transport capacity

  • 文章类型: Journal Article
    一些糖苷药物可以通过肠道葡萄糖转运蛋白(IGT)转运。口服药物制剂中使用的表面活性剂可以影响转运蛋白的功能。本研究旨在探讨常用表面活性剂的作用,泊洛沙姆188和吐温80,对IGTs的药物转运能力的影响。先前的研究表明天麻素是IGT的最佳药物底物。以天麻素作为探针药物,通过药代动力学和原位单次灌肠评价这两种表面活性剂对SD大鼠肠道吸收的影响。然后,使用RT-PCR和蛋白质印迹法检查了两种表面活性剂对葡萄糖转运蛋白和紧密连接蛋白表达的影响。此外,通过苏木精-伊红染色评价表面活性剂对肠道通透性的影响.结果发现,所有实验为泊洛沙姆188(0.5%,2.0%和8.0%)和Tween80(0.1%和2.0%)与空白组没有显着差异。然而,当使用0.5%吐温80时,天麻素的AUC(0-∞)增加约32%。IGT表达的变化与天麻素的肠道吸收有关。在0.5%Tween80时观察到IGT的表达显著增加。总之,泊洛沙姆188在推荐的使用范围内对IGT的药物转运能力影响最小。然而,0.5%吐温80后,IGTs的表达增加,显著增强了IGTs的药物转运能力。然而,0.1%和2.0%吐温80均无显著影响。
    Some glycoside drugs can be transported through intestinal glucose transporters (IGTs). The surfactants used in oral drug preparations can affect the function of transporter proteins. This study aimed to investigate the effect of commonly used surfactants, Poloxamer 188 and Tween 80, on the drug transport capacity of IGTs. Previous studies have shown that gastrodin is the optimal drug substrate for IGTs. Gastrodin was used as a probe drug to evaluate the effect of these two surfactants on intestinal absorption in SD rats through pharmacokinetic and in situ single-pass intestinal perfusion. Then, the effects of the two surfactants on the expression of glucose transporters and tight-junction proteins were examined using RT-PCR and western blotting. Additionally, the effect of surfactants on intestinal permeability was evaluated through hematoxylin-eosin staining. The results found that all experimental for Poloxamer 188 (0.5%, 2.0% and 8.0%) and Tween 80 (0.1% and 2.0%) were not significantly different from those of the blank group. However, the AUC(0-∞) of gastrodin increased by approximately 32% when 0.5% Tween 80 was used. The changes in IGT expression correlated with the intestinal absorption of gastrodin. A significant increase in the expression of IGTs was observed at 0.5% Tween 80. In conclusion, Poloxamer 188 had minimal effect on the drug transport capacity of IGTs within the recommended limits of use. However, the expression of IGTs increased in response to 0.5% Tween 80, which significantly enhanced the drug transport capacity of IGTs. However, 0.1% and 2.0% Tween 80 had no significant effect.
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  • 文章类型: Journal Article
    为了避免冬季不利条件对植物发育的负面影响,温带树木进入休眠期,称为休眠期。冬季休眠是一个复杂的过程,涉及多个信号通路,先前的研究表明,细胞之间以及芽和树枝之间的转运能力可能会在整个休眠期调节进程。然而,在果树中,参与这种调节的动力学和分子参与者仍然描述得很差。
    这里,为了验证运输能力调节果树休眠进程的假设,我们结合了生理,成像和转录组学方法来表征甜樱桃(PrunusaviumL.)花芽休眠期间的分子途径和转运能力。
    我们的结果表明,在休眠期间,运输能力降低,并且可能受到环境信号的调节。此外,我们证明,休眠释放与运输能力的恢复并不同步,而是发生在芽在温度升高的影响下能够生长时。我们强调了休眠期间与转运能力有关的关键基因。
    根据在六个冬季进行的长期观察,我们提出了关于转运能力的环境和分子调控的假设,与甜樱桃的休眠和恢复生长有关。
    UNASSIGNED: To avoid the negative impacts of winter unfavorable conditions for plant development, temperate trees enter a rest period called dormancy. Winter dormancy is a complex process that involves multiple signaling pathways and previous studies have suggested that transport capacity between cells and between the buds and the twig may regulate the progression throughout dormancy stages. However, the dynamics and molecular actors involved in this regulation are still poorly described in fruit trees.
    UNASSIGNED: Here, in order to validate the hypothesis that transport capacity regulates dormancy progression in fruit trees, we combined physiological, imaging and transcriptomic approaches to characterize molecular pathways and transport capacity during dormancy in sweet cherry (Prunus avium L.) flower buds.
