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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.
V.I. Kushch I. Sevostianov L. Mishnaevsky Jr 《International Journal of Solids and Structures》2008,45(18-19):5103-5117
The paper addresses the problem of calculation of the local stress field and effective elastic properties of a unidirectional fiber reinforced composite with anisotropic constituents. For this aim, the representative unit cell approach has been utilized. The micro geometry of the composite is modeled by a periodic structure with a unit cell containing multiple circular fibers. The number of fibers is sufficient to account for the micro structure statistics of composite. A new method based on the multipole expansion technique is developed to obtain the exact series solution for the micro stress field. The method combines the principle of superposition, technique of complex potentials and some new results in the theory of special functions. A proper choice of potentials and new results for their series expansions allow one to reduce the boundary-value problem for the multiple-connected domain to an ordinary, well-posed set of linear algebraic equations. This reduction provides high numerical efficiency of the developed method. Exact expressions for the components of the effective stiffness tensor have been obtained by analytical averaging of the strain and stress fields. 相似文献
3.
CONG Fuzhong & LI YongSchool of Mathematics Information Science Shandong Institute of Business Technology Yantai China Office of Mathematics Changchun Flight Academy of the Air Force Changchun China Department of Mathematics Jilin University Changchun China 《中国科学A辑(英文版)》2004,47(5):675-686
An effective stability result for generalized Hamiltonian systems is obtained by applying the simultaneous approximation technique due to Lochak. Among these systems, dimensions of action variables and angle variables might be distinct. 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.
Numerical schemes for systems with multiple spatio-temporal scales are investigated. The multiscale schemes use asymptotic results for this type of systems which guarantee the existence of an effective dynamics for some suitably defined modes varying slowly on the largest scales. The multiscale schemes are analyzed in general, then illustrated on a specific example of a moderately large deterministic system displaying chaotic behavior due to Lorenz. Issues like consistency, accuracy, and efficiency are discussed in detail. The role of possible hidden slow variables as well as additional effects arising on the diffusive time-scale are also investigated. As a byproduct we obtain a rather complete characterization of the effective dynamics in Lorenz model. 相似文献
6.
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
7.
TAN Xiaojiang 《数学年刊B辑(英文版)》2002,23(4):531-538
Lei X be an arbitrary smooth irreducible complex projective curve, E (?) X a rank two vector bundle generated by its sections. The author first represents E as a triple {D1,D2,f}, where D1 , D2 are two effective divisors with d = deg(D1) + deg(D2), and f ∈ H0(X, [D1] |D2) is a collection of polynomials. E is the extension of [D2] by [D1] which is determined by f. By using f and the Brill-Noether matrix of D1 + D2, the author constructs a 2g X d matrix WE whose zero space gives Im{H0(X,[D1]) (?) H0(X, [D1] |D1)}(?)Im{H0(X, E) (?) H0(X,[D2]) (?) H0(X,[D2] |D2)}. From this and H0(X,E) = H0(X, [D1]) (?) Im{H0(X, E) (?) H0(X, [D2])}, it is got in particular that dimH0(X, E) = deg(E) - rank(WE) + 2. 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.
The K+−nucleus cross sections have been calculated in relativistic non-linear models taking into account the in-medium modifications of nucleons and mesons properties. More precisely, we have taken into account both the dressing of the nucleon effective mass by the scalar nuclear field in the target and the coupling of the mesons exchanged between the K+ and the nucleons to the polarization of the medium. First, using the most recent relativistic non-linear models, the in-medium σ, ω and ρ meson masses have been obtained in the nuclear matter rest frame. The influence of the non-linear contributions on the K+−nucleus cross sections has then been studied. Finally, we have compared our results with the experimental data. 相似文献