7-(1,7-双取代-1,4-二氢-4-酮-1,8-萘啶-3-甲酰氨基)头孢菌素的合成

本文报道了以1,7-双取代-1,4-二氢-4-酮-1,8-萘啶-3-羧酸,用混合酸酐法与7-ACA,7-ADCA,7-ACT和7-ACD缩合,合成了24个1,7-双取代-1,4-二氢-4-酮-1,8-萘啶-3-甲酰胺头孢菌素衍生物,通过葡聚糖凝胶(Sephadex LH-20)及离心薄层层析纯化精制,得到纯品。体外抑菌试验结果表明:大多数新头孢菌素衍生物对革兰氏阳性菌具有较好的抗菌作用。尚有一些新头孢菌素衍生物对某些革兰氏阴性菌具有中等敏感程度。     

A new and weakly antispasmodic protoberberine alkaloid from Rhizoma Coptidis

A new protoberberine alkaloid, 3‐hydroxy‐2‐methoxy‐9,10‐methylenedioxy‐8‐oxo‐protoberberine, along with three known compounds, was isolated from Rhizoma Coptidis. The new compound displayed weak antispasmodic activity against acetylcholine‐induced contraction in isolated guinea‐pig ileum with an IC₅₀ of 83.7 μm . Copyright © 2010 John Wiley & Sons, Ltd.     

Creutzfeldt--Jakob Disease in Recipients of Human Growth Hormone in the United Kingdom: A Clinical and Radiographic Study

In the past 3 years there have been five further cases, in additionto one case reported in 1985, of Creutzfeldt-Jakob disease inrecipients of human growth hormone in the United Kingdom. Theclinical findings of two of these cases are described, demonstratinga typical presentation with a predominantly cerebellar syndromeat onset which is not commonly a presenting feature of sporadicCreutzfeldt-Jakob disease. In one case a ^99mTc hexamethylpropylenaminesingle photon emission tomographic scan showed marked impairmentof tracer uptake in the basal ganglia and cerebral cortex ata time when the clinical picture was predominantly cerebellar.This technique may be useful in early diagnosis. In the othercase post mortem examination of the brain showed prominent amyloiddeposition in the cerebellum, which has not been described previouslyin pituitary-hormone related Creutzfeldt-Jakob disease. Thepreviously published cases of growth hormone-related Creutzfeldt-Jakobdisease are reviewed and reasons for the particular clinicalpattern seen are discussed.     

Development of specific receptors for N-formylated chemotactic peptides in a human monocyte cell line stimulated with lymphokines

A human monocyte-like cell line, U937, when grown in continuous culture, does not secrete lysosomal enzymes or migrate towards chemotactic factors. When the cells are stimulated by lymphokines, however, they develop the ability both to migrate directionally and to secrete enzymes in response to several types of chemoattractants. The development, by stimulated cells, of chemotactic and secretory responses to one class of chemoattractants, the N- formylated peptides, is accompanied by the appearance on the cells of specific binding sites for these substances. Using tritiated N-formyl- methionyl-leueyl-phenylalanine (fMet-Leu-[(3)H]Phe) as a ligand, it was determined that unstimulated U937 cells possess no detectable binding sites. However, after stimulation with lymphocyte culture supernates for 24, 48, and 72 h, they developed 4,505 (+/-) 1,138, 22,150(+/-) 4,030, and 37,200 (+/-) 8,000 sites/cell, respectively. The dissociation constants for the interaction of fMet-Leu-[SH]Phe with the binding sites were approximately the same regardless of stimulation time and ranged between 15 and 30 nM. The binding of fMet-Leu-[(3)H]Phe by stimulated U937 cells was rapid and readily reversed by the addition of a large excess of unlabeled peptide. The affinity of a series of N-formylated peptides for binding to U937 cells exactly reflected the potency of the peptides in inducing lysosomal enzyme secretion and chemotaxis. The availability of a continuous human monocytic cell line that can be induced to express receptors for N-formylated peptides will provide a useful tool not only for the characterization of such receptors but also for the delineation of regulatory mechanisms involved in cellular differentiation and the chemotactic response.     

