大鼠脊髓慢性压迫及减压后神经细胞凋亡及其相关基因的表达

目的：观察慢性压迫性脊髓损伤后及减压后神经细胞凋亡和Bcl-2mRNA，P53mRNA,CASPASE-3神经功能恢复的影响。方法：将55只同龄Wistar大鼠，置入后路渐进式压迫装置，制作成慢性压迫性脊髓损伤模型。随机分为假手术对照组（A组5只），慢性脊髓压迫组（B组25只），减压组（C组25只）。应用原原位末端脱氧核糖核苷酸转移酶介导dUTP标记（TUNEL）技术及原位杂交检测方法，观察各组细胞凋亡率及细胞凋亡相关基因Bcl-2mRNA、P53mRNA、CASPASE－3在慢性压迫性脊髓损伤后及减压后的表达，分别于损伤后及减压后1、3、7、14、28d对慢性脊髓损伤区进行细胞凋亡及原位杂交检测。结果：A、B、C三组均发现神经细胞凋亡及细胞凋亡相关基因Bcl-2mRNA、P53mRNA，CASPASE－3的表达，A、B、C三组细胞凋亡率及阳性细胞灰度值比较，差异有显著性意义（P＜0．05）。阳性细胞表达程度与细胞凋亡的减少及神经功能的恢复相一致。结论：慢性压迫性脊髓损伤可导致大量的神经细胞凋亡，同时激活内源性保护机制，使脊髓发生适应性改变，减压可能通过激活此机制而减轻神经细胞凋亡，起到保护作用。     

2型糖尿病患者高危因素分析

目的 分析2型糖尿病患者各种高危险因素控制状况及其与慢性并发症的关系。方法 记录464例50岁以上的2型糖尿病患者收缩压、舒张压、血脂、糖化血红蛋白和体质指数，按有无并发症分为两组进行分析。结果 有并发症组糖尿病病程、血压、总胆固醇、低密度脂蛋白胆固醇和血纤维蛋白原明显增高。Wald卡方分析显示糖尿病病程和收缩压有统计学意义。多数患者这些危险因素未得到很好的控制。结论 糖尿病患者存在着多种高危因素，有慢性并发症者更为严重，应注意综合治疗。     

Antiviral triterpenes fromPrunella vulgaris

Two triterpenes 1 and 2 with antiviral activity againstHerpes simplex virus type 1in vitro were isolated fromPrunella vulgaris. Each compound caused a significant reduction in viral cytopathic effect whenvero cells were exposed to them for 72 hours after viral challenge. They were identified asbetulinic acid(1) and 2α, 3α-dihydroxyurs-12-en-28-oic acid(2) on the basis of their spectroscopic properties. The antiviral activity of them was estimated as EC₅₀=30 μg/ml(1) and 8 μg/ml(2), respectively by plaque reduction assay.     

Z-3-(2-羟基丁烯基)苯酞的合成研究

研究目的探讨苯酞类天然产物的合成方法及其生物活性。研究方法以邻苯二甲酐为底物，首先引入丁烯基，再进行烯丙位氧化，制得目标化合物。结果通过丁基锂反应，得到了具有药物活性的丁烯基苯酞，然后利用SeO2烯丙位氧化，首次合成了Z－3－（2－羟基丁烯基）苯酞。结论此合成方法原料易得，方法简便，为苯酞类化合物的合成研究提供了一个新的途径。     

磺胺噻二嗪硫酮衍生物的合成及其抑菌活性

利用药物化学骈合原理设计并合成了一系列新的３，５－二取代１，３，５－噻二嗪－２－硫酮类化合物，其结构经红外光谱，紫外光谱及元素分析证实，抑菌活性试验显示了良好的抑菌活性。     

Fipamezole (JP-1730) is a potent alpha2 adrenergic receptor antagonist that reduces levodopa-induced dyskinesia in the MPTP-lesioned primate model of Parkinson's disease.

Previous studies in the MPTP-lesioned primate model of Parkinson's disease have demonstrated that alpha(2) adrenergic receptor antagonists such as idazoxan, rauwolscine, and yohimbine can alleviate L-dopa-induced dyskinesia and, in the case of idazoxan, enhance the duration of anti-parkinsonian action of L-dopa. Here we describe a novel alpha(2) antagonist, fipamezole (JP-1730), which has high affinity at human alpha(2A) (K(i), 9.2 nM), alpha(2B) (17 nM), and alpha(2C) (55 nM) receptors. In functional assays, the potent antagonist properties of JP-1730 were demonstrated by its ability to reduce adrenaline-induced (35)S-GTPgammaS binding with K(B) values of 8.4 nM, 16 nM, 4.7 nM at human alpha(2A), alpha(2B), and alpha(2C) receptors, respectively. Assessment of the ability of JP-1730 to bind to a range of 30 other binding sites showed that JP-1730 also had moderate affinity at histamine H1 and H3 receptors and the serotonin (5-HT) transporter (IC(50) 100 nM to 1 microM). In the MPTP-lesioned marmoset, JP-1730 (10 mg/kg) significantly reduced L-dopa-induced dyskinesia without compromising the anti-parkinsonian action of L-dopa. The duration of action of the combination of L-dopa and JP-1730 (10 mg/kg) was 66% greater than that of L-dopa alone. These data suggest that JP-1730 is a potent alpha(2) adrenergic receptor antagonist with potential as an anti-dyskinetic agent in the treatment of Parkinson's disease.     

