Albatrellus confluens (Alb. & Schwein.) Kotl. & Pouz.: Natural Fungal Compounds and Synthetic Derivatives with In Vitro Anthelmintic Activities and Antiproliferative Effects against Two Human Cancer Cell Lines

Neglected tropical diseases affect the world’s poorest populations with soil-transmitted helminthiasis and schistosomiasis being among the most prevalent ones. Mass drug administration is currently the most important control measure, but the use of the few available drugs is giving rise to increased resistance of the parasites to the drugs. Different approaches are needed to come up with new therapeutic agents against these helminths. Fungi are a source of secondary metabolites, but most fungi remain largely uninvestigated as anthelmintics. In this report, the anthelmintic activity of Albatrellus confluens against Caenorhabditis elegans was investigated using bio-assay guided isolation. Grifolin (1) and neogrifolin (2) were identified as responsible for the anthelmintic activity. Derivatives 4–6 were synthesized to investigate the effect of varying the prenyl chain length on anthelmintic activity. The isolated compounds 1 and 2 and synthetic derivatives 4–6, as well as their educts 7–10, were tested against Schistosoma mansoni (adult and newly transformed schistosomula), Strongyloides ratti, Heligmosomoides polygyrus, Necator americanus, and Ancylostoma ceylanicum. Prenyl-2-orcinol (4) and geranylgeranyl-2-orcinol (6) showed promising activity against newly transformed schistosomula. The compounds 1, 2, 4, 5, and 6 were also screened for antiproliferative or cytotoxic activity against two human cancer lines, viz. prostate adenocarcinoma cells (PC-3) and colorectal adenocarcinoma cells (HT-29). Compound 6 was determined to be the most effective against both cell lines with IC₅₀ values of 16.1 µM in PC-3 prostate cells and 33.7 µM in HT-29 colorectal cells.     

Energetic Bio-Activation of Some Organic Molecules and Their Antioxidant Activity in the Pulp of the Moroccan Argan Tree «Argania spinosa L.»

Argania spinosa L. Skeels is an emblematic tree in Morocco, known worldwide for its medicinal and nutritional value. Its fruits contain kernels used to prepare an edible oil, the leaves are used to feed livestock, and its wood is used as fuel. If the oil acquires high importance, the other components of the fruit of the argan are undervalued. Our objective is to invest the waste of the argan industry. Particularly, our study aimed to assess the effect of thermal activation of argan pulp on its therapeutic value, its phenolic profile and its functional and physicochemical properties. After heat treatment, the HPLC analysis for the average total phenolic content varied from 2% to 37%, depending on temperature. The antioxidant activity was increased with heat treatment. Higher values of antioxidant activity, polyphenol and pigment content were recorded at 70 °C. Functional properties analysis indicated that water solubility index and water absorption capacity were significantly affected by heat stress. Physicochemical analysis showed that moisture content, titratable acidity and soluble solids were affected.     

Solutions globales d'un problème de Cauchy linéaire

On résoud le problème de Cauchy pour des opérateurs aux dérivées partielles à coefficients polynomiaux par rapport aux variables d'espace dans des classes de Gevrey projectives. Nos résultats sont des versions globales du théorème de Cauchy-Kowalewski et du théorème de Nagumo.     

Gaussian Estimates for Random Walks on Some Unimodular p-adic Groups

It is shown in this paper that the transition kernels corresponding to simple random walks on certain unimodular solvable p-adic groups admit upper Gaussian estimates.      

Blow-up Results for Some Nonlinear Delay Differential Equations

In this work we study the blow up phenomena for some scalar delay differential equations. In particular, we make connection with the blow up of ordinary differential equations that are related to the delay differential equations. The first author is supported by a Grant from TWAS under contract No: 03-030 RG/MATHS/AF/AC. The second author is supported by a grant from the Lebanese National Council for Scientific Research.     

