title: Antitumor effect of resorcinol derivatives from the roots of Ardisia brevicaulis by inducing apoptosis.
abstract: Two new resorcinol derivatives 2-methoxy-4-hydroxy-6-(8Z-pentadecenyl)-benzene-1-O-acetate (1) and 2-methoxy-4-hydroxy-6-pentadecyl-benzene-1-O-acetate (2), together with four known compounds 2-methoxy-4-hydroxy-6-tridecyl-benzene-1-O-acetate (ardisiphenol D, 3), 5-(8Z-pentadecenyl)resorcinol (4), 5-pentadecylresorcinol (5), 5-tridecylresorcinol (6), have been isolated from the roots of Ardisia brevicaulis in our previous work. In the present study, the inhibitory effect of 1-6 on the proliferation of human pancreatic PANC-1, human lung A549, human gastrointestinal carcinoma SGC 7901, human breast MCF-7, and human prostate PC-3 cancer cells was evaluated by the methyl thiazolyl tetrazolium method. Compounds 1-6 all showed inhibitory activities against the proliferation of PANC-1, A549, SGC7901, MCF-7, and PC-3 cancer cells. Compound 3, the most active agent and the main constituent with the highest yield, induced apoptosis of PANC-1 cells (the most sensitive cell line among the cell lines screened) via the activation of caspase-3 and caspase-9, up-regulation of the ratio of bax/bcl-2 protein expression.
authors.affiliation: School of Pharmacy, Yantai University, Yantai, China.
authors.forename: Li-Ping
authors.initials: LP
authors.lastname: Chen
authors.forename: Feng
authors.initials: F
authors.lastname: Zhao
authors.forename: Yao
authors.initials: Y
authors.lastname: Wang
authors.forename: Lian-Lian
authors.initials: LL
authors.lastname: Zhao
authors.forename: Qiu-Ping
authors.initials: QP
authors.lastname: Li
authors.forename: Hong-Wei
authors.initials: HW
authors.lastname: Liu
mesh_terms: D000972:Antineoplastic Agents, Phytogenic / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects; D031644:Ardisia / Q000737:chemistry*; D053148:Caspase 3 / Q000378:metabolism; D053453:Caspase 9 / Q000378:metabolism; D049109:Cell Proliferation / Q000187:drug effects; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D018517:Plant Roots / Q000737:chemistry; D012118:Resorcinols / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology*
chemical_list: C560964:2-methoxy-4-hydroxy-6-pentadecyl-benzene-1-O-acetate; D000972:Antineoplastic Agents, Phytogenic; D012118:Resorcinols; D053148:Caspase 3; D053453:Caspase 9