Isolation and characterization of aromatase inhibitors from Brassaiopsis glomerulata (Araliaceae)
| Autor: | Bin Su, A. Douglas Kinghorn, Soedarsono Riswan, John M. Pezzuto, Robert W. Brueggemeier, Harry H. S. Fong, Marcy J. Balunas |
|---|---|
| Rok vydání: | 2009 |
| Předmět: |
chemistry.chemical_classification
biology medicine.medical_treatment Linoleic acid Ethyl acetate Fatty acid Plant Science biology.organism_classification Biochemistry Article Steroid chemistry.chemical_compound Enzyme chemistry Brassaiopsis glomerulata biology.protein medicine Araliaceae Aromatase Agronomy and Crop Science Biotechnology |
| Zdroj: | Phytochemistry Letters. 2:29-33 |
| ISSN: | 1874-3900 |
| DOI: | 10.1016/j.phytol.2008.10.009 |
| Popis: | The hexane- and ethyl acetate-soluble extracts of the leaves of Brassaiopsis glomerulata (Blume) Regel (Araliaceae), collected in Indonesia, were found to inhibit aromatase, the rate-limiting enzyme in the production of estrogens from androgens, in both enzyme- and cell-based aromatase inhibition (AI) assays. Bioassay-guided fractionation led to the isolation of six known compounds of the steroid and triterpenoid classes (1-6) from the hexane extract, of which 6β-hydroxystimasta-4-en-3-one (5), was moderately active in the cell-based AI assay. Fractionation of the ethyl acetate extract afforded seven pure isolates (7-13) of the modified peptide, fatty acid, monoterpenoid, and benzenoid types, including six known compounds and the new natural product, N-benzoyl-L-phenylalanine methyl ester (9). The absolute stereochemistry of 9 and the other two peptides, 7 and 8, was determined by Marfey's analysis. Linoleic acid (10) was found to be active in the enzyme-based AI assay, while 9 and (-)-dehydrololiolide (12) showed activity in the cell-based AI assay. |
| Databáze: | OpenAIRE |
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