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- Title
Identification of a Prenyl Chalcone as a Competitive Lipoxygenase Inhibitor: Screening, Biochemical Evaluation and Molecular Modeling Studies.
- Authors
Zeraik, Maria Luiza; Pauli, Ivani; Dutra, Luiz A.; Cruz, Raquel S.; Valli, Marilia; Paracatu, Luana C.; de Faria, Carolina M. Q. G.; Ximenes, Valdecir F.; Regasini, Luis O.; Andricopulo, Adriano D.; Bolzani, Vanderlan S.
- Abstract
Cyclooxygenase (COX) and lipoxygenase (LOX) are key targets for the development of new anti-inflammatory agents. LOX, which is involved in the biosynthesis of mediators in inflammation and allergic reactions, was selected for a biochemical screening campaign to identify LOX inhibitors by employing the main natural product library of Brazilian biodiversity. Two prenyl chalcones were identified as potent inhibitors of LOX-1 in the screening. The most active compound, (E)-2-O-farnesyl chalcone, decreased the rate of oxygen consumption to an extent similar to that of the positive control, nordihydroguaiaretic acid. Additionally, studies on the mechanism of the action indicated that (E)-2-O-farnesyl chalcone is a competitive LOX-1 inhibitor. Molecular modeling studies indicated the importance of the prenyl moieties for the binding of the inhibitors to the LOX binding site, which is related to their pharmacological properties.
- Subjects
CHALCONE; INFLAMMATORY mediators; BINDING sites; OXYGEN consumption; CHALCONES; ANTI-inflammatory agents
- Publication
Molecules, 2021, Vol 26, Issue 8, p2205
- ISSN
1420-3049
- Publication type
Article
- DOI
10.3390/molecules26082205