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2013-06-30 - Colloque/Présentation - poster - Anglais - 1 page(s)

Pardo Antonelle , Mespouille Laetitia , Dubois Philippe , Blankert Bertrand , Duez Pierre , "Molecularly imprinted polymers: Towards receptor mimics for drug discovery" in 24th International Symposium on Pharmaceutical and Biomedical Analysis, Bologne, Italie, 2013

  • Codes CREF : Chimie des polymères de synthèse (DI131C), Chimie analytique (DI1314), Pharmacognosie (DI3410), Sciences pharmaceutiques (DI3400), Techniques séparatives (DI2729)
  • Unités de recherche UMONS : Analyse pharmaceutique (M130), Chimie thérapeutique et Pharmacognosie (M136), Matériaux Polymères et Composites (S816)
  • Instituts UMONS : Institut de Recherche en Science et Ingénierie des Matériaux (Matériaux), Institut des Sciences et Technologies de la Santé (Santé)

Abstract(s) :

(Anglais) Molecularly Imprinted Polymers (MIPs) are based on the molecular recognition properties of synthetic cross-linked materials owing to the introduction of template molecule during the formation of the polymeric 3D structure. In the field of drug discovery, molecularly imprinted polymers have the potential to play an important role as receptor mimics [1,2,3]. However, imprinted cavities with high rigidity don’t allow to mimic the flexibility and mobility exhibited by receptor/enzyme binding pockets. In order to find a compromise between flexibility and rigidity, quercetin imprinted polymers (Qu MIPs) (Fig. 1) were prepared by modifying the synthesis reagents composition. Corresponding control polymers (non-imprinted polymers, NIPs), formulated in a similar fashion, without introduction of the quercetin template molecule, were produced, treated and studied similarly to MIPs. Quercetin was chosen as a representative template considering it is one of the most active compounds in the flavonoids family and is commonly found in medicinal and food herbal products. The Qu MIPs were evaluated as sorbents for SPE and HPLC in order to confirm the presence of imprinted cavities and to evaluate their selectivity, respectively. Three different polymerization methods were investigated to obtain optimal chromatographic materials: bulk polymerization (BP), precipitation polymerization (PP) and suspension polymerization (SP) in a perfluorocarbon liquid. Particles size and shape were characterized by scanning electron microscopy (SEM). The micrographs obtained by SEM revealed the large distribution of sizes and the irregular shape of particles prepared by BP. On the contrary, spherical beads with a well-controlled size distribution were obtained by PP and SP indicating better perspectives for their use in chromatography. The performances of MIPs-SPE relatively to NIPs-SPE were defined by the Imprinting Effect (IF = Rate of quercetin retention on the MIP / Rate of quercetin retention on the NIP). Successful imprinting of the MIPs is confirmed when the retention appears distinctly superior on MIPs than on NIPs. The best IF values (up to 5) were obtained for MIPs prepared by the SP method. The MIPs were packed into HPLC columns in order to study their selectivity towards a set of analogues and non-analogues of quercetin. Thanks to the improved chromatographic efficiency afforded by SP, the developed MIPs are highly promising for the screening of lead compounds from complex systems such as natural products.


Mots-clés :
  • (Anglais) Molecularly Imprinted Polymers
  • (Anglais) Solid-phase extraction
  • (Anglais) Screening
  • (Anglais) Pharmaceutical analysis
  • (Anglais) Molecular recognition