Pentanes

戊烷
  • 文章类型: Journal Article
    随着城市努力实现树冠覆盖率的大幅增加和人为挥发性有机化合物(AVOC)排放的减少,准确评估生物VOCs(BVOCs)对空气质量的影响变得越来越重要。在这项研究中,我们旨在量化未来城市绿化对臭氧产生的影响。密集城市地区的BVOC排放通常在区域模型中得到粗略表示。我们建立了高分辨率(30m)MEGAN(《自然》3.2版的气体和气溶胶排放模型),以估算纽约市都会区(NYC-MEGAN)的夏季生物异戊二烯排放。将受观测约束的箱模型与NYC-MEGAN异戊二烯排放耦合成功地再现了城市核心中观测到的异戊二烯浓度。然后,我们从可能的城市绿化情景中估算了未来的异戊二烯排放量,并评估了对未来臭氧生产的潜在影响。NYC-MEGAN预测,在炎热的夏季,纽约市的异戊二烯排放量是粗分辨率(1.33km)生物排放清单系统3.61版(BEIS)的两倍。我们发现BVOCs在炎热的夏季驱动臭氧产生,即使在市中心,尽管AVOC排放量很大。如果高异戊二烯排放物种(例如,橡树)种植,未来城市核心地区的异戊二烯排放量可能增加1.4-2.2倍,在当前的NOx浓度下,这将导致臭氧超标日的峰值臭氧增加8-19ppbv。我们建议在氮氧化物浓度较高的城市种植非异戊二烯或低异戊二烯排放的树木,以避免未来臭氧超标事件的频率和严重程度增加。
    As cities strive for ambitious increases in tree canopy cover and reductions in anthropogenic volatile organic compound (AVOC) emissions, accurate assessments of the impacts of biogenic VOCs (BVOCs) on air quality become more important. In this study, we aim to quantify the impact of future urban greening on ozone production. BVOC emissions in dense urban areas are often coarsely represented in regional models. We set up a high-resolution (30 m) MEGAN (The Model of Emissions of Gases and Aerosols from Nature version 3.2) to estimate summertime biogenic isoprene emissions in the New York City metro area (NYC-MEGAN). Coupling an observation-constrained box model with NYC-MEGAN isoprene emissions successfully reproduced the observed isoprene concentrations in the city core. We then estimated future isoprene emissions from likely urban greening scenarios and evaluated the potential impact on future ozone production. NYC-MEGAN predicts up to twice as much isoprene emissions in NYC as the coarse-resolution (1.33 km) Biogenic Emission Inventory System version 3.61 (BEIS) on hot summer days. We find that BVOCs drive ozone production on hot summer days, even in the city core, despite large AVOC emissions. If high isoprene emitting species (e.g., oak trees) are planted, future isoprene emissions could increase by 1.4-2.2 times in the city core, which would result in 8-19 ppbv increases in peak ozone on ozone exceedance days with current NOx concentrations. We recommend planting non- or low-isoprene emitting trees in cities with high NOx concentrations to avoid an increase in the frequency and severity of future ozone exceedance events.
