Chalcones as Modulators of Neutrophil Oxidative Burst under Physiological and High Glucose Conditions

• Type: Article in International Scientific Journal
• Date: 2020

Authors

Sousa, A (Author) Other; Lucas, M (Author) Other; Ribeiro, D (Author) Other; Correia, CM (Author) Other; Silva, VLM (Author) Other; Silva, AMS (Author) Other; Eduarda Fernandes (Author) FFUP; Freitas, M (Author) Other

Journal

Title: Journal of Natural Products

Vol. 83

Pages: 3131-3140

ISSN: 0163-3864

Publisher: American Chemical Society

Indexing

ISI Web of Knowledge - 0 Citations

Scopus - 2 Citations

Other information

Authenticus ID: P-00S-Z09

DOI: 10.1021/acs.jnatprod.0c00728

Abstract (EN): Several epidemiological studies indicate that neutrophils, under hyperglycemic conditions, are involved in the perpetuation of the inflammatory status, a characteristic of diabetes mellitus, leading to the production of prodigious quantities of reactive species and the release of neutrophil extracellular traps (NETs). Accordingly, our aim was to study the ability of a panel of 25 structurally related chalcones to modulate human neutrophil oxidative burst and the production of NETs under physiological and high glucose conditions. In general, all chalcones presented similar effects under physiological and high glucose conditions. 2',4-Dihydroxy-3-methoxychalcone (3), here studied for the first time, was the most active (IC50 <= 5 mu M) on the inhibition of neutrophil oxidative burst, showing the importance of the presence of hydroxy substituents at the C-2' and C-4 positions of the A and B rings, respectively, and a 3-methoxy substituent at B ring of the chalcone scaffold. In the present experimental conditions, NETs release only occurred under high glucose levels. The pentahydroxylated chalcone 1 was the only one that was able to modulate the NETs release. This study provided important considerations about the chalcones' scaffold and their modulatory effect on human neutrophil activities at physiological and high glucose conditions, evidencing their potential use as complementary antidiabetic agents.

Language: English

Type (Professor's evaluation): Scientific

No. of pages: 10