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.     

Phase I-II study of gamma interferon and 5-fluorouracil for patients with metastatic renal cell carcinoma

We have completed a phase I/II trial to evaluate the toxicity and efficacy of the combination of gamma interferon and 5-fluorouracil in metastatic renal cell carcinoma. Gamma interferon was administered at a weekly dose of 100 micrograms. 5-fluorouracil was given as a 5 day continuous infusion days 1-5 of each 21 day cycle. In the phase I portion of the trial, the gamma interferon dose was held constant, while the 5-fluorouracil was escalated from 500 to 800 mg/m2/day. Serum neopterin and beta 2 microglobulin were measured prior to and 48 hours after each dose of gamma interferon for the first six weeks of treatment. Dose limiting toxicity was not encountered in the phase I part of the trial; therefore the phase II study was initiated at the 800 mg/m2/day dose of 5-fluorouracil. No responses were seen among 34 patients treated on the phase II trial. Forty-six percent of patients experienced disease stabilization and the remainder progressed through treatment. In the phase I trial, increments in neopterin and beta 2 microglobulin levels differed significantly between patients treated with lower and higher doses of 5-fluorouracil. We conclude that the addition of 5-fluorouracil to gamma interferon does not appear to enhance the cytokines clinical activity. Incremental increases in macrophage activation markers with escalating 5-fluorouracil doses suggests a role for 5-fluorouracil beyond its usual proposed cytotoxic activity and warrants further investigation into potential immunologic effects of this drug.     

Motility Disorders after Roux-en-Y Gastrojejunostomy

About 30% of patients who have a Roux-en-Y gastrojejunostomy after gastrectomy suffer from abdominal pain, nausea, vomiting of food and bloating made worse by eating. This syndrome, called the Roux stasis syndrome, is caused, in part, by a motility disorder of the Roux limb. Transection of the jejunum during the construction of the limb separates the limb from the natural small intestinal pacemaker located in the duodenum. Ectopic pacemakers then appear in the limb and trigger retrograde contractions in its proximal portion. These contractions slow transit through the limb and result in Roux stasis. Current nonsurgical treatment of the syndrome includes the use of prokinetic agents and intestinal pacing, neither of which has demonstrated long-term benefits. A near-total gastrectomy may speed upper gastrointestinal transit somewhat, but stasis in the Roux limb often persists. Our current approach aims at preventing the syndrome by the use of an ‘uncut’ Roux limb, an operation which preserves myoneural continuity between the duodenal pacemaker and the Roux limb and so prevents the appearance of ectopic pacemakers and stasis in the limb.     

《中国海洋药物》杂志刊载论文的引文分析

采用文献计量学方法,对１９８９年－１９９３年《中国海洋药物》杂志刊载论文的引文进行了分析。结果表明,此间共刊载论文１８１篇,共有引文１３０１条,每篇论文平均引文量为７．９８条。自引率为１２．７６％,在全部引文中,期刊占６５．１０％,图书占２７．６０％,其中占７．３０％;语种分布中文占６５．７２％,英文占２９．１３％,日文占５．０７％,俄文占０．０８％。１０年文献累计利用率,中文为８３．２７％,外文     

武陵地区民间146种“七”药考证与分析

为统一对民族民间“七”药的认识,解决“七”药命名中同物异名或同名异物的难题,经过多年对武陵地区“七”药的实地考察和核对有关标本,文献,考证出了该地区１４６种“七”药的名实,分析了“七”药的生态环境,基原,性味,功效及化学成分。并对“七”药的科学命名和应用开发提出了建议。     

无锡市垃圾无害化处理的卫生学评价

<正> 随着创建卫生城市的开展,垃圾处理日益受到重视,无锡市建立的垃圾处理厂,对垃圾处理采用二次发酵工艺,即“好氧堆肥发酵”、“自然堆肥贮存发酵”。现将发酵结果报道如下。1 材料与方法1.1 实验室条件下(温度26±1℃,相对湿度60％±5％)饲养家蝇1龄蛆500条,家蝇蛹500只。1.2 透气塑料筒20只(自制),编号1～20号1.3 垃圾处理厂的垃圾处理采用2次发酵,第1次机械通风好氧堆肥发酵10d,取出后入库,再第2次自然堆肥贮存发酵10d。     

