水分去除的方法及其在药物合成中的应用

化学药合成过程中水分残留不利于反应的进行,还影响药物及制剂的稳定性、理化性质、溶出及药理作用等,因此水分几乎是大多数药物合成中的必测项目,通过有效除水严格控制反应体系中水分的含量至关重要。本文综述了水分的存在形式,常见除水剂和脱水剂的种类、作用原理与除水能力,以及在药物合成的应用,为药物合成反应中水分的去除提供参考。     

NRP-1单克隆抗体对乳腺癌裸鼠移植瘤生长的影响

 目的 探讨NRP-1单克隆抗体（NRP-1 MAb）的特异性，以及不同剂量的NRP-1 MAb治疗乳腺癌裸鼠移植瘤的疗效。方法 Western blot和共聚焦免疫荧光法检测NRP-1 MAb是否识别MCF7细胞上NRP-1蛋白。将MCF7细胞接种于BALB/c裸鼠皮下建立乳腺癌细胞移植瘤模型，并进行瘤组织传代。传代的肿瘤体积生长至300~500 mm3时，随机分为对照组、NRP-1 MAb低剂量组、中剂量组和高剂量组，每组6只，给药7次。观察荷瘤裸鼠一般状况，测量瘤体大小及裸鼠体重。实验结束时剥离瘤体称重，提取组织蛋白，Western blot检测组织中VEGF蛋白和NRP-1蛋白的表达量。结果 NRP-1MAb成功识别MCF7细胞上的NRP-1蛋白；NRP-1 MAb能够有效抑制MCF7细胞裸鼠移植瘤的生长，低剂量组（1 mg/kg）抑瘤率为47.01%，中剂量组（5 mg/kg）抑瘤率为65.70%，高剂量组（10 mg/kg）抑瘤率为69.19%。。结论 NRP-1 MAb能够识别并有效结合MCF7细胞膜上的NRP-1蛋白，且可抑制MCF7细胞移植瘤的生长，NRP-1 MAb抑制移植瘤的增长可能与下调NRP-1和VEGF表达有关。     

Systematic review of acceptability,cardiovascular, neurological,bone health and HRT outcomes following risk reducing surgery in BRCA carriers

Primary surgical prevention in the form of risk-reducing salpingo-oophorectomy (RRSO) is the most effective option and the gold standard for ovarian cancer (OC) risk-reduction, particularly given the absence of an effective national OC screening programme. However, premenopausal RRSO leads to premature surgical menopause with detrimental long-term health sequelae particularly in women who do not/are unable to take hormone replacement therapy (HRT). HRT uptake in women undergoing pre-menopausal oophorectomy appears low and is dependent on informed counselling, the safety of HRT and efficacy in mitigating the health sequelae of premature menopause. Acceptance of a central role for the fallopian tube in OC etiopathogenesis, coupled with the detrimental consequences of premature menopause, has led to the attractive proposal of early-salpingectomy with delayed oophorectomy as an alternative OC surgical prevention strategy in premenopausal women who have completed childbearing but decline or wish to delay RRSO. The successful implementation of risk reducing surgery for OC prevention depends on the acceptability of surgery to both, recipients (e.g. BRCA1/BRCA2 carriers) and intervention deliverers (healthcare professionals/researchers). Acceptability is also informed by an understanding of health outcomes following risk reducing surgery and the safety of HRT. It is therefore vital to understand the effects of surgery on important health outcomes such as cardiovascular health, neurological function and bone health. We present a comprehensive review of acceptability, the selected health outcomes mentioned above and HRT safety following risk reducing surgery.     

子宫腔碘水加压法输卵管再通术的临床研究

目的寻求一种简便快速、安全有效、经济实用,将造影诊断与输卵管再通治疗结合起来的新方法。方法应用双腔球囊胶管插入子宫腔,充盈球囊堵塞子宫颈内口,用助推器注入碘海醇充盈子宫腔及输卵管,电视动态观察实时点片,完成造影诊断。当发现输卵管阻塞时,用手助推加压,逐渐增高宫腔内压力,使阻塞输卵管被造影剂压力钝性开通。结果本组2698例,插管成功2685例。其中,原发不孕806例,继发不孕1868例,其他24例,输卵管阻塞3082支(右1561支、左1521支),占实有输卵管的59%,加压开通率为77.8%(2397/3082);通而不畅343支(右175支、左168支),加压开通率:93.9%(322/343),出现静脉逆流27例。除局部疼痛及少量阴道流血外,无严重并发症病及病死率。结论该法简便快速,安全有效,经济实用,将造影诊断与输卵管再通相结合,深受患者欢迎,值得推广应用。     

Measurement of kinetic parameters in skeletal muscle by magnetic resonance imaging with an intravascular agent.

