A5018497910- Antioxidant Activity and Oxidative Stress
- Synthesis of Organic Compounds
- Bioactive Compounds and Antitumor Agents
- Retinoids in leukemia and cellular processes
- Free Radicals and Antioxidants
- Synthesis and biological activity
- Circadian rhythm and melatonin
- Marine Sponges and Natural Products
- Chemical Synthesis and Analysis
- Synthetic Organic Chemistry Methods
- Natural Compound Pharmacology Studies
- Organic Chemistry Cycloaddition Reactions
- Synthesis and Reactions of Organic Compounds
- Crystallization and Solubility Studies
- X-ray Diffraction in Crystallography
- Natural product bioactivities and synthesis
- Multicomponent Synthesis of Heterocycles
- Molecular spectroscopy and chirality
- Phytochemistry and Biological Activities
- Estrogen and related hormone effects
- Inflammatory mediators and NSAID effects
- Vitamin C and Antioxidants Research
- Hydrogels: synthesis, properties, applications
- Synthesis and Characterization of Pyrroles
- Receptor Mechanisms and Signaling
Université d'Angers
2016-2024
Institut des Sciences Moléculaires
2017-2021
Université Bretagne Loire
2018
Centre National de la Recherche Scientifique
2007-2017
Université d'Orléans
2016-2017
Université de Bordeaux
2017
Institut de Chimie Organique et Analytique
2016-2017
Génétique Moléculaire Génomique Microbiologie
2014
Université de Rouen Normandie
2013
Nantes Université
2007-2013
Abstract Systemic vitamin E metabolites have been proposed as signaling molecules, but their physiological role is unknown. Here we show, by library screening of potential human metabolites, that long-chain ω-carboxylates are potent allosteric inhibitors 5-lipoxygenase, a key enzyme in the biosynthesis chemoattractant and vasoactive leukotrienes. 13-((2 R )-6-hydroxy-2,5,7,8-tetramethylchroman-2-yl)-2,6,10-trimethyltridecanoic acid (α-T-13′-COOH) can be synthesized from α-tocopherol...
Background and Purpose The paradigm that GPCRs are able to prolong or initiate cellular signalling through intracellular receptors recently emerged. Melatonin binds G protein‐coupled MT 1 2 receptors. In contrast most other hormones targeting GPCRs, melatonin its synthetic analogues amphiphilic molecules easily penetrating into cells, but the existence of is still unclear mainly due a lack appropriate tools. Experimental Approach We therefore designed synthesized series hydrophilic receptor...
Whether chemists or biologists, researchers dealing with metabolomics require tools to decipher complex mixtures. As a part of and initially dedicated identifying bioactive natural products, dereplication aims at reducing the usual time-consuming process known compounds isolation. Mass spectrometry nuclear magnetic resonance are most commonly reported analytical during analysis. Though it has low sensitivity, 13C NMR many advantages for such study. Notably, is nonspecific allowing...
Abstract The synthesis of new derivatives embelin, a natural inhibitor X‐linked apoptosis protein (XIAP) is described. design these molecules involved introduction aromatic groups directly linked to the benzoquinone core. To allow large flexibility in nature and length added chain, strategy involves first aSuzuki–Miyaura reaction with functionalized aromatics, yielding generation molecules. Then, by appropriate use functional groups, second representative embelin was prepared.
Testing libraries of phenylboronic acid derivatives and diols revealed a new crosslinking couple for the formation viscoelastic hydrogels with tunable properties long-term stability.
The synthesis and applications of the first water-soluble benzene derivative bearing a set three different orthogonal bioconjugatable groups (aminooxy, azido thiol) are described. combined use 5-amino isophthalic acid scaffold unusual acid-labile protecting for temporarily masking aminooxy thiol moieties has enabled development highly convergent approach towards such trivalent bioconjugation platform in good yields. potential utility this "ready-to-use" cross-linking reagent creating complex...
