丹参和透明质酸钠注射液对骨性关节炎治疗作用的实验研究

采取家兔膝关节制动方法建立骨性关节炎动物模型，用丹参注射液和透明质酸钠注射液关节腔内注射进行治疗，分别在制动后3、6、9周测量关节活动度，取关节软骨制成标本经光镜和透射电镜观察。结果显示，与单纯制动组比较，丹参治疗组和透明质酸钠治疗组的关节活动度明显改善，关节病变出现晚，程度轻，以早期最明显。表明丹参和透明质酸钠具有延缓和减轻关节退变的作用，对骨性关节炎早期有一定的治疗作用。     

基于数学模型的非洛地平缓释片检验指标综合评价的探讨

目的为客观评价合格药品的生产质量状况,有效区分其存在的差异程度,通过建立一定的数学模型,对特定药品每一项可定量的检验指标进行综合评价。方法本数学模型将药品的检验指标参数以理论最佳点做理想值,以药品合格标准做下限值,转化成各指标的评价指数,并使各评价指数同量齐次;各检验指标的评价指数经过带权重的理想点法计算,得到综合评价结果;其中,运用专家经验评定法确定各检验指标的权重。结果数学模型确立后,尝试以非洛地平缓释片各项检验数据为例进行试评价,获得了较为符合客观实际的结果,说明了用数学模型评价药品检验的各项指标的可行性和可操作性,该方法也可以推广至其他药品检验指标的综合结果判断。结论利用数学模型对药品检验结果进行评价的方法,可以成为药品质量监督管理的新思路,也可以为药品按质定价提供参考性依据。     

仙人掌中的两个新酚性羧酸酯

从仙人掌块茎中分得二个新酚性羟酸酯和六个已知化合物。根据其理化性质和波谱学方法鉴定它们的结构为2－（4－羟基－苄基－）苹果到－4－正丁酯（1）－2－（4－羟基－苄基）－苹果酸－4－甲酯（2），2－（4－羟基－苄基）－苹果酸（3），蒲公英萜醇－3－乙酸酯（4），软木三萜酮（5），羽扇豆－3－酮（6），亚油酸甲酯（7）和油酸甲酯（8），其中（1）和（2）为新化合物，（3），（4），（6），（7）和（8）为首的次从仙人掌中分得。     

260例住院患者抗菌药应用调查

目的:调查临床抗菌药使用现状,加强用药管理。方法:查阅某医院260例住院患者的电子病历,按照设定指标进行统计分析。结果:抗菌药使用率65.00%(≥2种56.80%);联用率47.93%;注射剂使用率85.80%;围手术期预防性用药率100.00%;无指征用药29.58%;菌检及药敏率仅为4.75%。使用频率高的多为价格昂贵的新型抗菌药。结论:不合理应用抗菌药的现象依然严重存在,应采取各种干预措施,加大监管力度,规范处方用药行为。     

Synthesis and evaluation of a 18F‐labeled 4‐phenylpiperidine‐4‐carbonitrile radioligand for σ1 receptor imaging

We report the design and synthesis of several 4‐phenylpiperidine‐4‐carbonitrile derivatives as σ₁ receptor ligands. In vitro radioligand competition binding assays showed that all the ligands exhibited low nanomolar affinity for σ₁ receptors (K_i(σ₁) = 1.22–2.14 nM) and extremely high subtype selectivity (K_i(σ₂) = 830–1710 nM; K_i(σ₂)/K_i(σ₁) = 680–887). [¹⁸F]9 was prepared in 42–46% isolated radiochemical yield, with a radiochemical purity of >99% by HPLC analysis after purification, via nucleophilic ¹⁸F^‐ substitution of the corresponding tosylate precursor. Biodistribution studies in mice demonstrated high initial brain uptakes and high brain‐to‐blood ratios. Administration of SA4503 or haloperidol 5 min prior to injection of [¹⁸F]9 significantly reduced the accumulation of radiotracers in organs known to contain σ₁ receptors. Two radioactive metabolites were observed in the brain at 30 min after radiotracer injection. [¹⁸F]9 may serve as a lead compound to develop suitable radiotracers for σ₁ receptor imaging with positron emission tomography.     

狼毒大戟中松香烷型二萜内酯的抗肿瘤活性研究

摘 要 目的： 对狼毒大戟中松香烷型二萜内酯类化学成分进行分离和结构鉴定,将得到的单体化合物与6种不同的人肿瘤细胞株相互作用探讨其抗肿瘤活性。方法: 通过硅胶、ODS等柱色谱与1D、2D-NMR波谱学测试技术结合,从狼毒大戟中分离并确定4个松香烷型二萜内酯类化合物：jolkinolide A (1)、jolkinolide B (2)、17 hydroxyjolkinolide A (3)、17-hydroxyjolkinolide B (4)。采用噻唑蓝比色法（MTT法）分别测定其与6种人肿瘤细胞株：肝癌HepG-2、乳腺癌MCF-7、胃癌SGC 7901、胃癌BGC-823、胃癌MGC-803、宫颈癌Hela相互作用结果,并计算抑制率与半抑制率(IC₅₀)。结果: 化合物2对肝癌HepG-2、乳腺癌MCF-7、宫颈癌Hela细胞的增殖有显著得抑制作用IC₅₀均＜25 μmol·L^-1,化合物4对乳腺癌MCF 7细胞的增殖有显著抑制作用IC₅₀＜30 μmol·L^-1。结论: 狼毒大戟中松香烷型二萜内酯类化合物具有显著的抗肿瘤活性。     

