Screening and identification of 3-aryl-quinolin-2-one derivatives as antiviral agents against influenza A

Quinolin-2-one represents an important and valuable chemical motif that possesses a wide variety of biological activities; however, the anti-influenza activities of quinolin-2-one-containing compounds were rarely reported. Herein, we describe the screening and identification of 3-aryl-quinolin-2-one derivatives as a novel class of antiviral agents. The 3-aryl-quinolinone derivatives were synthesized via an efficient copper-catalyzed reaction cascade that we previously developed. Using this synthetic method, preliminary structure–activity relationships of this scaffold against the influenza A virus infection were systematically explored. The most potent compound 34 displayed IC₅₀ values of 2.14 and 4.88 μM against the replication of H3N2 (A/HK/8/68) and H1N1 (A/WSN/33) strains, respectively, without apparent cytotoxicity on MDCK cells. We further demonstrated that 27 and 34 potently inhibited the plaque formation of the IAV, rendering this scaffold attractive for pursuing novel anti-influenza agents.     

检测Ⅳ型胶原蛋白直接双抗夹心法的建立与评价

目的 :建立血清 型胶原蛋白 (COL - )浓度测定的直接双抗夹心法 ,为临床诊断肝纤维化提供一种新的指标。方法 :采用本科室自制的 COL - 单克隆酶标抗体、多克隆抗体建立的直接双抗夹心法 ,同时采用日本试剂盒测定 6 0份正常和肝脏病人血清 COL- 浓度做对照比较。结果 :两种方法无显著性差异 (P>0 .0 5 ,t=0 .16 6 ) ;两法相关分析 ,γ=0 .834,回归方程为 Y=0 .5 9X+ 70 .874。结论 :直接双抗夹心法测定血清 COL- 操作简便、特异、准确 ,可作为辅助诊断肝纤维化的可靠指标 ,并可在临床推广应用     

复杂原发性视网膜脱离的综合疗法

目的：探讨综合疗法对原发性视网膜脱离的手术效果及并发症。方法：采用环扎巩膜外势压及眼内注气等综合疗法。结果：治疗成功率由８５％提高到９０％。结论：综合疗法治疗原发性视网膜脱离是一种行之有效的方法。     

肾性骨病的骨膜下骨吸收

笔者采用手骨直接Ｘ线放大摄影和双手Ｘ线平片来研究慢性肾衰血透病人５１例。特征性的指骨骨膜下吸收放大摄影发现２５例占４９％;平片为１１例占２１．６％,结果表明,放大摄影的阳性率明显高于平片（Ｐ＜０．００５）,骨膜下吸收的二,三指中间指骨桡侧及指骨末端是肾性骨病的“靶区”,认为二者无显著差异（Ｐ＞０．５０）。骨膜下吸收还与血透时间,血磷,血钙和碱性磷酸酶水平相关。     

高晶体-高胶体渗透压溶液对受机械性损伤的海马神经细胞容积的影响

观察机械性损伤的海马神经细胞在不同浓度高晶体－ 高胶体渗透压溶液中容积的变化。取原代培养大白鼠胚胎的海马神经细胞,用超声波机械损伤细胞后暴露于含０．５ ｇ／Ｌ、１ ｇ／Ｌ和２．５ ｇ／Ｌ氯化钠的细胞培养基中１５ ｍ ｉｎ。结果显示机械性损伤的细胞明显肿胀（Ｐ＜ ０．０５）。当细胞暴露于不同浓度的高晶体－ 高胶体溶液１５ ｍ ｉｎ 后, 细胞容积与同一实验时间的对照值相比明显下降, 并保持至第７ ｄ （Ｐ＜ ０．０５）。表明受到机械性损伤的海马神经细胞在高晶体－ 高胶体渗透压环境中的容积调节功能丧失或减弱。     

动力加压髁螺钉治疗股骨髁部骨折临床与实验研究

本研究结合１４例股骨髁间、髁上骨折以动力加压髁螺钉（Ｄynamic Ｃondylar Ｓcrew ＤＣＳ）固定。目的：为临床提供应用ＤＣＳ的实验数据。方法：采用成人新鲜尸体股骨髁部标本,按照ＡＯ/ＡＳＩＦ分类,模拟Ｙ形骨折模型,以ＤＣＳ固定,置于ＷＤ－１０Ｅ万能电子力学实验机上其抗拉伸、抗扭转、抗村缩、抗剪切强度。结果：ＤＣＳ有较好的固定强度。临床应用１４例,随访６个月至１年,优良率为８５．７１％。结论：ＤＣＳ适合于     

