Practical approaches to labelling terminal alkynes with deuterium

Base catalysed exchange with sodium hydroxide, calcium oxide or N,N,N,N-tetramethylguanidine in deuterium oxide is a viable procedure for the preparation of terminally deuterated alkynes for those alkynes stable to strong base. The use of silver perchlorate as a catalyst is an alternative practical option when labelling alkynes which are sensitive to base or contain functionalities which would lead to labelling elsewhere in the molecule. Labelling with this catalyst takes place smoothly at ambient temperature in a mixture of N,N-dimethylformamide and deuterium oxide.     

Case studies in swelling polymeric gastric retentive tablets

Swelling tablets administered in the fed state have been shown to provide therapeutic advantages in two marketed products, with the duration of delivery characterised with respect to food and tablet size. Metformin extended-release tablets are a diffusion-based swelling tablet demonstrating once-daily efficacy with good gastrointestinal solubility. Ciprofloxacin extended-release tablets are based on an erosional matrix that delivers the drug to the upper gastrointestinal tract over 6 h to provide once-daily efficacy with reduced incidences of nausea and diarrhoea. Furosemide extended-release tablets are another example of an erosional matrix designed to deliver furosemide to the duodenum and upper jejunum over 6 h to provide a more gradual diuresis and naturesis compared with the immediate-release product.     

DP、EP化疗方案治疗非小细胞肺癌的临床疗效及其对血清血管内皮生长因子的影响

目的对比DP、EP化疗方案治疗非小细胞肺癌（NSCLC）的临床疗效及其对血清血管内皮生长因子（VEGF）的影响。方法102例晚期NSCLC患者随机分为DP组（n=58）和EP组（n=44）。DP组静脉注射多西紫杉醇75mg／m2，dl；静脉滴注顺铂75mg／m2，d1～4；EP组静脉滴注依托泊苷0．1g／d，d1～5；顺铂用法同上。两组28d为1个周期，治疗3个周期，化疗前后常规给予止呕类药物及对症治疗。检测两组临床疗效和血清VEGF水平。结果DP组、EP组，总有效率分别为74．14％和29．55％，DP组总有效率明显高于EP组。与治疗前比较，两组治疗后血清VEGF水平均明显降低。DP组治疗后血清VEGF水平明显低于EP组治疗后。结论DP治疗中晚期NSCLC临床疗效确切，有效率、生存率均较高。     

川芎茶调散加减治疗三叉神经痛42例疗效分析

目的：探讨川芎茶调散加减对三又神经痛的治疗效果，以供参考。方法：选择2009年10月-2012年9月我院三叉神经痛患者84例作为研究对象，根据随机分组。A组接受卡马西平治疗，B组同时接受川芎茶调散加减治疗。连续治疗4周后评价疗效，对比两组患者总有效率的差异性。结果：对比两组总有效率发现，B组明显高于A组，差异具有统计学意义（P〈0．05）。结论：采用川芎茶调散加减辅助治疗三叉神经痛具有一定的优越性，值得推广应用。     

蛋白激酶A RⅡβ结构及功能的研究进展

蛋白激酶A(PKA)是由1个调节亚基(R亚基)二聚体和两个催化亚基(C亚基)组成的四聚体,全酶无活性。R亚基有RⅠα、RⅠβ、RⅡα和RⅡβ4种亚型,分别具有不同的理化性质。RⅡβ亚基氨基端包含1个二聚化/对接结构域,PKA通过此结构域与腺苷酸激酶锚定蛋白结合锚定于细胞的特定位点。羧基端是两个串联的高度保守的环核苷酸结构域,与PKA全酶解聚以及激活有关。两个RC异二聚体通过RⅡβ亚基中的β4~β5环相锚定。细胞质中存在足够的Mg ATP时将导致RⅡβ亚基自身磷酸化。RⅡβ在特定组织表达,主要表达于内分泌腺、脑和脂肪组织。生物信息学分析表明,RⅡβ与其他R亚基的序列有很大差别,只有大约50%的序列相同,提示RⅡβ可能具有不同的生物学功能。因此,目前对PKA RⅡβ的功能及其作用机制的研究已逐渐成为热点。     

Fetal and perinatal stem cells in cardiac regeneration: Moving forward to the paracrine era