冠心病不同临床类型患者血浆、血小板脂质过氧化损伤与TXA_2/PGI_2平衡的研究

作者观察98例正常人和109例不同临床类型冠心病人血浆、血小板LPO、SOD,SeGSHP_x,RBC—SOD及血浆TXB_2、6-keto-PGF_(1α)的变化,发现各型冠心病组均有LPO、PL—LPO、TxB_2、TxB_2/6-keto-PGF_(1α)比值明显升高,6-keto-PGF_(1α),SOD、PLSOD、RBC-SOD,SOD/LPO及SeGSHPX/LPO比值明显降低。但各型程度不同,以急性心肌梗塞和不稳定性心绞痛改变突出。血浆LPO与6-keto-PGF_(1α)呈显著负相关。提示脂质过氧化损伤与TXA_2/PGI_2平衡密切相关。认为SOD/LPO、SeGSHPx/LPO,TXB_2/6-keto-PGF_(1α)比值在冠心病诊断中是重要有意义的指标,血小板SOD/LPO比值能更敏感地反映冠心病人氧化与抗氧化能力的平衡状态。     

Sclerosing epithelioid fiberosarcoma: short T2 on MR imaging

A case of sclerosing epithelioid fibrosarcoma and its appearance on MRI is presented. The tumor showed a zonal architecture on MRI with a large central core of very low signal intensity and a peripheral rim of intermediate to high signal intensity on T1- and T2-weighted spin echo pulse sequences. The core showed decreased cellularity with dense collagen deposition on histologic examination, and the peripheral zone increased cellularity with increased nuclear atypia. The presence of a prominent region of very low signal intensity on T1- and T2-weighted images can be seen with neural tumors, giant cell tumor of the tendon sheath, aggressive fibromatosis, and, in rare instances, with soft tissue sarcomas rich in collagen.     

血清sIL—2r表达水平与脓毒血症的严重程度及预后的关系

目的：探讨脓毒血症患者血清中可溶性白细胞介素２受体（ｓＩＬ２ｒ）的表达水平以及与该病严重程度及预后的关系。方法：采用双抗体夹心酶联免疫分析法检测２９例脓毒血症患者血清ｓＩＬ２ｒ表达水平的动态变化，并以３０例正常人作为对照；用ＡＰＡＣＨＥⅡ评分方法对脓毒血症患者进行疾病严重度评分。结果：①脓毒血症患者血清ｓＩＬ２ｒ表达水平较正常人明显升高（Ｐ＜００１）；②脓毒血症患者中死亡者与存活者的血清ｓＩＬ２ｒ表达水平比较，感染初期及晚期死亡者明显高于存活者（Ｐ＜００５）；③以本组患者感染ｄ１的ＡＰＡＣＨＥⅡ评分的中位数１６为分界点，将患者分为２组，２组的血清ｓＩＬ２ｒ水平有显著差别（Ｐ＜００５）。结论：脓毒血症患者血清ｓＩＬ２ｒ表达水平明显升高；该指标与脓毒血症患者的疾病的严重程度及预后有密切的关系。此项指标的检测对判断脓毒血症患者的病情严重度及预后可能有重要意义     

Pharmacology of KB‐R7943: A Na+–Ca2+ exchange inhibitor

The Na⁺–Ca²⁺ exchange (NCX) system plays a pivotal role in regulating intracellular Ca²⁺ concentration in cardiomyocytes, neuronal cells, kidney and a variety of other cells. It performs a particularly important function in regulating cardiac contractility and electrical activity. One of the leading NCX inhibitors is KB‐R9743 (KBR) that appears to exhibit selectivity for Ca²⁺‐influx‐mode NCX activity (reverse mode of NCX). In this article we reviewed pharmacology of KBR and provide a brief summary of studies with other NCX inhibitors, such as SEA0400 (SEA) and SN‐6 (SN). Potential clinical usefulness of KBR and other NCX inhibitors is still controversial but the reviewed findings may be helpful in designing more selective and clinically useful NCX inhibitors for the treatment of cardiac, neuronal and kidney diseases.