摘要：高密度城市开发强度大、人口密集,建设用地与山地缺少缓冲带,山洪对生命财产的威胁日趋增大。按照韧性城市和海绵城市的建设要求,采用“渗、截、拦、蓄、用、排”的总体思路,强化山洪源头减量和蓄滞,保障山洪穿城下泄安全,构建完善的“截洪控源-过程蓄滞-下泄安全”山洪截滞系统,并与防洪排涝系统充分衔接与协调,补齐城市防洪排涝体系源头关键一环。

摘要：This paper investigates the H∞ filtering problem for a class of linear continuous-time systems with both time delay and saturation. Such systems have time delay in their state equations and saturation in their output equations, and their process and measurement noises have unknown statistical characteristics and bounded energies. Based on the Lyapunov-Krasovskii stability theorem and the linear matrix inequalities （LMIs） technique, a generalized dynamic filter architecture is proposed, and a filter design method is developed. The linear H∞ filter designed by the method can guarantee the H∞ performance. The parameters of the designed filter can be obtained by solving a kind of LMI. An illustrative example shows that the design method proposed in this paper is very effective.

摘要：According to the structure features of Fe80P20, A series of clusters Fe4P were designed and focused on studying the stability of local structure, charge distribution and chemical bond, Using the DFT method, energy and structure of Fe4P clusters were optimized and analyzed. The computational results showed that the energy of cluster 1（2） has the lowest energy, and the possibility of its existence in the Fe80P20 is high. Analyzing the transition states among the clusters, it was found that the clusters in the doublet state are more stable than those in the quartet state. The numbers of the Fe-P bond in the clusters play important roles in the cluster stability and electrons transfer properties, The more numbers of Fe-P bonds in the clusters, the higher the cluster stability, and the weaker the ability of P atom to get electron, The number of Fe atoms, which has bonding interactions with the P atom, is direct proportional to the average 3d orbit population of Fe atom. Basing on the orbital population, average magnetic moments of each Fe atom in the Fe4P clusters were calculated, and they are all smaller than that of single metal Fe atom. This suggests that all Fe4P clusters have soft magnetic property and they are expected to be perfect material for preparing soft magnetic apparatus.

摘要：材料的弹性极限是弹簧设计中极为重要的参数,对弹簧的特性有显著影响。针对直径为0.3 mm的阀门弹簧用07Cr17Ni7Al微细丝,通过室温拉伸、单臂弯曲法、光学显微镜、X射线衍射、扫描电镜研究了冷拉拔变形量对丝材强度、弹性极限、弹性后效和微观组织的影响,采用不同数学模型对变形量-马氏体含量、变形量-弹性极限、应力-弹性后效进行了分析。结果表明:固溶态07Cr17Ni7Al丝材由奥氏体和少量铁素体组成,冷拉拔使奥氏体转变为马氏体,随变形量增大,形变诱发马氏体增加。马氏体含量-冷拉等效应变关系符合Olson-Cohen模型,当冷拉等效应变达到1.64时,马氏体含量约92%,形变诱发马氏体达到饱和。丝材的抗拉强度-冷拉等效应变呈线性关系,变形量越大,抗拉强度越高。弹性极限随变形量增大而提高,弹性极限-冷拉等效应变呈“S”形曲线关系,且符合DoseResp模型,当冷拉等效应变达到1.64以上,弹性极限提高程度变小并趋于平缓。弹性后效随应力的提高而增加,符合PWL2模型,存在“弹性后效临界应力”,当应力超过该临界值后,弹性后效随应力增加的速率会提高2~11倍。冷拉等效应变为1.64~2.41时,丝材具有良好的力学性能和弹性性能。

摘要：目的分析抗肿瘤药物临床试验受试者筛选失败的原因以及纳排标准对受试者进入临床试验的影响,探讨提高受试者成功筛选入组的策略,为研究机构和申办方制定纳排标准提供参考依据。方法选取2016年1月1日—2022年6月30日中国医学科学院北京协和医学院肿瘤医院药物临床试验研究中心开展的40项药物临床试验资料,通过频数、百分构成比对收集到的受试者筛选失败数据和方案中的纳排指标进行统计描述。结果在涵盖8个瘤种的40个抗肿瘤药物临床试验项目中,筛选失败受试者425例,<65岁受试者居多(333例,78.4%),筛选失败的主要原因包括受试者自愿退出(71例,16.7%)、基因突变不符合(61例,14.3%)、肿瘤转移(52例,12.2%)、其他疾病治疗未恢复(38例,8.9%)、骨髓功能未达标(19例,4.5%)、肝功能不符合要求(15例,3.5%)。在纳排指标中,对受试者年龄(100%)、美国东部肿瘤协作组(ECOG)评分(97.5%)、骨髓功能[中性粒细胞绝对计数(ANC):95.0%、血小板计数(PLT):97.5%、血红蛋白(HB):97.5%]、肝功能[总胆红素(T-BiL):95.0%、丙氨酸氨基转移酶(ALT):87.5%、天冬氨酸氨基转移酶(AST):95.0%]、肾功能[肌酐(Cr):80.0%,以及病毒筛查(人体免疫缺陷病毒(HIV):80.0%、乙型肝炎病毒(HBV):70.0%、丙型肝炎病毒(HCV):62.5%]的要求相对严格。结论该院抗肿瘤药物临床试验中受试者筛选失败的主要原因是受试者自愿退出、肿瘤脑转移以及生化检测指标不合格,这与临床试验纳排标准的设定密切相关。深入了解受试者特征,精准设定合适纳排标准,持续改进试验设计,加强与受试者沟通,提供更多相关信息,有助于提高抗肿瘤药物临床试验筛选成功率。