    UNASSIGNED: Our results show that transport capacity is reduced during dormancy and could be regulated by environmental signals. Moreover, we demonstrate that dormancy release is not synchronized with the transport capacity resumption but occurs when the bud is capable of growth under the influence of warmer temperatures. We highlight key genes involved in transport capacity during dormancy.
    UNASSIGNED: Based on long-term observations conducted during six winter seasons, we propose hypotheses on the environmental and molecular regulation of transport capacity, in relation to dormancy and growth resumption in sweet cherry.
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  • 文章类型: Journal Article
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  • 文章类型: Journal Article
    使用肠道葡萄糖转运蛋白(IGT)设计口服药物递送系统可能是提高药物口服生物利用度的策略之一。然而,对影响IGT药物转运能力的生物学因素知之甚少。天麻素是一种镇静药物,其结构与葡萄糖非常相似。它是一种高度水溶性的酚类葡萄糖苷。它几乎不能通过简单扩散进入肠道,但表现出超过80%的良好口服生物利用度。我们证实天麻素通过肠道葡萄糖转运途径被吸收。在通过该途径报道的糖苷活性成分中,它具有最高的口服生物利用度。因此,天麻素是IGT中选择性最强的药物底物,可用于评价IGT的药物转运能力。显然,菌株是影响药物吸收的主要生物学因素之一。本研究首先通过药代动力学实验和天麻素的单次肠道灌注实验,比较了IGTs在SD大鼠和Wistar大鼠之间以及C57小鼠和KM小鼠之间的药物转运能力。然后,十二指肠中的钠依赖性葡萄糖转运蛋白1型(SGLT1)和钠非依赖性葡萄糖转运蛋白2型(GLUT2),空肠,使用RT-qPCR和Western印迹定量这些动物的回肠和结肠。结果表明,天麻素在Wistar大鼠体内的口服生物利用度明显高于SD大鼠,在KM小鼠体内明显高于C57小鼠。天麻素的吸收在SD大鼠不同肠段之间差异显著,C57小鼠和KM小鼠,除了Wistar老鼠.RT-qPCR和Westernblot表明,SGLT1和GLUT2在SD大鼠和C57小鼠中的表达分布为十二指肠≈空肠>回肠>结肠。SGLT1表达在KM小鼠不同肠段之间没有差异,而GLUT2的肠道表达分布为十二指肠≈空肠≈回肠>结肠。然而,SGLT1和GLUT2的表达在Wistar大鼠不同肠段之间没有差异。据报道,SGLT1和GLUT2在人体内的表达分布为十二指肠>空肠>回肠>结肠。因此,SD大鼠和C57小鼠的肠道SGLT1和GLUT2的表达分布与人类更为相似。总之,IGTs的药物转运能力在不同品系大鼠和小鼠中存在差异。SD大鼠和C57小鼠更适合评价通过肠道葡萄糖转运途径吸收的糖苷类活性成分的药代动力学。
    Designing oral drug delivery systems using intestinal glucose transporters (IGTs) may be one of the strategies for improving oral bioavailability of drugs. However, little is known about the biological factors affecting the drug transport capacity of IGTs. Gastrodin is a sedative drug with a structure very similar to glucose. It is a highly water-soluble phenolic glucoside. It can hardly enter the intestine through simple diffusion but exhibits good oral bioavailability of over 80%. We confirmed that gastrodin is absorbed via the intestinal glucose transport pathway. It has the highest oral bioavailability among the reported glycosides\' active ingredients through this pathway. Thus, gastrodin is the most selective drug substrate of IGTs and can be used to evaluate the drug transport capacity of IGTs. Obviously, strain is one of the main biological factors affecting drug absorption. This study firstly compared the drug transport capacity of IGTs between SD rats and Wistar rats and between C57 mice and KM mice by pharmacokinetic experiments and single-pass intestinal perfusion experiments of gastrodin. Then, the sodium-dependent glucose transporter type 1 (SGLT1) and sodium-independent glucose transporters type 2 (GLUT2) in the duodenum, jejunum, ileum and colon of these animals were quantified using RT-qPCR and Western blot. The results showed that the oral bioavailability of gastrodin in Wistar rats was significantly higher than in SD rats and significantly higher in KM mice than in C57 mice. Gastrodin absorption significantly differed among different intestinal segments in SD rats, C57 mice and KM mice, except Wistar rats. RT-qPCR and Western blot demonstrated that the intestinal expression distribution of SGLT1 and GLUT2 in SD rats and C57 mice was duodenum ≈ jejunum > ileum > colon. SGLT1 expression did not differ among different intestinal segments in KM mice, whereas the intestinal expression distribution of GLUT2 was duodenum ≈ jejunum ≈ ileum > colon. However, the expression of SGLT1 and GLUT2 did not differ among different intestinal segments in Wistar rats. It was reported that the intestinal expression distribution of SGLT1 and GLUT2 in humans is duodenum > jejunum > ileum > colon. Hence, the intestinal expression distribution of SGLT1 and GLUT2 of SD rats and C57 mice was more similar to that in humans. In conclusion, the drug transport capacity of IGTs differs in different strains of rats and mice. SD rats and C57 mice are more suitable for evaluating the pharmacokinetics of glycosides\' active ingredients absorbed via the intestinal glucose transport pathway.
