Cytotoxic bufadienolides from the whole plants of Helleborus foetidus. (February 2018)

• Record Type: Journal Article
• Authors: Yokosuka, Akihito; Iguchi, Tomoki; Kawahata, Riko; Mimaki, Yoshihiro
• Is Part Of: Phytochemistry letters. Volume 23(2018)
• Page Start: 94
• Page End: 99
• Publication Date: 2018-02
• Subjects: Bufadienolides -- Bufadienolide glucosides -- Helleborus foetidus -- Ranunculaceae -- HL-60 cells -- A549 cells -- Apoptosis; Botanical chemistry -- Periodicals; Chimie végétale -- Périodiques; 572.205
• DOI: 10.1016/j.phytol.2017.10.017
• Languages: English
• ISSNs: 1874-3900

Abstract

Graphical abstract: Highlights: Two new bufadienolides and three known bufadienolide glucosides were isolated from Helleborus foetidus . The cytotoxicity of the isolated compounds against HL-60 and A549 cells were evaluated. Compound 1 induced HL-60 cell death via the mitochondrial-dependent apoptotic pathway. Abstract: Two new bufadienolides (1 and2 ) and three known bufadienolide glucosides (3 –5 ) were isolated from the whole plants of Helleborus foetidus (Ranunculaceae). The structures of1 and2 were determined spectroscopically. Compound1 displayed potent cytotoxicity against HL-60 and A549 cells, with IC50 values of 0.035 and 0.029 μM, respectively. HL-60 cells treated with1 displayed typical characteristics of apoptosis, such as nuclear chromatin condensation, DNA fragmentation, accumulation of sub-G1 cells, and marked activation of caspase-3. Moreover, the loss of mitochondrial membrane potential and release of cytochrome c into the cytosol suggested that1 induced HL-60 cell death via the mitochondrial-dependent apoptotic pathway.