|Reference : Effect of benzoic acid analogs on myeloperoxidase activity measured by a new technique t...|
|Scientific congresses and symposiums : Poster|
|Human health sciences : Pharmacy, pharmacology & toxicology|
Life sciences : Biochemistry, biophysics & molecular biology
|Effect of benzoic acid analogs on myeloperoxidase activity measured by a new technique to study their direct interaction with the enzyme.|
|Franck, Thierry [Université de Liège - ULg > Département clinique des animaux de compagnie et des équidés > Anesthésiologie gén. et pathologie chirurg. des grds animaux >]|
|Mazloum, Ali [ > > ]|
|Mouithys-Mickalad, Ange [Université de Liège - ULg > > Centre de l'oxygène : Recherche et développement (C.O.R.D.) >]|
|Deby-Dupont, Ginette [Université de Liège - ULg > > Centre de l'Oxygène, Recherche et Développement (CORD) > >]|
|Neven, Philippe [Université de Liège - ULg > Faculté de Pharmacie > Laboratoire de pharmacologie > >]|
|Serteyn, Didier [Université de Liège - ULg > Département clinique des animaux de compagnie et des équidés > Anesthésiologie gén. et pathologie chirurg. des grds animaux >]|
|The 7th International Human Peroxidase Meeting|
|22-25 May, 2011|
|[en] SIEFED ; Myeloperoxidase activity ; pharmacological tool ; Benzoic acid ; gallic acid|
|[en] Myeloperoxidase (MPO) plays a key role in inflammatory response and constitutes a target for new drug development. The effects of some benzoic acid analogs were studied on the specific activity of human MPO measured by SIEFED (“Specific Immunologic Extraction Followed by Enzymatic Detection”), an original method that consists of incubation of the compound with MPO, followed by capture of the enzyme by specific antibodies, washing (elimination of the compounds) and enzymatic detection of the immunocaptured enzyme. The compounds tested at 10-4, 10-5 and 10-6 M were studied in terms of structure activity relationship.
Gallic acid (3,4,5-trihydroxybenzoic acid) with 3 hydroxyl groups had an important dose dependent inhibitory effect on MPO activity. Other molecules with less or without hydroxyl groups [3,4-dihydroxybenzoic acid, 2-hydroxybenzoic acid (salicylic acid) and benzoic acid] had rather an activator effect at 10-5 and 10-6 M. 2,4,6-Trihydroxybenzoic acid, with two hydroxyl groups adjacent to the carboxyl group, had a less efficient inhibitory effect. Caffeic acid (3,4-dihydroxycinnamic acid) with a propenoic acid group presented a dose dependent inhibitory effect on MPO activity contrary to its analog 3,4-dihydroxybenzoic acid. The esterification of the carboxyl group of gallic acid to obtain propyl gallate induced an activation of MPO at 10-5 and 10-6 M. Finally, the substitution of one or two hydroxyl groups by methoxyl ones (ferulic and syringic acids) decreased the efficiency of the molecules on the enzyme inhibition.
The SIEFED technique appears as an innovative pharmacological tool to study the direct interaction of compounds with MPO. Number and position of hydroxyl groups and the extension of the carboxyl group of benzoic acid play a crucial role in the inhibition of MPO activity probably by facilitating the interaction with the active site or another elements of the enzyme structure.
|Centre de l’Oxygène, Recherche et Développement - CORD|
|This work was supported by a research grant from the "Region Wallonne"|
|Researchers ; Professionals ; Students|
|SIEFED is protected by an international patent (WO/2005/075986)|
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