Inhibition of LOX by flavonoids: a structure-activity relationship study

• Type: Article in International Scientific Journal
• Date: 2014

Authors

Daniela Ribeiro (Author) Other; Marisa Freitas (Author) Other; Sara M Tome (Author) Other; Artur M S Silva (Author) Other; Graca Porto (Author) Other; Eurico J Cabrita (Author) Other; Manuel M B Marques (Author) Other; Eduarda Fernandes (Author) FFUP

Journal

Title: European Journal of Medicinal Chemistry

Vol. 72

Pages: 137-145

ISSN: 0223-5234

Publisher: Elsevier

Indexing

ISI Web of Knowledge - 44 Citations

Scopus - 65 Citations

Scientific classification

FOS: Medical and Health sciences > Basic medicine

CORDIS: Health sciences

Other information

Authenticus ID: P-008-K7B

DOI: 10.1016/j.ejmech.2013.11.030

Abstract (EN): The lipoxygenase (LOX) products have been identified as mediators of a series of inflammatory diseases, namely rheumatoid arthritis, inflammatory bowel disease, psoriasis, allergic rhinitis, atherosclerosis and certain types of cancer. Hence, LOX inhibitors are of interest for the modulation of these phenomena and resolution of the inflammatory processes. During LOX activity, peroxyl radical complexes are part of the reaction and may function as sources of free radicals. Thus antioxidants, such as flavonoids, capable of inhibiting lipid peroxidation and scavenging free radicals, may act as LOX inhibitors. The aim of this work was to assess the structure activity relationship among a series of flavonoids concerning 5-LOX inhibition, through a systematic study of the inhibition of the formation of LTB4 in human neutrophils. The type of inhibition of the flavonoids was further studied using soybean LOX, type I, and Saturation Transfer Difference H-1 NMR (STD-H-1 NMR) was used to characterize the binding epitopes of the compounds to LOX-1. The obtained results reinforce flavonoids as effective inhibitors of LTB4 production in human neutrophils. It was also possible to establish a structure/activity relationship for the inhibitory activity and the type of inhibition.

Language: English

Type (Professor's evaluation): Scientific

No. of pages: 9