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  • 文章类型: Journal Article
    乌尔米亚湖被称为世界上第二个高盐湖,表面积约为5200km2。随着人类活动导致湖泊的水输入减少,在过去的几十年中,易受风蚀和粉尘排放影响的地区有所扩大。自2017年以来,本研究试图测量Urmia湖边缘的风蚀。为了定量了解干涸的乌尔米亚湖地区的风蚀参数,并在风蚀强度方面优先考虑不同的区域,有必要在干涸海岸的不同地区建立风蚀测量和监测站。在萨尔玛斯等六个易蚀地区建立了风蚀测量和监测站,JabalKandi,Soporghan,Miandoab,Khaselou和Ajabshir.确定了Urmia湖干燥边缘的风蚀参数,例如运输能力和土壤流失。为此,在具有相同中心的两个圆的布局中使用BSNE陷阱。每次风蚀事件后,将沉积物捕集器清空并称重;然后,计算了颗粒物的垂直和水平分布。最大运输能力值的比较-fmax(kg/m。年)和土壤损失-SL(吨/公顷。yr)2017年的风尘颗粒物表明,Urmia湖边缘的两个主要风蚀中心是Ajabshir和JabalKandi。哈塞尔鲁的车站,Salmas,Soporghan和Mianduab的排名下降。结果表明,转移能力值分别为351.97和297.30kg/m/年,土壤流失量分别为18.04和35.4吨/公顷/年,分别,对于风蚀潜力大的车站,即,AjabShir和JabalKandi,在2017年。此外,2019年,上述站的这些值显著降低,因此从转移能力获得的值达到54.93和40.39千克/米/年,土壤流失量达到3.70和2.43吨/公顷。对运输能力和土壤流失的调查结果显示,由于2017年至2019年湖泊水位上升以及生物和工程保护措施(非活的防风林),风蚀率呈下降趋势。
    Urmia Lake has been known as the second hypersaline lake in the world, with the surface area of approximately 5200 km2. With decreasing the water input of the lake due to anthropogenic activities, the susceptible areas to wind erosion and dust emission were extended during the last decades. The present study attempted to measure wind erosion on the edge of Urmia Lake for three years since 2017. In order to provide a quantitative understanding of wind erosion parameters in the dried up Urmia Lake area, and to prioritize different areas in terms of wind erosion intensity, it was necessary to establish wind erosion measurement and monitoring stations in different areas of dried up shores. Wind erosion measurement and monitoring stations were established in six erodible areas such as Salmas, Jabal Kandi, Soporghan, Miandoab, Khaselou and Ajabshir. Wind erosion parameters such as transport capacity and soil loss in the dried margin of Urmia Lake were determined. For this purpose, BSNE traps were used in the layout of two circles having an identical center. After each wind erosion event, sediment traps were emptied and weighted; then, the vertical and horizontal distribution of the particulate matters was calculated. Comparison of the values of maximum transport capacity-fmax (kg/m.yr) and soil loss- SL (ton/ha.yr) of aeolian particulate in 2017 showed that the two main centers of wind erosion on the edge of Urmia Lake were Ajabshir and Jabal Kandi. The stations of Khaselou, Salmas, Soporghan and Mianduab were in the declined ranking. Results showed that the transfer capacity values were 351.97 and 297.30 kg/m/year and soil losses were 18.04 and 35.4 ton/ha/year, respectively, for the stations with high wind erosion potential, i.e., Ajab Shir and Jabal Kandi, in 2017. Furthermore, these values were significantly reduced for the mentioned stations in 2019, so that the values obtained from the transfer capacity reached 54.93 and 40.39 kg/m/year and soil losses reached 3.70 and 2.43 ton/ha. Investigating the results of transport capacity and soil loss showed the decreasing trend in wind erosion rate due to the increasing water level of the lake as well as biological and engineering conservation practices (non-live windbreaks) from 2017 to 2019.
