硫色满酮3位Mannich碱衍生物的合成及其抗真菌活性

目的 设计、合成硫色满酮3位Mannich碱类化合物，并对其抗真菌活性进行初步评价。方法 以对氟苯硫酚为原料，经多步反应合成目标化合物，并测定目标化合物的抗真菌活性。结果共合成了10个未见文献报道的新化合物，经红外光谱、核磁共振氟谱及元素分析确证了其结构。其中化合物3对大部分供试真菌活性强于或相当于对照品克霉唑。结论 硫色满目3位取代Mannich碱具有较强的抗真菌活性。     

Salicylate enhances necrosis and apoptosis mediated by the mitochondrial permeability transition.

Onset of the mitochondrial permeability transition (MPT) causes both necrotic and apoptotic cell death in cultured hepatocytes. Salicylate lowers the threshold for onset of the MPT. In this study, our aim was to determine whether nontoxic concentrations of salicylate potentiate MPT-mediated cell killing. In necrotic killing models to rat hepatocytes, salicylate (1 mM) enhanced calcium ionophore (Br-A23187)- and tert-butylhydroperoxide (t-BuOOH)-induced cell death, which was blocked or delayed by cyclosporin A (CsA, 2 microM), a specific inhibitor of the MPT. In hepatocyte apoptosis induced by tumor necrosis factor-alpha (TNF-alpha), salicylate accelerated cell killing after low-dose TNF-alpha (1 ng/ml), which by itself induced little apoptosis. Salicylate enhancement of apoptosis was associated with onset of the MPT and accelerated caspase 3 activation. Salicylate also augmented killing of MCF-7 human breast tumor cells by etoposide and PLC/PRF/5 human hepatoma cells by tumor necrosis factor-related apoptosis-inducing ligand (TRAIL). In conclusion, salicylate potentiates both necrotic and apoptotic cell killing by promoting onset of the MPT. Enhancement by salicylate of MPT-dependent apoptosis may play a role in protection by aspirin and other nonsteroidal anti-inflammatory drugs against colon, lung, and breast cancer.     

去窦弓神经大鼠的心血管及肾脏的形态学改变(英文)

目的　研究去窦弓神经 (SAD)对正常血压大鼠的血流动力学及心、肾、血管等器官病理形态学的影响。方法　采用SD大鼠施行SAD手术 ,术后 18周行股动脉插管 ,在清醒、自由活动状态下计算机实时记录 2 4h动脉收缩压、舒张压和心率 ,并计算血压波动性 (BPV)和心率波动性 (HRV)。处死动物后 ,取心、脑、肾及脾观察大体及光学显微镜下结构变化。结果　SAD术后 18周 ,SAD大鼠的血压和心率水平与假手术组相比无显著差异 ,但 2 4hBPV明显高于假手术组 ,HRV明显低于假手术组 ;大鼠心、肾及血管有明显的类似于高血压靶器官损伤的病理改变。结论　SAD可使大鼠的心、肾和血管发生类似于高血压靶器官损伤的病理改变。     

宫颈癌患者外周血Th1/Th2细胞因子表达水平的研究

目的 :分析 2 7例宫颈癌患者外周血单个核细胞 (PBMC)中Th1/Th2 两类细胞因子的表达水平 ,并与正常人比较 ,了解宫颈癌患者的免疫漂移现象。方法 :利用RT PCR技术检测 2 7例宫颈癌患者PBMC中Th1/Th2 两类细胞因子的mRNA表达水平。结果 :2 7例宫颈癌中IFN γ、IL 2、IL 4、IL 6和IL 10的表达阳性率依次为2 /2 7、3 /2 7、18/2 7、14 /2 7和 18/2 7。结论 :宫颈癌患者高表达Th2 类细胞因子 ,低表达Th1类细胞因子 ,出现典型的Th2 漂移现象 ,为宫颈癌的生物治疗提供可能。     

检测食管癌标本中PCNA和p16及Ki-67的临床意义

对西京医院进行根治性放疗的食管鳞状细胞癌患者 64例 ,照射剂量DT64～ 70Gy ,进行前瞻性研究 ,对其治疗前活检标本进行SP免疫组化染色 ,计数其阳性细胞数 ,并计算阳性率 ,观察其阳性率与食管癌放疗疗效及预后的关系。结果PCNA阳性率 5 1%～ 67 1% ,中央值 3 2 0 % ,PCNA阳性率 >40 %者较低于此值者预后明显差。p16在低分化癌中较高分化癌阳性表达率低 ,且随着病期的进展阳性表达率降低 ,P <0 0 5 ;Ki 67与近期疗效及预后未见明显差异。初步研究结果提示 ,PCNA阳性率是判断放疗疗效有意义的指标 ,且与p16联合检测对食管鳞癌放疗前恶性程度评定和预后估计有重要意义     