The purpose of this work was to investigate the use of an intravascular contrast agent to determine perfusion kinetics in skeletal muscle. A two-compartment kinetic model was used to represent the flux of contrast agent between the intravascular space and extravascular extracellular space (EES). The relationship between the image signal-to-noise ratio (SNR) and errors in estimating permeability surface area product (Ktrans), interstitial volume (ve), and plasma volume (vp) for linear and nonlinear curve-fitting methods was estimated from Monte Carlo simulations. Similar results were obtained for both methods. For an image SNR of 60, the estimated errors in these parameters were 10%, 22%, and 17%, respectively. In vivo experiments were conducted in rabbits to examine physiological differences between these parameters in the soleus (SOL) and tibialis anterior (TA) muscles in the hind limb. Values for Ktrans were significantly higher in the SOL (3.2+/-0.9 vs. 2.0+/-0.5x10(-3) min-1), as were values for vp (3.4+/-0.8 vs. 2.1+/-0.7%). Differences in ve for the two muscles (8.7+/-2.2 vs. 8.5+/-1.6%) were not found to be significant. These results demonstrate that relevant physiological metrics can be calculated in skeletal muscle using MRI with an intravascular contrast agent.     

Antiproliferative, cytotoxic and apoptogenic activity of Indian toad (Bufo melanostictus, Schneider) skin extract on U937 and K562 cells.

The antiproliferative, cytotoxic and apoptogenic activities of Bufo melanostictus (Indian common toad) skin extract (TSE) on U937 and K562 leukemic cell line has been investigated. TSE significantly (P<0.001) reduced the time-dependent cell proliferation and decreased MTT values in U937 and K562 cells. TSE (IC50 doses) suppressed the proliferating cell nuclear antigen expression in both the cells. It was demonstrated that, TSE (IC50 doses) primarily arrested the U937 and K562 cells at G1 phase of the cell cycle. Confocal microscopy showed the altered fragmented nuclei and apoptotic bodies formation in TSE (IC50 doses) treated U937 and K562 cells. Membrane blebbing, cell surface shrinkage and perforation were observed through scanning electron microscope. TSE-induced DNA fragmentation in U937 and K562 cells was reflected in single-cell gel electrophoresis. TSE significantly (P<0.001) increase the length-width ratio of DNA mass as compared to control in comet assay. The flow cytometric analysis of annexin-V binding to the cancer cells further supported the apoptotogenic activity of TSE. The effect of TSE on normal human peripheral blood mononuclear cells viability and cytotoxicity was studied in culture and found to be less cytotoxic than on the U937 and K562 cells. The findings from the present study suggested that TSE might possess potent antineoplastic agent having antiproliferative, cytotoxic and apoptogenic activity against U937 and K562 myeloid leukemic cells.     

胸膜腔造影和注射粘连剂对难治性气胸的诊治

目的：为更清晰地显示顽固性气胸的漏气部位和性质，为不能耐受手术者摸索一种新的治疗手段。方法：选择１８例患者，先用７６％泛影葡胺行胸膜腔造影，而后在局部注入少量粘连剂。结果：造影后发现多发性肺大泡８例，单发性肺大泡６例，肺大泡伴粘连带４例。病变分别位于左上肺，右上肺，中下肺野及叶间裂。注射粘连剂后，１５例一次成功，３例第二次成功。随防６～１８个月，未见复发。结论：该方法易掌握，无明显副作用。病变显示明显，易被患者接受，具有明显的临床效果和推广价值     

心肌造影超声心动图评估心肌缺血程度的实验研究

本实验制作不同程度心肌缺血的动物模型，以声处理５％人血白蛋白为超声造影剂进行心肌灌注造影，探讨ＭＣＥ时间－强度曲线各指标与心肌缺血程度间的关系。结果表明：心肌显影的峰值强度和曲线下面积均与缺血程度呈显著负相关（相关系数分别为ｒ＝－０．９８，Ｐ值＜０．００５；ｒ＝－０．９４，Ｐ值＜０．０５），且能区分轻度、中度和重度三种程度的心肌缺血；而三项时间指标与心肌缺血程度间未发现显著性差异。本实验的初步结果表明，ＭＣＥ是一项活体评估局部心肌血流灌注的有效方法。     

膨润土对药用混悬液助悬性能的考察

本文报道了无机胶体膨润土(Bentonite)作为助悬剂在炉甘石洗剂中的应用,并与有机助悬剂及另一种无机胶体XVT—M进行比较,显示了其优异的助悬性能。