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  • 文章类型: Journal Article
    目前儿茶素与蛋白质相互作用的研究主要集中在非共价交联,然而,自由基诱导的儿茶素和β-乳球蛋白(BLG)之间交联的机理尚不清楚。在这项研究中,BLG结合四种儿茶素[表儿茶素(EC),表没食子儿茶素(EGC),表儿茶素没食子酸酯(ECG),和表没食子儿茶素没食子酸酯(EGCG)]。通过圆二色谱研究了配合物的结构变化,紫外可见(UV-vis)光谱和酸和8-苯胺基-1-萘磺酸(ANS)荧光光谱。构建M细胞模子评价庞杂消化产物的经肠上皮转运能力。结果表明,儿茶素通过C-S和C-N键与BLG共价结合,其结合含量为EGCG>EGC>ECG>EC。此外,儿茶素可以改变BLG的二级结构,随着α-螺旋的减少和不规则线圈的减少,导致蛋白质的空间结构松散。此外,儿茶素可以进一步提高BLG的消化率。M细胞模型消化产物转运能力约为Caco-2细胞模型的2倍,表明M细胞模型具有较好的抗原转运能力。组间的差异表明,消化产物的运输效率随着儿茶素的存在而降低,其中BLG-EGCG和BLG-EGC组比BLG-EC和BLG-ECG组转运更强。BLG-儿茶素复合物的转运效率低于BLG,表明儿茶素对肠屏障通透性具有保护和修复作用。
    The current research on interaction between catechin and protein has focused on non-covalent crosslinking, however, the mechanism of free radical-induced crosslinking between catechin and β-lactoglobulin (BLG) is not known. In this study, BLG bound to four catechins [epicatechin (EC), epigallocatechin (EGC), epicatechin gallate (ECG), and epigallocatechin gallate (EGCG)]. The structure change of complex was investigated by circular dichroism spectroscopy, ultraviolet-visible (UV-vis) spectroscopy and Acid and 8-Anilino-1-naphthalenesulfonic acid (ANS) fluorescence spectroscopy. M cell model was constructed to evaluate the transintestinal epithelial transport capacity of complex digestive products. The results showed that catechins were covalently bound to BLG by C-S and C-N bonds and their binding content was EGCG>EGC>ECG>EC. Moreover, catechins could change the secondary structure of BLG, with the decrease of α-helix and reduction of the irregular coilings, which leads to the loose spatial structure of the protein. Moreover, the catechin could enhance further the digestibility of BLG. Transport capacity of digestive products of M cell model was about twice of that of the Caco-2 cell model, indicating that M cell model had better antigen transport capacity. The difference between groups indicated that the transport efficiency of digestive products was decreased with the presence of catechin, in which BLG-EGCG and BLG-EGC groups were transported more strong than those of BLG-EC and BLG-ECG groups. The transport efficiency of BLG-catechin complexes were lower than that of BLG, indicating that catechin had the protective and repair roles on intestinal barrier permeability.
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  • 文章类型: Journal Article
    糖基化显著改变了食品和体内蛋白质的物理化学和生物功能特性。在本研究中,在生理条件下,乙二醛修饰了人血清白蛋白(HSA)作为脂肪酸的主要转运蛋白。去除了可逆的白蛋白结合的乙二醛,采用液相色谱-串联质谱(LC-MS/MS)对糖基化终产物进行定量。蛋白质结合的赖氨酸和精氨酸残基的总修饰达到4.2和9.6%,分别。这些修饰对长链脂肪酸转运能力的影响通过自旋标记的脂肪酸探针通过电子顺磁共振波谱表征。随着糖基化程度的增加,解离常数为0.74±0.09μM的天然HSA的七个结合位点的等效性被抵消,仅剩下三个高亲和力位点2、4和5(0.46±0.07μM)。其他四个位点移至低亲和力,具有明显更高的解离常数(1.32±0.35μM)。胰蛋白酶肽作图使我们能够将这些发现与特定结合位点的分子变化联系起来。鉴定的修饰热点是赖氨酸351、286、159和精氨酸144、485、117。对尿毒症患者与健康对照的血浆蛋白样品的进一步研究首次揭示了体内情况。
    Glycation significantly alters the physicochemical and biofunctional properties of proteins in foods and in vivo. In the present study, human serum albumin (HSA) as the major transporter of fatty acids was modified with glyoxal under physiological conditions. Reversibly albumin-bound glyoxal was removed, and advanced glycation end products were quantitated by liquid chromatography-tandem mass spectrometry (LC-MS/MS). The total modification of protein-bound lysine and arginine residues reached up to 4.2 and 9.6%, respectively. The impact of these modifications on the transport capacity of long-chain fatty acids was characterized by spin-labeled fatty acid probes via electron paramagnetic resonance spectroscopy. With increasing degree of glycation, the equivalence of the seven binding sites of native HSA with a dissociation constant of 0.74 ± 0.09 μM was set off with only the three high-affinity sites 2, 4, and 5 remaining (0.46 ± 0.07 μM). The other four sites were shifted to low affinities with significantly higher dissociation constants (1.32 ± 0.35 μM). Tryptic peptide mapping enabled us to relate these findings to molecular changes at specific binding sites. Modification hotspots identified were lysine 351, 286, 159 and arginine 144, 485, 117. Further investigation of plasma protein samples of uremic patients vs healthy controls gave first insights into the in vivo situation.