Clinical analysis of 276 cases of non-palpable TO breast cancer

Objective Discussion of diagnosis, treatment and prognosis of non-palpable TO breast cancer. Methods Between 1978 and 1997, 9,980 female patients with operable breast cancer were treated surgically, of which 276 were determined to have TO breast cancer. Most TO breast cancers could be detected promptly with careful examination of presenting symptoms, such as nipple discharge, local thickening of the breast, nipple erosion, nipple retraction and postmenopausal mastalgia, while 12 cases were detected by routine mammography of the contralateral breast. Results All patients were treated surgically and their tissue subjected to histopathological examination. Most cases (73.0%) were noninvasive or early invasive carcinoma. Axillary lymph nodes metastases were found in 7.69% of 234 mastectomy cases. Conclusion The survival rate was significantly increased if the tumor was in an early stage. The 5-, 10-, 15-years survival rates were 98.1%, 94.6% and 90.3%, respectively.     

抗癌作用新靶点及其抑制剂的研究进展

针对靶点分子或某种发生发展机制来设计抗肿瘤药物的研究工作已取得了相当大的成就.这类药物的特异性强,疗效显著,因此,针对这些新靶点进行药物设计可以使抗肿瘤药物的研究产生一次新的革命.本综述旨在讨论目前抗肿瘤药物研究的潜在的新靶点以及它们相应的抑制剂或拮抗剂.     

高效液相色谱法测定维生素E烟酸酯胶囊的含量

目的:采用高效液相色谱法测定维生素E烟酸酯胶囊的含量。方法:以Phenomenex Luna C18(250 mm×4.6 mm,5 μm)柱为分析柱,甲醇-0.01％三氟醋酸乙腈(80:20)为流动相,流速1.5 mL·min～1,检测波长264 nm。结果:维生素E烟酸酯在84-839 μg·mL-1范围内峰面积与浓度线性关系良好(r=1.000);平均回收率为100.4％,RSD<1％。结论:本方法准确、简便、快速,适用于测定维生素E烟酸酯胶囊的含量。     

卵巢上皮性癌155例的治疗与预后

目的：探讨卵巢上皮性癌的治疗与影响预后的因素。方法：对１９７０年１月至１９９２年１２月在我院治疗的１５５例卵巢上皮性癌进行回顾性分析。全部手术切除标本经病理检查诊断并按ＦＩＧＯ分期标准进行分期，４２例行２次手术，４例行３次手术。除６例外，余１４９例均于手术后行化疗，３２例于第２次术后再次行化疗，９例因复发再次化疗。结果：２年、５年、１０年的生存率分别为Ⅰ期９２．４％、８７．０％、７０．６％；Ⅱ期９１．９％、６３．６％、４７．８％；Ⅲ期５９．９％、３８．２％、１９．２％；Ⅳ期２５．０％、２５．０％、０．０％（Ｐ＜０．００１）。６例未化疗者均在术后２年内死亡。结果表明，预后与临床分期、细胞分化、残留癌灶大小有关。５年生存率中，Ⅰ期为８７．０％和Ⅲ期为３８．２％（Ｐ＜０．００１）；Ｇ１的５年生存率为９５．９％，Ｇ３为１１．８％（Ｐ＜０．００１）；无残留癌灶者为９７．６％，残留癌灶＞２ｃｍ者为２１．２％（Ｐ＜０．００１）。结论：在卵巢上皮性癌初次手术时残留癌灶＜２ｃｍ，并于术后尽早开始化疗，可提高生存率。     

骨髓基质细胞与玻璃陶瓷复合培养体内成骨的实验研究

目的 观察骨髓基质细胞（BMSC）与钙磷陶瓷（BGC）复合后形成骨组织的生物学机制,为形成组织工程化新生骨组织提供理论依据。方法 将BMSC与BGC复合植入动物体内后进行大体观察、组织学染色,观察其成骨过程。结果 一定浓度的BMSC与BGC复合植入动物体内可产生成熟新生骨组织,其成骨过程与局部血运、材料孔隙、孔径有关。结论 利用组织工程学方法可以形成新生骨组织,为进一步研究组织工程化新生组织的体内移植手段和方法提供了新的思路和可能。