dr. Antonio Cala's seminar
Giovedì, 05 Luglio 2018 dalle ore 11:00 alle ore 12:00
Room 6302 - PRC building
Active Dihydrochalcones from APple Trees (ADAPT): towards added value to Anjou apple production - a mirror project to ExPoApple
ABSTRACT: Apples have a good image, often associated to an “healthy” fruit. Apple trees (Malus x domestica Brokh.) are widely cultivated all around the world, whereas apple is the first fruit produced in Europe. In France, the “Région des Pays de la Loire” appears as the second national producer of apples, apple trees being the main cultivated surfaces in this area. Natural products have a long history of providing important medicinal agents or inspiring the development of new drugs. Here our project ADAPT is focused on dihydrochalcones (DHCs), a class of secondary metabolites characteristically produced by apple trees with a limited occurrence in the rest of the plant kingdom and generally described as a class of minor flavonoids. Nevertheless, some recent studies have shown that some DHCs exhibit significant pharmacological effects (anti-inflammatory, anti-tumoral). Unfortunately, as the DHCs are mainly found in the peel, seeds and core of the fruit (and in leaves), most of the apple DHCs are not ingested when eating an apple, especially if fruits are eaten peeled. ADAPT aims first at identifying relevant biological targets for DHCs through a virtual (i.e. computer-aided) screening approach. During ADAPT project, a close collaboration along with fruitful discussions will help modeling chemists and organic chemists to go through a second stage dedicated to the in silico optimization of the previously identified hits and to the rankings of the potential ligands based on their calculated affinity with the biological targets. IRHS-ResPom (INRA) will provide selected apple trees leaves from a local production. SONAS will extract and purify natural DHCs from this renewable natural source to use them as starting materials for the chemical synthesis. SONAS will then embark on the (semi-)synthesis of the most promising compounds. Biological evaluation will then be conducted with all the (semi-)synthesized structures. ADAPT will thus increase the knowledge associated to dihydrochalcones and their biological activities. Previously reported studies on the significant but under-exploited pharmacological profile of this class of secondary metabolites and the expertise of the partners in medicinal chemistry, more specifically in the development of new anti-inflammatory agents, give to ADAPT a great rate of success.
HOST: Stefan Martens