PM-3, a benzo-gamma-pyran derivative isolated from propolis, inhibits growth of MCF-7 human breast cancer cells.
Propolis has numerous biologic activities including antibiotic, antifungal, antiviral and anti-inflammatory properties. Several components isolated from propolis have been shown to have anticancer activity. This study demonstrates that the compound PM-3 (3-[2-dimethyl-8-(3-methyl-2-butenyl)benzopyran]-6-propenoic acid) isolated from Brazilian propolis markedly inhibits the growth of MCF-7 human breast cancer cells. This effect was associated with inhibition of cell cycle progression and induction of apoptosis. Treatment of MCF-7 cells with PM-3 arrested cells in the G1 phase and resulted in a decrease in the protein levels of cyclin D1 and cyclin E. PM-3 also inhibited the expression of cyclin D1 at the transcriptional level when examined in cyclin D1 promoter luciferase assays. Induction of apoptosis by PM-3 occurred within 48 hours after treatment of MCF-7 cells. The MCF-7 treated cells also displayed a decrease in the level of the estrogen receptor (ER) protein and inhibition of estrogen response element (ERE) promoter activity. Therefore, PM-3 merits further investigation with respect to breast cancer chemoprevention or therapy.
Luo
J
J
Herbert Irving Comprehensive Cancer Center, Columbia Presbyterian Medical Center, College of Physicians and Surgeons, Columbia University, New York, NY 10032, USA.
Soh
J W
JW
Xing
W Q
WQ
Mao
Y
Y
Matsuno
T
T
Weinstein
I B
IB
D017304:Annexin A5 / Q000378:metabolism; D000970:Antineoplastic Agents / Q000494:pharmacology*; D017209:Apoptosis; D001578:Benzopyrans / Q000737:chemistry / Q000494:pharmacology*; D015152:Blotting, Northern; D015153:Blotting, Western; D001943:Breast Neoplasms / Q000188:drug therapy*; D002453:Cell Cycle / Q000187:drug effects; D002455:Cell Division; D004396:Coloring Agents / Q000494:pharmacology; D019938:Cyclin D1 / Q000096:biosynthesis; D019927:Cyclin E / Q000096:biosynthesis; D004305:Dose-Response Relationship, Drug; D015536:Down-Regulation; D004797:Enzyme-Linked Immunosorbent Assay; D005434:Flow Cytometry; D017930:Genes, Reporter; D006801:Humans; D008689:Methacrylates / Q000737:chemistry / Q000494:pharmacology*; D008956:Models, Chemical; D010936:Plant Extracts / Q000494:pharmacology*; D011401:Promoter Regions, Genetic; D011429:Propolis / Q000378:metabolism*; D011960:Receptors, Estrogen / Q000096:biosynthesis / Q000187:drug effects; D020218:Response Elements; D013778:Tetrazolium Salts / Q000494:pharmacology; D013844:Thiazoles / Q000494:pharmacology; D013997:Time Factors; D014158:Transcription, Genetic; D014162:Transfection; D014407:Tumor Cells, Cultured
C433934:3-(2-dimethyl-8-(3-methyl-2-butenyl)benzopyran)-6-propenoic acid; D017304:Annexin A5; D000970:Antineoplastic Agents; D001578:Benzopyrans; D004396:Coloring Agents; D019927:Cyclin E; D008689:Methacrylates; D010936:Plant Extracts; D011960:Receptors, Estrogen; D013778:Tetrazolium Salts; D013844:Thiazoles; D019938:Cyclin D1; D011429:Propolis; C022616:thiazolyl blue