Cytotoxic Bufadienolides from the Leaves of Melianthus major.
Kibrom Gebreheiwot BedaneLukas BriegerCarsten StrohmannEan-Jeong SeoThomas EfferthMichael SpitellerPublished in: Journal of natural products (2020)
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.
Keyphrases
- breast cancer cells
- high resolution
- multidrug resistant
- south africa
- induced apoptosis
- adverse drug
- cell cycle arrest
- magnetic resonance
- electronic health record
- bone marrow
- drug resistant
- solid state
- acinetobacter baumannii
- hiv positive
- gram negative
- emergency department
- endoplasmic reticulum stress
- molecular docking
- staphylococcus aureus
- oxidative stress
- big data
- klebsiella pneumoniae
- pseudomonas aeruginosa
- signaling pathway
- machine learning
- dual energy
- escherichia coli
- computed tomography
- human immunodeficiency virus
- cell death
- molecular dynamics simulations
- men who have sex with men
- artificial intelligence