培丙酯治疗缺血性心肌病疗效观察

目的 研究培丙酯对缺血性心肌病的治疗作用.方法 选择缺血性心肌病患者80例,随机分为培丙酯治疗组及5-单硝酸异山梨酯对照组.治疗2周,分别比较心功能、血液流变学、炎症指标变化情况.结果 2周后,2组患者病情均有改善,治疗组疗效更佳.结论 培丙酯治疗缺血性心肌病可以明显改善心肌缺血及心功能不全表现,疗效显著,是治疗缺血性心肌病的有效方法之一.     

没食子酸丙酯对脑缺血大鼠神经元SAPK/JNK及p38MAPK激活的抑制作用

目的探讨没食子酸丙酯对大鼠脑缺血再灌注模型缺血区周边组织神经元损伤的保护作用及其可能机制。方法通过Nissl和TUNEL染色法检测阳性神经元数量，蛋白免疫印迹、免疫组化法观察活化型Caspase-3，SAPK/JNK，p38MAPK及其磷酸化组分的表达。结果没食子酸丙酯干预后，SAPK/JNK，p-SAPK/JNK(1 h)，p38MAPK，p-p38MAPK(6 h)及活化型Caspase-3(12 h)表达均减弱，TUNEL阳性神经元减少(24 h)，Nissl阳性神经元增多(24 h)，神经元凋亡率明显降低。结论没食子酸丙酯保护缺血再灌注后神经元损伤的机制可能与抑制SAPK/JNK及p38MAPK的激活有关。     

Monoliths with chiral surface functionalization for enantioselective capillary electrochromatography

The state-of-the-art in CEC enantiomer separations with monolithic capillary columns is comprehensively reviewed. The various types of monolithic columns comprising in situ organic polymer monoliths, molecularly imprinted polymer (MIP) monoliths, silica monoliths and monoliths made from particles are discussed with a focus on materials’ synthesis, chemistry and properties as well as column aspects. Monolithic MIP-type porous layer open-tubular (PLOT) columns are treated herein as well. From this survey of the literature, the authors come to the conclusion that monolithic silica capillaries appear to become the preferred column type for CEC enantiomer separations of low-molecular drugs and other chiral pharmaceuticals or chemicals.     

Effect of the herbicide pendimethalin on rat uterine weight and gene expression and in silico receptor binding analysis

The endocrine disrupting potential of the herbicide pendimethalin was investigated in vivo on the uterotrophic response and on the expression of estrogen-regulated genes examined by quantitative real-time RT PCR. Receptor binding characteristics of pendimethalin were analyzed by an in silico method. Pendimethalin (150, 225, 300 and 600 mg/kg/day) was administered by oral gavage to immature female rats for 3 days, with ethinylestradiol (0.001 mg/kg/day) as positive control. Pendimethalin caused a small but significant increase in absolute uterine weight at and above 300 mg/kg/day and in relative uterine weight at 600 mg/kg/day. Estrogen receptor (ER)-alpha mRNA levels were not affected, whereas ER-beta mRNA was up-regulated at the highest dose. Progesterone receptor mRNA level was not significantly changed, while insulin-like growth factor-I mRNA was reduced, significantly at 225 mg/kg/day to 65% of control. Androgen receptor (AR) mRNA showed a marked down-regulation at doses of 225 mg/kg/day and above. The expression pattern differed from that of ethinylestradiol. In silico analysis revealed potential binding of pendimethalin to ER-beta and AR, but virtually no binding to ER-alpha. These data demonstrate that pendimethalin exhibits estrogenic activity also in vivo. However, its uterotrophic effect, which is an ER-alpha-mediated response, is very small, and it appears that in vivo actions should rather be sought in ER-beta-regulated functions.     

