化学药物在癫痫治疗中的应用

癫痫是一种常见的破坏性脑部疾病,主要表现为大脑神经元同步异常放电所引起的突然性、一过性、反复性中枢神经系统功能失常,在任何年龄均可发病。癫痫首选化学药物治疗,但由于传统抗癫痫药物的耐受性和副作用,临床上出现了一批新型抗癫痫药,一些中草药的药效和化学成分分析研究也在加大开展。该文综述了新型抗癫痫药和中草药在癫痫治疗中的应用。     

抗癫痫药物的分析方法研究

对各种抗癫痫药物的分析方法做了详细总结,为广大药师和药物分析者提供了便利.     

抗癫痫药瑞替加滨的合成研究

对抗癫痫原料药瑞替加滨的合成工艺进行了改进,对硝基苯胺和氯甲酸乙酯为起始原料,为起始原料,经取代、还原、缩合等反应得到目标产物瑞替加滨二盐酸盐,目标化合物的结构经熔点(MP)、核磁共振氢谱(1H-NMR)和质谱(MS)确证。与文献报道相比,本工艺避免了使用高温,高压的反应条件和有危险性的催化剂,以常温、常压和常用试剂代替。所使用的原料易得,反应条件温和,操作安全,可作为工业化生产一个新的选择。     

丁苯酞对癫痫患者认知功能障碍和血清S100B蛋白及BDNF水平相关性研究

目的:观察丁苯酞对癫痫患者认知功能损害的改善效果,及对血清S100B蛋白及血清BDNF表达水平的影响,为丁苯酞的临床应用提供依据。方法:本试验通过随机方式把与入选标准相符的癫痫病人分别归入对照组与给药组,两组区别在于后者在接受抗癫痫药物干预的同时还进行了丁苯酞药物治疗。对健康组、对照组与给药组研究对象分别在干预前、干预3个月、干预6个月时实施认知功能评估、血清内BDNF与S100B水平测定。结果:相较对照组,给药组S100B蛋白水平降低,BDNF水平则上升,且两项均表现出显著差别(P0.05)。结论:丁苯酞治疗癫痫患者认知功能障碍与S100B蛋白和BDNF的表达有关。     

抗癫痫治疗药物左乙拉西坦的合成研究

以蛋氨酸为原料经还原脱硫甲基化、酯化、氨解、酰胺化及分子内缩和成环4步反应合成得到了左乙拉西坦,总收率44.6%。     

慢性脑供血不足患者认知功能障碍的临床治疗效果观察

目的对慢性脑供血不足患者的认知功能进行评定,并与对照组进行比较。方法选择56例确诊的慢性脑供血不足患者行简易智能状况量表(MMSE),画钟表测试(CDT)检查,将其结果与正常对照组进行比较。病例组治疗后再次进行MMSE、CDT检查,将其结果与治疗前进行比较。结果对照组评分与病例组认知功能量表评分结果差异具有显著性(P<0.05)。治疗后认知功治能量表评分结果高于治疗前,差异均有统计学意义(P<0.05)。病例组治疗后认知功治能量表评分结果与对照组比较差异仍有统计学意义(P<0.05)。结论慢性脑供血不足患者在记忆力、视空间能力、执行功能等认知功能方面较正常老年人下降,但未达到痴呆标准。早期治疗,可以改善其认知功能障碍。     

慢性前列腺炎伴勃起功能障碍患者的性激素水平改变

目的探讨性激素水平改变在慢性前列腺炎伴勃起功能障碍发病中的作用。方法将无CP及ED的体检健康男性20例设为正常组;将CP不伴ED患者20例设为对照组;将CP伴ED患者20例设为实验组。按统一标准抽血取样,采用化学发光法测定6项性激素指标(T、E2、FSH、LH、P、PRL)。将以上3组数据进行两两比较。结果对照组与正常组比较,性激素各项指标差别均无统计学意义(P>0.05);实验组与正常组、对照组比较,T降低、E2增高(P<0.01)。结论性激素水平改变在慢性前列腺炎伴勃起功能障碍发病中可能起重要作用。     

慢性脑缺血致认知功能障碍大鼠神经细胞Caspase-3表达及GDNF给药的影响

目的观察慢性脑缺血后致认知功能障碍大鼠神经细胞半胱氨酸蛋白酶(Caspase-3)表达,并探讨胶质细胞源性神经营养因子(GDNF)对大鼠认知功能障碍和Caspase-3表达的影响。方法采用双侧颈总动脉永久结扎方法制备慢性前脑缺血大鼠模型,随机分为对照组、GDNF组和生理盐水组,分别在术后1月、2月,根据逃避潜伏期对各组大鼠进行记忆功能测定,应用免疫组织化学方法检测Caspase-3表达。结果双侧颈总动脉结扎1、2月组与对照组相比,逃避潜伏期明显延长;GDNF组与生理盐水组比较,逃避潜伏期明显缩短;与对照组相比,缺血组大鼠额叶皮层、海马的Caspase-3阳性细胞数明显增多,与生理盐水组比较,1、2月GDNF组大鼠额叶皮层、海马的Caspase-3阳性细胞数明显减少。结论GDNF可改善认知功能,其机制可能是通过影响Caspase-3凋亡关键蛋白酶表达,抑制神经细胞凋亡。     