摘要：Rice blast and bacterial blight are important diseases of rice(Oryza sativa)caused by the fungus Magnaporthe oryzae and the bacterium Xanthomonas oryzae ***(Xoo),*** rice varieties for broadspectrum resistance is considered the most effective and sustainable approach to controlling both *** dominant resistance genes have been extensively used in rice breeding and production,generating diseaseresistant varieties by altering susceptibility(S)genes that facilitate pathogen compatibility remains ***,using CRISPR/Cas9 technology,we generated loss-of-function mutants of the S genes Pi21 and Bsr-d1 and showed that they had increased resistance to *** also generated a knockout mutant of the S gene Xa5 that showed increased resistance to ***,a triple mutant of all three S genes had significantly enhanced resistance to both *** and ***,the triple mutant was comparable to the wild type in regard to key agronomic traits,including plant height,effective panicle number per plant,grain number per panicle,seed setting rate,and thousand-grain *** results demonstrate that the simultaneous editing of multiple S genes is a powerful strategy for generating new rice varieties with broadspectrum resistance.

摘要：We designed and synthesized a series of 2-thioxo-4-thiazolidinone derivatives and evaluated them on peroxisome proliferator activated receptor γ（PPARγ） binding *** the biological assays,compounds 18 and 38 were highlighted with K_i values of 12.15 nmol/Land 14.46 nmol/L,*** structure-activity relationship（SAR） was analyzed to screen privileged structural ***,molecular fitting of these compounds onto the approved drug Rosightazone in the PPARγligand binding domain was performed to elucidate the SAR and explore potential receptor-ligand *** results demonstrate that the 2-thioxo-4-thiazolidinones can be considered as new promising molecular probes with excellent binding activities to PPARγ.

摘要：Caspases, a family of cysteine proteases, comprise of highly homologous enzymes that play an important role in apoptotic cell death. Caspase-3 shows key functions in apoptosis, mediating apoptotic cascade from the intrinsic and extrinsic activation pathways. Therefore, caspase-3 is an attractive target for therapeutic intervention. For instance, inhibitors of caspase-3 have been described as promising cardioprotectants, neuroprotectants and antiarthritic agents. A novel peptidomimetic inhibitor of caspase-3, has been designed, which still has the properties of a reversible inhibitor, while the P1 site at the C-terminal remains, and only L-amino acid has been replaced by D-amino acid. Also presented here is the synthesis of the inhibitor and its inhibitory activity against caspase-3, which was tested by the fluorescent activity assay.

摘要：Thirteen thiomorpholine-bearing compounds were designed and synthesized as dipeptidyl peptidase IV（DPP-IV） inhibitors, with natural and non-natural L-amino acids as the starting *** structures were characterized by ~1H NMR,^（13）C NMR and *** target compounds were screened for the DPP-IV inhibition,and the preliminary SAR result was ***, compounds 4c,4d and 4f with good DPP-IV inhibition in vitro were further evaluated through a mouse oral glucose tolerance test （OGTT）.The preliminary result showed the potential value for further studies on those thiomorpholine-bearing compounds as DPP-IV inhibitors.

摘要：Hydrogen,regarded as a promising energy carrier to alleviate the current energy crisis,can be generated from hydrogen evolution reaction(HER),whereas its efficiency is impeded by the activity of ***,effective strategies,such as strain and interfacial engineering,are imposed to tune the catalysis performance of novel two-dimensional(2D)phosphorus carbide(PC)layers using first-principle *** findings show that P site in pristine monolayer PC(ML-PC)exhibits higher HER performance than C ***,constructing bilayer PC sheet(BL-PC)can change the coordinate configuration of P atom to form 3-coordination-P atom(3-co-P)and 4-coordination-P atom(4-co-P),and the original activity of 3-co-P site is higher than the 4-co-P *** an external compressive strain is applied,the activity of the 4-co-P site is enhanced whereas the external strain can barely affect that of 3-co-P ***,the graphene substrate enhances the overall activity of the BL-PC because the graphene substrate optimizes the?GH*value of 4-co-P site,although it can barely affect the HER activity of 3-co-P site and *** desirable properties render 2 D PC-based material promising candidates for HER catalysts and shed light on the wide utilization in electrocatalysis.