Analogs of the marine natural product scalaradial lacking the α,β-unsaturated aldehyde: effects on human synovial fluid phospholipase A2 and macrophage lipid mediator production
Autor: | Mei-Li Sung, Yeung-Wai Lock, Anthony F. Kreft, Keith B. Glaser, Dennis Kubrak, Jean Bauer |
---|---|
Rok vydání: | 1994 |
Předmět: |
chemistry.chemical_classification
Natural product biology Chemistry Stereochemistry Organic Chemistry Clinical Biochemistry Pharmaceutical Science Lipid signaling Biochemistry Aldehyde chemistry.chemical_compound Phospholipase A2 Drug Discovery biology.protein Molecular Medicine Macrophage Synovial fluid lipids (amino acids peptides and proteins) Reactivity (chemistry) Triol Molecular Biology |
Zdroj: | Bioorganic & Medicinal Chemistry Letters. 4:1873-1878 |
ISSN: | 0960-894X |
DOI: | 10.1016/s0960-894x(01)80388-7 |
Popis: | The role of the α,β-unsaturated aldehyde in the inhibition of PLA2 by scalaradial was investigated by reduction to the triol and oxidation to the diacid. The results demonstrate that the reactivity of the α,β-unsaturated aldehyde of scalaradial is not absolutely essential to its ability to inhibit PLA2 and lipid mediator production in the intact cell but adds significantly to its inhibitory potency. |
Databáze: | OpenAIRE |
Externí odkaz: |