老年癫痫患者的发作型态与急救处置原则

近年来,随着我国人口进入老龄化阶段,中枢神经系统疾病如脑血管病、神经系统退行性疾病发病率明显增加,从而使老年人癫痫的发病率明显增高。已成为神经内科老年人排第3位的慢性疾病。老年癫痫绝大多数为继发症状性癫痫。病因以脑血管病占居首位。调查表明,老年人癫痫中约40%是由脑血管病引起的,以脑梗死居首位,其次是脑出血、蛛网膜下腔出血。其他常见的病因还有代谢性中毒(如酒精中毒、低血糖、非酮性高血糖)、脑肿瘤、脑外伤和颅脑手术后、痴呆和中枢神经系统炎症。但仍有约15%的老年人癫痫找不到明确的病因。     

Discovery of a Metabolic Signature Predisposing High Risk Patients with Mild Cognitive Impairment to Converting to Alzheimer’s Disease

Assessing dementia conversion in patients with mild cognitive impairment (MCI) remains challenging owing to pathological heterogeneity. While many MCI patients ultimately proceed to Alzheimer’s disease (AD), a subset of patients remain stable for various times. Our aim was to characterize the plasma metabolites of nineteen MCI patients proceeding to AD (P-MCI) and twenty-nine stable MCI (S-MCI) patients by untargeted metabolomics profiling. Alterations in the plasma metabolites between the P-MCI and S-MCI groups, as well as between the P-MCI and AD groups, were compared over the observation period. With the help of machine learning-based stratification, a 20-metabolite signature panel was identified that was associated with the presence and progression of AD. Furthermore, when the metabolic signature panel was used for classification of the three patient groups, this gave an accuracy of 73.5% using the panel. Moreover, when specifically classifying the P-MCI and S-MCI subjects, a fivefold cross-validation accuracy of 80.3% was obtained using the random forest model. Importantly, indole-3-propionic acid, a bacteria-generated metabolite from tryptophan, was identified as a predictor of AD progression, suggesting a role for gut microbiota in AD pathophysiology. Our study establishes a metabolite panel to assist in the stratification of MCI patients and to predict conversion to AD.     

Impact of Amyloid Pathology in Mild Cognitive Impairment Subjects: The Longitudinal Cognition and Surface Morphometry Data

The amyloid framework forms the central medical theory related to Alzheimer disease (AD), and the in vivo demonstration of amyloid positivity is essential for diagnosing AD. On the basis of a longitudinal cohort design, the study investigated clinical progressive patterns by obtaining cognitive and structural measurements from a group of patients with amnestic mild cognitive impairment (MCI); the measurements were classified by the positivity (Aβ+) or absence (Aβ−) of the amyloid biomarker. We enrolled 185 patients (64 controls, 121 patients with MCI). The patients with MCI were classified into two groups on the basis of their [¹⁸F]flubetaben or [¹⁸F]florbetapir amyloid positron-emission tomography scan (Aβ+ vs. Aβ−, 67 vs. 54 patients) results. Data from annual cognitive measurements and three-dimensional T1 magnetic resonance imaging scans were used for between-group comparisons. To obtain longitudinal cognitive test scores, generalized estimating equations were applied. A linear mixed effects model was used to compare the time effect of cortical thickness degeneration. The cognitive decline trajectory of the Aβ+ group was obvious, whereas the Aβ− and control groups did not exhibit a noticeable decline over time. The group effects of cortical thickness indicated decreased entorhinal cortex in the Aβ+ group and supramarginal gyrus in the Aβ− group. The topology of neurodegeneration in the Aβ− group was emphasized in posterior cortical regions. A comparison of the changes in the Aβ+ and Aβ− groups over time revealed a higher rate of cortical thickness decline in the Aβ+ group than in the Aβ− group in the default mode network. The Aβ+ and Aβ− groups experienced different APOE ε4 effects. For cortical–cognitive correlations, the regions associated with cognitive decline in the Aβ+ group were mainly localized in the perisylvian and anterior cingulate regions. By contrast, the degenerative topography of Aβ− MCI was scattered. The memory learning curves, cognitive decline patterns, and cortical degeneration topographies of the two MCI groups were revealed to be different, suggesting a difference in pathophysiology. Longitudinal analysis may help to differentiate between these two MCI groups if biomarker access is unavailable in clinical settings.     

