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1.
外固定架在前臂严重粉碎及多段骨折中的应用   总被引:1,自引:0,他引:1  
目的:探讨应用单侧多功能外固定支架治疗前臂骨干严重粉碎性及多段骨折的临床疗效。方法:回顾性分析本院1993至2002年间收治的前臂骨干严重粉碎性及多段骨折患共22例。其中开放性骨折5例,均急诊清创复位外固定架固定;闭合性骨折17例,以切开复位单侧多功能外固定架固定结合简单内固定为主要治疗方法。运用Anderson标准进行前臂功能评价。结果:22例患中发生1例骨延迟愈合,1例骨不愈合,均经二次手术植骨后得到愈合。按Anderson标准评价,优7例,良10例,不满意3例,失败2例,优良率78%。结论:单侧多功能外固定支架在前臂尺桡骨骨干严重粉碎性及多段骨折的治疗中有独特的优势,闭合复位外固定架固定或切开复位外固定架固定结合运用简单的内固定可发挥内外固定各自长处,在取得良好固定作用的同时,减少骨折端血运的破坏,达到生物学固定的要求.  相似文献   
2.
胫骨平台骨折49例手术治疗体会   总被引:1,自引:1,他引:0  
本院自2000年1月至2005年1月共收治胫骨平台骨折病人75例,其中行手术治疗病人50例,1例病人因胫骨平台骨折和胫骨上段粉碎骨折行双钢板内固定后,膝部以下动静脉血栓大量形成.截肢治疗,故未计在内.……  相似文献   
3.
目的:制备局麻止痛膜并建立其质量控制方法。方法:以聚乙烯醇-124为基质制备局麻止痛膜,并采用高效液相色谱法测定其中主药盐酸达克罗宁的含量。结果:盐酸达克罗宁检测浓度在40.8~408μg/ml范围内与峰面积线性关系良好(r=0.9 998),平均回收率为101.3%(RSD=1.3%,n=6)。结论:局麻止痛膜的制备工艺简单,质量稳定,控制方法可行。  相似文献   
4.
目的探讨晚期非小细胞肺癌患者血中T细胞亚群、CD4+CD25+调解性T细胞(Treg)及免疫球蛋白的改变,观察康莱特注射液(KLT)联合化疗对晚期非小细胞肺癌患者免疫功能的影响。方法将68例晚期非小细胞肺癌患者随机分为2组,对照组应用多西他赛、顺铂联合化疗,不予康莱特及其他提高免疫力的治疗措施;治疗组同时给予康莱特注射液200 m L静点,连用14 d。2组均以21 d为1个周期,2个周期后评价T细胞亚群及免疫球蛋白的变化情况。另选30例健康人作为正常对照组。结果化疗前对照组及治疗组患者T细胞亚群CD3+、CD4+、CD8+比例及CD4+CD25+Treg与正常对照组比较差异有统计学意义(P均0.05)。化疗后对照组免疫球蛋白、CD3+、CD4+、CD8+、CD4+/CD8+比值及治疗组CD4+CD25+Treg与化疗前比较差异有统计学意义(P均0.05)。化疗后对照组与治疗组CD3+、CD4+、CD8+及CD4+/CD8+比值、Ig G比较差异有统计学意义(P均0.05)。结论康莱特注射液可保护晚期非小细胞肺癌患者的免疫功能,降低免疫耐受。  相似文献   
5.
Amide is a fundamental group that is present in molecular structures of all domains of organic chemistry and the construction of this motif with high atom economy is the focus of the current research. Specifically, N-methyl amides are valuable building blocks in natural products and pharmaceutical science. Due to the volatile nature of methyl amine, the generation of N-methyl amides using simple acids with high atom economy is rare. Herein, we disclose an atom economic protocol to prepare this valuable motif under DABCO/Fe3O4 cooperative catalysis. This protocol is operationally simple and compatible with a range of aliphatic and (hetero)aromatic acids with very good yields (60–99%). Moreover, the Fe3O4 can be easily recovered and high efficiency is maintained for up to ten cycles.

The generation of N-methyl amides using simple acids with high atom economy is rare owning to the volatile nature of methyl amine. Herein, an atom economic protocol was disclosed to prepare this valuable motif under DABCO/Fe3O4 cooperative catalysis.

