Identification and Evaluation of New Potential Inhibitors of Human Neuraminidase 1 Extracted from L.: A Preliminary Study.
Fiche publication
Date publication
avril 2021
Journal
Biomedicines
Auteurs
Membres identifiés du Cancéropôle Est :
Dr DUCA Laurent, Dr BENNASROUNE Amar
Tous les auteurs :
Albrecht C, Akissi ZLE, Yao-Kouassi PA, Alabdul Magid A, Maurice P, Duca L, Voutquenne-Nazabadioko L, Bennasroune A
Lien Pubmed
Résumé
Sialidases, also called neuraminidases, are involved in several human pathologies such as neurodegenerative disorders, cancers, as well as infectious and cardiovascular diseases. Several studies have shown that neuraminidases, such as neuraminidase 1 (NEU-1), may be promising pharmacological targets. Therefore, the discovery of new selective inhibitors of NEU-1 are necessary to better understand the biological functions of this sialidase. In the present study, we describe the isolation and characterization of nine known compounds from L. leaves. This plant, known to have several therapeutic properties, belongs to the family of Poaceae and is found in the neotropics and in tropical Africa and Madagascar. Among the purified compounds, feddeiketone B, 2,3-dihydroxy-1-(4-hydroxy-3,5-diméthoxyphényl)-l-propanone, and syringylglycerol were shown to present structural analogy with DANA, and their effects on membrane NEU-1 sialidase activity were evaluated. Our results show that they possess inhibitory effects against NEU-1-mediated sialidase activity at the plasma membrane. In conclusion, we identified new natural bioactive molecules extracted from as inhibitors of human NEU-1 of strong interest to elucidate the biological functions of this sialidase and to target this protein involved in several pathophysiological contexts.
Mots clés
Elastin Receptor Complex, Olyra latifolia, natural bioactive molecules, neuraminidase 1, sialidase activity
Référence
Biomedicines. 2021 Apr 11;9(4):