A study towards drug discovery for the management of type 2 diabetes mellitus through inhibition of the carbohydrate-hydrolyzing enzymes alpha-amylase and alpha-glucosidase by chalcone derivatives

• Type: Article in International Scientific Journal
• Date: 2019

Authors

Rocha, S (Author) Other; Sousa, A (Author) Other; Ribeiro, D (Author) Other; Correia, CM (Author) Other; Silva, VLM (Author) Other; Santos, CMM (Author) Other; Silva, AMS (Author) Other; Araujo, AN (Author) FFUP; Eduarda Fernandes (Author) FFUP; Freitas, M (Author) Other

Journal

Title: Food and Function

Vol. 10

Pages: 5510-5520

ISSN: 2042-6496

Publisher: Royal Society of Chemistry

Indexing

ISI Web of Knowledge - 1 Citation

Scopus - 11 Citations

Other information

Authenticus ID: P-00R-363

DOI: 10.1039/c9fo01298b

Abstract (EN): The inhibition of carbohydrate-hydrolyzing enzymes, alpha-amylase and alpha-glucosidase, is one of the major therapeutic strategies for the treatment of type 2 diabetes mellitus. Chalcones have been recognized for their multiple biological activities, including antidiabetic properties, through unclear mechanisms. In the present work, a panel of chalcones bearing hydroxy, methoxy, methyl, nitro, chloro, fluoro and bromo substituents were evaluated against alpha-amylase and alpha-glucosidase activities, most of them for the first time. The results showed that the substitution patterns and the type of substituents of chalcones influence their inhibitory activity. The presence of hydroxy groups at C-2 '- and C-4 ' of the A ring and at C-3 and C-4 of the B ring favors the intended effect. Chalcones holding nitro groups and chloro substituents, together with a hydroxy group in the chalcone scaffold, showed strong inhibition of the alpha-glucosidase activity. The present study provides related scaffolds that may serve as the basis for the design and synthesis of new structures in order to obtain the ideal antidiabetic chalcone.

Language: English

Type (Professor's evaluation): Scientific

No. of pages: 11