Microwave-Assisted Desulfation of the Hemolytic Saponins Extracted from Holothuria scabra Viscera

Saponins are plant and marine animal specific metabolites that are commonly considered as molecular vectors for chemical defenses against unicellular and pluricellular organisms. Their toxicity is attributed to their membranolytic properties. Modifying the molecular structures of saponins by quantitative and selective chemical reactions is increasingly considered to tune the biological properties of these molecules (i) to prepare congeners with specific activities for biomedical applications and (ii) to afford experimental data related to their structure–activity relationship. In the present study, we focused on the sulfated saponins contained in the viscera of Holothuria scabra, a sea cucumber present in the Indian Ocean and abundantly consumed on the Asian food market. Using mass spectrometry, we first qualitatively and quantitatively assessed the saponin content within the viscera of H. scabra. We detected 26 sulfated saponins presenting 5 different elemental compositions. Microwave activation under alkaline conditions in aqueous solutions was developed and optimized to quantitatively and specifically induce the desulfation of the natural saponins, by a specific loss of H₂SO₄. By comparing the hemolytic activities of the natural and desulfated extracts, we clearly identified the sulfate function as highly responsible for the saponin toxicity.     

Discovery of an NAD+ analogue with enhanced specificity for PARP1

Among various protein posttranslational modifiers, poly-ADP-ribose polymerase 1 (PARP1) is a key player for regulating numerous cellular processes and events through enzymatic attachments of target proteins with ADP-ribose units donated by nicotinamide adenine dinucleotide (NAD⁺). Human PARP1 is involved in the pathogenesis and progression of many diseases. PARP1 inhibitors have received approvals for cancer treatment. Despite these successes, our understanding about PARP1 remains limited, partially due to the presence of various ADP-ribosylation reactions catalyzed by other PARPs and their overlapped cellular functions. Here we report a synthetic NAD⁺ featuring an adenosyl 3′-azido substitution. Acting as an ADP-ribose donor with high activity and specificity for human PARP1, this compound enables labelling and profiling of possible protein substrates of endogenous PARP1. It provides a unique and valuable tool for studying PARP1 in biology and pathology and may shed light on the development of PARP isoform-specific modulators.

An analogue of nicotinamide adenine dinucleotide (NAD⁺) featuring an azido group at 3′-OH of adenosine moiety is found to possess high specificity for human PARP1-catalyzed protein poly-ADP-ribosylation.     

New ligands and structural insights into the catalytic asymmetric addition of organozinc reagents to ketones

The catalytic asymmetric addition of alkyl groups to ketones has received considerable attention. Outlined herein is the synthesis of two new ligands based on the C₂-symmetric 11,12-diamino-9,10-dihydro-9,10-ethanoanthracene. The scope of the new ligands has been evaluated in the catalytic asymmetric addition of diethylzinc to a variety of ketones. Enantioselectivities as high as 99% have been achieved. The structures of two of these ligands have been determined by X-ray crystallography and are compared with related structures. Additionally, the structure of a titanium complex bound to a bis(sulfonamide) diol ligand is reported.     

Non-universal shear viscosity from Einstein gravity

A very famous result of gauge/gravity duality is the universality of the ratio of shear viscosity to entropy density in every field theory holographically dual to classical, two-derivative (Einstein) gravity. We present a way to obtain deviation from this universality by breaking the rotational symmetry spontaneously. In anisotropic fluids additional shear modes exist and their corresponding shear viscosities may be non-universal. We confirm this by explicitly calculating the shear viscosities in a transversely isotropic background, a p-wave superfluid, and study its critical behavior. This is a first decisive step towards further applications of gauge/gravity duality to physical systems.     

A <Emphasis Type="Italic">p</Emphasis>-adic RANSAC algorithm for stereo vision using Hensel lifting

A p-adic variation of the Ran(dom) Sa(mple) C(onsensus) method for solving the relative pose problem in stereo vision is developed. From two 2-adically encoded images a random sample of five pairs of corresponding points is taken, and the equations for the essential matrix are solved by lifting solutions modulo 2 to the 2-adic integers. A recently devised p-adic hierarchical classification algorithm imitiating the known LBG quantization method classifies the solutions for all the samples after having determined the number of clusters using the known intra-inter validity of clusterings. In the successful case, a cluster ranking will determine the cluster containing a 2-adic approximation to the “true” solution of the problem.     

Atomic masses above146Gd derived from a shell model analysis of high spin states

From a shell model analysis of high-spin states in neutron deficient nuclei above¹⁴⁶Gd we have derived the ground state masses of theN=82 and 83 isotones of Eu, Tb, Dy, Ho, and Er. The results can be used to calculate the energies of aligned multiparticle yrast configurations. They also link ten α-decay chains to the nuclei with known masses, providing many new absolute mass values which are compared with predictions. An examination of the two-proton separation energies atN=82 shows an 0.5 MeV break in the nuclear mass surface atZ=64.     

Arithmetic and other properties of certain Delphic semigroups. II

Summary This paper continues [2]. We show that the sets of infinitely divisible elements of the Delphic semigroups ⁺ (of positive renewal sequences) and P (of standard p-functions) are additively convex, and do a Choquet analysis in each case. We draw up the (M, m) diagram for members of , and deduce from it that the product topology on is metrizable. Finally we look at the arithmetic of , showing that the simples are residual in it, and partially identifying I ₀, the set of infinitely divisible elements without simple factors. Many examples are given.I am indebted to Professor D. G. Kendall for his constant help and encouragement in the course of the research leading to this paper and [2].