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.     

大理地区正常人血清TT_3、TT_4水平

对比大理地区健康汉族人与白族人血清总三碘甲状腺原氨酸（ＴＴ３）、总甲状腺素（ＴＴ４）含量,建立本地区健康人ＴＴ３、ＴＴ４正常参考值。方法：对１００７例健康人（汉族６９１例,白族３１６例）进行血清ＴＴ３、ＴＴ４、ＲＩＡ检测。结果：健康汉族人与白族人血清ＴＴ３、ＴＴ４测定值相近,经统计学处理无显著性差异（Ｐ＞００５）;６０～７５岁年龄组的健康老年人血清ＴＴ３、ＴＴ４含量比其他年龄组明显降低（Ｐ＜００１）。结论：经检测得出的各年龄ＴＴ３、ＴＴ４水平,不论白族或汉族,男性或女性,均可作为正常参考值;６０岁以上健康老人ＴＴ３、ＴＴ４含量低于其他年龄是老年人正常的生理变化。     

D-amphetamine-induced depletion of energy and dopamine in the rat striatum is attenuated by nicotinamide pretreatment

The present study examined the effects of nicotinamide on the D-amphetamine (AMPH)-induced dopamine (DA) depletion and energy metabolism change in the rat striatum. In chronic studies, co-administration of AMPH with desipramine, a drug that retards the metabolism of AMPH, (10 mg/kg, intraperitoneal [i.p.], respectively) caused a significant decrease of striatal DA content measured 7 days later. Pretreatment with nicotinamide (500 mg/kg, i.p.), the precursor molecule for the electron carrier molecule nicotinamide adenine dinucleotide (NAD), attenuated this effect of AMPH, whereas itself exerted no long-term effect on striatal DA content. In acute studies, a decrease in striatal adenosine triphospate/adenosine diphosphate (ATP/ADP) ratio was found 3 h after co-injection of AMPH and desipramine. However, nicotinamide pretreatment blocked the reduced striatal ATP/ADP ratio and resulted in a striking increase in striatal NAD content in AMPH-treated rats. Furthermore, nicotinamide was noted to increase striatal ATP/ADP ratio and NAD content in saline-treated rats. These findings suggest that nicotinamide protects against AMPH-induced DAergic neurotoxicity in the striatum of rats via energy supplement.     

两种LASIK微型角膜刀的临床应用探讨

目的　比较ＫＮ－ ５０００ 型微型角膜刀与Ｍｏｒｉａ 微型角膜刀在ＬＡＳＩＫ 术中制作角膜瓣时的优缺点。方法　选用连续病例５６ 例１０３ 眼,随机分ＫＮ 组和Ｍｏｒｉａ 组,ＫＮ 组２８ 例５３眼,术前近视度数平均为－ ９－２１±７－４１Ｄ,散光≤－５－００Ｄ,Ｍｏｒｉａ 组２８ 人５０ 眼,术前近视度数平均为－１０－４７±３－７３Ｄ,散光≤－２－５０Ｄ,术中分别用ＫＮ－５０００ 微型角膜刀和Ｍｏｒｉａ 微型角膜刀制作角膜瓣。结果　两组病例角膜瓣边缘整齐。基质面：ＫＮ组全部术眼光滑、规则,Ｍｏｒｉａ 组部分术眼有“搓衣板”现象。瓣异常：ＫＮ组游离瓣２ 眼,Ｍｏｒｉａ 组不全瓣５ 眼。ＫＮ组角膜瓣质量优于Ｍｏｒｉａ 组,瓣异常率低于Ｍｏｒｉａ 组。结论　ＫＮ－ ５０００ 微型角膜刀在ＬＡＳＩＫ术中制瓣时性能及安全性、稳定性优于Ｍｏｒｉａ 组微型角膜刀。ＫＮ－ ５０００ 微型角膜刀还具有良好的易学性和进行ＬＡＳＩＫ角膜板层移植的功能。     

腹腔镜与腹腔镜辅助乙状结肠代阴道术治疗MRKH综合征

目的 :总结使用全腹腔镜和腹腔镜辅助下乙状结肠阴道成形术各成功治疗1例Mayer Rokitansky Kuster Hauser综合征 (MRKH综合征 )的经验。方法 :全腹腔镜下使用腔镜闭合切割器切断乙状结肠的近端和远端。自肛门插入腔内圆型吻合器 ,将降结肠与直肠吻合。经会阴于尿道膀胱与直肠之间造穴。将带血管蒂的乙状结肠牵入穴道 ,完成阴道成形。腹腔镜辅助下阴道成形中 ,腔镜闭合切割器切断乙状结肠的远端后 ,于左下腹壁做一辅助切口 ,将近端乙状结肠经此切口拉出至腹腔外。切断乙状结肠近端 ,将乙状结肠的远端开口缝合 2层 ,使之成盲端。近侧端开口置入吻合器之钉钻 ,再行荷包缝合送回腹腔 ,用吻合器行肠吻合。其余步骤同全腹腔镜手术步骤。术后根据临床检查或磁共振成像测量新成形阴道的长度和宽度。结果 :全腹腔镜手术新成形的阴道长 18cm ,宽 4cm。腹腔镜辅助手术新形成的阴道长 19cm ,宽 4cm。两例新形成的阴道黏膜湿润 ,呈粉红色。无术中和术后并发症的发生。结论 :经腹腔镜乙状结肠移植段的长度完全能达到开腹手术的要求。与开放手术比较 ,全腹腔镜乙状结肠代阴道手术在腹壁上不留手术瘢痕 ,美容效果理想。而腹腔镜辅助下阴道成形 ,虽腹壁留有小手术疤痕 ,但操作简便 ,手术时间短 ,手术费用低     

1314例育龄妇女缺铁性贫血发病现状调查

目的 :研究育龄妇女缺铁性贫血 (IDA)的发病现状及营养状况与IDA的关系。方法 :检测青岛市城市及农村 1314例妊娠期和非妊娠期育龄妇女的外周血红蛋白浓度 (Hb)、平均红细胞体积 (MCV)、平均红细胞血红蛋白量 (MCH)、血清铁蛋白 (SF) ,并进行个人问卷调查 ,应用营养计算软件评价膳食营养。结果 :1314例育龄妇女IDA发病率为 2 0 .4 0 % ,其中非孕妇的发病率高于孕妇。农村育龄妇女的发病率明显高于城市。孕妇中孕≥ 2 8周组发病率最高 (4 0 % ) ,与其他孕周组相比差异有高度显著性 (P <0 .0 1)。营养评价结果显示非孕妇组热量、维生素A、E、B1、B2 、PP、C的缺乏率高于孕妇组(P <0 .0 0 1)。结论 :农村育龄妇女及孕 2 8周以上的孕妇为IDA高发人群。应加强对农村育龄妇女的膳食营养宣教及指导 ,对孕晚期的孕妇及时采取有针对性的干预措施。