Knee dislocation: treatment of high-velocity knee dislocation

BACKGROUND: We report the outcomes of patients treated with a new arthroscopic treatment modality for knee dislocation after high-velocity trauma. METHODS: Twenty-three patients (12 men, 11 women; 25 knees) with traumatic knee dislocation were treated with this technique. Under arthroscopy with gravity inflow irrigation, the ruptured posterior cruciate ligament was reconstructed with a patellar bone-tendon-bone graft, and the anterior cruciate ligament was debrided subacutely. The collateral ligament, meniscus, and capsules were repaired through additional incisions. RESULTS: The average interval between injury and surgery was 11.1+/-5 days (range, 5 to 25 days). After a mean follow-up period of 27.2+/-7.86 months, the mean extension was 1+/-2 degrees and the average flexion was 129.6+/-4.91 degrees. The mean Lysholm score was 84. There were no major complications. CONCLUSION: Arthroscopic posterior cruciate ligament reconstruction seems to be an effective treatment for traumatic knee dislocation.     

周围型肺癌阻塞性病变的CT表现

目的：确定ＣＴ 图像上周围型肺癌之肺部阻塞性病变的诊断作用。方法：１８ 例周围型肺癌和１２ 例良性肺肿块对照者均经常规ＣＴ 扫描,绝大多数病人经肿块部位及其上下一层的深呼吸时相ＣＴ 扫描。结果：周围型肺癌的肺部阻塞性病变计有肺不张、阻塞性肺炎、阻塞性肺气肿及肺静脉癌栓。结论：注重ＣＴ 图像上周围型肺癌的各种肺部阻塞性病变,可为肺癌确诊提供重要的诊断依据。     

科玛嘉培养基与沙氏培养基分离酵母菌的比较

目的应用科玛嘉显色培养基(Chromagar)对120份妇科门诊病人分泌物标本进行念珠菌的分离培养.与常用的沙氏培养基(Sabourand's Agar)比较.方法用接种环分别将标本接种于两种培养基上,37℃培养,24 h和48 h各观察一次,并记录菌落生长时间、大小及颜色.结果①科玛嘉显色培养基菌落的不同颜色可筛选出不同的念珠菌,如绿色菌落为白色念珠菌、蓝灰色菌落为热带念珠菌、粉红色菌落为克柔氏假丝酵母菌、白色菌落为其它念珠菌;②科玛嘉显色培养基菌落大小明显较沙氏培养基菌落大;③科玛嘉显色培养法具有操作简便、快速等优点.结论新培养基(科玛嘉显色培养基)在分离诊断致病性酵母菌方面优于沙氏培养基.     

Development and regulation of substance P expression in neurons of the tadpole optic tectum.

Activity-dependent synaptic plasticity is characteristic of developing visual systems. Using the frog retinotectal system, we investigated the extent to which afferent input affects neurotransmitter expression in a target structure. We have concentrated on a particular subpopulation of tectal cells that is immunoreactive to substance P (SP). Early in development, SP expression in tectal neurons was restricted to the anterior lateral region of the tectum. As tadpoles developed, this expression expanded into progressively more posterior and medial regions in a manner that closely followed the gradient of tectal maturation. At all times, however, anterior and lateral tectal regions had a greater percent of SP-like immunoreactive (SP-ir) cells than posterior and medial ones. Horseradish peroxidase (HRP) labeling of the retinal ganglion cell projection in conjunction with SP immunocytochemistry demonstrated that innervation by retinal ganglion cell terminals preceded the expression of SP by tectal cells. This suggested that the optic nerve may influence SP differentiation and/or expression. In support of this idea, transection of the optic nerve resulted in a decrease in SP expression in the deafferented tectal lobe of tadpoles. This result, opposite to that seen previously in the adult, also indicates that optic nerve-dependent regulation of SP expression in the developing and mature systems occurs through different pathways.