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.     

抑那通在前列腺癌内分泌治疗中的临床意义

目的为提高晚期前列腺癌内分泌治疗效果,１９９０年７月～１９９２年７月间对１７例前列腺癌患者进行了抑那通（药物除睾）的临床观察。方法随访３～５年获得可评价资料１６例病例,采用免疫酶联法测定ＰＳＡ变化,放免法检测性激素水平,用Ｉ－ＰＳＳ表调查排尿及生活质量,对前列腺及转移病灶、全身状况的变化进行对比观察。结果抑那通治疗后睾酮降至去势水平（Ｐ＜０．０１）,前列腺特异抗原及其他肿瘤标记物提示反应性良好,症状及全身状况明显改善。结论每月注射一次抑那通,如果与抗男性素剂联合使用可获得更安全有效的治疗效果。     

Epidemiological characteristics of uveitis in Switzerland

Since January 1990, data from uveitis patients have been systematically stored in a computer data bank. During the period from January 1990 to March 1993, 435 new patients (185 female and 250 male, mean age 43 years; range 6–92) were seen at the Uveitis Clinic of the Hopital Jules Gonin. These 435 patients (630 eyes) were subdivided into anterior uveitis (268 patients — 62%), intermediate uveitis (47 patients — 11%), posterior uveitis (89 patients — 20%) and panuveitis (31 patients — 7%). The incidence of uveitis for the referral area considered was calculated to be 17 per 100,000 inhabitants per year. A specifie diagnosis was found in 312 cases (72%). The most frequently diagnosed entities were HLA-B27-associated acute anterior uveitis (67 cases — 15.4%), uveitis associated with acute herpes zoster ophthalmicus (40 cases — 9.2%), toxoplasmosis (39 cases — 9%), typical pars planitis (29 cases — 6.7%), sarcoidosis (29 cases — 6.7%), Fuchs' heterochromic cyclitis (27 cases — 6.2%), herpetic anterior uveitis (21 cases — 4.8%) and acute retinal necrosis (11 cases — 2.5%). Incidence and distribution of most disease entities correspond to those of other European series.     

电教多媒体数据库管理系统的设计

目的：设计研制一个面向院校电教中心的多媒体数据库管理系统,以便用现代信息技术管理电教中心众多的信息资料。方法：在国产MIS开发平台Multibase2．0上,用原型法进行无编程设计开发。结果：制作的数据库管理系统运行稳定,操作方便,维护简单,查询功能新颖而强大,基本功能设计具有较强的针对性,能够满足电教中心日常工作的需要。结论：采用国产无编程MIS开发平台Multibase完全可以开发出实用的多媒体数据库管理系统,本数据库管理系统可向军内外院校推广使用。     

侧柏叶乙酸乙酯提取物对豚鼠离体气管平滑肌的作用

用离体豚鼠气管条,探讨侧柏叶乙酸乙酯提取物对气管平滑肌作用。结果表明,侧柏叶乙酸乙酯提取物能抑制乙酰胆碱,氯化钾所致气管平滑肌收缩,而且能使乙酰胆碱收缩气管平没肌的量效曲线右移,并抑制最大效应,其作用为剂量依赖性心肌肥厚提示侧柏叶乙酸乙酯提取物松驰气管平滑肌作用机制可能与影响Ｃａ＾２＋的跨膜转运有关。     

NADPH-diaphorase-containing neurons in cortex, subcortical white matter and neostriatum are selectively spared in Alzheimer's disease

To investigate the involvement of NADPH-diaphorase (NADPH-d)-containing neurons in Alzheimer's disease (AD), NADPH-d enzyme histochemistry in vibratome sections was applied to the superior frontal and superior temporal cortex and the neostriatum in 5 AD and 6 aged control brains. Overall there was a neuronal loss and atrophy in the cortex of AD. Despite slight morphological neuronal changes in the cortex of AD, we found no significant difference in the number of NADPH-d-positive neurons in both cortex and neostriatum between control and AD cases. These results provide further evidence for a selective preservation of NADPH-d neurons in AD. In order to check whether nNOS-immunoreactive neurons are identical to NADPH-d-positive neurons in the human brain, we examined the frontal and temporal cortex and neostriatum of normal human brains in serial cryostat sections. We found that nNOS-containing neurons paralleled NADPH-d-positive neurons in these brain regions. Copyrightz1999S.KargerAG,Basel     

环维黄杨星D对实验性脑缺血的保护作用

目的：探讨环维黄杨星D(Cycloirobuxiure D，CVB-D)对大鼠局灶性脑缺血再灌注损伤及PC12细胞缺氧性损伤的保护作用。方法：采用线栓法制成局灶性脑缺血再灌注大鼠模型和连二亚硫酸钠(Na2S2O4)引起的PC12细胞缺氧损伤模型，探讨CVB-D对模型大鼠神经行为、脑梗塞范围、脑含水量、脑指数的影响，以及其对PC12细胞缺氧样损伤的保护作用。结果：CVB-D能降低模型大鼠神经行为学评分、脑梗塞率、脑指数、脑含水量，抑制Na2S2O4造成的PC12细胞缺氧样损伤，降低LDH的漏出，增加细胞存活率。结论：CVB-D对实验性脑缺血有保护作用。     

先天性多脏器缺如及发育不全1例报告

1临床资料患儿,男,1d,因生后腹胀不排气排便20h,于2002年2月9日3pm入院。体检:T36.5℃,R45次/min,P160次/min,面色灰暗,发育及营养差,反应弱,呈嗜睡状。胸廓无畸形,左肺呼吸音粗糙,右肺呼吸音低。心率160次/min,律齐,各瓣膜区未闻及杂音。腹部膨隆,未见肠型及蠕动波,全腹有压痛,肝脾均未触及,下腹部叩诊浊音,肠鸣音弱。肛门外观正常。肛诊:进入4cm后为盲端,不能插入细肛管,无胎便,仅有少量白色粘液。实验室检查:血WBC25.0×109/L,N0.75,L0.25,Hb182g/L,RBC5.70×1012/L。B超:腹腔内有大片液性暗区,内有散在斑点及斑片状强回声,肠管内…     

短音诱发听性脑干反应的特性观察

目的 了解短音（tone pip）诱发的听性脑干反应（TP－ABR）的特征及其各频率反应阈与纯音听阈的关系。方法 对正常听力青年人30耳分别采用短声（click）、短音（0.5、1、2、4、6、8kHz）测试，记录各自不同强度下ABR的波形，观察V波潜伏期的改变。结果 tone pip与常规click声诱发的ABR极为相似，均有很高的可重复性和可靠性；ABR反应阈均较其主观听阈高，尤其是频率越低，反应阈越高，低频个体差异较大；随频率（0.5-8kHz）和强度（40－120dB peSPL）增加Ⅰ波Ⅴ潜伏期递减；各频率的反应阈与音听阈均有较好的相关性。结论 短音刺激记录的TP－ABR具有频率特性，其反应阈在相应频率的客观听力评估中有应用价值。