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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.
Horst Guido Müller 《Colloid and polymer science》1941,96(1):11-19
Zusammenfassung Einige charakteristische ?nderungen physikalischer Werkstoffeigenschaften beim heterogenen Zerfall übers?ttigter Mischkristalle
werden am Beispiel der fl?chenzentrierten Eisen-Nickel-Kupfer-Legierungen beschrieben. Bei der Behandlung des Einflusses der
Ausscheidungsvorg?nge auf die Rekristallisationserscheinungen tritt die Bedeutung des übers?ttigungsgrades der zerfallenden
festen L?sung für den Ablauf dieser Zustands?nderungen besonders klar zutage. Kritische Stadien der Ausscheidung und der Koagulation
der heterogenen Phasen sind bei diesen Legierungen für die Erzeugung besonders hochwertiger magnetischer Eigenschaften verantwortlich.
Der vorliegende Bericht wurde von Herrn Prof., Dr. Wo. Ostwald angeregt. Für das diesem Arbeitsgebiet entgegengebrachte Interesse
m?chte ich Herrn Prof. Ostwald meinen besten Dank aussprechen. 相似文献
3.
Kerstin Paech Adrian Dumitru Jürgen Schaffner-Bielich Stefan Schramm Horst Stöcker Gebhard Zeeb Detlef Zschiesche 《Acta Physica Hungarica A》2004,21(2-4):151-156
The measured particle ratios in central heavy-ion collisions are investigated within a chemical and thermal equilibrium chiral SU(3) σ?ω approach. Contrary to the commonly adopted non-interacting gas calculations, the chiral SU(3) model predicts modified effective hadron masses and effective chemical potentials in the medium and a transition to a chirally restored phase at high temperatures or chemical potentials. the influence of three different types of phase transitions is investigated. We show that the deduced freeze-out values considerably depend on the underlying model while the quality of the fit is approximately the same. 相似文献
4.
The association of complex formation with static quenching in CT systems was investigated. Evaluation of the data made evident
that the inner filter effect must be allowed for. Time-resolved and temperature-dependent stationary measurements of fluorescence
led to the separation of dynamic and static quenching components. The static quenching constant is discussed with respect
to the equilibrium constant of complex formation determined by absorption spectroscopy. 相似文献
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Horst Szambien 《Results in Mathematics》1992,22(1-2):619-621
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Pulsed laser deposition with a Nd:YAG laser was used to grow thin films from a pre-synthesized Ti3SiC2 MAX-phase formulated ablation target on oxidized Si(1 0 0) and MgO(1 0 0) substrates. The depositions were carried out in a substrate temperature range from 300 to 900 K, and the pressure in the deposition chamber ranged from vacuum (10−5 Pa) to 0.05 Pa Argon background pressure. The properties of the films have been investigated by Rutherford backscattering spectrometry for film thickness and stoichiometric composition and X-ray diffraction for the crystallinity of the films. The silicon content of the films varied with the energy density of the laser beam. To suppress especially the silicon re-sputtering from the substrate, the energy of the incoming particles must be below a threshold of 20 eV. Therefore, the energy density of the laser beam must not be too high. At constant deposition energy density the film thickness depends strongly on the background pressure. The X-ray diffraction measurements show patterns that are typical of amorphous films, i.e. no Ti3SiC2 related reflections were found. Only a very weak TiC(2 0 0) reflection was seen, indicating the presence of a small amount of crystalline TiC. 相似文献
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