Cardiovascular disease (CD) is a major burden for Western society. Regenerative medicine has provided encouraging results, yet it has not addressed the focal defects causing CD and mainly related to the inefficient repair programme of the heart. In this scenario, stem cells have been broadly investigated and their paracrine effect proposed as a possible working strategy to boost endogenous mechanisms of repair and regeneration from within the cardiac tissue.The scientific community is now focusing on identifying the most effective stem cell secretome, as the whole of bioactive factors and extracellular vesicles secreted by stem cells and endowed with regenerative potential. Indeed, the adult stem cell-paracrine potential for cardiac regeneration have been widely analyzed with positive outcome. Nevertheless, low yield, invasive sampling and controversial self-renewal may limit adult stem cell application. On the contrary, fetal and perinatal stem cells, which can be easily isolated from leftover sample via prenatal screening during gestation or as clinical waste material after birth, can offer an ideal alternative. These broadly multipotent immature progenitors share features with both adult and embryonic stem cells, show high self-renewal, but they are not tumorigenic neither cause any ethical concern. While fetal and perinatal stem cells demonstrated to improve cardiac function when injected in the injured heart, the comprehensive characterization of their secretome for future applications is still at its infancy.In this review, we will discuss the paracrine potential of the fetal and perinatal stem cell secretome to provide cardiac repair and resurge the dormant mechanisms of cardiac regeneration for future therapy.     

急性心源性肺水肿临床疗效与X线胸片的相关性分析

目的研究急性心源性肺水肿治疗效果和X线胸片表现之间的关系,为临床评估疗效提供帮助。方法由2名有经验的放射科医师采用盲法回顾性分析48例急性心源性肺水肿患者治疗前后的X线胸片好转率,所得的数据做χ2检验,并用Kappa检验对2人评判的结果做一致性分析。结果医师甲、乙所得的结论均为:急性心源性肺水肿临床治疗后好转者,X线胸片好转率的差异有统计学意义(P<0.05)。甲乙医师间阅片的一致性分析差异有统计学意义(P<0.05),说明甲乙2名医师对治疗前后X线表现好转与否的诊断结果有较好的一致性。讨论急性心源性肺水肿治疗过程中复查X线胸片,是评估临床疗效的一种有效的方法 。     

Solifenacin-induced delirium and hallucinations

Solifenacin-induced cognitive adverse effects have not been reported frequently, but solifenacin-induced delirium and hallucinations with successful switching to darifenacin, without additional drug, have not been reported in the literature. In this case report, we present an 80-year-old Caucasian male with insomnia and anxiety symptoms and overactive bladder who developed delirium and hallucinations when treated with solifenacin and trazodone. After solifenacin discontinuation and switching to darifenacin, symptoms significantly improved immediately. Such a case has not yet been described in literature; however, an adverse effect associated with solifenacin can occur, as this report clearly demonstrates.     

Sexual dysfunction related to antiepileptic drugs in patients with epilepsy

Introduction: Epilepsy is a common disease that is mostly treated with antiepileptic drugs (AEDs). However, the sexual dysfunction (SD) side effects related to the use of AEDs have not received sufficient attention.

Areas covered: The purpose of this review is to examine the current evidence on SD-related side effects of AEDs. The incidence, clinical features and major types of SD are summarized. Furthermore, various AEDs that may cause SDs are addressed in detail. Finally, we briefly summarize the treatments for SD related to AEDs.

Expert opinion: SD related to AEDs is common. Symptoms include erectile dysfunction (ED), hyposexuality, hypersexuality and ejaculatory dysfunction. Traditional AEDs such as valproate and enzyme-inducing AEDs (EIAEDs) may produce high incidences of decreased libido. Recently, sexual function changes related to new AEDs have been reported. Topiramate, pregabalin and gabapentin may cause SD, whereas oxcarbazepine, lamotrigine and levetiracetam may improve sexual function. Although the treatment for SD related to AEDs remains unclear, switching to another AED may be an option. Further studies are necessary to better understand and treat SD related to AEDs.     

腹腔镜与开腹手术治疗急性阑尾炎的对比分析

目的对比分析腹腔镜与开腹手术治疗急性阑尾炎的疗效,总结其临床应用价值。方法选取我院2009年6月～2011年6月86例急性阑尾炎的患者,随机分为观察组(腹腔镜手术)和对照组(开腹手术)各43例,观察比较两组疗效。结果两组疗效比较差异显著(P<0.05),具有统计学意义。结论腹腔镜手术治疗急性阑尾炎效果显著,具有无创、恢复快、出血少等优点,安全可靠。