Inhibitory effects of 3′‐methyl‐3‐hydroxy‐chalcone on proliferation of human malignant tumor cells and on skin carcinogenesis

Abstract

3′-methyl-3-hydroxy-chalcone (3Me-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 3Me-3-C-induced inhibition of cell proliferation. In addition, 3Me-3-C also suppressed the promoting activity of 12-0-tetradecanoylphorbol-13-acetate on skin carcinogenesis in 7,12-dimethylbenz[a]anthracene-initiated mice.