Cytotoxic Bufadienolides from the Leaves of Melianthus major
| Autor: | Kibrom Gebreheiwot Bedane, Ean-Jeong Seo, Lukas Brieger, Carsten Strohmann, Michael Spiteller, Thomas Efferth |
|---|---|
| Rok vydání: | 2020 |
| Předmět: |
Pharmacology
biology 010405 organic chemistry Chemistry Ccrf cem Organic Chemistry Pharmaceutical Science medicine.disease biology.organism_classification 01 natural sciences Molecular biology Melianthus major 0104 chemical sciences Analytical Chemistry 010404 medicinal & biomolecular chemistry Leukemia Complementary and alternative medicine Drug Discovery medicine Ic50 values Molecular Medicine Cytotoxic T cell Breast cancer cells Cytotoxicity Two-dimensional nuclear magnetic resonance spectroscopy |
| Zdroj: | Journal of Natural Products. 83:2122-2128 |
| ISSN: | 1520-6025 0163-3864 |
| Popis: | Melianthus major is a medicinal plant endemic to South Africa. Its leaf extract led to the isolation of five new bufadienolides, 2β-acetoxy-3,5-di-O-acetylhellebrigenin (1), 2β-acetoxy-3-O-acetylhellebrigenin (2), 2β-acetoxy-14-deoxy-15β,16β-epoxymelianthugenin (4), 2β-acetoxy-14-deoxy-15β,16β-epoxymelianthusigenin (5), and 2β-hydroxymelianthusigenin (6), and four known analogues. The structures of the compounds were elucidated using NMR and HRESIMS data analyses. The relative configurations were defined by single-crystal X-ray crystallography and NOESY correlations. The isolated compounds exhibited strong cytotoxicity against MCF-7 breast cancer cells and sensitive CCRF-CEM and multidrug-resistant CEM/ADR5000 leukemia cells. Compound 1 showed the most potent activity, with IC50 values of 0.1 μM toward CCRF-CEM and CEM/ADR5000 and 0.3 μM toward MCF-7. |
| Databáze: | OpenAIRE |
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