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Potent Apoptosis-Inducing Activity of Erypoegin K, an Isoflavone Isolated From Erythrina Poeppigiana, Against Human Leukemia HL-60 Cells

Potent Apoptosis-Inducing Activity of Erypoegin K, an Isoflavone Isolated From Erythrina Poeppigiana, Against Human Leukemia HL-60 Cells

Kiyomi Hikita, Natsuki Hattori, Aya Takeda, Yuko Yamakage, Rina Shibata, Saori Yamada, Kuniki Kato, Tomiyasu Murata, Hitoshi Tanaka, Norio Kaneda

J Nat Med. 2018 Jan;72(1):260-266.

PMID: 29151157

Abstract:

Erypoegin K is an isoflavone isolated from the stem bark of Erythrina poeppigiana. It contains a furan group at the A-ring of the core isoflavone structure and can inhibit the activity of glyoxalase I, an enzyme that catalyzes the detoxification of methylglyoxal (MG), a by-product of glycolysis. In the present study, we found that erypoegin K has a potent cytotoxic effect on human leukemia HL-60 cells. Its cytotoxic effect was much stronger than that of a known glyoxalase I inhibitor S-p-bromobenzylglutathione cyclopentyl diester. Conversely, erypoegin K demonstrated weak cytotoxicity toward normal human peripheral lymphocytes. The treatment of HL-60 cells with erypoegin K significantly induced caspase-3 activity, whereas the pretreatment of the cells with caspase-3 inhibitor suppressed erypoegin K-induced cell death. Furthermore, nuclear condensation and apoptotic genome DNA fragmentation were observed in erypoegin K-treated HL-60 cells. These results indicated that the observed cell death was mediated by apoptosis. In addition, the toxic compound MG was highly accumulated in the culture medium of erypoegin K-treated HL-60 cells, suggesting that cell apoptosis was triggered by extracellular MG. The present study showed that erypoegin K has a potent apoptosis-inducing effect on cancerous cell lines, such as HL-60.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP166038002	S-p-Bromobenzylglutathione cyclopentyl diester		166038-00-2	Price

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