Bufadienolides from the whole plants of Helleborus foetidus and their cytotoxicity.

Affiliation

Department of Medicinal Pharmacognosy, School of Pharmacy, Tokyo University of Pharmacy and Life Sciences, 1432-1 Horinouchi, Hachioji, Tokyo, 192-0392, Japan. Electronic address: [Email]

Abstract

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.

Keywords

A549 cells,Apoptosis,Bufadienolide glucosides,Bufadienolides,Cytotoxicity,HL-60 cells,Helleborus foetidus,Ranunculaceae,

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