非肿瘤性肩关节损伤与人工肩关节置换

目的:分析假体的选择与手术操作技术对非肿瘤性肩关节损伤人工肩关节置换术治疗的影响。方法:选择2001-04/2006-10在上海长征医院、西藏军区总医院、扬州第一人民医院等进行肩关节置换术患者33例。肱骨急性近端粉碎性骨折28例:行单极人工肩关节置换术17例,双极人工肩关节置换术1例,全肩关节置换术3例。肱骨头缺血坏死2例、骨性关节炎3例,均行全肩关节置换术。术后9个月时22例患者参加随访,18个月时17例参加随访,30个月时5例参加随访。结果:33例患者均进入结果分析。①1例肱骨假体留置过长致肩关节上举运动痛、静止不痛,翻修术后缓解。其余32例完全不疼。②术后患者上举85°～130°,平均(98.7±6.0)°,外旋17°～36°,平均(30.0±5.7)°。内旋75°～101°,平均(82.5±4.8)°。③患者假体置位较好,除1例肱骨假体未完全插入髓腔,翻修后正常。④材料与组织的生物相容性能:符合美国FDA及欧洲CE标准。结论:针对患者的具体情况选用合适的人工肩关节假体,术中假体固定方法的选择以及术后外固定材料的佩戴对肩袖功能有重要影响。     

骨髓间充质干细胞向胰岛素分泌细胞诱导分化的动态观察

目的:探讨体外诱导骨髓间充质干细胞向胰岛素分泌细胞分化的可能性,并观察其动态变化。方法:实验于2005-09/2007-03在山东大学齐鲁医院完成。①标本来源:骨髓标本15例来自山东大学齐鲁医院成人骨髓检查结果正常者,均签署捐献同意书。②实验方法:无菌条件下取骨髓2.0～5.0mL,采用percoll分离液和贴壁法获得纯化的成人骨髓间充质干细胞。③实验评估:流式细胞仪行细胞表面抗原检测,在适当的条件下诱导其分化为成骨细胞和脂肪细胞。采用两步法向胰岛素分泌细胞诱导,观察其在碱性成纤维细胞生长因子、活化素A、胰岛素样生长因子、尼克酰胺等因子刺激下向胰岛素分泌细胞分化的动态变化。双硫踪染色鉴定胰岛样细胞团,酶联免疫吸附试验检测细胞分泌胰岛素的情况,RT-PCR检测胰岛细胞特异基因的表达。结果:①骨髓间充质干细胞的生长特性及免疫表型:分离培养获得的贴壁细胞,呈形态均一的梭形,流式细胞仪检测CD34、CD45表达阴性,CD29、CD44表达阳性。②向成骨细胞和脂肪细胞的诱导分化:此类细胞经茜素红染色、油红O染色均呈阳性,可诱导分化为成骨细胞和脂肪细胞。③向胰岛素分泌细胞的诱导分化:第1步诱导后出现细胞簇,双硫腙染色不着色,胰岛素分泌量少,仅检测到PDX-1基因的表达,证实其为胰岛前体细胞。第2步诱导后细胞簇数目逐渐上升,至诱导14d大部分细胞簇经双硫腙染色都呈红色。④诱导后培养上清中胰岛素含量:诱导第3,7,14,21天的胰岛素分泌量分别为(15.3±4.9),(34.1±5.6),(40.4±5.3),(39.8±5.1)mU/L。⑤胰岛细胞特异基因的表达:诱导7d仅检测到PDX-1基因的表达,insulin1、insulin2和Glut2基因均不表达。诱导14,21d检测到insulin2、PDX-1基因表达,insulin1基因弱表达,Glut2基因不表达。结论:体外分离、纯化得到的骨髓间充质干细胞诱导7d可分化出胰岛前体细胞,不具功能性;诱导14d后可成功地分化出成熟的具有功能性的胰岛素分泌细胞。     

