New triazole derivatives as antifungal agents: synthesis via click reaction, in vitro evaluation and molecular docking studies

A series of 1-(1H-1,2,4-triazol-1-yl)-2-(2,4-difluorophenyl)-3-substituted-2-propanols (5a-5y) which are analogues of fluconazole, have been designed and synthesized via Cu(I)-catalyzed azide-alkyne cycloaddition on the basis of computational docking experiments to the active site of the cytochrome P450 14α-demethylase (CYP51). The in vitro antifungal activities of all the target compounds were evaluated against eight human pathogenic fungi. Compound 5l showed the best antifungal activities.     

应用寡核苷酸微阵列检测肺癌样品中的P53和K-ras基因点突变

对影响寡核苷酸微阵列检测点突变的敏感性和特异性的各种因素,如杂交液,杂交温度,标记引物浓度及其比例等,进行了研究,采用不对称PCR扩增有利于敏感性提高,多重不对称PCR不影响杂交的特异性,且敏感性有所增加,对30例肺癌标本进行寡核苷酸微阵列检测,发现12例标本发生了P53基因来点突变,K-ras突变有5例,与测序结果相比,P53基因突变符合率达到80％,由于检测样本较少且检测位点不完全,因而未得到K－ras和P53基因突变与肿瘤的种类,病期及吸烟之间的明显相关性。     

Effects of Break Crops on Yield and Grain Protein Concentration of Barley in a Boreal Climate

Rotation with dicotyledonous crops to break cereal monoculture has proven to be beneficial to successive cereals. In two fields where the soil had been subjected to prolonged, continuous cereal production, two 3-year rotation trials were established. In the first year, faba bean, turnip rape and barley were grown, as first crops, in large blocks and their residues tilled into the soil after harvest. In the following year, barley, buckwheat, caraway, faba bean, hemp and white lupin were sown, as second crops, in each block and incorporated either at flowering stage (except barley) or after harvest. In the third year, barley was grown in all plots and its yield and grain protein concentration were determined. Mineral N in the plough layer was determined two months after incorporation of crops and again before sowing barley in the following year. The effect of faba bean and turnip rape on improving barley yields and grain protein concentration was still detectable two years after they were grown. The yield response of barley was not sensitive to the growth stage of second crops when they were incorporated, but was to different second crops, showing clear benefits averaging 6-7% after white lupin, faba bean and hemp but no benefit from caraway or buckwheat. The effect of increased N in the plough layer derived from rotation crops on barley yields was minor. Incorporation of plants at flowering stage slightly increased third-year barley grain protein concentration but posed a great potential for N loss compared with incorporation of crop residues after harvest, showing the value of either delayed incorporation or using catch crops.     

基于基因组技术的维生素 C 生产菌株生理功能解析与应用

维生素C是我国主要的大宗发酵产品之一,年产量占世界总产量的80%以上。二步发酵法是维生素C工业生产的主要方法,主要通过两个发酵步骤转化L-山梨糖为2-酮基-L-古龙酸。本文综述了最近几年针对维生素C二步发酵过程关键科学问题的研究进展,重点讲述了以维生素C生产菌株基因组为基础的一系列系统生物学技术在解析维生素C生产菌株生理功能及其相互作用关系的应用,同时也为如何提高其它大宗发酵产品生产效率提供了可借鉴的方法和策略。     

Predictive power of splenic thickness for post-hepatectomy liver failure in HBV-associated hepatocellular carcinoma patients

Background

The purpose of this case series is to investigate the relationship between splenic thickness (ST) and postoperative outcomes after hepatic resection in hepatitis B virus (HBV)-associated hepatocellular carcinoma (HCC) patients.

Methods

The clinical data of 320 patients with HBV-associated HCC who had undergone liver resection were retrospectively analyzed. The value of ST in predicting postoperative outcomes was evaluated.

