Design, synthesis and biological evaluation of novel amino acid ureido derivatives as aminopeptidase N/CD13 inhibitors

A series of amino acid ureido derivatives as aminopeptidase N (APN/CD13) inhibitors were synthesized and evaluated for their APN inhibitory activities and anti-cancer effects. The results showed that most of these amino acid ureido derivatives exhibited good inhibition against APN, several of which were better than Bestatin. The most active compound 12j (IC(50) = 1.1 μM, compared with Bestatin IC(50) = 8.1 μM) not only possessed much better APN inhibitory activity and anti-proliferation effect on cancer cells, but also exhibited significant block effect of human cancer cell invasion compared with the positive control, Bestatin. These amino acid ureido derivatives could be possibly developed as new APN inhibitors for cancer chemotherapy in the future.     

硝尔库勒湖可培养放线菌多样性及其功能酶和抗细菌活性

【目的】认识和了解硝尔库勒湖可培养放线菌的多样性、功能酶和抗细菌活性特点,为今后的开发和利用奠定基础。【方法】应用可培养技术和基于16S r RNA基因序列的系统发育分析硝尔库勒盐湖沉积物中放线菌的多样性。常规方法检测样品成分因子,并筛选了嗜盐放线菌的蛋白酶、淀粉酶和酯酶活性;抑菌圈法检测放线菌新种的抗细菌活性。【结果】分离获得了51个OTUs,分属于24个不同的属,其中15个OTUs代表了放线菌新种;链霉菌属是优势菌属,占全部分离菌株数量的16.25%。硝尔库勒湖放线菌类群数量一定程度上受样品成分因子的协同影响。代表新种的菌株展示了良好的功能酶活性和抗细菌活性,其中代表链霉菌新种的菌株XHU5011不仅具有多种酶活性,而且具有强大的抗金黄葡萄球菌、耻垢分枝杆菌和荧光假单胞菌的能力,具有很好的开发潜能。【结论】硝尔库勒盐湖中存在丰富的可培养放线菌多样性,潜藏着大量的放线菌新资源,并且具有很好的功能酶和天然产物挖掘潜力。     

基于MSAP和SSR标记的高粱甲基化连锁群LGC、LGD的构建

以高粱(Sorghum bicolor(L.)Moench)品种‘B_2V_4’和‘1383-2’杂交获得的F_2群体为材料,通过SSR和MSAP标记检测高粱基因组差异,构建其甲基化遗传连锁群。结果显示,高粱甲基化连锁群LGC含有3个SSR标记和23个甲基化标记,覆盖高粱基因组44.3 cM;甲基化连锁群LGD含有4个SSR标记和8个甲基化标记,覆盖高粱基因组46.2 cM。LGC上甲基化位点仅来源于EcoRⅠ/MspⅠ酶切组合,而LGD上有来源于EcoRⅠ/MspⅠ和EcoRⅠ/HpaⅡ两种酶切组合的甲基化位点。在LGC连锁群Xtxp 69附近检测到一个密集的甲基化位点区域。研究结果表明MSAP标记可以快速检测植物基因组甲基化差异,适用于构建甲基化连锁群。     

PAC对谷子花后土壤氮素供应和叶片抗氧化特性的影响

全基施肥方式会造成作物全生育期内营养供应失衡,导致生育后期缺氮早衰。为探究聚天门冬氨酸和壳聚糖复配剂(PAC)保障谷子(Setariaitalica)花后氮素供应和调控叶片抗氧化特性的机制,建立全基施肥背景下东北春谷防衰增产的生产技术,于2020–2021年在中国农业科学院作物科学研究所公主岭试验站开展大田试验,以谷子品种张杂谷13号和华优谷9号为材料,设置常规氮素(CN)和PAC配合氮素(PN) 6个氮素水平(0、75、112.5、150、225和337.5 kg·hm^–2)播种前进行全基施肥处理。结果表明,与常规氮肥处理相比,相同施氮量下,PAC处理后,两品种谷子花期和灌浆中期0–20cm和20–40 cm土层土壤硝态氮和铵态氮含量升高,花后叶面积显著增大,叶面积降幅减小;花后0–40天旗叶超氧化物歧化酶、过氧化物酶及过氧化氢酶活性升高,丙二醛含量降低。因此, PAC有效保障了谷子生育中、后期土壤氮素的供应,提高了叶片抗氧化能力,延缓了叶片衰老进程,进而提高产量。2020年和2021年Z13的增产幅度分别为11.24%–21.55%和8.65%–14.22%,...     

