Design,synthesis and evaluation of carbamate-containing sialyltransferase inhibitors

A series of carbamate-containing sialyltransferase inhibitors were designed and synthesized to simulate phosphate-linkedCMP-Neu5Ac. Their inhibitory activities were assayed against recombinant human ST3Gal I and ST6Gal I by using the Schmidt’sHPLC-based assay. The synthetic compound 15g showed moderate inhibitory activity. These findings implied that carbamate might serve as a bioisosteric replacement for a phosphate group in sialyltransferase inhibitor design to improve the membrane permeability.     

严重创伤急救程序-时间控制模式研究

目的探讨在医院内建立严重创伤的急救程序-时间控制模式对严重创伤的救治效果。方法选取2013年1月~2013年12月期间在中山市人民医院就诊的严重创伤患者80例作为研究组,其中男性60例,女性20例;平均年龄37.8岁。致伤原因:道路交通伤58例,工程事故及高处坠落伤12例,意外伤害10例。2012年类似创伤患者64例作为对照组,其中男性48例,女性16例;平均年龄36.5岁。致伤原因:道路交通伤46例,工程事故及高处坠落10例,意外伤害8例。记录两组患者在急诊抢救室滞留时间、检查检验时间、就诊至手术时间。结果两组在性别、年龄、致伤机制及院前指数(PHI)等指标分布无统计学意义(P0.05)。急救程序-时间控制组死亡4例,死亡率为5%;对照组死亡6例,死亡率为9.37%(P0.05)。急救程序-时间控制组在急诊抢救室滞留时间、检查检验时间、就诊至手术时间较对照组明显缩短(P0.05)。结论建立严重创伤急救程序-时间控制模式可提高严重创伤的院内救治水平,规范院内救治中伤情评估、紧急手术和损害控制各环节流程,建立操作性强、效率较高的严重创伤院内救治管理模式,可显著提高救治成功率,降低死亡率。     

硝呋莫司与大鼠犬猴和人血浆蛋白结合率的测定

目的建立硝呋莫司与SD大鼠、比格犬、食蟹猴和人血浆蛋白结合率的测定方法,计算硝呋莫司与4个不同种属的血浆蛋白结合率。方法采用体外快速平衡透析法,将透析后的血浆和缓冲液分别加入对应的空白基质,用乙酸乙酯萃取后采用HPLC法测定。结果硝呋莫司在样品中的线性范围为0.1⁵μg·ml^-1,在不同血浆中的色谱方法专属性良好,提取回收率为（73.64±1.00）%^81.20±0.66%。硝呋莫司在人、犬、大鼠、猴中的血浆蛋白结合率范围为46.0%⁵8.2%、40.7%⁴2.6%、38.7%⁴3.8%、30.8%⁴2.8%。结论硝呋莫司与4种血浆蛋白的结合率中等,且在不同种属的血浆蛋白结合率随药物浓度不同存在一定种属差异。     

2型糖尿病患者血清IGF-1水平与颈动脉粥样斑块的相关性研究

目的探讨2型糖尿病(T2DM)患者血清胰岛素样生长因子-1(IGF-1)水平与双侧颈动脉粥样硬化斑块的相关性。方法应用超声检测186例患者双侧颈动脉内膜-中膜厚度,根据超声检查结果将其分为:(1)A组(颈动脉粥样硬化斑块阳性的T2DM患者)96例;(2)B组(颈动脉粥样硬化斑块阴性的T2DM患者)90例。并采用免疫放射分析法检测两组患者的血清IGF-1水平。结果 A组患者的血清IGF-1水平与B组比较显著降低,差异有显著统计学意义(P<0.01);T2DM患者血清IGF-1水平与双侧颈动脉粥样斑块的程度呈显著负相关(r=0.649,P<0.01)。结论 IGF-1参与了T2DM大血管病变的发生、发展,IGF-1水平与颈动脉粥样斑块程度密切相关。     

Retroperitoneal Bronchogenic Cyst Presenting Paraadrenal Tumor Incidentally Detected by 18F-FDG PET/CT

A follow-up ¹⁸F-fluorodeoxyglucose (¹⁸F-FDG) PET/CT scan of a 57-year-old asymptomatic male who had undergone total thyroidectomy for thyroid cancer revealed a 5.0 × 4.0-cm, well-defined, ovoid-shaped mass around the left adrenal gland without definite FDG uptake. On the adrenal CT scan, the left paraadrenal tumor showed high attenuation on the precontrast scan without enhancement. The average Hounsfield unit (HU) was 58.1 on the precontrast scan and 58.4 on the postcontrast scan. The patient underwent laparoscopic adrenalectomy for resection of the left paraadrenal tumor. The final histopathologic examination revealed a bronchogenic cyst. Although retroperitoneal bronchogenic cysts are rare, they should be considered in the differential diagnosis of retroperitoneal cystic tumors. The preoperative diagnosis is difficult, but a contrast-enhanced CT scan or ¹⁸F-FDG PET/CT scan may be useful for differentiating hyperattenuated cysts from other soft tissue masses.