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  • 文章类型: Journal Article
    及时有效的溶栓对于改善急性动脉血栓栓塞性疾病患者的预后至关重要。而常规溶栓治疗方法仍存在局限性和并发症。在这里,我们的研究试图研究一种新的双模式策略,整合超声(US)和近红外光(NIR)与建立中空介孔二氧化硅纳米探针(HMSN),其中含有精氨酸-甘氨酸-天冬氨酸(RGD)肽(血栓靶向),全氟戊烷(PFP)(具有相变和稳定空化的溶栓)和吲哚菁绿(ICG)(具有光热转化的溶栓)。HMSN作为载体,表面与靶向RGD结合以实现血栓的高靶向性和渗透性,通过加载PFP和ICG,以实现US和NIR对血栓的协同诊断和治疗。从而为动脉血栓的一体化诊治提供新的策略。从体外和体内评估来看,RGD/ICG/PFP@HMSN可聚集并穿透血栓部位,最后建立了US和NIR协同作用下的双模式定向发展和溶栓治疗,为动脉血栓的准确诊断和治疗提供有力的技术支持。
    Efficient thrombolysis in time is crucial for prognostic improvement of patients with acute arterial thromboembolic disease, while limitations and complications still exist in conventional thrombolytic treatment methods. Herein, our study sought to investigate a novel dual-mode strategy that integrated ultrasound (US) and near-infrared light (NIR) with establishment of hollow mesoporous silica nanoprobe (HMSN) which contains Arginine-glycine-aspartate (RGD) peptide (thrombus targeting), perfluoropentane (PFP) (thrombolysis with phase-change and stable cavitation) and indocyanine green (ICG) (thrombolysis with photothermal conversion). HMSN is used as the carrier, the surface is coupled with targeted RGD to achieve high targeting and permeability of thrombus, PFP and ICG are loaded to achieve the collaborative diagnosis and treatment of thrombus by US and NIR, so as to provide a new strategy for the integration of diagnosis and treatment of arterial thrombus. From the in vitro and in vivo evaluation, RGD/ICG/PFP@HMSN can aggregate and penetrate at the site of thrombus, and finally establish the dual-mode directional development and thrombolytic treatment under the synergistic effect of US and NIR, providing strong technical support for the accurate diagnosis and treatment of arterial thrombosis.
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  • 文章类型: Journal Article
    许多树木的叶子会释放出挥发性有机化合物(缩写为BVOCs),保护他们免受各种损害,如食草动物,病原体,和热应力。例如,异戊二烯是高度挥发性的并且已知增强对热应力的抗性。在这项研究中,我们分析了在叶片中生产异戊二烯以减轻损害的最佳季节时间表。我们假设光合速率,热应力,异戊二烯的压力抑制作用可能在整个季节有所不同。我们使用Pontryagin的最大原理寻求异戊二烯生产的季节性时间表,以最大程度地提高总的净光合作用。异戊二烯生产率由随时间的推移增强的叶片保护的成本和收益之间的平衡变化决定。如果热应激在盛夏达到高峰,异戊二烯产量可以在夏季达到最高水平。然而,如果在短时间内由于热应力而损失了大部分叶子,最佳时间表包括在热应力达到峰值后达到异戊二烯产量的峰值。盛夏时期较高的光合速率和较高的异戊二烯挥发性使得春季异戊二烯产量达到高峰。通过区分直接影响和未来预期的影响,可以清楚地理解这些结果。
    The leaves of many trees emit volatile organic compounds (abbreviated as BVOCs), which protect them from various damages, such as herbivory, pathogens, and heat stress. For example, isoprene is highly volatile and is known to enhance the resistance to heat stress. In this study, we analyze the optimal seasonal schedule for producing isoprene in leaves to mitigate damage. We assume that photosynthetic rate, heat stress, and the stress-suppressing effect of isoprene may vary throughout the season. We seek the seasonal schedule of isoprene production that maximizes the total net photosynthesis using Pontryagin\'s maximum principle. The isoprene production rate is determined by the changing balance between the cost and benefit of enhanced leaf protection over time. If heat stress peaks in midsummer, isoprene production can reach its highest levels during the summer. However, if a large portion of leaves is lost due to heat stress in a short period, the optimal schedule involves peaking isoprene production after the peak of heat stress. Both high photosynthetic rate and high isoprene volatility in midsummer make the peak of isoprene production in spring. These results can be clearly understood by distinguishing immediate impacts and the impacts of future expectations.
