抗肿瘤药物研究Ⅰ:去甲斑蝥素氨基酸衍生物的合成与抗癌活性

In order to search for new compounds with higher anti-cancer activities and lower toxicities, 19 amino acid derivatives of norcantharidin, of which 16 are unknown compounds, were designed and synthesized. Preliminary screening results revealed that 2-(syn-exo-7-oxabicyclo [2. 2. 1] heptane-2, 3-dicarboxylic imido)-N-phenyl glutaramic acid exhibited a fairly apparent inhibitory activity against human-hepatoma cells in vitro (inhibitory rate 39.4% at 0.025 μtmol/ml).     

A new pyeloureteral drainage catheter

We describe a new pyeloureteral drainage catheter that can be used for both genitourinary tract stenting and drainage, as well as tamponade of bleeding from the renal parenchyma or subcutaneous tissue. Primary indications for the use of this catheter and recommendations on insertion techniques are presented. With the exception of one case of minor kinking of the catheter, we have had no complications or failures with this catheter. While insertion through an unprotected tissue track is somewhat difficult, we have had good success introducing the catheter through a 24-F or larger Teflon working sheath. The catheter has excellent patient retention properties. It can be converted from external to internal drainage or vice versa simply and quickly on the ward.     

European cervical cancer screening：experiences and results

1　ＯｖｅｒｖｉｅｗｏｆｆｅｍａｌｅｍａｌｉｇｎａｎｃｉｅｓｉｎＥｕｒｏｐｅＣａｎｃｅｒｉｎｃｉｄｅｎｃｅａｎｄｍｏｒｔａｌｉｔｙｅｓｔｉｍａｔｅｓｆｏｒ 1995ｗｅｒｅｒｅｐｏｒｔｅｄｒｅｃｅｎｔｌｙｆｏｒ 38ｃｏｕｎｔｒｉｅｓｉｎＥｕｒｏｐｅ[1] .Ｔｈｅｒｅｗｅｒｅｅｓｔｉｍａｔｅｄ 2 .6ｍｉｌｌｉｏｎｎｅｗｃａｓｅｓｏｆｃａｎｃｅｒｉｎＥｕｒｏｐｅｉｎ 1995 ,ｒｅｐｒｅｓｅｎｔｉｎｇｏｖｅｒｏｎｅ ｑｕａｒｔｅｒｏｆｔｈｅｗｏｒｌｄｂｕｒｄｅｎｏｆｃａｎｃｅｒｗｈｉｌｅＥｕｒｏｐｅ’ｓｉｎｈａｂｉ…     

Temperature-dependent effects of EDTA on the membrane glycoprotein IIb- IIIa complex and platelet aggregability

In agreement with previous studies, we observed that incubation of washed human platelets with EDTA at 37 degrees C for short periods caused an irreversible loss of their aggregation response to adenosine diphosphate and markedly diminished their capacity to bind fibrinogen. AP-2 is a monoclonal antibody that reacts with a determinant specific to the glycoprotein (GP) IIb-IIIa complex. We now report that in a direct binding assay, the number of sites for AP-2 on platelets incubated with EDTA at 37 degrees C fell to approximately 30% of those present on control platelets. This effect of EDTA was not observed at room temperature. Analysis of the treated platelets by sodium dodecyl sulfate-polyacrylamide gel electrophoresis revealed normal amounts of GP IIb and GP IIIa. However, studies using crossed immunoelectrophoresis with 125I-AP-2, 125I-Tab (anti-GP IIb), or 125I- AP-3 (anti-GP IIIa) in intermediate gels showed that at 37 degrees C, EDTA was inducing an irreversible change in GP IIb-IIIa complexes. A reduction in size and probable dissociation of the GP IIb-IIIa precipitate was accompanied by the appearance of precipitates having the characteristics of those given by free GP IIb and free GP IIIa and the location of a major new cathodal precipitate, which bound Tab and AP-3 but not AP-2. Membrane modifications associated with the loss of antigenic determinants on GP IIb-IIIa may explain EDTA-induced loss of platelet aggregability at 37 degrees C.     

p53 gene mutations in multiple myeloma are associated with advanced forms of malignancy

The frequency and type of p53 gene mutations was investigated in a series of 52 cases of multiple myeloma (MM) representative of the different clinical phases and forms of the disease (indolent, 12 cases; chronic, 24 cases; acute/leukemic, 16 cases). DNAs were analyzed for p53 gene mutations in exons 5 to 9 by polymerase chain reaction (PCR), single-strand conformation polymorphism (SSCP), and direct sequencing of PCR-amplified fragments. Point mutations were detected in 7 of 52 patients (13%) (5 at exon 8; 1 at exon 6; 1 at exon 7), and were specifically associated with the more advanced and clinically aggressive acute/leukemic forms of MM (7 of 16 [43%].) Three of the mutated cases had been evaluated at clinical presentation in earlier phases of the disease (indolent or chronic) and were found to be negative for p53 mutation. Moreover, three patients with p53 mutation had not received chemotherapy at the time of investigation. These results support the notion that the development of MM is a multistep process and suggest that alterations in the p53 gene may represent an important late event in MM tumor progression.     

甲状腺相关性眼病伴眼外肌肌腱受累1例

目的：报告1例甲状腺相关性眼病的非典型CT扫描表现。方法：一位64岁的中国女性出现复视3mo,无视力模糊。14a前她曾患甲状腺功能亢进症伴多结节甲状腺肿并行甲状腺切除术。眼科检查发现双眼下斜视并向上注视受限。左眼red desaturation并Ⅰ级相对性瞳孔传入障碍。T3,T4和促甲状腺激素（thyroid stimulating hormone,TSH）正常。TSH受体、抗体水平高,与Graves＇病一致。磁共振成像（magnetic resonance imaging,MRI）显示双下直肌弥漫性增大,肌腱受累。结果：给予几周期静脉注射甲基强的松龙继之以口服强的松后视力无提高,反之继续下降。行左眼眼眶减压术,术后其左眼视力有所改善。结论：有肌腱受累的眼外肌增大不能排除甲状腺相关性眼眶病（thyroid assciated orbitopathy,TAO）的可能。