国人全膝关节假体置换胫骨近端截骨面至腘血管距离的测量及意义

目的:测量国人全膝关节假体置换术胫骨近端截骨面后缘至腘窝血管之间的距离,以期为临床全膝关节置换术中避免损伤腘窝血管提供参考数据。方法:选择2006-06/12于解放军第二军医大学长征医院体检的50名正常成人(53膝),男29名(31膝),女21名(22膝)。所有观察对象均知情同意,且得到医院伦理道德委员会批准。对所有膝关节进行MRI扫描,在胫骨外侧平台以下10mm水平横断面上辨认腘动静脉,并测量胫骨近端截骨面后缘至腘窝动静脉的距离。结果:53膝全部进入结果分析,无脱落。①男性胫骨近端截骨面后缘至腘动脉、腘静脉平均距离为(6.7±2.5,7.3±2.3)mm,95%可信区间分别为5.8～7.6mm,6.5～8.1mm。②女性胫骨近端截骨面后缘至腘动脉、腘静脉平均距离为(6.6±1.9,7.1±2.7)mm,95%可信区间分别为:5.8～7.4mm,5.9～8.3mm。③不同性别观察对象胫骨近端截骨面后缘至腘血管的距离差异无显著性意义(P>0.05)。结论:腘窝血管紧邻全膝关节假体置换术胫骨近端截骨面后缘,不同性别间无明显差异。全膝关节假体置换术中进行胫骨近端截骨,特别是后方操作时需特别谨慎,以避免损伤腘窝血管。     

不同相对分子质量玻璃酸钠对膝关节镜术后关节功能恢复的作用比较

目的:观察关节腔内留置不同相对分子质量玻璃酸钠对膝关节镜术后早期疼痛及功能恢复的影响。方法:于2005-11/2006-05选择北京大学人民医院骨关节科收治的行膝关节镜手术患者60例。关节镜手术中根据不同诊断分别行半月板成形术、游离体取出术以及软骨成形术。60例患者按随机数字表法分为3个实验组,分别为Mr1.5×106～2.5×106玻璃酸钠组,Mr3×106玻璃酸钠组,Mr6×106玻璃酸钠组。术后关节腔内注入不同相对分子质量玻璃酸钠2.0～2.5mL,并被动屈伸膝关节20次,使玻璃酸钠均匀分布于关节内。术后第1天开始股四头肌力量锻炼,坐在床边屈膝活动,并可下床。术后1周拆除缝线,术后6周门诊复查。分别于术前、术后1,2,3d,1,6周采用同一评分量表进行自觉疼痛程度、日常生活活动能力、膝关节屈曲角度测评,评分越高,功能恢复越好。结果:纳入患者60例,均进入结果分析。①自觉疼痛程度测定:术后6周Mr1.5×106～2.5×106,3×106,6×106玻璃酸钠组自觉疼痛程度评分均高于术前[分别为(8.5±1.3),(7.3±2.2)分;(8.5±1.3),(7.3±2.2)分;(8.5±1.3),(7.3±2.2)分]。②日常生活活动能力测定:术后6周Mr1.5×106～2.5×106,3×106,6×106玻璃酸钠组日常生活活动能力评分均高于术前[分别为(60.5±8.4),(59.3±7.0)分;(63.4±8.2),(59.4±8.3)分;(66.9±3.8),(53.8±19.0)分]。③膝关节屈曲角度评分:术后6周Mr1.5×106～2.5×106,3×106,6×106玻璃酸钠组膝关节屈曲角度评分均高于术前[分别为(9.1±1.4),(5.8±2.7)分;(8.1±3.1),(7.2±3.5)分;(6.3±3.8),(5.5±3.1)分]。④综合评分:术后6周Mr1.5×106～2.5×106,3×106,6×106玻璃酸钠组综合评分均高于术前[分别为(88.1±7.7),(79.8±11.1)分;(91.4±6.8),(84.9±13.7)分;(91.2±10.7),(73.5±23.7)分]。关节腔内留置3种不同相对分子质量玻璃酸钠在膝关节镜术后近期各项评分差异均无显著性意义(P>0.05)。结论:关节腔内留置不同相对分子质量玻璃酸钠在膝关节镜术后近期康复中具有相似的效果。