A multi pathway coupled domino strategy: I2/TBHP-promoted synthesis of imidazopyridines and thiazoles via sp3, sp2 and sp C–H functionalization

I₂/TBHP-promoted, one-pot, multi pathway synthesis of imidazopyridines and thiazoles has been achieved through readily available ethylarenes, ethylenearenes and ethynearenes. I₂/TBHP as an initiator and oxidant is used to realize the C–H functionalization of this domino reaction. Simple and available starting materials, wide range of functional group tolerance, high potential for drug activity of the products and application in production are the advantageous features of this method.

One-pot, multi-pathway, and atom economic synthesis of imidazoles and thiazoles has been achieved. In the catalytic system, I₂/TBHP as an initiator and oxidant is used to realize sp³, sp² and sp C–H functionalization.     

类风镇痛Ⅰ号治疗类风湿性关节炎的临床研究

目的:观察中药类风镇痛Ⅰ号冲剂治疗类风湿性关节炎的临床疗效,从免疫学方向探讨中西医结合治疗类风湿性关节炎的作用机制.方法:将70例类风湿性关节炎患者随机分为治疗组(类风镇痛Ⅰ号与常规西药联用)36例,对照组(单纯西药)34例,治疗2个月后比较两组临床疗效以及主要症状、体征的变化,检测常规类风湿性关节炎临床指标、免疫球蛋白、淋巴细胞因子如白细胞介素-6及其受体(IL-6、IL-6R)、IL-8和肿瘤坏死因子-α(TNF-α)水平的变化.结果:治疗组主要症状与体征的改善及疗效的总有效率均明显优于对照组(P<0.05或P<0.01),免疫球蛋白IgG、血沉、IL-8和TNF-α下降幅度也明显大于对照组(P<0.05或P<0.01).结论:类风镇痛Ⅰ号能提高类风湿性关节炎的临床疗效,减少西药的不良反应,具有调节机体免疫功能,改善类风湿性关节炎免疫损伤等多种综合效应.     

Disclosing the Hidden Structure and Underlying Mutational Mechanism of a Novel Type of Duplication CNV Responsible for Hereditary Multiple Osteochondromas

The additional mutational complexity associated with copy number variation (CNV) can provide important clues as to the underlying mechanisms of CNV formation. Correct annotation of the additional mutational complexity is, however, a prerequisite for establishing the mutational mechanism. We illustrate this point through the characterization of a novel ～230 kb EXT1 duplication CNV causing autosomal dominant hereditary multiple osteochondromas. Whole‐genome sequencing initially identified the CNV as having a 22‐bp insertion at the breakpoint junction and, unprecedentedly, multiple breakpoint‐flanking micromutations on both sides of the duplication. Further investigation revealed that this genomic rearrangement had a duplication‐inverted triplication–duplication structure, the inverted triplication being a 41‐bp sequence synthesized from a nearby template. This permitted the identification of the sequence determinants of both the initiation (an inverted Alu repeat) and termination (a triplex‐forming sequence) of break‐induced replication and suggested a possible model for the repair of replication‐associated double‐strand breaks.     

Different doses of partial liver irradiation promotes hepatic regeneration in rat

The aim of this study is to investigate whether partial liver irradiation promotes hepatic regeneration in rat. Left-half liver of rat was irradiated to 10 Gy, and the Right-half to 0, 5, 10 and 15 Gy, respectively. Then, serum alanine aminotransferase (ALT), aspartate aminotransferase (AST) and alkaline phosphatase (ALP) levels were evaluated on 0 day, 15-day, 30-day, 45-day and 60-day after liver irradiation. Next, the serum HGF, NF-κB and TGF-β1 levels were also analyzed on 60-day after liver irradiation. Lastly, the cyclinD1 protein expression was appraised by western blots on 60-day after liver irradiation. ALT, AST and ALP levels were reduced compared with that of controls. The serum HGF, NF-κB and TGF-β1 levels, and the cyclinD1 protein expression in liver irradiation group were increased compared with that of controls group. However, hepatic regeneration of higher dose-irradiated cirrhotic liver was triggered a more enhanced regeneration, compared with that of higher doses group. In summary, these results suggest that different doses of partial liver irradiation promotes hepatic regeneration in rat.     

