Probing sponge-derived terpenoids for human 15-lipoxygenase inhibitors
| Autor: | Jennifer Carroll, Phillip Crews, Erika N. Jonsson, Michael S. Hartman, Theodore R. Holman, Rainer Ebel |
|---|---|
| Rok vydání: | 2001 |
| Předmět: |
Jaspaquinol
biology Molecular Structure Chemistry Stereochemistry Terpenes Organic Chemistry Aplysinellidae Jaspis splendens Stereoisomerism biology.organism_classification Terpenoid Porifera Sponge Inhibitory Concentration 50 Structure-Activity Relationship Lipoxygenase Inhibitors Ic50 values Animals Humans IC50 |
| Zdroj: | The Journal of organic chemistry. 66(21) |
| ISSN: | 0022-3263 |
| Popis: | A human 15-lipoxygenase (15-HLO) assay has been employed to discover new marine-sponge-derived bioactive compounds. Extracts from two different sponges, Jaspis splendens (order Choristida, family Jaspidae) and Suberea sp. (order Verongida, family Aplysinellidae), exhibited potent IC(50) values of 0.4 and 0.1 microg/mL, respectively. Both are sources of terpenoids, and the former is a known source of (+)-jasplakinolide (7), which is inactive as a 15-HLO inhibitor. The terpenoids included (+)-(5S,6S)-subersin (1, IC(50)100 microM), (-)-(5R,10R)-subersic acid (2, IC(50) = 15 microM), jaspaquinol (3, IC(50) = 0.3 microM), and (-)-jaspic acid (4, IC(50) = 1.4 microM). Structure elucidations and lipoxygenase activity studies of these compounds are reported. |
| Databáze: | OpenAIRE |
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