Amide is a fundamental group that is present in molecular structures of all domains of organic chemistry.1 It is widely distributed in natural products, synthetic drugs and functional polymers, and is also the key chemical connection in proteins.2 It has been shown that amide bond formation alone accounts for 65% of all preliminary screening reactions in the pharmaceutical industry.3 This means the generation of amide bonds with high atom efficiency is of high practical importance. And not surprisingly, ‘amide formation avoiding poor atom economy reagents’ was voted as the top challenge for organic chemistry by the ACS Green Chemistry Institute in 2007.3From synthetic point of view, the ideal way to produce amide bonds would be the direct coupling of readily available carboxylic acids and amines, but this process is thermodynamically unfavourable due to the formation of the corresponding carboxylate-ammonium salt,4 therefore, stoichiometric amount of coupling reagents, such as DCC, DIC, EDCI, HATU, HBTU, HCTU, SOCl2, BOP, acid chloride etc, are generally required to sidestep thermal conditions for amide bond formation.5 These reagents are highly successful, but the process generally suffers from poor atom economy and side products removal issue especially in the large-scale applications.5 To overcome these drawbacks, “nonclassical” amide bonds formation routes were investigated.6 In these processes, the catalyst takes the role of a coupling reagent in generating an active ester suitable for amidation in a waste-free manner. However, these processes have not been applied in the preparation of N-methyl amides, probably because the methyl amine was delivered in its hydrochloride salt, alcoholic or aqueous form due to its volatile nature.On a different note, N-methyl amides are extensively presented in numerous natural products and pharmaceutical molecules, as shown in Fig. 1,7 and the methylation of amides is a promising way to improve the pharmacological property of molecules.8 However, the synthesis of N-methyl amides compounds relies heavily on non-catalytic approaches.5,9 Catalytic approaches were also investigated by Hisaeda,10 Kundu,11 Li,12 Guo,13 Yu,14 Maruoka,15 Wang,16 Chen,17 Lamaty18 and their co-workers starting from nitriles, primiary amides, aldoximes, aldehydes, lignin, carbamoylsilane and alcohols. Until recently, Thakur,19 Marce,20 Sadeghzadeh21 and their co-workers developed elegant N-methyl amidation approach starting from carboxylic acids under nano-MgO, diatomite Earth@IL/ZrCl4 and Mg(NO3)2·6H2O catalysis respectively, while limitations like poor substrate scope or sophisticated tailored catalyst still persist. Mindful of all the above issues, developing an N-methyl amidation process of simple carboxylic acids, which is still of great challenge in synthesis, and establishing a broad (hetero)aryl scope with high atom economy from commercial available reagents and catalysts were critical considerations in this study. Moreover, the significance of N-methyl amides combined with our interests in the development of green synthetic approaches motivated us to explore the direct coupling of the carboxylic acids and isothiocyanates. To the best of our knowledge, this is the first successful work using isothiocyanatomethane to prepare N-methyl amides.Open in a separate windowFig. 1Marketed drugs bearing N-methyl amide group.Our initial investigation begins with phenylacetic acid and isothiocyanatomethane as model substrate for condition optimization. Using acetonitrile as solvent, only trace amount of product was detected under catalyst free or p-toluenesulfonic acid (PTSA) catalysis conditions (
EntryAdditiveTime (h)CatalystYield (%)
1245
224PTSA
348TEA17
448DBU45
548DMAP43
648DBN51
748DABCO65
8LiBr48DABCO71
9Mn(OAc)248DABCO75
10MnO48DABCO79
11MgO48DABCO88
12Al2O348DABCO85
13Fe3O448DABCO98
14Fe3O424DABCO75
15bFe3O448DABCO80
Open in a separate windowaReactions were run on 1 mmol 1a and 1.1 mmol 2a with 10 mol% catalyst and 10 mol% additive in 1 mL of MeCN at 85 °C for 48 hours unless otherwise noted.bReaction was conducted at 60 °C.Firstly, different acids were employed to react with isothiocyanatomethane and the results were summarized in Open in a separate windowaReactions were run on 1 mmol 1 and 1.1 mmol 2 with 10 mol% DABCO and 10 mol% Fe3O4 in 1 mL of MeCN for 48 hours at 85 °C unless otherwise noted.Subsequently, aromatic and heteroaromatic acids were tested for their compatibility with current reaction conditions and the results were summarized in Fig. 1) respectively, and all could be convenient prepared using current procedure with excellent yields.Substrate scope for the amidation reactiona
