title: The cytotoxicity of eutigosides from Eurya emarginata against HL-60 promyelocytic leukemia cells.
abstract: Two phenolic glucosides, eutigoside B and eutigoside C were isolated from the fresh leaves of Eurya emarginata. These two phenolic glucosides exerted a significant inhibitory effect on the growth of HL-60 promyelocytic leukemia cells. Furthermore, when the HL-60 cells were treated with eutigoside C, several apoptotic characteristics such as DNA fragmentation, morphologic changes, and increase of the population of sub-G1 hypodiploid cells were observed. In order to understand the mechanism of apoptosis induction by eutigoside C, we examined the changes of Bcl-2 and Bax expression levels. The eutigoside C reduced Bcl-2 protein and mRNA levels, but slightly increased Bax protein and mRNA levels in a time-dependent manner. When we examined the activation of caspase-3, an effector of apoptosis, the eutigoside C increased the expression of active form (19-kDa) of caspase-3 and the increase of their activities was demonstrated by the cleavage of poly (ADP-ribose) polymerase, a substrate of caspase-3, to 85-kDa. The results suggest that the inhibitory effect of eutigoside C from E. emarginata on the growth of HL-60 appears to arise from the induction of apoptosis via the down-regulation of Bcl-2 and the activation of caspase.
authors.affiliation: Department of Medicine, Cheju National University, Jeju 690-756, Korea.
authors.forename: Soo Yeong
authors.initials: SY
authors.lastname: Park
authors.forename: Hong Chul
authors.initials: HC
authors.lastname: Yang
authors.forename: Ji Young
authors.initials: JY
authors.lastname: Moon
authors.forename: Nam Ho
authors.initials: NH
authors.lastname: Lee
authors.forename: Se Jae
authors.initials: SJ
authors.lastname: Kim
authors.forename: Ji Hoon
authors.initials: JH
authors.lastname: Kang
authors.forename: Young Ki
authors.initials: YK
authors.lastname: Lee
authors.forename: Deok Bae
authors.initials: DB
authors.lastname: Park
authors.forename: Eun Sook
authors.initials: ES
authors.lastname: Yoo
authors.forename: Hee Kyoung
authors.initials: HK
authors.lastname: Kang
mesh_terms: D000972:Antineoplastic Agents, Phytogenic / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects; D053148:Caspase 3; D020169:Caspases / Q000032:analysis; D003374:Coumarins; D005960:Glucosides / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D018922:HL-60 Cells / Q000187:drug effects*; D006801:Humans; D010636:Phenols / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D019253:Proto-Oncogene Proteins c-bcl-2 / Q000032:analysis; D028242:Theaceae / Q000737:chemistry*
chemical_list: D000972:Antineoplastic Agents, Phytogenic; D003374:Coumarins; D005960:Glucosides; D010636:Phenols; D019253:Proto-Oncogene Proteins c-bcl-2; C505498:eutigoside A; C505499:eutigoside C; C505407:CASP3 protein, human; D053148:Caspase 3; D020169:Caspases