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  • 文章类型: Journal Article
    医学成像模式,如磁共振成像(MRI),超声,和荧光成像,在肿瘤诊断的临床实践中获得了广泛的认可。每种成像模式都有自己独特的原则,优势,和限制,因此,需要一种多模式方法来全面了解疾病过程。为了提高诊断精度,医生经常整合来自多种成像模式的数据,推动多模态成像技术研究的进步。
    在这项研究中,通过开环聚合制备了血卟啉-聚乳酸(HP-PLLA)聚合物,并使用FT-IR进行了全面表征,1H-NMR,XRD,和TGA。通过乳液-溶剂蒸发制备包封全氟戊烷(PFP)和水杨酸的基于HP-PLLA的纳米颗粒。使用DLS和TEM评估ζ电位和平均直径。通过细胞迁移评估生物相容性,溶血,和细胞毒性测定。超声成像是用专用设备进行的,CESTMRI使用7.0T动物扫描仪进行。
    我们设计并制备了一种新型的双模纳米成像探针SA/PFP@HP-PLLANP。PFP增强US成像,而水杨酸支持CEST成像。平均尺寸为74.43±1.12nm,多分散指数为0.175±0.015,表面ζ电位为-64.1±2.11mV。这些NP表现出优异的生物相容性和稳定性。体外和体内实验均证实了SA/PFP@HP-PLLANP提高肿瘤特征和诊断精度的能力。
    SA/PFP@HP-PLLANP展示了有希望的双模态成像功能,表明它们作为造影剂的临床前和临床应用的潜力。
    UNASSIGNED: Medical imaging modalities, such as magnetic resonance imaging (MRI), ultrasound, and fluorescence imaging, have gained widespread acceptance in clinical practice for tumor diagnosis. Each imaging modality has its own unique principles, advantages, and limitations, thus necessitating a multimodal approach for a comprehensive disease understanding of the disease process. To enhance diagnostic precision, physicians frequently integrate data from multiple imaging modalities, driving research advancements in multimodal imaging technology research.
    UNASSIGNED: In this study, hematoporphyrin-poly (lactic acid) (HP-PLLA) polymer was prepared via ring-opening polymerization and thoroughly characterized using FT-IR, 1H-NMR, XRD, and TGA. HP-PLLA based nanoparticles encapsulating perfluoropentane (PFP) and salicylic acid were prepared via emulsion-solvent evaporation. Zeta potential and mean diameter were assessed using DLS and TEM. Biocompatibility was evaluated via cell migration, hemolysis, and cytotoxicity assays. Ultrasonic imaging was performed with a dedicated apparatus, while CEST MRI was conducted using a 7.0 T animal scanner.
    UNASSIGNED: We designed and prepared a novel dual-mode nanoimaging probe SA/PFP@HP-PLLA NPs. PFP enhanced US imaging, while salicylic acid bolstered CEST imaging. With an average size of 74.43 ± 1.12 nm, a polydispersity index of 0.175 ± 0.015, and a surface zeta potential of -64.1 ± 2.11 mV. These NPs exhibit excellent biocompatibility and stability. Both in vitro and in vivo experiments confirmed the SA/PFP@HP-PLLA NP\'s ability to improve tumor characterization and diagnostic precision.
    UNASSIGNED: The SA/PFP@HP-PLLA NPs demonstrate promising dual-modality imaging capabilities, indicating their potential for preclinical and clinical use as a contrast agent.