Results

A total of 320 patients were enrolled in the study. An increase in ST was significantly associated with an increase in portal vein diameter (PVD), indocyanine green retention rate 15 min (ICG R15), and total bilirubin (TBIL); however, it was negatively correlated with platelet count (PLT). Post-hepatectomy liver failure (PHLF) occurred in 35 (10.9%) patients. Multivariate logistic regression analysis showed that ST was an independent predictor of morbidity and mortality after hepatectomy. Meanwhile, ST was associated with an almost sixfold increased risk for developing perioperative complications (OR 5.678; 95% CI 2.873 to 11.224; P?<?0.001) and almost 13-fold increased risk for mortality after hepatectomy (OR 13.007; 95% CI 1.238 to 136.627; P?=?0.033).The area under the receiver operating characteristic (ROC) curve (AUC) of ST for predicting the incidence of PHLF was 0.754 (95% confidence interval (CI) 0.667 to 0.841; P?<?0.001), with a sensitivity of 57.1% and a specificity of 82.5%, which were significantly greater than those of the ICG R15 level (AUC 0.670; 95% CI 0.560 to 0.779; P?<?0.001). The critical value of ST was 43.5 mm.

Conclusions

ST, which is an easy, inexpensive, and routinely available perioperative marker, showed a favorable predictive value for postoperative outcomes in HBV-associated HCC patients.

     

Protective Effects of Pidotimod Against Salmonella Infections

International Journal of Peptide Research and Therapeutics - Pidotimod has been shown to exhibit immunomodulatory activities and exert protective effects against bacterial infections. This study...     

脂氧素A_4对大鼠急性肝衰竭的保护作用

目的观察脂氧素A4(LXA4)对大鼠急性肝衰竭的保护作用并初步探讨其机制。方法采用D-氨基半乳糖(D-GalN)+脂多糖(LPS)建立大鼠急性肝衰竭动物模型。30只大鼠随机分为四组:正常组、模型组、脂氧素组、四氢化吡咯二硫代氨基甲酸酯(PDTC)组。肝组织病理切片观察肝组织损伤情况;自动生化仪检测肝功能;ELISA法检测血清TNF-α及IL-6水平;免疫组化法检测肝组织核因子κB(NF-κB)表达。结果大鼠急性肝衰竭时,肝组织炎症坏死明显,肝脏转氨酶明显升高,血清IL-6及TNF-α水平显著升高,肝组织NF-κB表达明显增强;脂氧素组及PDTC组组织学改变均明显好转,肝脏转氨酶、细胞因子及NF-κB表达明显下降(与模型组比较,P0.01,);脂氧素组及PDTC组比较,上述指标之间P0.01。结论 LXA4对大鼠急性肝衰竭有明显的保护作用,这种保护作用部分是通过阻断肝组织NF-κB活化,减少促炎细胞因子的释放来实现的。     

Spatial and temporal variation of atmospheric nitrogen deposition in the North China Plain

A monitoring network of nine sites was established to determine the spatial and temporal variation of atmospheric nitrogen (N) deposition in the North China Plain (NCP) over a two-year period. The annual bulk deposition of inorganic N in the North China Plain ranged from 18.4 to 38.5 kg/hm² and averaged 28.0 kg/hm². The concentration of NH₄ -N and NO₃^--N in rainwater averaged 3.76 and 1.85 mg/L, respectively, which were significantly higher than the values at background sites in China (normally less than 0.5 mg/L). Annual bulk deposition of inorganic N in the Beijing area (32.5 kg/hm²) was higher than that in Shandong and Hebei provinces (21.2 kg/hm² on an average). Also bulk N deposition was much greater in Dongbeiwang and Fangshan than in Yanqing and Shunyi counties. Significant spatial variation of bulk deposition was observed in the Beijing area because of variation of precipitation, and 60% of bulk deposition occurred from June to September. Bulk deposition of NH₄ -N was 2.0 times that of NO₃^--N deposition at the rural monitoring sites. However, the situation was reversed at the Beijing Academy of Agricultural-Forestry Sciences (BAAFS), the unique urban monitoring site. The results suggest that reduced N in precipitation is dominant in rural regions, but oxidized N is the major form in urban regions. The positive relationship between inorganic N deposition and precipitation can be fitted by a power equation (r²= 0.67), showing an increase of NH₄ -N and NO₃^--N inputs with increased precipitation. Wet deposition of N accounted for 73% of the bulk deposition, implying that dry deposition of N, particularly NH₄ -N from dust, is important in the North China Plain.