2. Academic Validation
  3. Cytotoxic Bufadienolides from the Leaves of Melianthus major

Cytotoxic Bufadienolides from the Leaves of Melianthus major

  • J Nat Prod. 2020 Jul 24;83(7):2122-2128. doi: 10.1021/acs.jnatprod.0c00060.
Kibrom Gebreheiwot Bedane 1,  Lukas Brieger,  Carsten Strohmann,  Ean-Jeong Seo 2,  Thomas Efferth 2,  Michael Spiteller
Affiliations

Affiliations

  • 1 Department of Chemistry, Addis Ababa University, P.O. Box 33658, Addis Ababa, Ethiopia.
  • 2 Department of Pharmaceutical Biology, Institute of Pharmacy and Biomedical Sciences, Johannes Gutenberg University, Staudinger Weg 5, 55128 Mainz, Germany.
PMID: 32663024 DOI: 10.1021/acs.jnatprod.0c00060
Abstract

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.

Figures