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  • 文章类型: Journal Article
    本研究旨在扩大纳米造影剂(NCA)在肌肉骨骼系统领域的应用。它旨在介绍新颖的方法,战略,以及对缺血性肌肉疾病的临床管理的见解,包括诊断,监测,评估,和治疗干预。
    我们开发了一种复合封装技术,该技术采用O-羧甲基壳聚糖(OCMC)和脂质体来封装含NCA的金纳米棒(GNR)和全氟戊烷(PFP)。这种纳米级造影剂的基本理化性质和性能被彻底表征。其体内和体外超声成像和光热成像的能力得到了认证,除了使用后肢缺血的小鼠模型进行全面的生物相容性评估,以确定其对骨骼肌微循环灌注的影响,以及它增加血流量和促进恢复的潜力。
    工程GNR@OCMC-脂质体/PFP纳米结构的平均尺寸为203.18±1.49nm,以尺寸均匀为特征,规则的形态,和良好的生物相容性。体外评估显示NCA的有效光热响应及其在近红外(NIR)照射下转化为微泡(MBs),从而提高超声的可见度。动物研究证明了纳米结构在小鼠后肢缺血位点的光热成像中的功效,其中NIR照射引起温度快速升高并显着增加血液循环。
    双模态超声/光热NCA,将GNR和PFP封装在复合壳-核架构中,合成成功。它表现出非凡的稳定性,生物相容性,和相变效率。重要的是,它有助于PFP的封装,使增强超声成像和光热成像后的NIR曝光。这一进步为缺血性肌肉疾病的综合诊断和治疗提供了关键的一步,标志着肌肉骨骼疗法纳米医学的关键发展。
    UNASSIGNED: This study aims to broaden the application of nano-contrast agents (NCAs) within the realm of the musculoskeletal system. It aims to introduce novel methods, strategies, and insights for the clinical management of ischemic muscle disorders, encompassing diagnosis, monitoring, evaluation, and therapeutic intervention.
    UNASSIGNED: We developed a composite encapsulation technique employing O-carboxymethyl chitosan (OCMC) and liposome to encapsulate NCA-containing gold nanorods (GNRs) and perfluoropentane (PFP). This nanoscale contrast agent was thoroughly characterized for its basic physicochemical properties and performance. Its capabilities for in vivo and in vitro ultrasound imaging and photothermal imaging were authenticated, alongside a comprehensive biocompatibility assessment to ascertain its effects on microcirculatory perfusion in skeletal muscle using a murine model of hindlimb ischemia, and its potential to augment blood flow and facilitate recovery.
    UNASSIGNED: The engineered GNR@OCMC-liposome/PFP nanostructure exhibited an average size of 203.18±1.49 nm, characterized by size uniformity, regular morphology, and a good biocompatibility profile. In vitro assessments revealed NCA\'s potent photothermal response and its transformation into microbubbles (MBs) under near-infrared (NIR) irradiation, thereby enhancing ultrasonographic visibility. Animal studies demonstrated the nanostructure\'s efficacy in photothermal imaging at ischemic loci in mouse hindlimbs, where NIR irradiation induced rapid temperature increases and significantly increased blood circulation.
    UNASSIGNED: The dual-modal ultrasound/photothermal NCA, encapsulating GNR and PFP within a composite shell-core architecture, was synthesized successfully. It demonstrated exceptional stability, biocompatibility, and phase transition efficiency. Importantly, it facilitates the encapsulation of PFP, enabling both enhanced ultrasound imaging and photothermal imaging following NIR light exposure. This advancement provides a critical step towards the integrated diagnosis and treatment of ischemic muscle diseases, signifying a pivotal development in nanomedicine for musculoskeletal therapeutics.
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  • 文章类型: Journal Article
    质体2-C-甲基赤藓糖醇4-磷酸(MEP)途径提供了多种必需植物类异戊二烯的前体,但是它的规定仍然没有得到很好的理解。使用代谢控制分析(MCA),我们检查了该途径的第一个酶,1-脱氧木酮糖5-磷酸合成酶(DXS),在多个灰杨树(Populus×canescens)品系中,其DXS活性得到了修饰。在照明中用13CO2动态标记单叶,气候控制的气体交换比色皿与质子转移反应质谱仪耦合,并计算了通过MEP途径的碳通量。碳被快速同化到MEP途径中间体中,并将释放的异戊二烯和IDPDMADP池标记为90%。DXS活性在过表达DXS基因的品系中增加了25%,在RNA干扰品系中减少了50%,而MEP途径中的碳通量在过表达品系中高出25-35%,而在RNA干扰品系中没有变化。在这些不同的遗传背景下,异戊二烯的排放也没有改变。通过将绝对通量与不同光照和温度条件下的DXS活性相关联,发现通量控制系数较低。在类异戊二烯最终产品中,异戊二烯本身在DXS转基因品系中没有变化,但是在RNA干扰系中测得的叶绿素和大多数类胡萝卜素的水平比在过表达系中低20-30%。因此,我们的数据表明,散发异戊二烯的灰杨树中的DXS在控制通过MEP途径的通量中仅起着次要作用。