Intrinsic integrated optical temperature sensor based on waveguide bend loss

Curvature of a multimode integrated optical waveguide reduces the numerical aperture and induces radiation losses. In this paper, we study this phenomenon and we present a geometrical approach to calculate the local numerical aperture and the intensity attenuation. We exploit the bending effect on the local numerical aperture to make a new intrinsic temperature sensor. The simulation results are validated for the silica/silicone integrated optical case. The principal performances of the silica/silicone temperature sensor are the extended temperatures range (−50 to 200 °C) with an excellent linearity response (1%) between 20 and 200 °C.     

Synthesis and spectral properties of non-symmetrical red and near IR emitter dibenzoBODIPYs

New symmetrical and non-symmetrical benzoBODIPYs have been synthesized from diketones. For the two series the 3 and 5 positions have been substituted by different aromatic rings and onto benzo sub-units different groups have been introduced. The methodology of diketones self-condensation provides symmetrical dyes. By cross-condensation reaction, these positions can be differentiated and specific functions connected to the desired positions. These molecules have been fully characterized and their optical properties analyzed by both experimental and theoretical means. They are red to NIR emitters with a range of emission from 679 to 780?nm in CH₂Cl₂. They show maxima of absorption between 651?nm and 732?nm, strong ε of around 100,000?M^?1?cm^?1 and quite good quantum yields from 16% to 75%. The thienyl moiety on α-positions of the nitrogens generates the highest red shifts. Meanwhile dimethylamino groups in the same positions bring, besides chemical properties, proton sensitive dyes. The bromine atom onto the dibenzo sub-units exhibits good reactivity through Sonogashira coupling reactions. This approach provides multifunctional red to NIR dyes with endless possibilities of combination of chemical properties.     

Synthesis and properties of fluorinated telechelic macromolecular diols prepared by radical grafting of fluorinated thiols onto hydroxyl-terminated polybutadienes

The radical grafting of C_nF_{2n +1} CH₂CH₂SH (n = 6,8) onto the double bonds of hydroxyl-terminated liquid polybutadienes (HTPBD) was studied. Various methods for investigating the amount of grafting (titration of residual thiol and fluorine analysis) were used and compared. The nature and the amount of the initiator, the quantity of thiol, the temperature and the time of the reaction. the solvent, and the microstructure of HTPBD were optimized. The kinetic aspect showed that the thiol disappeared according to a first-norder law. A method using up to 100% of grafting fluorinated mercaptan was described and standards were set up with fluorine contents of 5–59% to evaluate the physicochemical properties of these thioether group-containing polymers: solubility, refractive index, intrinsic and dynamic viscosities, and thermal characteristics (glass transition and decomposition temperatures). Finally, the surface properties of these standards showed improvements of surface energy as low as 9 mN m^?1 for a totally saturated fluorinated HTPBD. © 1993 John Wiley & Sons, Inc.     

Seed coat metabolite profiling of cowpea (Vigna unguiculata L. Walp.) accessions from Ghana using UPLC-PDA-QTOF-MS and chemometrics

Abstract

Cowpea (Vigna unguiculata L. Walp.) is an important grain legume in Africa exhibiting high morpho-genetic diversity. However, not much information exists on the phytochemical profiles of its hulls. This study explored the metabolite profiles of seed-coats from thirteen cowpea accessions of varying phenotypes using UPLC-QTOF-MS and chemometric analysis. A total of 34 secondary metabolites were identified, which comprised phenolic acids, flavonoids, anthocyanins, sphingolipids and fatty acids. Quantification of selected phenolic compounds revealed marked variations among the cowpea accessions. The chemical profiles of the test accessions were distinguished by multivariate analysis, and the results revealed a marked influence of seed-coat pigmentation on the observed differences in their metabolite profiles. Moreover, delphinidin (traces to 2257.6 µg/g), catechin glucoside (traces to 2840.6 µg/g), catechin (traces to 2089.2 µg/g) and epicatechin (26.3 to 3222.7 µg/g) contributed to the segregation amongst the studied samples. The concentrations of the discriminant metabolites were greater in the dark seeded cowpeas compared to their lighter seeded counterparts. The findings represent a useful contribution to the literature on cowpea seed coat metabolites, and also reveal their potential for use in the development of food and pharmaceutical products.