Partitioning of anti-inflammatory steroid drugs into phosphatidylcholine and phosphatidylcholine-cholesterol small unilamellar vesicles as studied by second-derivative spectrophotometry

The partition coefficients (Kps) of six anti-inflammatory steroid drugs, dexamethasone (DMS), betamethasone (BMS), triamcinolone acetonide (TCLA), fluocinolone acetonide (FCLA), betamethasone 17,21-dipropionate (BMSDP), and clobetasole propionate (CBSP), for phosphatidylcholine (PC), and PC-cholesterol small unilamellar vesicles (SUVs) were determined by a second-derivative spectrophotometric method. The Kp values were obtained with a relative standard deviation of below 10% and the following order was observed: BMS< or =DMS相似文献   

A note on the independence of premiss rule

In this note, we prove that certain theories of (many‐sorted) intuitionistic predicate logic are closed under the independence of premiss rule (IPR). As corollaries, we show that and extended by some non‐classical axioms and non‐constructive axioms are closed under IPR.     

Micro-determination of total phthalate esters in biological samples by gas-liquid chromatography.

A method was investigated in which all of the phthalate esters in biological samples were determined as phthalic acid by gas-liquid chromatography. The method is based on the separation of phthalate esters from the sample with n-hexane, saponification of the esters with an alkaline ethanolic solution to give phthalic acid, purification of the acid by extraction with diethyl ether and column chromatography using silica gel, and conversion of the acid into bis(2,2,2-trifluoroethyl) phthalate with a 2,2,2-trifluoroethanol solution containing boron trifluoride. The derivative obtained is highly sensitive to an electron-capture detector, giving a sensitivity of 0.1 pg. Biological samples fortified with di(2-ethylhexyl) phthalate at levels of 5-100 ppb were analyzed, with recoveries of 70-100%.     

Ionic salt permeabilities and membrane potentials of asymmetric polypeptide membrane

Asymmetric membrane potentials and transport properties of polypeptide membrane consisting of two layers with poly(L-glutamic acid) and poly (γ-methylL-glutamate) were studied in the pH range of 2 to 6 at 25 °C. Under the condition adopted, the poly (L-glutamic acid) layer of the membrane underwentα helix to coil transition which was confirmed by ATR-IR measurements. The membrane potentials of the asymmetric membrane between two identical solutions of KCl,Δψ _asym, which is called asymmetric potential, were observed.Δψ _asym values were effected by the structural transition of poly (L-glutamic acid) layer. As a result, the effective charge density of the membrane, which was derived by the asymmetric membrane potential measurements, had a maximum at the transition region of pH=4.8. On the other hand, the permeation coefficient of KCl,P _i, was higher in the direction from poly (L-glutamic acid) side to poly (γ-methylL-glutamate) side, “G →M direction”, than in the oppositeM →G direction. Furthermore,P _i inG →M direction was dependent on the solution pH, that is,P _i decreased when pH was increased to 4.8 and increased on further increasing of pH These membrane behaviors were described in terms of the competition between structural transition and variation of fixed charge density owing to the helix to coil transition of the asymmetric polypeptide membrane.     

Thermoswitching property in TCNQ salts of ionenes containing poly(ethylene oxide) segments

Ionene polymers characterized by the alternating structure of ionene and crystalline poly(ethylene oxide) (PEO) segments were prepared as a function of PEO segment size. A microstructure of these ionenes and their 7,7,8,8-tetracyanoquinodimethane (TCNQ) salts were investigated with x-ray diffraction patterns, thermal scanning behavior, and polarizing micrographs. On the basis of this microstructure, the change in resistivity with temperature was studied. In Arrhenius' plots of the resistivity the simple salts in which the spherulites consisting of the PEO segments were observed showed a sharp decrease in resistivity with a rise in temperature [critical temperature resistor (CTR)] at about the melting point of the PEO segments, whereas the other simple salts in which the spherulites were not observed showed linear temperature dependence. The switching properties were confirmed similarly in repetitive heating/cooling cycles. This CTR characteristic was attributed to an increase in continuity in the conduction paths by melting spherulites. The apparent switching properties were not observed in the complex salts.     