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  • 文章类型: Journal Article
    外生菌根真菌影响寄主植物的根系水分运输。为了描述真菌伴侣如何改变根水关系的确切机制,了解真菌跨膜水通道的功能很重要,即,水通道蛋白,对称性途径中的关键组成部分。在本文中,我们讨论了真菌水通道蛋白在根水运输中的作用。我们还强调了使用综合方法来解决水通道蛋白和根水关系研究未来热点中不断出现的问题的机会。
    Ectomycorrhizal fungi influence root water transport of host plants. To delineate the exact mechanisms of how fungal partner alters root water relations, it is important to understand the functions of fungal transmembrane water channels, i.e., aquaporins, the key component in the symplastic pathways. In this paper, we discussed what roles the fungal aquaporins may play in root water transport. We also highlighted the opportunities of using integrated approaches to address rising questions in future hotspots of aquaporin and root water relations research.
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  • 文章类型: Journal Article
    L-Type amino acid transporter 1 (LAT1)-utilizing prodrugs has been designed to improve drug delivery and targeting into the brain or cancer cells, since LAT1 is highly and selectively expressed on the blood-brain barrier as well as over-expressed in several types of cancer. However, less is known about the affinity of these compounds for the secondary transport mechanisms. The aim of this study was to evaluate interactions of nine LAT1-utilizing prodrugs with organic anion transporting polypeptides (OATPs). These results showed that LAT1-utilizing prodrugs can indeed, interact with OATPs, although it was considered to be minor compared to LAT1; the Km values of these compounds for LAT1 were 1-7 µM while the ones for OATPs were 73-406 µM. Moreover, utilization of LAT1 was 2-12-times more effective (compared as intrinsic clearance) than of OATPs, whose utilization seemed to be less significant at therapeutically used concentrations. According to these results, affinity for OATPs raised from the structural features of the parent drug moiety regardless of the structure of the promoiety. In conclusion, the present study shows that it is important to evaluate secondary transport mechanisms carefully, since they may have a role in pharmacokinetics of LAT1-utilizing prodrugs if LAT1 becomes saturated or un-functional.
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  • 文章类型: Journal Article
    Measurements of vein density and foliar minor vein phloem cell numbers, minor vein phloem cell sizes, and transfer cell wall ingrowths provide quantitative proxies for the leaf\'s capacities to load and export photosynthates. While overall infrastructural capacity for sugar loading and sugar export correlated positively and closely with photosynthetic capacity, the specific targets of the adjustment of minor vein organization varied with phloem-loading mechanism, plant life-cycle characteristics, and environmental growth conditions. Among apoplastic loaders, for which sugar loading into the phloem depends on cell membrane-spanning transport proteins, variation in minor vein density, phloem cell number, and level of cell wall ingrowth (when present) were consistently associated with photosynthetic capacity. Among active symplastic loaders, for which sugar loading into the phloem depends on cytosolic enzymes, variation in vein density and phloem cell size were consistently associated with photosynthetic capacity. All of these anatomical features were also subject to acclimatory adjustment depending on species and environmental conditions, with increased levels of these features supporting higher rates of photosynthesis. We present a procedure for the preparation of leaf tissue for minor vein analysis, using both light and transmission electron microscopy, that facilitates quantification of not only phloem features but also xylem features that provide proxies for foliar water import capacity.
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