Hyposensitive canopy conductance renders ecosystems vulnerable to meteorological droughts

Increased meteorological drought intensity with rising atmospheric demand for water (hereafter vapor pressure deficit [VPD]) increases the risk of tree mortality and ecosystem dysfunction worldwide. Ecosystem-scale water-use strategy is increasingly recognized as a key factor in regulating drought-related ecosystem responses. However, the link between water-use strategy and ecosystem vulnerability to meteorological droughts is poorly established. Using the global flux observations, historic hydroclimatic data, remote-sensing products, and plant functional-trait archive, we identified potentially vulnerable ecosystems, examining how ecosystem water-use strategy, quantified by the percentage bias (δ) of the empirical canopy conductance sensitivity to VPD relative to the theoretical value, mediated ecosystem responses to droughts. We found that prevailing soil water availability substantially impacted δ in dryland regions where ecosystems with insufficient soil moisture usually showed conservative water-use strategy, while ecosystems in humid regions exhibited more pronounced climatic adaptability. Hyposensitive and hypersensitive ecosystems, classified based on δ falling below or above the theoretical sensitivity, respectively, achieved similar net ecosystem productivity during droughts, employing different structural and functional strategies. However, hyposensitive ecosystems, risking their hydraulic system with a permissive water-use strategy, were unable to recover from droughts as quickly as hypersensitive ones. Our findings highlight that processed-based models predicting current functions and future performance of vegetation should account for the greater vulnerability of hyposensitive ecosystems to intensifying atmospheric and soil droughts.     

Improved Tandem All‐Polymer Solar Cells Performance by Using Spectrally Matched Subcells

All‐polymer solar cells (all‐PSCs) are attractive as alternatives to fabricate thermally and mechanically stable solar cells, especially with recent improvements in their power conversion efficiency (PCE). In this work, efficient all‐PSCs with near‐infrared response (up to 850 nm) are developed using newly designed regioregular polymer donors with relatively narrow optical gap. These all‐PSCs systems achieve PCEs up to 6.0% after incorporating fluorine into the polymer backbone. More importantly, these polymers exhibit absorbance that is complementary to previously reported wide bandgap polymer donors. Thus, the superior properties of the newly designed polymers afford opportunities to fabricate the first spectrally matched all‐polymer tandem solar cells with high performance. A PCE of 8.3% is then demonstrated which is the highest efficiency so far for all‐polymer tandem solar cells. The design of narrow bandgap polymers provides new directions to enhance the PCE of emerging single‐junction and tandem all polymer solar cells.     

SiO2‐Enhanced Structural Stability and Strong Adhesion with a New Binder of Konjac Glucomannan Enables Stable Cycling of Silicon Anodes for Lithium‐Ion Batteries

Silicon‐based anodes with high theoretical capacity have intriguing potential applications for next‐generation high‐energy lithium‐ion batteries, but suffer from huge volumetric change that causes pulverization of electrodes. Rational design and construction of effective electrode structures combined with versatile binders remain a significant challenge. Here, a unique natural binder of konjac glucomannan (KGM) is developed and an amorphous protective layer of SiO₂ is fabricated on the surface of Si nanoparticles (Si@SiO₂) to enhance the adhesion. Benefiting from a plethora of hydroxyl groups, the KGM binder with inherently high adhesion and superior mechanical properties provides abundant contact sites to active materials. Molecular mechanics simulations and experimental results demonstrate that the enhanced adhesion between KGM and Si@SiO₂ can bond the particles tightly to form a robust electrode. In addition to bridging KGM molecules, the SiO₂‐functionalized surface may serve as a buffer layer to alleviate the stresses of Si nanoparticles resulting from the volume change. The as‐fabricated KGM/Si@SiO₂ electrode exhibits outstanding structural stability upon long‐term cycles. A highly reversible capacity of 1278 mAh g^?1 can be achieved over 1000 cycles at a current density of 2 A g^?1, and the capacity decay is as small as 0.056% per cycle.     

Peptide MSI-1 inhibited MCR-1 and regulated outer membrane vesicles to combat immune evasion of Escherichia coli

Polymyxin resistance is conferred by MCR-1 (mobile colistin resistance 1)-induced lipopolysaccharide (LPS) modification of G⁻ bacteria. However, the peptide MSI-1 exerts potent antimicrobial activity against mcr-1-carrying bacteria. To further investigate the potential role of MCR-1 in improving bacterial virulence and facilitating immune evasion, and the immunomodulatory effect of peptide MSI-1, we first explored outer membrane vesicle (OMV) alterations of mcr-1-carrying bacteria in the presence and absence of sub-MIC MSI-1, and host immune activation during bacterial infection and OMV stimulation. Our results demonstrated that LPS remodelling induced by MCR-1 negatively affected OMV formation and protein cargo by E. coli. In addition, MCR-1 diminished LPS-stimulated pyroptosis but facilitated mitochondrial dysfunction, further aggravating apoptosis in macrophages induced by OMVs of E. coli. Similarly, TLR4-mediated NF-κB activation was markedly alleviated once LPS was modified by MCR-1. However, peptide MSI-1 at the sub-MIC level inhibited the expression of MCR-1, further partly rescuing OMV alteration and attenuation of immune responses in the presence of MCR-1 during both infection and OMV stimulation, which can be exploited for anti-infective therapy.