螺旋CT增强扫描及肺动脉造影在肺动脉栓塞中的诊断价值

目的 评价螺旋CT增强扫描和肺动脉造影在肺动脉栓塞（PE）的诊断价值.方法 对11例同时行螺旋CT增强扫描和肺动脉造影、临床诊断PE的患者的影像学原始资料进行回顾性分析,逐支判断肺动脉的栓子情况.结果 11例患者共发现9支肺动脉主干栓塞及51支肺段动脉栓塞,其中CT增强诊断肺动脉主干栓塞敏感性和特异性均为100%,诊断肺段动脉栓塞敏感性66.7%、特异性91.9%;而肺动脉造影诊断肺动脉主干栓塞的敏感性88.9%、特异性100%,诊断肺段动脉栓塞的敏感性60.8%、特异性83.8%.结论 螺旋CT增强扫描对PE诊断有更高的敏感性和特异性,将成为首选的影像学检查方法.     

The protective effect of picroside II against hypoxia/reoxygenation injury in neonatal rat cardiomyocytes

Context: Picroside II, an iridoid glucoside found in the root of Picrorhiza scrophulariiflora Pennell (Scrophulariaceae), has been demonstrated to possess potent antioxidant activity. However, whether picroside II has a protective effect against hypoxia/reoxygenation (H/R)-induced cardiomyocyte injury is poorly understood. Objective: To explore the cardioprotective role of picroside II against oxidative stress induced by H/R injury in neonatal rat cardiacmyocytes. Materials and methods: The viability and cellular damage of cardiomyocytes were assessed by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolim bromide (MTT) and lactate dehydrogenase (LDH) assays, respectively. The activities of superoxide dismutase (SOD) and glutathione peroxidase (GSH-Px), the levels of reduced (GSH) and oxidized glutathione (GSSG), and the contents of malondialdehyde (MDA) were determined by a colorimetric method. The levels of intracellular reactive oxygen species (ROS) and calcium were evaluated by flow cytometric analysis. Results: We analyzed the effective half-maximal concentration for protection from the dose-response curves and obtained the concentration of 50 μg/mL as EC(50). Pretreated cardiomyocytes with picroside II (50-200 μg/mL), prior to H/R exposure, inhibited LDH activity in culture media and increased cell viability in a dose-dependent manner. This protective effect was accompanied by significantly increasing reduced GSH contents and the activities of SOD and GSH-Px and attenuating MDA and GSSG contents in response to H/R injury. Furthermore, treatment with picroside II also inhibited ROS production and calcium accumulation in cardiomyocytes. Discussion and conclusion: The present study demonstrates that picroside II protects cardiomyocytes against oxidative-stress injury induced by H/R through reduction of ROS production and calcium accumulation and enhancement of the activity of antioxidant defense.     

贵州省IgA肾病临床与病理特征相关性分析

目的 研究贵州省IgA肾病(IgAN)患者的临床表现与病理类型两者之间的关系,以探讨贵州省IgAN的发病率,进一步评价肾活检在肾脏病诊治中的作用及临床意义.方法 方法对730例有肾穿刺活检适应证的患者行B超介导下肾活检,并作光镜、免疫荧光、电镜检查,对其中确诊为lgA肾病者作病理及临床特点分析.结果 (1)贵州省lgA...     

洋葱伯克霍尔德菌群(Bcc)及干扰菌在不同增菌培养基中的生长研究

目的：考察Bcc以及Bcc与干扰菌的混合物在不同的增菌培养基中能否生长和增殖;探讨不同的 Bcc菌种对增菌培养基的营养需求和抗生素的耐受是否存在差异。方法：将Bcc的代表菌株、干扰菌以及 Bcc与干扰菌的混合物分别接种至TSB、10倍稀释的TSB、添加10 mg·L-1庆大霉素的TSB和添加250000 U·L-1多粘菌素B的TSB中培养,划线分离至选择性培养基上观察结果,并对可疑菌落进行分离和鉴定。结果：只接种Bcc的4种增菌培养基均能使之良好地增殖。低量的Bcc(约102 cfu)与高量的干扰菌 (104 cfu)的混合接种,除了神秘伯克霍尔德菌CMCC(B)23010外,4种增菌培养基能使Bcc增殖并被检出。结论：添加抗生素的TSB与未添加抗生素的相比没有表现出明显的优势。TSB可以作为Bcc检验时的增菌培养基使用。生长缓慢且活力弱的Bcc菌株在特定条件下有可能会被漏检。