Inhibitory effects of 3'-methyl-3-hydroxy-chalcone on proliferation of human malignant tumor cells and on skin carcinogenesis.
3'-methyl-3-hydroxy-chalcone (3'Me-3-C), a derivative of chalcone, inhibited the proliferation of various kinds of human malignant tumor cells, such as HGC-27 (gastric cancer), HeLa (cervical carcinoma), PANC-1 (pancreatic cancer) and GOTO (neuroblastoma). Flow-cytometric analysis of HGC-27 cells revealed that 3'Me-3-C perturbed the cell cycle, i.e., it delayed passage through the S phase, and/or caused arrest in the G0/G1 phase. 3'Me-3-C inhibited the binding of [6,7-3H]estradiol to type-II estrogen-binding sites dose-dependently, and altered the pattern of protein synthesis and phosphorylation, which may explain 3'Me-3-C-induced inhibition of cell proliferation. In addition, 3'Me-3-C also suppressed the promoting activity of 12-0-tetradecanoylphorbol-13-acetate on skin carcinogenesis in 7,12-dimethylbenz[a]anthracene-initiated mice.
Department of Biochemistry, Kyoto Prefectural University of Medicine, Japan.
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Satomi
D015127:9,10-Dimethyl-1,2-benzanthracene; D000818:Animals; D002455:Cell Division / Q000187:drug effects; D002599:Chalcone / Q000031:analogs & derivatives* / Q000494:pharmacology; D047188:Chalcones; D004305:Dose-Response Relationship, Drug; D006367:HeLa Cells / Q000473:pathology; D006801:Humans; D051379:Mice; D009363:Neoplasm Proteins / Q000378:metabolism; D009369:Neoplasms / Q000139:chemically induced / Q000473:pathology*; D010212:Papilloma / Q000139:chemically induced; D010766:Phosphorylation; D012878:Skin Neoplasms / Q000139:chemically induced*; D013274:Stomach Neoplasms / Q000473:pathology; D013755:Tetradecanoylphorbol Acetate; D013997:Time Factors; D014407:Tumor Cells, Cultured
D047188:Chalcones; D009363:Neoplasm Proteins; C083298:3'-methyl-3-hydroxychalcone; D015127:9,10-Dimethyl-1,2-benzanthracene; D002599:Chalcone; D013755:Tetradecanoylphorbol Acetate