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.     

卵巢癌患者手术前后IL-2,sIL-2R及mIL-2R水平改变的临床意义

探讨卵巢癌患的细胞状态以及ＩＬ－２血清游离白细胞介素－２受体,外周血单个核细胞膜结构型白细胞介素－２受体与临床的关系。方法＾３Ｈ－ＴｄＲ参入法测３１例卵巢癌患ＩＬ－２产生水平,ＥＬＩＳＡ法检测血清ｓＩＬ－２Ｒ水平,ＡＰＡＡＰ免疫组化检测外周血单个核细胞膜结合型ＩＬ－２Ｒ表达细胞。     

综合医院确诊的39例肺结核患者转诊结果随访调查

目的;了解并评价综合医院内科确诊的活动性肺结核病例转诊结果。方法：对我院呼吸内科１９９５年８月－１９９８年８月确认的３９例活动性肺结核患者（不包括结核性胸膜炎）转往结构防治专业机构的结果进行信访和电话随访。结果：仍的３９例活动性肺结核患者中有３５例在确诊后１周内结核病接受０．５ａ－１ａ的全地化疗,３３例获得良好效果,２例死亡,死因分别为肺间质纤维化合并感染肺心病及呼吸衰竭。３例慢性纤维空洞型肺结核     

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.     

图像细胞分析与癌基因检测辅助诊断直肠癌

目的提高直肠癌术前活检的诊断率。方法对１７例术前活检未证实为直肠癌的患者的活检标本（实验组）和１５例正常肠粘膜活检标本（对照组）的石蜡包埋块进行常规病理检查、细胞图像分析（ＩＣＭ）、ｐ５３与ｒａｓ癌基因产物检测。结果实验组ＩＣＭ结果５３％为异倍体,癌基因检测结果ｐ５３与ｒａｓ基因表达阳性率分别为７１％、４７％。对照组的ＩＣＭ与癌基因检测结果均阴性。实验组中,常规病理检查１１例为不典型增生,５例为慢性炎症。常规病理检查为不典型增生的病例中经ＩＣＭ、癌基因检测８例为异倍体,ｐ５３与ｒａｓ基因表达阳性分别为１１和７例;慢性炎症病例中则既无异倍体,又无ｐ５３与ｒａｓ基因表达,二者之间,异倍体和两种基因表达阳性率差异均有显著意义（Ｐ＜００５）。ＩＣＭ与癌基因检测结果有较好的一致性。结论ＩＣＭ与癌基因检测,可以作为常规病理的补充,提高直肠良恶性病变的鉴别力。     

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。