Synthesis and Characterization of A Small Molecule CFTR Chloride Channel Inhibitor

A thiazolidinone CFTR inhibitor (CFTRinh-72) was synthesized by a three-step procedure with tri-fluromethylaniline as the starting material. The synthesized CFTR inhibitor was characterized structurally bymeans of ^1H NMR and functionally in a CFTR-expressing cell line FRT/hCFTR/EYFP-H148Q by both fluo-rescent and electrophysiological methods. A large amount(100g) of high-quality small molecule thiazolidi-none CFTR chloride channel inhibitor, CFTRinh-72, can be produced with this simple three-step synthetic pro-cedure. The structure of the final product 2-thioxo-3-(3-trifluromethylphenyl )-5-[4-carboxyphenyl-methylene]-4-thiazolidinone was confirmed by ^1H NMR. The overall yield was 58% with a purity over 99%as analyzed by HPLC. The synthesized CFTRinh-72 specifically inhibited CFTR chloride channel function in acell-based fluorescence assay(Kd≈1.5μmol/L) and in a Ussing chamber-based short-circuit current assay(Kd≈0. 2μmol/L), indicating better quality than that of the commercial combinatorial compound. The syn-thesized inhibitor is nontoxic to cultured cells at a high concentration and to mouse at a high dose. The syn-thetic procedure developed here can be used to produce a large amount of the high-quality CFTRinh-72 suitablefor antidiarrheal studies and for creation of cystic fibrosis models in large animals. The procedure can be usedto synthesize radiolabled CFTRinh-72 for in νiνo pharmacokinetics studies.     

椎管内巨大脊膜囊肿的诊断和治疗

目的探讨椎管内巨大脊膜囊肿的临床特征及手术疗效。方法本组收治17例椎管内巨大脊膜囊肿,男性9例,女性8例,年龄13～61岁,平均37.6岁。病程3个月～9年,平均1.7年。临床表现为胸背部、腰背部疼痛不适及下肢麻木疼痛者11例,骶尾会阴部麻木不适4例,大小便费力困难者2例。结果手术后临床症状均获得不同程度的改善,其中2例会阴部麻木不适和1例小便费力困难者改善不明显。术后随访3～38个月,平均13.4个月,未见囊肿复发。结论MRI检查对本病的诊断非常有意义。手术切除囊肿壁和封闭漏口效果确切。     

CO2激光治疗口腔粘液腺囊肿82例

用CO2 激光治疗口腔粘液腺囊肿 82例 ,有效率 10 0 % ,该疗法操作简单 ,安全 ,患者痛苦小 ,组织损伤轻。     

CO_2激光治疗粘液腺囊肿98例报告

粘液腺囊肿是口腔科常见病之一，多因损伤或反复损伤而致粘液腺排泄管阻塞。目前，该病的治疗方法可采取２％碘酊或三氯醋酸灌注，此法需反复冲洗、灌注，不仅操作繁琐，而且三氯醋腐蚀性强，易损伤正常粘膜；另外手术治疗只适应囊肿与粘膜无粘连者，不仅切除囊肿后易复发，或局部易形成疤痕，而且止血困难。笔者运用二氧化碳激光治疗，具有复发率低、无继发感染、出血少，操作简便的优点。     

CO_2激光治疗面部皮脂腺囊肿112例报告

本文报告了ＣＯ２激光治疗面部皮脂腺囊肿的方法，结果表明此法具有出血少、痛苦轻、愈合快、遗留痕迹不明显等优点。     

CO2激光散焦治疗甲状腺囊肿53例临床分析

我们应用低功率CO2激光散焦治疗甲状腺囊肿，已有二年多时间。这工作的开展是在我们用激光治疗腱鞘囊肿的基础上发展起来的。通过临床观察CO2激光能使腱鞘囊肿消失，免除手术之痛苦，而我们想到甲状囊肿切除术有三大危险：1．易出血，2．喉返神经损伤影响发音;3．甲状旁腺损伤会使病人抽搐，即使成功地摘除也难免不复发（我们的53例病人有5例手术后复发）。     

飞行人员鼻窦囊肿的诊治和医学鉴定

目的探讨飞行人员鼻窦囊肿（CNS）的发生机制、临床诊治和医学鉴定原则。方法总结飞行人员CNS资料46份,对其进行分类：结果黏膜囊肿44例,黏液囊肿和含牙囊肿各1例。上颌窦囊肿39例,蝶窦囊肿3例,筛窦囊肿、额窦囊肿、上颌窦＋额窦囊肿、上颌窦＋蝶窦囊肿各1例。Ⅰ类（地面有症状或体检时发现）37例,Ⅱ类（地面无症状,飞行中有继发性气压伤表现）9例。手术治疗16例,观察30例：飞行合格41例,永久停飞5例。结论飞行中气压变化的反复刺激可能是飞行人员CNS的发生机制之一,Ⅱ类CNS是医学停飞的重要原因。     

Natural Compound Curcumin Corrects the Gating Defect of G551DMutant Cystic Fibrosis Transmembrane Conductance Regulator

In the present study, we identified the natural compound curcumin to be an effective G551D-CFTR activator by cell-based fluorescent assay and electrophysiological measurement. We demonstrated that curcumin can restore the impaired chloride conductance of G551D mutant CFTR. The activity is rapid, reversible, and cAMP-dependent. Our study identified a new natural lead compound for the pharmacological therapy of cystic fibrosis caused by G551D mutation of CFTR.     

穿刺抽液、注药与He-Ne弱激光综合治疗耳廊假性囊肿

目的:观察穿刺抽液、注药加弱He-Ne激光局部照射综合治疗耳廓假性囊肿的疗效。方法:穿刺抽出囊液、囊腔注入去炎松后He-Ne弱激光局部照射,每日一次,每次15分钟。五天为一疗程。结果:经1～3个疗程,34例全部治愈,无一例并发感染。随访6～24个月无复发,结论:穿刺抽液、注药+弱He-Ne激光综合治疗耳廓假性囊肿,方法简单,效果好,无副作用。     

CO2激光治疗皮脂腺囊肿54例疗效总结

皮脂腺囊肿属临床常见病,过去以手术治疗为主。1988年1月至1990年4月我科应用CO_2激光治疗皮脂腺囊肿54例,疗效满意。现报告如下: