Bufadienolides from the whole plants of Helleborus foetidus and their cytotoxicity

• Published in: Phytochemistry (Oxford) 2020-04, Vol.172, p.112277-112277, Article 112277
• Main Authors: Iguchi, Tomoki, Yokosuka, Akihito, Kawahata, Riko, Andou, Madoka, Mimaki, Yoshihiro
• Format: Article
• Language: English
• Subjects: A549 cells; Apoptosis; Bufadienolide glucosides; Bufadienolides; Bufanolides; Cytotoxicity; Glucosides; Helleborus; Helleborus foetidus; HL-60 Cells; HL-60 cells; Humans; Ranunculaceae
• ISSN: 0031-9422; 1873-3700
• DOI: 10.1016/j.phytochem.2020.112277

Two undescribed bufadienolide glucosides and four undescribed bufadienolides were isolated from the whole plants of Helleborus foetidus (Ranunculaceae). Their structures were determined by extensive spectroscopic analysis and the results of hydrolytic cleavage. The isolated compounds exhibited cytotoxic activities against HL-60 and A549 cells with IC50 values ranging from 0.019 to 3.0 μM. The isolated compounds also showed the Na+/K+ ATPase inhibitory activity. The undescribed compound 16β-formyloxy-10,14-dihydroxy-5β-[(β-d-glucopyranosyl)oxy]-19-norbufa-3,20,22-trienolide induced apoptosis in HL-60 cells through a mitochondria-dependent apoptotic pathway. Two undescribed bufadienolide glucosides and four undescribed bufadienolides were isolated from the whole plants of Helleborus foetidus (Ranunculaceae). The isolated compounds exhibited cytotoxic activities against HL-60 human leukemia cells and A549 human lung adenocarcinoma cells. [Display omitted] •Six undescribed bufadienolide derivatives were isolated from Helleborous foetidus.•Structures were determined by spectroscopic analysis and the results of hydrolysis.•Six compounds showed cytotoxicity against both HL-60 and A549 cells.•The undescribed bufadienolide glycoside induced apoptosis in HL-60 cells.