C-PG血小板聚集试验在单采血小板捐献者筛查中的应用

本研究探讨以阳离子没食子酸丙酯（C-PG）为激活剂的血小板聚集试验用于单采血小板捐献者筛查的可行性,并调查血小板献血者血小板功能缺陷的发生率.测定不同浓度C-PG诱导的健康献血者的血小板聚集率,以确定C-PG的最适应用浓度;检测30名志愿者服用阿司匹林前和服药24小时后的血小板聚集率,以确定血小板功能不良的筛查界点值;检测483例血小板捐献者的C-PG诱导的血小板聚集率,并对聚集功能不良者进行活化血浆凝固时间（APCT）测定.结果表明：血小板聚集率随C-PG浓度的增加而升高,当C-PG浓度达200μmol/L时,血小板聚集率达最高;服用阿司匹林24小时后的血小板聚集率与服药前相比,均表现明显减低（P＜0.001）,但以C-PG诱导180秒时的血小板聚集率减低最显著.血小板功能不良的筛查界点值确定为C-PG诱导180秒时的血小板聚集率小于20%;在483例血小板捐献者中,检出25例有血小板聚集功能不良,其中有11例表现为血小板促凝血活性减低.结论：C-PG诱导的血小板聚集试验能有效的检出血小板功能不良者,适用于血小板捐献者血小板功能的筛选;在血小板献血者中,血小板功能缺陷者的检出率大约为5%.     

Allergic contact dermatitis from propyl gallate: dose response comparison using various application methods

The antioxidant propyl gallate, in a deodorant product, caused an allergic contact dermatitis in 1 subject during developmental controlled use testing. Subsequent dose response elicitation studies with this subject revealed a differing threshold of sensitivity to propyl gallate dependent upon application method. Increasing the level of occlusion increased the elicitation response. Responsiveness from greatest to least was: occluded patch on the upper arm greater than semi-occluded axilla greater than open application on the antecubital fossa. The thresholds determined for propyl gallate (w/v in 25:75 ethanol:water) were: (a) 0.0025% for the upper arm occluded patch; (b) 0.0035% for the underarm without shaving; (c) 0.005% for the underarm with shaving; (d) 0.015% for the antecubital fossa. Occluded patch responsiveness to propyl gallate was monitored and remained unchanged throughout a 2-year period. These data are useful in understanding the relationship between occlusive allergic contact dermatitis patch testing and clinical contact dermatitis.     

The sensitizing capacity of the antioxidants propyl, octyl, and dodecyl gallate and some related gallic acid esters

8 alkyl gallates, including the widely used antioxidants propyl, octyl, and dodecyl (= lauryl) gallate, have been subjected to experimental sensitization in guinea pigs. Using a modern sensitization procedure, the results showed that all gallates are moderate to strong contact sensitizers: dodecyl (= lauryl) gallate was found to be the strongest. A characteristic correlation between side chain length and mean response was observed, giving a maximum of sensitization at a length of 12 carbon atoms (dodecyl gallate). A literature review revealed that the frequency of reports of allergic contact dermatitis from antioxidants of the gallate type has increased in the last 4 years. In most cases, the moderate sensitizer propyl gallate was the source of sensitization.     

A totally synthetic lipopeptide-based self-adjuvanting vaccine induces neutralizing antibodies against heat-stable enterotoxin from enterotoxigenic Escherichia coli

ST-based lipopeptide vaccine candidates were constructed in which ST was chemically synthesized and folded into the correct conformation prior to ligation to a module containing a T-helper cell epitope (T(H)) and the Toll-like receptor 2 (TLR2) agonist, S-[2,3-bis(palmitoyloxy)propyl]cysteine (P2C). Two different chemistries, thioether-based and oxime-based, were then used to ligate ST to the lipidated T(H) epitope. The enterotoxic activity of synthetic ST and the ST-based lipopeptide vaccines was determined in mice followed by an evaluation of immunological efficacy. The importance of the fine detail in chemical composition used in vaccine design was demonstrated by the findings that (i) the oxime-based vaccine exhibited little or no toxicity but the thioether-based vaccine, exhibited residual toxicity in suckling mice, (ii) although each of the synthetic vaccines generated specific anti-ST antibodies, it was the low titer antibodies induced by the oxime-based vaccine that demonstrated better neutralizing activity suggesting that the chemical linkage also affects the specificity of antibodies, (iii) the geometric arrangement of ST within a vaccine can profoundly affect the specificity and biological function of the antibodies that are elicited, and (iv) the lipopeptide-based ST vaccine candidate assembled using oxime chemistry induced a better neutralizing antibody response to ST when administered by the mucosal (intranasal) route.