Open in a separate windowaReactions were run on 1 mmol 1 and 1.1 mmol 2 with 10 mol% DABCO and 10 mol% Fe3O4 in 1 mL of MeCN for 48 hours at 85 °C unless otherwise noted.Furthermore, to demonstrate the synthetic utilization of our methodology, the preparation of bioactive compounds was demonstrated Scheme 1. Compounds 3as is a patent HDAC4 inhibitor.22 Under the standard reaction conditions, 3as could be obtained from commercial available 1as in 92% yield. Our procedure is much more atom economy as it excluded the usage of activating reagent and excess amount of base. In a recent report, Yang group reported their pilot-scale synthesis of substituted phenylacetamides to tetrahydroisoquinoline-2-ones.23 In their practice, corrosive thionyl chloride was applied as activating reagent and large excess amount of methyl amine was required, however, moderate yield of 3a was obtained, while our method can achieve better yield along with the exclusion of corrosive thionyl chloride. Following this report, tetrahydroisoquinoline-2-one 4a could be obtained in 82% yield, which could be used in the preparation of various bioactive 4-aryl-tetrahydroisoquinolines 5a with known procedure.24Open in a separate windowScheme 1Application of N-methyl amide.Finally, owing to the magnetic nature of Fe3O4, we try to recover the Fe3O4 from the reaction system and test its efficiency. As the Fe3O4 is always stick to the magnetic stir bar, after the termination of the reaction, the reaction solution was pour out and the tub along with the magnetic stir bar was rinsed with MeCN three times, oven dried and used for the next cycle. The results shown that the Fe3O4 could be used 10 times and still maintained very good efficiency (Fig. 2).Open in a separate windowFig. 2The efficiency of recovered Fe3O4.Combined with the literature reports and experimantal observation,25 a plausable mechanism was proposed in Scheme 2. Firstly, the carboxylic acid reacts with the Fe3O4 to get iron (II and III) carboxylate A, which will coordinate to the intermediate B generated from DABCO and isothiocyanate to get intermediate C. Then, one of the carboxylate attack intermediate B to release DABCO and generates intermediate D. Intermediate D go through an intramolecular addition to generate intermediate E, which go through a rearrangement reaction to get intermediate F with the release of carbonyl sulfide. Finally, the protonation of F with carboxylic acid to get the final product and regenerate the iron (II and III) carboxylate A.Open in a separate windowScheme 2Proposed reaction mechanism.  相似文献   
6.
Detection of circulating antibodies to linear peptide antigens derived from ANXA1 and DDX53 in lung cancer     
Weili Wang  Songlei Guan  Shilong Sun  Yonglong Jin  Kuang-Hui Lee  Yubing Chen  Jun Wei 《Tumour biology》2014,35(5):4901-4905
The EarlyCDT®-Lung test was the first autoantibody-based diagnostic tool for lung cancer, which was developed with a panel of recombinant protein antigens. To confirm whether the antibody test developed with linear peptide antigens has a similar power to that developed with the whole protein molecules, the present work was then undertaken to develop an in-house enzyme-linked immunosorbent assay with linear peptide antigens derived from annexin A1 (ANXA1) and DEAD box protein 53 (DDX53), which have been used to develop the EarlyCDT®-Lung test. A total of 272 patients with non-small cell lung cancer (NSCLC) and 227 control subjects matched in age and smoking history were recruited. Student’s t test showed that the levels of circulating IgG to ANXA1-derived peptide antigens were significantly higher in patients with NSCLC than control subjects (t?=?5.66, P?<?0.0001), in which the increased anti-ANXA1 IgG levels were observed only in patients at stages I, II, or III, but not in those at stage IV. However, the levels of circulating IgG to DDX53-derived peptide antigens were not significantly altered in NSCLC (t?=?1.78, P?=?0.076). Receiver operating characteristic analysis showed that the sensitivity against specificity of >90 % was 23.7 % for ANXA1 IgG assay and 13.8 % for DDX53 IgG assay. This work suggests that the linear peptide antigen derived from ANXA1 may be suitable for the development of diagnostic tool for lung cancer although further screening is needed to identify more such peptide antigens derived from tumor-associated antigens.  相似文献   
7.
紫外线减毒日本血吸虫尾蚴免疫小鼠的皮肤组织细胞反应   总被引:2,自引:0,他引:2  
吕芳丽  李雍龙  刘国元  韩家俊  石佑恩 《中国寄生虫学与寄生虫病杂志》1997,(3)
目的 :探讨紫外线减毒血吸虫尾蚴免疫宿主的皮肤组织在抗攻击感染中的作用。方法 :88只小鼠分为 4组 ,1、2组分别以 50± 3条紫外线减毒日本血吸虫尾蚴免疫或日本血吸虫尾蚴感染 ,5wk后以 10 0 0± 10 0条尾蚴进行攻击感染 ;3、4组分别以减毒尾蚴或尾蚴 10 0 0± 10 0条免疫或初次感染。各组均于感染或接种后 6- 12 0 h定时取局部皮肤组织作病理观察。结果 :( 1)免疫攻击组皮肤组织内炎症细胞杀伤童虫现象最明显、炎症反应最强且持续时间最长 ,嗜酸性粒细胞( EOS)浸润百分数最高 ;( 2 )感染攻击组呈现相似炎症反应但程度略轻 ;( 3)免疫对照组减毒童虫在皮肤内滞留时间延长 ,至 12 0 h皮下仍可见较多童虫 ;( 4 )感染对照组皮肤内的童虫数于 72 h后明显减少 ,童虫周围轻微炎症反应。电镜观察可见免疫攻击组童虫内部结构破坏 ,虫体周围 EOS、淋巴细胞增多 ,肥大细胞颗粒溶解。结论 :提示皮肤组织的细胞免疫反应在血吸虫减毒尾蚴免疫的宿主抗攻击感染保护性免疫中起重要作用。  相似文献   
8.
