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1.
Enantiomeric Cyclic Peptides with Different Caco‐2 Permeability Suggest Carrier‐Mediated Transport 下载免费PDF全文
B. Sc. Eduard Puig Prof. Dr. Beat Ernst Prof. Dr. Horst Kessler 《Chemistry (Weinheim an der Bergstrasse, Germany)》2015,21(22):8023-8027
Recently, oral absorption of cyclic hexapeptides was improved by N‐methylation of their backbone amides. However, the number and position of N‐methylations or of solvent exposed NHs did not correlate to intestinal permeability, measured in a Caco‐2 model. In this study, we investigate enantiomeric pairs of three polar and two lipophilic peptides to demonstrate the participation of carrier‐mediated transporters. As expected, all the enantiomeric peptides exhibited identical lipophilicity (logD7.4) and passive transcellular permeability determined by the parallel artificial membrane permeability assay (PAMPA). However, the enantiomeric polar peptides exhibited different Caco‐2 permeability (Papp) in both directions a–b and b–a. The same trend was observed for one of the lipophilic peptide, whereas the second lipophilic enantiomer pair showed identical Caco‐2 permeability (within the errors). These findings provide the first evidence for the involvement of carrier‐mediated transport for peptides, especially for those of polar nature. 相似文献
2.
本文简要报导了有机阳离子聚和物(氯化N,N—二甲基二烯丙基铵—二氧化硫)的合成方法,并对其作为粘土稳定剂的性能进行了评价。结果表明,该共聚物稳定粘土的能力高于目前国内外广泛使用的同类聚合物TDC。 相似文献
3.
We present in this paper an efficient approach for solving the problem of planning the long-term (multiyear) operation of a multireservoir hydroelectric power system for the critical period with a monthly variable load. This load is equal to a certain percentage of the total generation at the end of the year, subject to satisfying a number of constraints on the hydrosystem, using the minimum norm formulation.The proposed method is efficient in computing time and in calculating the total expected benefits from the system during the critical period. Numerical results are reported for a real system in operation consisting of two rivers. Each river has two series reservoirs.This work was supported by the Natural Science and Engineering Research Council of Canada, Grant No. A4146. 相似文献
4.
采用交替沉积磁控溅射工艺制备了超薄多层的FeCoB SiO2 磁性纳米颗粒膜 .利用x射线衍射仪、扫描探针显微镜、透射电子显微镜分析了薄膜的微结构和形貌特征 .采用振动样品磁强计、四探针法、微波矢量分析仪及谐振腔法测量薄膜试样的磁电性能和微波复磁导率 .重点对SiO2 介质相含量、薄膜微结构对电磁性能产生重要影响的机理做了分析和探讨 .结果表明 :这类FeCoB SiO2 磁性纳米颗粒膜具有良好的软磁性能和高频电磁性能 ,2GHz时的磁导率 μ′高于 70 ,可以应用于高频微磁器件或微波吸收材料的设计 相似文献
5.
The steady-state two-phase flow non-linear equation is considered in the case when one of phases has low effective permeability in some periodic set, while on the complementary set it is high; the second phase has no contrast of permeabilities in different zones. A homogenization procedure gives the homogenized model with macroscopic effective permeability of the second phase depending on the gradient and on the second order derivatives of the macroscopic pressure of the first phase. This effect cannot be obtained by classical (one small parameter) homogenization. To cite this article: G.P. Panasenko, G. Virnovsky, C. R. Mecanique 331 (2003). 相似文献
6.
绿豆子叶衰老过程中线粒体膜对几种氨基酸的透性 总被引:5,自引:0,他引:5
采用线粒体膨胀技术就不同衰老程度的绿豆子叶线粒体膜对氨基酸的透性进行了测定,结果表明,随着绿豆子叶的衰老,离体线粒体膜在脯氨酸、丝氨酸和甘氨酸等渗溶液中的膨胀率从2d龄至5d龄子叶逐渐下降,5d龄时,线粒体结构与功能已受到明显破坏,文中对膨胀率下降的原因进行了讨论。 相似文献
7.
探讨了粘合衬与粘合工艺对服装透气性、透湿性及透水性影响的规律。得出服装的舒适性虽由面料决定,但辅料(粘合衬)的影响也不可忽视。粘合衬的涂胶种类,粘合衬本身的透气性与透湿性,以及非织造粘合衬底布的单位重量,机织粘合衬底布的覆盖系数等,均对服装舒适性有影响,从而为衬料的选择,以及粘合工艺参数的设定,提供了依据。 相似文献
8.
铸膜液的溶剂体系(溶剂和非溶剂)对不对称膜形态的形成有重要作用。为了探索溶剂和透气性间的关系,本文考虑到了制备BCA梯度密度不对称膜的各种溶剂的一系列物理参数,得到了一些定性结果,并指出了更全面、明确、解释两者关系的研究方向。 相似文献
9.
10.
Akira Shimazu Tukasa Miyazaki Shigeru Katayama Yasuo Ito 《Journal of Polymer Science.Polymer Physics》2003,41(3):308-318
The ortho‐positronium (o‐Ps) lifetime τ3 and its intensity I3 in various fluorinated polyimides were determined by the positron annihilation technique and were studied with the spin–lattice relaxation time T1 and the propylene permeability, solubility, diffusivity, and permselectivity for propylene/propane in them. τ3, I3, and the distribution of τ3 changed when the bulky moieties in the polyimides were changed. The polyimides, having both large τ3 and I3 values, exhibited a short T1 and a high permeability with a low permselectivity. The propylene permeability and diffusivity were exponentially correlated with the product of I3 and the average free‐volume hole size estimated from τ3. In highly plasticized states induced by the sorption of propylene, the permeability increased with the propylene pressure in excellent agreement with the change in the free‐volume hole properties probed by o‐Ps. The large and broad distribution of the free‐volume holes and increased local chain mobility for the 2,2‐bis(3,4‐decarboxyphenyl) hexafluoropropane dianhydride‐based polyimides are thought to be important physical properties for promoting penetrant‐induced plasticization. These results suggest that o‐Ps is a powerful probe of not only the free‐volume holes but also the corresponding permeation mechanism and penetrant‐induced plasticization phenomenon. © 2003 Wiley Periodicals, Inc. J Polym Sci Part B: Polym Phys 41: 308–318, 2003 相似文献