Studies on metabolites and metabolic pathways of bulleyaconitine A in rat liver microsomes using LC‐MSn combined with specific inhibitors

Bulleyaconitine A (BLA) from Aconitum bulleyanum plants is usually used as anti‐inflammatory drug in some Asian countries. It has a variety of bioactivities, and at the same time some toxicities. Since the bioactivities and toxicities of BLA are closely related to its metabolism, the metabolites and the metabolic pathways of BLA in rat liver microsomes were investigated by HPLC–MSⁿ. In this research, the 12 metabolites of BLA were identified according to the results of HPLC‐MSⁿ data and the relevant literature. The results showed that there are multiple metabolites of BLA in rat liver microsomes, including demethylation, deacetylation, dehydrogenation deacetylation and hydroxylation. The major metabolic pathways of BLA in rat liver microsomes were clarified by HPLC‐MS combined with specific inhibitors of CYP450 isoforms. As a result, CYP3A and 2C were found to be the principal CYP isoforms contributing to the metabolism of BLA. Moreover, CYP2D6 and 2E1 are also more important CYP isoforms for the metabolism of BLA. While CYP1A2 only affected the formation rate of M11, its effect on the metabolism of BLA is very small. Copyright © 2014 John Wiley & Sons, Ltd.     

The behavior of differential forms under purely inseparable extensions

Let F be a field of characteristic 2. In this paper we give a complete computation of the kernel of the homomorphism $H_2^{m+1}(F)?H_2^{m+1}(L)$ induced by scalar extension, where $L/F$ is a purely inseparable extension (of any degree), $H_2^{m+1}(F)$ is the cokernel of the Artin–Schreier operator $?:{\mathrm{\Omega }}_F^m?{\mathrm{\Omega }}_F^m/\mathrm{d}{\mathrm{\Omega }}_F^{m?1}$ given by: $x\frac{\mathrm{d}{x}_1}{x_1}\wedge ?\wedge \frac{\mathrm{d}{x}_m}{x_m}?(x^2?x)\frac{\mathrm{d}{x}_1}{x_1}\wedge ?\wedge \frac{\mathrm{d}{x}_m}{x_m}+\mathrm{d}{\mathrm{\Omega }}_F^{m?1}$, where ${\mathrm{\Omega }}_F^m$ is the space of absolute m-differential forms over F and d is the differential operator. Other related results are included.     

Solid‐state 31P NMR investigation on the status of guanine nucleotides in paclitaxel‐stabilized microtubules

Microtubule dynamics is a target for many chemotherapeutic drugs. In order to understand the biochemical effects of paclitaxel on the GTPase activity of tubulin, the status of guanine nucleotides in microtubules was investigated by ³¹P cross‐polarization magic angle spinning (CPMAS) NMR. Microtubules were freshly prepared in vitro in the presence of paclitaxel and then lyophilized in sucrose buffer for solid‐state NMR experiments. A ³¹P CPMAS NMR spectrum with the SNR of 25 was successfully acquired from the lyophilized microtubule sample. The broadness of the ³¹P spectral lines in the spectrum indicates that the molecular environments around the guanine nucleotides inside tubulin may not be as crystalline as reported by many diffraction studies. Deconvolution of the spectrum into four spectral components was carried out in comparison with the ³¹P NMR spectra obtained from five control samples. The spectral analysis suggested that about 13% of the nucleotides were present as GTP and 37% as GDP in the β‐tubulin (E‐site) of the microtubules. It was found that most of the GDPs were present as GDP‐P_i complex in the microtubules, which seems to be one of the effects of paclitaxel binding. Copyright © 2015 John Wiley & Sons, Ltd.     

Convergence of solutions for the fractional Cahn–Hilliard system

This paper deals with the Cauchy–Dirichlet problem for the fractional Cahn–Hilliard equation. The main results consist of global (in time) existence of weak solutions, characterization of parabolic smoothing effects (implying under proper condition eventual boundedness of trajectories), and convergence of each solution to a (single) equilibrium. In particular, to prove the convergence result, a variant of the so-called ?ojasiewicz–Simon inequality is provided for the fractional Dirichlet Laplacian and (possibly) non-analytic (but $C^1$) nonlinearities.     

非线性互补问题的一种全局收敛的显式光滑Newton方法

本针对Po函数非线性互补问题，给出了一种显式光滑Newton方法，该方法将光滑参数μ进行显式迭代而不依赖于Newton方向的搜索过程，并在适当的假设条件下，证明了算法的全局收敛性。     

On universal subsets of Banach spaces

We prove that to most of the known hypercyclic operators A on separable Banach spaces there exist compact (compact convex, compact connected) subsets K of E such that each compact (compact convex, compact connected) subset of E can be approximated with respect to Hausdorff's distance by for suitable . Received July 8, 1997, in final form October 17, 1997     

ICP－AES法测定金属矿产品中的磷

本文研究了铁矿石、铬矿石、锰矿石中的微量磷的电感耦合等离子体发射光谱法的测定。方法简便，具有很好的精密度和准确度。标准样品的分析结果基本与标称值相吻合，回收率在９５％－１０５％之间。     

Congruence criteria for finite subsets of complex projective and complex hyperbolic spaces

We investigate congruence classes and direct congruence classes of m-tuples in the complex projective space ℂP ⁿ . For direct congruence one allows only isometries which are induced by linear (instead of semilinear) mappings. We establish a canonical bijection between the set of direct congruence classes of m-tuples of points in ℂP ⁿ and the set of equivalence classes of positive semidefinite Hermitean m×m-matrices of rank at most n+1 with 1's on the diagonal. As a corollary we get that the direct congruence class of an m-tuple is uniquely determined by the direct congruence classes of all of its triangles, provided that no pair of points of the m-tuple has distance π/2. Examples show that the situation changes drastically if one replaces direct congruence classes by congruence classes or if distances π/2 are allowed. Finally we do the same kind of investigation also for the complex hyperbolic space ℂH ⁿ . Most of the results are completely analogous, however, there are also some interesting differences. Received: 15 January 1996     

A dual graph-norm refinement indicator for finite volume approximations of the Euler equations

Summary. We generalise and apply a refinement indicator of the type originally designed by Mackenzie, Süli and Warnecke in [15] and [16] for linear Friedrichs systems to the Euler equations of inviscid, compressible fluid flow. The Euler equations are symmetrized by means of entropy variables and locally linearized about a constant state to obtain a symmetric hyperbolic system to which an a posteriori error analysis of the type introduced in [15] can be applied. We discuss the details of the implementation of the refinement indicator into the DLR--Code which is based on a finite volume method of box type on an unstructured grid and present numerical results. Received May 15, 1995 / Revised version received April 17, 1996