一氧化氮对感染日本血吸虫小鼠肝脏纤维化程度的影响   总被引:4,自引:0,他引:4  
龙小纯  刘文琪  方正明  李雍龙 《中国血吸虫病防治杂志》2004,16(4):249-252
目的 研究一氧化氮 (NO)对感染日本血吸虫小鼠早期肝脏纤维化的影响。方法  NMRI小鼠感染日本血吸虫后第 2 3天起 ,连续用诱导型一氧化氮合酶 (i NOS)的抑制剂氨基胍(Am inoguanidine,AMG)处理小鼠 ,同时设未经抑制的对照组 ,分别在感染后第 38、4 5天观察小鼠肝脏的病理变化。天狼猩红染色 -偏振光显微镜观察并结合图像分析的方法 ,分析肝脏中 、 型胶原的动态变化 ;化学显色法检测肝脏匀浆中能间接反映肝脏纤维化程度的羟脯氨酸的浓度。结果 感染后 38d,肝脏中 、 型胶原的增生程度及 、 型胶原面积比值明显高于对照组 ,但羟脯氨酸的含量与对照组相比差异无显著性 (P>0 .0 5 ) ;感染后 4 5 d,肝脏中 型胶原的增生程度和 、 型胶原面积比值明显高于对照组 ,AMG处理组中羟脯氨酸的含量较对照组高 (P<0 .0 5 )。结论  NO可抑制日本血吸虫感染小鼠肝脏早期纤维化  相似文献   
9.
Long-term follow-up and successful treatment of pulmonary alveolar proteinosis without hypercholesterolemia with statin therapy: a case report     
Shenyun Shi  Rujia Wang  Ling Chen  Yan Li  Yingwei Zhang  Xiaoyan Xin  Shangwen Yang  Yihua Wang  Yonglong Xiao  Kaifeng Xu 《The Journal of international medical research》2021,49(4)
Pulmonary alveolar proteinosis (PAP) is a rare disorder characterized by the accumulation of excessive surfactant lipids and proteins in alveolar macrophages and alveoli. Oral statin therapy is a novel treatment for PAP with hypercholesterolemia. However, this treatment has never been described in a patient without hypercholesterolemia. Here, we present a case of successful treatment with atorvastatin for a patient with possibly unclassified PAP without hypercholesterolemia who responded poorly to whole lung lavage therapy and inhaled granulocyte-macrophage colony-stimulating factor. After 18 months of atorvastatin treatment, the patient experienced improvements in dyspnea, radiographic abnormalities and pulmonary function. The present case study supports the feasibility of statin therapy for PAP regardless of the level of cholesterol.  相似文献   
10.
The serological diagnosis of human clonorchiasis by time-resolved fluoroimmunoassay based on GST2-specific IgG4 detection     
Jin Xu  Lexun Wang  Chuanhuan Deng  Xuchu Hu  Ran Li  Tingjin Chen  Dan Ning  Yingsong Wu  Yan Huang  Xuerong Li  Zhongdao Wu  Xinbing Yu  Yonglong Li 《Parasitology research》2014,113(1):149-155
Due to its delayed fluorescence of a lanthanide chelate, high accuracy and low background the broad linear range, long fluorescent life-time and large Stoke's shift of europium chelates, the time-resolved fluorescence has been developed for higher sensitive immunoassay. In this article, a simple, sensitive and specific method-time-resolved fluoroimmunoassay (TRFIA) was adopted for immunoassay of clonorchiasis, and recombinant glutathione transferases 2 of Clonorchis sinensis (rCsGST2) was used as a diagnostic antigen. To evaluate this novel assay for clinical applications, 409 serum samples were investigated. The diagnostic accuracy of the antigen was evaluated by receiver-operating characteristic (ROC) analysis. The area under the ROC curve (AUC) was 0.965, 95 % confidence interval (CI, 0.946, 0.985). To eliminate the random influence of ambient temperature, test parameters, photometric instruments and so on, the cut-off value was expressed as ratios between the fluorescence of sample and that of a well-defined negative control serum, and the deduced cut-off value was 9.3605. At the optimum cut-off criteria, the technique has a sensitivity of 95.80 %, specificity of 93.60 %. And the cross reactivity revealed that its cross reactivity with Schistosoma japonicum, round worm, hook worm, whip worm, and Toxoplasma gondii was 9.3, 8.3, 7.6, 9.8, and 5.0 %, respectively. Kappa score of agreement between TRFIA and microscopic examination of stools was 0.892, P?<?0.05. These combined results showed that our method is feasible and could be used for the clinical determination of clonorchiasis.  相似文献   
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