新辅助化疗联合生物治疗对低位直肠癌患者免疫功能的影响

目的 探讨新辅助化疗联合生物治疗对低位直肠癌患者手术治疗前细胞免疫功能的影响.方法 选取直肠癌Dukes C期患者15例,术前采用新辅助化疗XELOX方案两个疗程后进行生物治疗.利用流式细胞仪测定新辅助化疗前及生物治疗前、后T淋巴细胞亚群、NKT细胞以及NK细胞的百分比,并评价患者的近期疗效.结果 患者新辅助化疗前免疫...     

Revealing the Influences of Sex Hormones and Sex Differences in Atrial Fibrillation and Vascular Cognitive Impairment

The impacts of sex differences on the biology of various organ systems and the influences of sex hormones on modulating health and disease have become increasingly relevant in clinical and biomedical research. A growing body of evidence has recently suggested fundamental sex differences in cardiovascular and cognitive function, including anatomy, pathophysiology, incidence and age of disease onset, symptoms affecting disease diagnosis, disease severity, progression, and treatment responses and outcomes. Atrial fibrillation (AF) is currently recognized as the most prevalent sustained arrhythmia and might contribute to the pathogenesis and progression of vascular cognitive impairment (VCI), including a range of cognitive deficits, from mild cognitive impairment to dementia. In this review, we describe sex-based differences and sex hormone functions in the physiology of the brain and vasculature and the pathophysiology of disorders therein, with special emphasis on AF and VCI. Deciphering how sex hormones and their receptor signaling (estrogen and androgen receptors) potentially impact on sex differences could help to reveal disease links between AF and VCI and identify therapeutic targets that may lead to potentially novel therapeutic interventions early in the disease course of AF and VCI.     

Fecal Volatile Organic Compounds and Microbiota Associated with the Progression of Cognitive Impairment in Alzheimer’s Disease

Metabolites produced by an altered gut microbiota might mediate the effects in the brain. Among metabolites, the fecal volatile organic compounds (VOCs) are considered to be potential biomarkers. In this study, we examined both the VOCs and bacterial taxa in the feces from healthy subjects and Alzheimer’s disease (AD) patients at early and middle stages. Remarkably, 29 fecal VOCs and 13 bacterial genera were differentiated from the healthy subjects and the AD patients. In general, higher amounts of acids and esters were found in in the feces of the AD patients and terpenes, sulfur compounds and aldehydes in the healthy subjects. At the early stage of AD, the most relevant VOCs with a higher abundance were short-chain fatty acids and their producing bacteria, Faecalibacterium and Lachnoclostridium. Coinciding with the development of dementia in the AD patients, parallel rises of heptanoic acid and Peptococcus were observed. At a more advanced stage of AD, the microbiota and volatiles shifted towards a profile in the feces with increases in hexanoic acid, Ruminococcus and Blautia. The most remarkable VOCs that were associated with the healthy subjects were 4-ethyl-phenol and dodecanol, together with their possible producers Clostridium and Coprococcus. Our results revealed a VOCs and microbiota crosstalk in AD development and their profiles in the feces were specific depending on the stage of AD. Additionally, some of the most significant fecal VOCs identified in our study could be used as potential biomarkers for the initiation and progression of AD.     

抗肝炎类瑶族药的研究现状

对瑶族民间抗肝炎植物药进行了较系统的研究和调查,有属于33科47种的植物药有抗肝炎作用。并对其中的野葛花、枸骨叶、白马骨和小紫金牛护肝作用进行了初步的研究。     

钾素对水稻生理功能的影响浅析

钾是作物生长发育不可缺少的营养元素之一,是决定水稻生理特性的重要因子。钾素可对水稻的蛋白质合成、光合和呼吸等产生影响,进而影响其产量和品质。     

老年COPD合并胸腰椎骨折PVP术对肺功能的改善研究

目的探讨椎体成形术(PVP)治疗慢性阻塞性肺疾病(COPD)合并胸腰椎骨折患者对肺功能改善情况及分析。方法选择胸腰段脊柱压缩性骨折合并COPD患者48例作为研究对象,手术前后分别测量肺功能并进行分析研究。结果椎体成形术后1周及1个月患者肺功能较术前均显著改善。结论 COPD合并胸腰椎骨折患者经椎体成形术后能有效改善肺通气功能,考虑可能与术后胸廓重建稳定性及疼痛减轻后病人膈肌及肋间肌功能改善有关;而且,我们认为另一个不容忽视的原因是术后病人疼痛减轻,敢于进行咳嗽及排痰,并且呼吸道平滑肌蠕动能力增加,使气道阻力大大降低,从而使肺功能得到一定改善。     

药物分子与血清白蛋白相互作用的研究进展

文章综述了药物分子与血清白蛋白相互作用的研究概况,内容涉及药物分子与血清白蛋白相互作用的研究方法,药物分子与血清白蛋白的结合反应特征,包括结合常数、结合位点数、结合距离、相互作用力的确定等涉及文献15篇。     

加入WTO对江苏医药行业的影响与对策

根据中国政府对医药行业入世所作的承诺 ,具体分析加入WTO对江苏医药行业的主要影响。针对江苏医药行业的发展现状 ,提出应采取的主要措施