Cytotoxic bufadienolides from the whole plants of Helleborus foetidus

被引:13
作者
Yokosuka, Akihito [1 ]
Iguchi, Tomoki [1 ]
Kawahata, Riko [1 ]
Mimaki, Yoshihiro [1 ]
机构
[1] Tokyo Univ Pharm & Life Sci, Sch Pharm, Dept Med Pharmacognosy, 1432-1 Horinouchi, Hachioji, Tokyo 1920392, Japan
关键词
Bufadienolides; Bufadienolide glucosides; Helleborus foetidus; Ranunculaceae; HL-60; cells; A549; Apoptosis; SPIROSTANOL GLYCOSIDES; ORIENTALIS; RHIZOMES;
D O I
10.1016/j.phytol.2017.10.017
中图分类号
Q94 [植物学];
学科分类号
071001 ;
摘要
Two new bufadienolides (1 and 2) and three known bufadienolide glucosides (3-5) were isolated from the whole plants of Helleborus foetidus (Ranunculaceae). The structures of 1 and 2 were determined spectroscopically. Compound 1 displayed potent cytotoxicity against HL-60 and A549 cells, with IC50 values of 0.035 and 0.029 mu M, respectively. HL-60 cells treated with 1displayed 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 that 1 induced HL-60 cell death via the mitochondrial-dependent apoptotic pathway.
引用
收藏
页码:94 / 99
页数:6
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