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…     

CT-guided stereotactic aspiration of brain abscesses

The effective treatment of intracranial abscess remains controversial. Progress in technology, linked with the development of neuronavigational systems, has made stereotactic aspiration and drainage of intracerebral abscesses effective and valid alternatives to traditional methods, namely, conservative medical treatment or open surgical excision. Between 1995 and 2002, 12 patients at our hospital underwent drainage of intracerebral abscesses under stereotactic guidance. Ten patients had solitary lesions and two had multiple abscesses. The appropriate antibiotic schemes were administered following culture of the aspirated material. The size of the abscess, the mass effect, and response to antibiotic treatment were followed up by repeated CT scans. All patients showed improvement and, at the end of treatment, returned to their previous activities. There were neither deaths nor any postoperative complication. A second aspiration was required in one patient due to recurrence of the abscess. The CT-guided stereotactic aspiration of brain abscesses helps achieve all treatment goals. It drains the contents of the abscess, reduces mass effect, and confirms diagnosis. It is minimally invasive, carries minimal morbidity and mortality, and can be performed on compromised patients under local anesthesia.     

CT-guided stereotactic aspiration of brain abscesses

The effective treatment of intracranial abscess remains controversial. Progress in technology, linked with the development of neuronavigational systems, has made stereotactic aspiration and drainage of intracerebral abscesses effective and valid alternatives to traditional methods, namely, conservative medical treatment or open surgical excision. Between 1995 and 2002, 12 patients at our hospital underwent drainage of intracerebral abscesses under stereotactic guidance. Ten patients had solitary lesions and two had multiple abscesses. The appropriate antibiotic schemes were administered following culture of the aspirated material. The size of the abscess, the mass effect, and response to antibiotic treatment were followed up by repeated CT scans. All patients showed improvement and, at the end of treatment, returned to their previous activities. There were neither deaths nor any postoperative complication. A second aspiration was required in one patient due to recurrence of the abscess. The CT-guided stereotactic aspiration of brain abscesses helps achieve all treatment goals. It drains the contents of the abscess, reduces mass effect, and confirms diagnosis. It is minimally invasive, carries minimal morbidity and mortality, and can be performed on compromised patients under local anesthesia.     

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.