Identification of differentially expressed proteins in human stage I lung adenocarcinoma and tumor-adjacent tissues with two-dimension gel electrophoresis profiling

Objective： The aim of this study was to establish reproducible two-dimensional electrophoretic assay used for profiling and identification of differentially expressed proteins in human stage I lung adenocarcinoma and paired normal tumor-adjacent tissue. Methods： The proteins from 12 human stage I lung adenocarcinoma tissues and normal tumor-adjacent tissues were separated using isoelectric focusing electrophoresis （the first dimension） and the subsequent homogeneous SDS-polyacrylamide gel electrophoresis （SDS-PAGE） （the second dimension）. The differentially expressed proteins were determined with PDQuest image analysis software, and identified using matrix-assisted laser desorption/ionization time of flight mass spectrometry （MALDI-TOF-MS） and database searching. Results： The well-reproducible 2-DE gel patterns of human stage I lung adenocarcinoma and normal tumor-adjacent tissues were profiled and 26 differentially expressed proteins uncovered. Nine of these 26 protein spots were cut out from the preparation gels and determined with MALDI-TOF-MS. Searching against the protein database, four candidate proteins were identified. They were 60S acidic ribosomal protein P2, Cathepsin B1, Apolipoprotein A-I precursor, and La 4.1 protein. Conclusion： In this study, high reproducible 2-DE gel protein images of human stage I lung adenocarcinoma and paired normal tumor-adjacent tissues were achieved successfully, and 4 differentially expressed proteins were revealed. These data will be helpful for screen of early biomarker and study of molecular mechanisms of human lung adenocarcinoma.     

中医各家学说课程新诠释

中医各家学说课程的定义、定位及其与中医经典理论的关系,以及中医各家学说的地位、现状、学习研究的意义等,学术界一直有争议。以中医经典著作为支撑的中医理论形成之后,关键就是如何灵活应用其性理论解决临床实际问题,而历代名医就是活用理论的成功典范,是“知常达变”的集中代表。因而,中医各家学说具有与中医经典课程同样重要的地位,应当引起中医教育工作者足够的重视。     

伴门静脉癌栓的原发性肝癌外科治疗：附335例报告

目的：探讨合并门静脉癌栓（PVTT）的肝癌手术治疗的指征与价值。方法：回顾性分析335例伴PVTT肝癌患者临床病理及随访资料,其中273例行手术治疗,包括规则性或非规则性肝切除术（HR）+PVTT清除术（HR组）,62例采用肝动脉化疗栓塞（TACE）治疗（TACE组）。比较两组患者治疗后的生存情况。结果：HR组及TACE组中位生存期分别为4.46个月和5.65个月,差异无统计学意义（P=0.455）;6、12个月生存率分别为30.7%,38.7%与12.1%、19.2%,差异均无统计学意义（均P>0.05）。结论：肝癌合并PVTT不是手术禁忌证,实施HR安全可行,但预后改善不明显,故要遵循个体化标准,慎重选择手术治疗。随着肝癌多学科协作（MDT）治疗及未来精准医学治疗模式的发展,以期能提高其整体治疗水平。

     

骨质疏松症骨折愈合的电子显微镜观察

本文对骨质疏松症患者股骨粗隆间骨折愈合前后,骨折部位的标本作电子显微镜观察,看到在其愈合过程中,早期的组织细胞学变化与普通的骨折愈合无明显差异。在后期,骨质疏松症患者的巨噬细胞破骨活动明显较强,吸收与破坏已形成的胶原纤维,使钙盐沉积受阻,愈合骨的强度下降。这一现象提示,对骨质疏松症骨折愈合缺陷的治疗,也许主要应集中在骨折愈合后期,设法抑制巨噬细胞破骨细胞的活性,保护已形成纤维结构,促进钙盐沉积,顺利完成模造。     

伊木萨克片对糖尿病性ED大鼠阴茎组织中eNoS和nNoS的影响

目的 研究维药伊木萨克片对DM性ED大鼠阴茎海绵体组织中eNOS和nNOS蛋白表达水平的影响.方法 取雄性SD大鼠70只,从中随机取10只为正常对照组,余60只以链脲佐菌素诱导建立DM模型后,行阿朴吗啡阴茎勃起实验筛选DM性ED模型,发生ED者随机分为DM性ED组、伊木萨克片组、胰岛素组、伊木萨克片 胰岛素(联用)组,未成DM者为STZ组.各组给药6周后,采用免疫组化SP法检测各组大鼠阴茎组织中eNOS、nNOS含量.结果 DM性ED组大鼠阴茎组织中eNOS、nNOS蛋白表达水平显著低于正常对照组(P＜0.01);伊木萨克片组、胰岛素组及联用组大鼠阴茎组织中eNOS、nNOS蛋白表达水平均显著高于DM性ED组(P＜0.01),但伊木萨克片组与胰岛素组显著低于联用组(P＜0.01, P＜0.01;P＜0.05,P＜0.01);STZ组与正常对照组之间的差异则无统计学意义(P＞0.05).结论 维药伊木萨克片可以显著提高DM性ED大鼠阴茎组织中eNOS、nNOS蛋白表达水平,并提示在胰岛素控制血糖的基础上效果可能更佳.