Geometric properties of covalently bonded DNA on single-crystalline diamond

Diamond is a promising candidate for bioapplications. Properties of hybridized DNA arrays on single-crystalline diamond are studied on a microscopic level by atomic force microscopy (AFM) in buffer solutions. Compact DNA layers in a thickness of 76 A are resolved by optimizing phase and height contrast in AFM. The height shows some long-range (30 nm) undulations of +/-5 A due to tip and DNA interactions. The axis of double helix DNA is oriented at about 36 degrees with respect to the diamond surface. DNA molecules can be removed by contact-mode AFM with forces >45 nN, indicating stronger DNA bonding than on gold substrates.     

Structure-activity relationships of neuromedin U. V. study on the stability of porcine neuromedin U-8 at the C-terminal asparagine amide under mild alkaline and acidic conditions

Porcine neuromedin U-8 (X-Asn-NH(2), X=H-Tyr-Phe-Leu-Phe-Arg-Pro-Arg) is occasionally unstable in the biological fluids used for bioassay as well as in the acidic solutions used for purification of synthetic peptides. In this study, HPLC examination of an incubate solution of X-Asn-NH(2) revealed that the main decomposition products in Tyrode's solution (pH 7.4) were either alpha- or beta-monocarboxylic acid analogs (X-Asn-OH or X-Asp-NH(2)), and that no dicarboxylic acid analog (X-Asp-OH) was produced. Further investigation, employing a model peptide (Y-Asn-NH(2), Y=Benzoyl-Pro-Arg) incubated in a 0.1 M sodium bicarbonate solution at 60 degrees C, revealed that the decomposition of C-terminal Asn-NH(2) occurred through the formation of an aminosuccinimide intermediate (Y-Asu), at a rate faster than that of Y-Asn-Ser peptide but slower than that of Y-Asn-Gly peptide. Mild acid hydrolysis of X-Asn-NH(2) examined in a 1 M HCl solution at 60 degrees C yielded X-Asn-OH and X-Asp-NH(2), which further decomposed to yield X-Asp-OH. The C-terminal degradation of X-Asn-NH(2) resulted in reduced biological and immunochemical binding activities.     

Electronic structures in coupled two quantum dots by 3D-mesh Hartree-Fock-Kohn-Sham calculation

To study the electronic structures of quantum dots in the framework of self-interaction-free including three dimensional effects, we adopt the theory of nonlocal effective potential introduced by Kohn and Sham [#!ks65!#]. For utilizing the advantageous point of the real space (3D) mesh method to solve the original nonlinear and nonlocal Hartree-Fock-Kohn-Sham (HFKS)-equation, we introduce a linearization of the equation in the local form by introducing the local Coulomb potentials which depend on explicitly the two single particle states. In practice, for solving the local form HFKS-equation, we use the Car-Parrinello-like relaxation method and the Coulomb potentials are obtained by solving the Poisson equation under proper boundary conditions. Firstly the observed energy gap between triplet- and singlet-states of N = 4 in DBS [#!tarucha96!#] is discussed to reproduce the addition energies and chemical potentials depending the magnetic field. Next the coupling between two-quantum dots in TBS [#!aht97!#] is studied by adding the square barrier between two dots. The spin-degeneracy [#!aht97!#] measured in gate-voltage depending on magnetic field is well reproduced in the limit of small mismatch. Finally, the electronic states in the ring structure are calculated and discussed how the ring size and magnetic field affect to the structures. Received 30 November 2000     

Phase diagram of the SrS–Ga2S3 system and its application to the single-crystal growth of SrGa2S4

Ce-doped SrGa₂S₄ compound is expected as a new host material of blue EL devices. However, the basic properties of bulk single crystals have not been fully clarified, since this compound has been mostly synthesized in the form of polycrystals or thin films. Here, we firstly present the pseudo-binary phase diagram of the SrS–Ga₂S₃ system constructed in accordance with our DTA data for single-crystal growth of SrGa₂S₄. It is shown that SrGa₂S₄ compound has a congruent melting point and a eutectic reaction in the side of excess of Ga₂S₃ concentration. On the basis of the phase diagram, single crystals of SrGa₂S₄ are grown using Ga₂S₃ as a self-flux in a horizontal Bridgman furnace. Colorless and transparent crystals having a typical size 2×2×2 mm³ are obtained.