    The plastidic 2-C-methylerythritol 4-phosphate (MEP) pathway supplies the precursors of a large variety of essential plant isoprenoids, but its regulation is still not well understood. Using metabolic control analysis (MCA), we examined the first enzyme of this pathway, 1-deoxyxylulose 5-phosphate synthase (DXS), in multiple grey poplar (Populus × canescens) lines modified in their DXS activity. Single leaves were dynamically labeled with 13CO2 in an illuminated, climate-controlled gas exchange cuvette coupled to a proton transfer reaction mass spectrometer, and the carbon flux through the MEP pathway was calculated. Carbon was rapidly assimilated into MEP pathway intermediates and labeled both the isoprene released and the IDP+DMADP pool by up to 90%. DXS activity was increased by 25% in lines overexpressing the DXS gene and reduced by 50% in RNA interference lines, while the carbon flux in the MEP pathway was 25-35% greater in overexpressing lines and unchanged in RNA interference lines. Isoprene emission was also not altered in these different genetic backgrounds. By correlating absolute flux to DXS activity under different conditions of light and temperature, the flux control coefficient was found to be low. Among isoprenoid end products, isoprene itself was unchanged in DXS transgenic lines, but the levels of the chlorophylls and most carotenoids measured were 20-30% less in RNA interference lines than in overexpression lines. Our data thus demonstrate that DXS in the isoprene-emitting grey poplar plays only a minor part in controlling flux through the MEP pathway.
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  • 文章类型: Journal Article
    异戊二烯是由一些植物排放的,是进入大气中最丰富的生物烃。多项研究已经阐明了异戊二烯对几种环境压力的保护作用,包括高温,过多的臭氧,和食草动物攻击。然而,异戊二烯排放通过促进臭氧产生和气溶胶形成而不利地影响大气化学。因此,了解对不同环境条件下异戊二烯排放的调节,例如,二氧化碳升高,对于理解植物如何应对气候变化至关重要。异戊二烯排放量随着CO2浓度的增加而减少;然而,这种反应的潜在机制目前尚不清楚.我们证明了高CO2介导的异戊二烯排放抑制与光合作用和光强度无关,但随着温度的升高而降低。此外,我们测量了在环境和高CO2下收获的杨树叶片中的甲基赤藓糖醇4-磷酸(MEP)途径代谢物,以确定为什么在高CO2下异戊二烯排放减少。我们发现,在高CO2下,羟甲基丁烯基二磷酸(HMBDP)增加,二甲基烯丙基二磷酸(DMADP)减少。这意味着高CO2阻碍了HMBDP向DMADP的转化,可能是通过抑制HMBDP还原酶活性,导致异戊二烯排放减少。我们进一步证明,尽管这种现象似乎与脱落酸(ABA)依赖性气孔调节相似,这是不相关的,因为ABA处理没有改变升高的CO2对抑制异戊二烯排放的影响。因此,这项研究提供了一个全面的了解MEP途径和异戊二烯排放的调控面对不断增加的CO2。
    Isoprene is emitted by some plants and is the most abundant biogenic hydrocarbon entering the atmosphere. Multiple studies have elucidated protective roles of isoprene against several environmental stresses, including high temperature, excessive ozone, and herbivory attack. However, isoprene emission adversely affects atmospheric chemistry by contributing to ozone production and aerosol formation. Thus, understanding the regulation of isoprene emission in response to varying environmental conditions, for example, elevated CO2, is critical to comprehend how plants will respond to climate change. Isoprene emission decreases with increasing CO2 concentration; however, the underlying mechanism of this response is currently unknown. We demonstrated that high-CO2-mediated suppression of isoprene emission is independent of photosynthesis and light intensity, but it is reduced with increasing temperature. Furthermore, we measured methylerythritol 4-phosphate (MEP) pathway metabolites in poplar leaves harvested at ambient and high CO2 to identify why isoprene emission is reduced under high CO2. We found that hydroxymethylbutenyl diphosphate (HMBDP) was increased and dimethylallyl diphosphate (DMADP) decreased at high CO2. This implies that high CO2 impeded the conversion of HMBDP to DMADP, possibly through the inhibition of HMBDP reductase activity, resulting in reduced isoprene emission. We further demonstrated that although this phenomenon appears similar to abscisic acid (ABA)-dependent stomatal regulation, it is unrelated as ABA treatment did not alter the effect of elevated CO2 on the suppression of isoprene emission. Thus, this study provides a comprehensive understanding of the regulation of the MEP pathway and isoprene emission in the face of increasing CO2.
