Kinetics of ultrasound-assisted extraction of antioxidant polyphenols from food by-products: Extraction and energy consumption optimization.

Ultrasound-assisted extraction (UAE) of antioxidant polyphenols from chicory grounds was studied in order to propose a suitable valorization of this food industry by-product. The main parameters influencing the extraction process were identified. A new mathematical model for multi-criteria optimization of UAE was proposed. This kinetic model permitted the following and the prediction of the yield of extracted polyphenols, the antioxidant activity of the obtained extracts and the energy consumption during the extraction process in wide ranges of temperature (20-60°C), ethanol content in the solvent (0-60% (vol.) in ethanol-water mixtures) and ultrasound power (0-100W). After experimental validation of the model, several simulations at different technological restrictions were performed to illustrate the potentiality of the model to find the optimal conditions for obtaining a given yield within minimal process duration or with minimal energy consumption. The advantage of ultrasound assistance was clearly demonstrated both for the reduction of extraction duration and for the reduction of energy consumption.

4-Oxo-1,4-dihydropyridines as selective CB2 cannabinoid receptor ligands: structural insights into the design of a novel inverse agonist series.

Growing evidence shows that CB(2) receptor is an attractive therapeutic target. Starting from a series of 4-oxo-1,4-dihydroquinoline-3-carboxamide as selective CB(2) agonists, we describe here the medicinal chemistry approach leading to the development of CB(2) receptor inverse agonists with a 4-oxo-1,4-dihydropyridine scaffold. The compounds reported here show high affinity and potency at the CB(2) receptor while showing only modest affinity for the centrally expressed CB(1) cannabinoid receptor. Further, we found that the functionality of this series is controlled by its C-6 substituent because agonists bear a methyl or a tert-butyl group and inverse agonists, a phenyl or 4-chlorophenyl group, respectively. Finally, in silico studies suggest that the C-6 substituent could modulate the conformation of W6.48 known to be critical in GPCR activation.