涎腺腺样囊性癌CKs及MSA免疫组化观察

目的：应用一组抗体探讨涎腺腺样性癌（ＡＣＣ）的免疫组化特征。方法：通过ＡＢＣ免疫组化染色检测了３０例涎腺ＡＣＣ中５４Ｋｄ及６６／５７Ｋｄ细胞角蛋白（ＣＫｓ）的分布。结果：ＡＣＣ基本上由５４Ｋｄ阳性细胞和ＭＳＡ阳性细胞构成,这两类细胞不同比例的肿瘤性增生形成ＡＣＣ的不同组织学构型。结论：ＡＣＣ免疫组化表型与正常省腺组织中的导管／腺泡单位的表型特征相似。     

不同底物对HUVEC在血管内支架上粘附生长的影响

目的研究不同底物对人脐静脉内皮细胞（ＨＵＶＥＣ）在支架上粘附及生长的影响。方法：分别用Ｆｉｂｒｉｎｅｃｔｉｎ、ｐｏｌｙＬｌｙｓｉｎｅ处理血管内支架后将其置入ＨＵＶＥＣ悬液,定时旋转血管内支架,使内皮细胞在支架上充分粘附。比较ＨＵＶＥＣ在底物处理的支架与裸支架上粘附率及生长状况的差异。结果：ＨＵＶＥＣ在裸支架、ｐｏｌｙＬｌｙｓｉｎｅ及Ｆｉｂｒｉｎｅｃｔｉｎ处理血管内支架上的粘附率分别为１９．９２％、３９．８２％、６４．９％,３者比较有统计学上的差异;ＨＵＶＥＣ在Ｆｉｂｒｉｎｅｃｔｉｎ处理的支架上的生长状况也优于其它两种情况。结论：底物Ｆｉｂｒｉｎｅｃｔｉｎ和ｐｏｌｙＬｌｙｓｉｎｅ处理能提高内皮细胞在支架上的粘附率。     

显性遗传性运动感觉性神经病Ⅱ型一个家系分析

目的本文报道一个在老年期发病的遗传性运动感觉性周围神经病Ⅱ型家族。方法对家族成员进行临床和电生理检查,其中１例病人进行腓肠神经活检。结果家族成员在老年期出现四肢无力和感觉减退。老年病人和无症状年轻病人的电生理检查均发现周围神经的诱发电位波幅显著下降。腓肠神经活检证实轴索性周围神经病。结论检查结果符合显性遗传性运动感觉性周围神经病Ⅱ型的诊断,电生理检查可以发现家族中的亚临床病人。     

Dose effects of flaxseed and its lignan on N-methyl-N-nitrosourea-induced mammary tumorigenesis in rats

Dietary supplementation with flaxseed or its lignan secoisolariciresinol diglycoside (SDG) has reduced dimethylbenz[a]anthracene-induced mammary tumor size and number in rats. The objective of this study was to determine whether flaxseed has a dose-dependent effect on N-methyl-N-nitrosourea (MNU)-induced mammary tumor promotion and whether this effect can be attributed to its SDG. Two days after injection with MNU (50 mg/kg body wt i.p.), female Sprague-Dawley rats were fed a high-fat (20% soybean oil) AIN-93G basal diet alone (BD) or supplemented with flaxseed (2.5% F and 5% F) or SDG by gavage [SDG in 2.5% F (LSDG) and SDG in 5% F (HSDG)] for 22 weeks. Although tumors tended to be smallest in the 5% F group throughout the experimental period, flaxseed feeding did not significantly affect tumor size, multiplicity, or incidence in comparison to BD. However, there was a dose-dependent effect of SDG on tumor multiplicity. Tumor multiplicity was lowest in the HSDG group and highest in the LSDG group throughout treatment (p < 0.05), indicating that HSDG inhibited, whereas LSDG promoted, MNU-induced mammary tumor development. Tumor invasiveness and grade were decreased in all treatment groups compared with the BD (p < 0.032). Thus, although flaxseed feeding had no significant effect on tumor growth indexes, flaxseed and SDG treatment, regardless of dose, appeared to delay the progression of MNU-induced mammary tumorigenesis. Disparities between this study and previous studies on flaxseed may be related to differences in experimental design, the use and dose of a different carcinogen, and protective effects by the alpha-linolenic acid present in the BD.