Structure–activity relationship studies of flavonoids as potent inhibitors of human platelet 12-hLO, reticulocyte 15-hLO-1, and prostate epithelial 15-hLO-2
| Autor: | Silvia Sepúlveda-Boza, Yesseny Vásquez-Martínez, Rachana V. Ohri, Theodore R. Holman, Victor Kenyon |
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| Rok vydání: | 2007 |
| Předmět: |
Male
Models Molecular Reticulocytes Clinical Biochemistry Flavonoid Drug Evaluation Preclinical Pharmaceutical Science Arachidonate 12-Lipoxygenase Biochemistry Isozyme Article Inhibitory Concentration 50 Structure-Activity Relationship chemistry.chemical_compound Lipoxygenase Drug Discovery Arachidonate 15-Lipoxygenase Humans Potency Structure–activity relationship Lipoxygenase Inhibitors Molecular Biology IC50 Flavonoids chemistry.chemical_classification Molecular Structure biology Chemistry Organic Chemistry Prostate Epithelial Cells Stereoisomerism Isoflavones Isoenzymes Enzyme inhibitor biology.protein Molecular Medicine |
| Zdroj: | Bioorganic & Medicinal Chemistry. 15:7408-7425 |
| ISSN: | 0968-0896 |
| Popis: | Human lipoxygenase (hLO) isozymes have been implicated in a number of disease states and have attracted much attention with respect to their inhibition. One class of inhibitors, the flavonoids, have been shown to be potent lipoxygenase inhibitors but their study has been restricted to those compounds found in nature, which have limited structural variability. We have therefore carried out a comprehensive study to determine the structural requirements for flavonoid potency and selectivity against platelet 12-hLO, reticulocyte 15-hLO-1, and prostate epithelial 15-hLO-2. We conclude from this study that catechols are essential for high potency, that isoflavones and isoflavonones tend to select against 12-hLO, that isoflavons tend to select against 15-hLO-1, but few flavonoids target 15-hLO-2. |
| Databáze: | OpenAIRE |
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