Acylated flavonoid glycosides from Barringtonia racemosa

Abstract

Using various chromatographic separations, three new acylated flavonoid glycosides, namely barringosides G–I (1–3), were isolated from the water-soluble extract of Barringtonia racemosa branches and leaves. The structure elucidation was performed by extensive analysis of the 1D and 2D NMR and HR-QTOF-MS data. Of the isolated compounds, barringoside I (3) showed moderate inhibitory effects on LPS-induced NO production in RAW264.7 cells with an IC₅₀ of 52.48?±?1.04?µM.     

Triterpene glycosides from the Vietnamese sea cucumber Holothuria edulis

Abstract

From the MeOH extract of the Vietnamese sea cucumber Holothuria edulis, eight triterpene glycosides (1–8), including one new compound namely holothurin A₅ (1), were isolated by using various chromatographic separations. Their structures were established by spectroscopic experiments including 1D, 2D NMR and HR-ESI-MS. Holothurin A₅ (1) has a hydroperoxy group at C-25. To the best of our knowledge, this is the first report of this group in triterpene saponins obtained from sea cucumbers to date. In addition, the in vitro cytotoxicity against five human cancer cell lines (HepG2, KB, LNCaP, MCF7 and SK-Mel2) of all isolated compounds was also evaluated using SRB assays.     

Photoinitiated cationic polymerisation of multifunctional systems

Different types of tridimensional polymer networks have been synthetised by photoinitiated cationic polymerisation of vinyl ether and epoxy-functionalised oligomers and polymers. The polymerisation kinetics was followed by real-time infrared (RTIR) spectroscopy, a technique that records directly conversion versus time profiles in a timescale as short as 1 s. The addition of a diacrylate monomer was shown to accelerate the ring-opening polymerisation of epoxidized polyisoprene, with formation of interpenetrating polymer networks having well contrasted properties. A dual polymer network has been generated by photocrosslinking of a polyisoprene functionalised with both epoxy and acrylate groups.     

Target Design of Novel Histone Deacetylase 6 Selective Inhibitors with 2-Mercaptoquinazolinone as the Cap Moiety

Epigenetic alterations found in all human cancers are promising targets for anticancer therapy. In this sense, histone deacetylase inhibitors (HDACIs) are interesting anticancer agents that play an important role in the epigenetic regulation of cancer cells. Here, we report 15 novel hydroxamic acid-based histone deacetylase inhibitors with quinazolinone core structures. Five compounds exhibited antiproliferative activity with IC₅₀ values of 3.4–37.8 µM. Compound 8 with a 2-mercaptoquinazolinone cap moiety displayed the highest antiproliferative efficacy against MCF-7 cells. For the HDAC6 target selectivity study, compound 8 displayed an IC₅₀ value of 2.3 µM, which is 29.3 times higher than those of HDAC3, HDAC4, HDAC8, and HDAC11. Western blot assay proved that compound 8 strongly inhibited tubulin acetylation, a substrate of HDAC6. Compound 8 also displayed stronger inhibition activity against HDAC11 than the control drug Belinostat. The inhibitory mechanism of action of compound 8 on HDAC enzymes was then explored using molecular docking study. The data revealed a high binding affinity (−7.92 kcal/mol) of compound 8 toward HDAC6. In addition, dock pose analysis also proved that compound 8 might serve as a potent inhibitor of HDAC11.     

The interior proximal extragradient method for solving equilibrium problems

In this article we present a new and efficient method for solving equilibrium problems on polyhedra. The method is based on an interior-quadratic proximal term which replaces the usual quadratic proximal term. This leads to an interior proximal type algorithm. Each iteration consists in a prediction step followed by a correction step as in the extragradient method. In a first algorithm each of these steps is obtained by solving an unconstrained minimization problem, while in a second algorithm the correction step is replaced by an Armijo-backtracking linesearch followed by an hyperplane projection step. We prove that our algorithms are convergent under mild assumptions: pseudomonotonicity for the two algorithms and a Lipschitz property for the first one. Finally we present some numerical experiments to illustrate the behavior of the proposed algorithms.     

Associated Primes of the Example of Brenner and Monsky

Recently, Brenner and Monsky found an example of an ideal in a hypersurface ring whose tight closure does not commute with localization, thus answered the localization problem in tight closure theory in the negative. In this article, we use Monsky's calculations to analyze the set of associated primes of the Frobenius powers of this ideal and show that this set is infinite.     

Existence of solutions in variational relation problems without convexity

Two main existence conditions for solutions of variational relation problems are established without convexity. The first one is based on a finite solvability property and the second one on generalized KKM mappings. These conditions unify and strengthen several existing results in the literature on the topic. A model of satisficing process by rejection is considered which gives an economic interpretation of the introduced concepts.     

A generalized distance and enhanced Ekeland’s variational principle for vector functions

We propose a definition of lower closed transitive relations and prove the existence of minimal elements for such a relation. This result is shown to contain probably a large part of existing versions of Ekeland’s variational principle (EVP). We introduce the notion of a weak τ-function p as a generalized distance and use it together with the above result on minimal elements to establish enhanced EVP for various settings, under relaxed lower semicontinuity assumptions. These principles conclude the existence not only of p-strict minimizers of p-perturbations of the considered vector function, but also p-sharp and p-strong minimizers. Our results are proved to be stronger than the classical EVP and many generalizations in the literature, even in the usual one-dimensional case, by numerous corollaries and examples. We include equivalent formulations of our enhanced EVP as well.     

To the theory of operator monotone and operator convex functions

We prove that a real function is operator monotone (operator convex) if the corresponding monotonicity (convexity) inequalities are valid for some normal state on the algebra of all bounded operators in an infinite-dimensional Hilbert space. We describe the class of convex operator functions with respect to a given von Neumann algebra in dependence of types of direct summands in this algebra. We prove that if a function from ℝ⁺ into ℝ⁺ is monotone with respect to a von Neumann algebra, then it is also operator monotone in the sense of the natural order on the set of positive self-adjoint operators affiliated with this algebra.