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  • 文章类型: Journal Article
    纤维大麻的植物化学(大麻,cv.研究了在立陶宛种植的Futura75和Felina32)。土壤特性(电导率,确定了栽培场的pH和主要元素)。通过HPLC/DAD/TOF和GC/MS技术确定了来自不同植物部位的大麻提取物和精油(EO)的化学成分。在主要选民中,β-石竹烯(≤46.64%)及其氧化物(≤14.53%),在EO中测定了α-pine烯(≤20.25%)或α-humulene(≤11.48)。大麻二酚(CBD)是大麻叶和花序甲醇提取物的挥发性成分中的主要化合物(≤64.56%)。2-单油酸甘油酯的可观数量(11.31%),在大麻籽提取物中检测到二十碳四烯酸甲酯(9.70%)和γ-谷甾醇(8.99%)。十六碳烯酸十八烯酯(≤31.27%),friedelan-3-one(≤21.49%),二氢苯并呋喃(≤17.07%)和γ-谷甾醇(14.03%)是大麻根甲醇提取物的主要成分,在不同的生长阶段收集。在戊烷中,大麻花提取物中的CBD含量最高(32.73%)。大麻酚酸(CBDA)在大麻叶提取物中的含量高达24.21%。大麻花戊烷提取物中四氢大麻酚(THC)异构体的总含量最高(≤22.43%)。总酚含量(TPC)从187.9变化到924.7(平均值,mg/L的没食子酸当量(GAE))在含水无壳大麻种子和花提取物中,分别。确定根提取物中的TPC高达321.0(mg/LGAE)。采用分光光度法DPPH●清除活性法检测大麻提取物和Eos的抗氧化活性(AA)。大麻叶EO的AA最高(从15.034到35.036mmol/L,TROLOX等效)。在根的情况下,最高的AA(1.556mmol/L,在种子成熟期收集的根提取物中发现了TROLOX)。电化学(循环和方波伏安法)测定与TPC相关。提取物的过氧化氢清除活性与TPC无关。
    The phytochemistry of fibre hemp (Cannabis sativa L., cv. Futura 75 and Felina 32) cultivated in Lithuania was investigated. The soil characteristics (conductivity, pH and major elements) of the cultivation field were determined. The chemical composition of hemp extracts and essential oils (EOs) from different plant parts was determined by the HPLC/DAD/TOF and GC/MS techniques. Among the major constituents, β-caryophyllene (≤46.64%) and its oxide (≤14.53%), α-pinene (≤20.25%) or α-humulene (≤11.48) were determined in EOs. Cannabidiol (CBD) was a predominant compound (≤64.56%) among the volatile constituents of the methanolic extracts of hemp leaves and inflorescences. Appreciable quantities of 2-monolinolein (11.31%), methyl eicosatetraenoate (9.70%) and γ-sitosterol (8.99%) were detected in hemp seed extracts. The octadecenyl ester of hexadecenoic acid (≤31.27%), friedelan-3-one (≤21.49%), dihydrobenzofuran (≤17.07%) and γ-sitosterol (14.03%) were major constituents of the methanolic extracts of hemp roots, collected during various growth stages. The CBD quantity was the highest in hemp flower extracts in pentane (32.73%). The amounts of cannabidiolic acid (CBDA) were up to 24.21% in hemp leaf extracts. The total content of tetrahydrocannabinol (THC) isomers was the highest in hemp flower pentane extracts (≤22.43%). The total phenolic content (TPC) varied from 187.9 to 924.7 (average means, mg/L of gallic acid equivalent (GAE)) in aqueous unshelled hemp seed and flower extracts, respectively. The TPC was determined to be up to 321.0 (mg/L GAE) in root extracts. The antioxidant activity (AA) of hemp extracts and Eos was tested by the spectrophotometric DPPH● scavenging activity method. The highest AA was recorded for hemp leaf EOs (from 15.034 to 35.036 mmol/L, TROLOX equivalent). In the case of roots, the highest AA (1.556 mmol/L, TROLOX) was found in the extracts of roots collected at the seed maturation stage. The electrochemical (cyclic and square wave voltammetry) assays correlated with the TPC. The hydrogen-peroxide-scavenging activity of extracts was independent of the TPC.
