Acide acétylsalicylique

L’acide acétylsalicylique (AAS), plus connu sous le nom commercial d’aspirine, est un anti-inflammatoire non stéroïdien. C’est la substance active de nombreux médicaments aux propriétés antalgiques, antipyrétiques et anti-inflammatoires. Il est surtout utilisé comme antiagrégant plaquettaire. C’est un acide faible, dont la base conjuguée est l’anion acétylsalicylate. C’est un des médicaments les plus consommés au monde. Étymologie L’acide acétylsalicylique est obtenu par acétylation de l’acide salicylique. Son nom vient du latin salix, « saule », cet acide ayant été isolé pour la première fois dans l’écorce de cette essence d’arbre. L’appellation aspirine vient d'Aspirin enregistrée comme nom de marque le par la société Bayer à Berlin. Le nom de marque a été formé à partir des éléments suivants :

Le préfixe A pour Acétyl, l'acétylation rendant ce métabolite secondaire de plantes toxique (son activité allélopathique leur sert de défense chimique contre les herbivore

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A Strategy to Conjugate Bioactive Fragments to Cytotoxic Diiron Bis(cyclopentadienyl) Complexes

Paul Joseph Dyson, Mouna Hadiji, Silvia Schoch

A series of bioactive molecules were synthesized from the condensation of aspirin or chlorambucil with terminal alkynes bearing alcohol or amine substituents. Insertion of the resulting alkynes into the iron-carbyne bond of readily accessible diiron bis(cyclopentadienyl) mu-aminocarbyne complexes, [1a,b]CF3SO3, afforded novel diiron complexes with a bridging vinyliminium ligand, [2-10]CF3SO3, functionalized with a bioactive moiety. All compounds were characterized by elemental analysis and IR and multinuclear NMR spectroscopy and in three cases by single-crystal X-ray diffraction. Moreover, the D2O solubility, stability in D2O and cell culture media, and octanol-water partition coefficients of diiron complexes were determined spectroscopically. The cytotoxicity of the complexes was assessed in the tumorigenic A2780 and A2780cisR and the nontumorigenic HEK 293T cell lines. Some complexes exhibit high potency and the ability to overcome resistance in A2780cisR cells (aspirin complexes) or high selectivity relative to HEK 293T cells (chlorambucil complexes). Further studies indicate that the complexes significantly trigger intracellular ROS production, irrespective of the nature of the bioactive fragment. DNA alkylation and protein binding studies were also undertaken.

AMER CHEMICAL SOC2021

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Combination therapy using aspirin-enhanced photodynamic selective drug delivery

Elodie Debefve, Hubert van den Bergh

In photodynamic therapy (PDT), excitation of a drug by light leads to a cascade of biochemical processes that can cause closure of blood vessels. It has been observed clinically that significant short-term leakage from the irradiated vasculature can occur prior to vessel closure and blood flow stasis. In this paper we demonstrate in a chicken embryo model that this leakage can be significantly enhanced by the presence of the cyclo-oxygenase inhibitor, aspirin. We also observe that following this aspirin-enhanced leakage, blood vessels close as effectively as after PDT in the absence of aspirin. Consequently we propose that this PDT-induced aspirin-enhanced leakage can be used to locally deliver a drug for combination therapy. This is then demonstrated in the chicken embryo using Visudyne as a PDT agent in combination with aspirin and fluorescein isothiocyanate dextran 10 kDa as leakage indicator. The latter represents a hypothetical drug to be delivered in various kinds of combination therapy. Two examples of this procedure would be the photodynamic treatment of choroidal neovasculature associated with exudative age-related macular degeneracy (AMD) where local delivery of an anti-angiogenic or an anti-inflammatory drug has been shown to be effective, or PDT of cancer where local dosing of a chemotherapeutic drug may well increase the treatment efficacy.

Elsevier2007

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Arene ruthenium and pentamethylcyclopentadienyl rhodium and iridium complexes containing N,O-chelating ligands derived from piroxicam: Synthesis, molecular structure and cytotoxicity

Paul Joseph Dyson, Tina Riedel

The non-steroidal anti-inflammatory and anti-arthritic drug piroxicam (LH) reacts with arene ruthenium dichloride dimers in refluxing dichloromethane to give the complexes [(eta(6)-arene)Ru(eta(2)-N,O-L)Cl] (3: arene = C6H5Me, 4: arene = p-MeC6H4Pri, 5: arene = C6Me6). The reaction seems to proceed via the intermediates [(eta(6)-arene)Ru(N-LH)Cl-2], which can be observed for arene = C6H5Me (1) and isolated in the case of arene = p-MeC6H4Pri (2). The analogous reaction with pentamethylcyclopentadienyl rhodium and iridium gives the complexes [(eta(5)-C5Me5)M(eta(2)-N,O-L)Cl] (6: M = Rh, 7: M = Ir). The single-crystal X-ray structure analyses of the p-cymene ruthenium derivatives 4 and 2 show the metal atom in the archetypical piano stool geometry; in 4 the piroxicamato ligand is coordinated in a bidentate fashion through the pyridine nitrogen atom and the enolic oxygen atom, while in 2 the intact piroxicam ligand is coordinated in a monodentate fashion through the pyridine nitrogen atom. The piroxicamato complexes 3-5 are weakly cytotoxic towards human ovarian cancer cells. (C) 2013 Elsevier B.V. All rights reserved.

Elsevier2014

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