Enantiomeric Cyclic Peptides with Different Caco‐2 Permeability Suggest Carrier‐Mediated Transport

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 (logD_7.4) and passive transcellular permeability determined by the parallel artificial membrane permeability assay (PAMPA). However, the enantiomeric polar peptides exhibited different Caco‐2 permeability (P_app) 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.     

On the domain dependence of solutions to the compressible Navier–Stokes equations of a barotropic fluid

We prove a general compactness result for the solution set of the compressible Navier–Stokes equations with respect to the variation of the underlying spatial domain. Among various corollaries, we then prove a general existence theorem for the system in question with no restrictions on smoothness of the spatial domain. Copyright © 2002 John Wiley & Sons, Ltd.     

On the duration of the total eclipse of a satellite of a body

This paper solves the problem of the duration of the total eclipseof a satellite of a body, provided that (a) the body is sphericalin shape and the mass distribution inside the body is sphericallysymmetrical; (b) the satellite is a very small object; (c) thesatellite's orbit around a body is circular and the satellitecan pass through the centre of its shadow; (d) a source of lightis the source of the conical body's shadow (umbra) and it doesnot change its apparent position in the sky; (e) there are noperturbations on the satellite's orbit. The solution presentedrepresents the general discussion of the problem based on utilizationof some parts of the theory of contraction mappings.     

Geometro-stochastic locality in quantum spacetime and quantum diffusions

The issue of the intrinsic nonlocality of quantum mechanics raised by J. S. Bell is examined from the point of view of the recently developed method of geometro-stochastic quantization and its applications to general relativistic quantum theory. This analysis reveals that a distinction should be made between the topological concept of locality used in formulating relativistic causality and a type of geometric locality based on the concept of fiber bundle, which can be used in extending the strong equivalence principle to the quantum domain. Both play an essential role in formulating a notion of geometro-stochastic propagation based on quantum diffusions, which throws new light on the EPR paradox, on the origin of the arrow of time, and on other fundamental issues in quantum cosmology and the theory of measurement.     

A Positive Doubly Power Bounded Operator with a Nonpositive Inverse Exists on any Infinite-dimensional AL-Space

In this paper we construct a positive doubly power bounded operator with a nonpositive inverse on an AL-space.     

Summing the derivative expansion of the effective action

The derivative expansion of the effective action is a perturbative development in derivatives of the fields. The expansion breaks down when some of the derivatives are too large. We show how to sum exactly the first and second derivatives and treat perturbatively derivatives higher than second.     

Thermodynamic non-additivity in disordered systems with extended phase space

Non-additivity effects in coupled dynamic-stochastic systems are investigated. It is shown that there is a mapping of the replica approach to disordered systems with finite replica indexn on Tsallis non-extensive statistics, if the average thermodynamic entropy of the dynamic subsystem differs from the information entropy for the probability distribution in the stochastic subsystem. The entropic indexq is determined by the entropy difference ΔS. In the case of incomplete information, the entropic indexq=1−n is shown to be related to the degree of lost information.     

Kinetics of the solution polymerization of dioxolane in the presence of water

Water acts as a cocatalyst in the polymerization of dioxolane initiated by the ion pair ～Si^⊕HSO₄^?. The dependence of the reaction rate on the water concentration exhibits a maximum, the width of which strongly depends on the concentration of dioxolane. The change of the coordinates of the maximum and its shape with the decrease of the monomer concentration causes the reaction rate to decrease with increasing conversion. The point at which the slope of the conversion curve changes is a function of initial concentration of water. There is a very fast decrease of the concentration of free water in the polymerizing system. The consumption of water is associated with some peculiarities. The amount of free water which remains in the system is a function of the concentration of the original initiator. The ratio [H₂O]_∞/[initiator] is constant over a rather broad range of initial concentration of water.