通率比较差异无统计学意义(P>0.05)。结论:栓塞后肿瘤供瘤血管再通与所用栓塞方法有关,四氧化三铁微粒与碘化油混悬液对肝癌患者进行栓塞治疗是一种更有效的方法。     

Analysis and stability of the constituents of Curcuma longa and Harpagophytum procumbens tinctures by HPLC-DAD and HPLC-ESI-MS

In the present study two methods based on liquid chromatography with diode array detection (HPLC-DAD) coupled to an electrospray ionisation (ESI-MS) interface were developed for the determination of constituents in the tinctures (60%, v/v, DER 1:5) of turmeric (Curcuma longa L.) and Devil's claw (Harpagophytum procumbens L.). The developed simple and effective assays permitted the quality control of both tinctures. The aim of this work was to assess the qualitative and quantitative profile of the constituents of two widely marketed commercial preparations and to evaluate chemical stability of their marker constituents during accelerated thermal stability test by HPLC analysis. Characteristic constituents of C. longa rhizomes are the curcuminoids, whereas characteristic constituents of H. procumbens are acylated iridoid glycosides and phenylethylalcohols. Constituents of Devil's claw tincture (mainly iridoids) were more stable than curcuminoids of turmeric.     

薏苡仁油抗消化系肿瘤的基础和临床研究

体内外动物实验发现薏苡仁油诱导消化系肿瘤细胞凋亡,抑制肿瘤细胞增殖,抑制肿瘤组织内血管形成,减少营养物质供应从而抑制肿瘤生长.与化疗药相反,薏苡仁油提高荷瘤动物的免疫功能.在临床上,薏苡仁油与化疗药联合应用治疗食管癌、胃癌、结直肠癌、胰腺癌和肝癌,均可提高疗效、病人卡氏生命质量评分和疼痛缓解率,提高病人低下的免疫功能,使外周血T淋巴细胞亚群CD3、CD4、CD4 / CD8水平及自然杀伤细胞(NK细胞)活性显著提高,具有良好的开发前景.     

复方莪术油栓联合奥硝唑治疗滴虫性阴道炎84例

目的观察奥硝唑联合复方莪术油栓治疗滴虫性阴道炎的临床疗效。方法将168例滴虫性阴道炎患者随机分为两组,各84例,治疗组给予奥硝唑片口服,并局部给予复方莪术油栓治疗,对照组仅局部给予复方莪术油栓治疗,7 d为1个疗程。停药1周后,随诊观察疗效。结果治疗组总有效率为97.61%显著优于对照组的89.29%(P<0.05)。结论奥硝唑联合复方莪术油栓治疗滴虫性阴道炎疗效满意,不良反应少,值得临床推广。     

千针万线草挥发油化学成分的研究

目的：研究千针万线草挥发油化学成分。方法：采用气相色谱及气相色谱一质谱法对千针万线草挥发油化学成分进行分析。结果：从千针万线草挥发油中鉴定出75个组分,占挥发油总量的99．03％．