Over the last twenty years, tocotrienol analogues raised great interest because of their higher level and larger domain biological activities when compared with tocopherols. Amongst most promising therapeutic application, anti-inflammatory potency has been evaluated through inhibition various mediators inflammation. Here, we worked on isolation two natural isoforms garcinoic acid (i.e., <i>δ</i> <i>γ</i>) from different sources, respectively, <i>Garcinia kola</i> seeds amplexicaulis</i>...
Abstract The efficient synthesis of novel polyhydroxy‐tetrahydropyrano‐pyrroles from acetylenic carbohydrate precursors in three to four steps is described. methodology involves, as key steps, the ring contraction pyridazine intermediates obtained by an inverse‐demand Diels–Alder reaction and subsequent intramolecular lactonization. (© Wiley‐VCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2007)
Naturally occurring substances are valuable resources for drug development. In this respect, chalcones known to be antiproliferative agents against prostate cancer cell lines through various mechanisms or targets. Based on the literature and preliminary results, we aimed study optimise efficiency of a series inhibit androgen-converting AKR1C3, promote cancer. A total 12 with different substitution patterns were synthesised. Structure-activity relationships associated these modifications...
Endogenous long-chain metabolites of vitamin E (LCMs) mediate immune functions by targeting 5-lipoxygenase (5-LOX) and increasing the systemic concentrations resolvin E3, a specialized proresolving lipid mediator. SAR studies on semisynthesized analogues highlight α-amplexichromanol (
Embelin is a natural product, inhibitor of XIAP (X-chromosome-linked Inhibitor APoptosis) with strong proapoptotic properties on cancer cells. In order to clarify the role two OH groups benzoquinone core, we have prepared by hemisynthesis close analogs embelin, where these been replaced in systematic manner OMe and OAc groups. Proapoptotic activities six embelin derivatives studied as single agent, or combination TRAIL, their abilities interact evaluated Surface Plasmon Biacore. Our results...
Fluorescent melatoninergic ligands have been designed by associating the 4-azamelatonin with different fluorophores.
Recent studies have highlighted the biological potential of tocotrienols, a vitamin E subfamily. The major natural sources tocotrienols are complex mixtures requiring particularly challenging purification processes. present study describes efficient semi-synthetic strategies toward relevant δ-( R)-tocotrienol derivatives, using as starting material R)-garcinoic acid, derivative isolated from Garcinia kola nuts, renewable vegetal source.
Abstract A selection of bioactive polyphenols different structural classes, such as the ellagitannins vescalagin and vescalin, flavanoids catechin, epicatechin, epigallocatechin gallate (EGCG), procyanidin B2, stilbenoids resveratrol piceatannol, were chemically modified to bear a biotin unit for enabling their immobilization on streptavidin‐coated sensor chips. These chips used evaluate in real time by surface plasmon resonance (SPR) interactions three surface‐bound polyphenolic ligands per...
Phytochemical investigation of the root extracts Hypericum perforatum led to isolation two biphenyl derivatives named hyperbiphenyls A and B (1 2) four known xanthones (3–6). These structures were elucidated by spectroscopic spectrometric methods including UV, NMR, HRMS. The absolute configuration was defined different approaches: biomimetic total synthesis racemic hyperbiphenyl followed 1H 19F NMR Mosher's esters analysis stereoselective B, permitting assignment S for both compounds....
Abstract New 5‐substituted vitamin E derivatives were semisynthesized, and their antibacterial activity against human Gram‐positive Gram‐negative pathogens was evaluated. Several analogues active methicillin‐resistant Staphylococcus aureus (MRSA) and/or epidermidis (MRSE); structure‐activity relationships (SARs) are discussed. As a result, it is shown that the presence of carboxylic acid function at C‐5 position end side chain crucial for activity. The bactericidal or bacteriostatic action...
Discovering new solutions for crop protection is a major challenge the next decades as result of ecotoxicological impact classical fungicides, emergence fungicide resistances, and consequence climate change on pathogen distribution. Previous work fungal mutants deficient in unfolded protein response (UPR) supported that targeting this pathway promising plant disease control strategy. In particular, we showed UPR involved virulence by altering cell against host defense compounds, such...