Back to Search
Start Over
Evaluation of hyperforin analogues for inhibition of 5-lipoxygenase.
- Source :
-
Medicinal chemistry (Shariqah (United Arab Emirates)) [Med Chem] 2005 May; Vol. 1 (3), pp. 287-91. - Publication Year :
- 2005
-
Abstract
- The acylphloroglucinol hyperforin, a constituent of the herb Hypericum perforatum (St. John's wort), was recently identified as potent and direct inhibitor of 5-lipoxygenase (5-LO), the key enzyme in the biosynthesis of proinflammatory leukotrienes. In this study, naturally occurring analogues of hyperforin, isolated from H. perforatum, as well as a series of synthetic derivatives obtained by chemical modification of hyperforin by acylation, alkylation or oxidation, were analysed for the inhibition of 5-LO. The efficacies of these compounds were evaluated in intact human polymorphonuclear leukocytes, but also the inhibitory effects on isolated recombinant human 5-LO were investigated. Our data show that some of the oxidised hyperforin derivatives possess even improved efficacy, whereas alkylation and acylation have detrimental effects.
- Subjects :
- Bridged Bicyclo Compounds chemistry
Cells, Cultured
Enzyme Inhibitors isolation & purification
Humans
Neutrophils drug effects
Neutrophils enzymology
Phloroglucinol chemistry
Enzyme Inhibitors chemistry
Enzyme Inhibitors pharmacology
Hypericum chemistry
Lipoxygenase Inhibitors
Phloroglucinol analogs & derivatives
Terpenes chemistry
Subjects
Details
- Language :
- English
- ISSN :
- 1573-4064
- Volume :
- 1
- Issue :
- 3
- Database :
- MEDLINE
- Journal :
- Medicinal chemistry (Shariqah (United Arab Emirates))
- Publication Type :
- Academic Journal
- Accession number :
- 16787324
- Full Text :
- https://doi.org/10.2174/1573406053765503