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1.
Enantiomeric Cyclic Peptides with Different Caco‐2 Permeability Suggest Carrier‐Mediated Transport
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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.
设V是一个n维线性空间,V_x~m(G)为V上的张量对称类.A为V的线性算子T的矩阵,K(A)为V_x~m(G)上的诱导线性算子K(T)的矩阵.本文从K(A)的数值半径Υ(K(A))和可分数值半径Υ_x(K(A))定义出发,研究了Υ(K(A))、Υ_x(K(A))与范数||A||_p(1≤p≤2)、广义矩阵函数d_x~G(A)的关系,得到了它们之间的两个不等式. 相似文献
3.
A new approach to identify the independent amplitudes along with their partial wave multipole expansions, for photo-and electro-production
is suggested, which is generally applicable to mesons with arbitrary spin-parity. These amplitudes facilitate direct identification
of different resonance contributions.
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.
本文报道了一种测角单晶NMR探头。该探头采用单线圃双调谐电路,工作频率在90MHz-110 MHz连续可调,可进行交叉极化大功率去耦实验。文中提出了一种简单而有效的测角装置,可使单晶绕三个互相垂直轴转动实现单晶的NMR测量。作为典型的应用例子,本文利用该探头实现了单晶DGO(2NH2CH2COOH·H2C2O4)屏蔽张量的测量。 相似文献
7.
The Stokes motions of three-dimensional screw-sensed slender particles in a homogeneous shear field are investigated, including the effects of buoyancy. Conclusions are drawn about the possibility of achieving a separation of mixtures of right- and left-handed particles. The linearity of the Stokes equations allows complex flows to be solved by adding the effects of the several terms which describe the flow in which the particle is immersed. The homogeneous shear flow considered here consists of three such terms; solutions for a series of 12 unit motions are sufficient to determine the hydrodynamic resistance tensors. The forces and torques experienced by screw-sensed particles are calculated from these 51 resistance tensors, using slender-filament theory. The results allow an estimate of the range of buoyancy parameters for which gravitational sedimentation can be neglected. The fundamental component of the particle motion is a rotation, at approximately the same angular velocity as that of the fluid. Superimposed on this are variations, of large period, in the particle orientation. A phase plane analysis is used to find the terminal orientations. Very long calculation times are required for the phase portrait. An approximate method based on azimuthally-averaged equations is developed to avoid the requirements for long time integration. 相似文献
8.
In this paper, a successive supersymmetric rank‐1 decomposition of a real higher‐order supersymmetric tensor is considered. To obtain such a decomposition, we design a greedy method based on iteratively computing the best supersymmetric rank‐1 approximation of the residual tensors. We further show that a supersymmetric canonical decomposition could be obtained when the method is applied to an orthogonally diagonalizable supersymmetric tensor, and in particular, when the order is 2, this method generates the eigenvalue decomposition for symmetric matrices. Details of the algorithm designed and the numerical results are reported in this paper. Copyright © 2007 John Wiley & Sons, Ltd. 相似文献
9.
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
10.