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  • 文章类型: Journal Article
    超过60%的蛋白质-蛋白质界面具有α-螺旋,作为这些生物分子相互作用的抑制剂的α-螺旋模拟物是普遍的治疗策略。然而,控制模拟物构象的方法,从而实现最大的功效,如骨干装订,可以是限制性的。或者,构象可以通过引入不稳定的相互作用来控制,例如顺式戊烷相互作用。这个策略,这是大自然经常采用的,不是引线优化的常见特征,大概是由于需要大量的合成努力。通过NMR和计算分析的流水线合成,我们设计了,制备并表征了交替的顺式-反配置的连续取代烃,which,通过避免正戊烷相互作用,采用明确定义的构象,以模拟α-螺旋的排列形式呈现官能团。p53模拟物的设计,以中等到良好的亲和力与Mdm2结合,证明了这些支架的治疗前景。
    With over 60 % of protein-protein interfaces featuring an α-helix, the use of α-helix mimetics as inhibitors of these interactions is a prevalent therapeutic strategy. However, methods to control the conformation of mimetics, thus enabling maximum efficacy, can be restrictive. Alternatively, conformation can be controlled through the introduction of destabilizing syn-pentane interactions. This tactic, which is often adopted by Nature, is not a common feature of lead optimization owing to the significant synthetic effort required. Through assembly-line synthesis with NMR and computational analysis, we have shown that alternating syn-anti configured contiguously substituted hydrocarbons, by avoiding syn-pentane interactions, adopt well-defined conformations that present functional groups in an arrangement that mimics the α-helix. The design of a p53 mimetic that binds to Mdm2 with moderate to good affinity, demonstrates the therapeutic promise of these scaffolds.
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  • 文章类型: Journal Article
    2019年捷克共和国发生了调味和加糖软饮料腐败的案例。喝完之后,消费者因病入院。腐败是由霉菌和有气味的物质引起的,1,3-戊二烯.食物变质的机理,随着山梨酸脱羧和霉菌生长产生的1,3-戊二烯的形成,被描述。这可能是全球报道的第二例青霉素过敏反应的病例史,解释了青霉素如何进入饮料。我们假设对青霉素或青霉霉菌产生的其他霉菌毒素的过敏反应所经历的健康问题的三个可能原因是最可能的原因。
    The case of spoilage of flavoured and sweetened soft drink occurred in the Czech Republic in 2019. After drinking it, the consumer was admitted to a hospital with sickness. The spoilage was caused by mould and an odorous substance, 1,3-pentadiene. The mechanism of food spoilage, with the formation of 1,3-pentadiene arising from the decarboxylation of sorbic acid and mould growth, is described. This could be the second case history reported worldwide of an allergic reaction to penicillin explaining how penicillin might get into the beverage. We hypothesise three possible causes of the health problem experienced with allergic reaction to penicillin or other mycotoxin produced by Penicillium mould as the most probable one.
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