Anti-tumorigenic chalcones.
On the basis of our recent findings that licochalcone A isolated from Xin-jiang licorice showed anti-inflammatory and anti-tumorigenic activities, we synthesized more than 40 chalcone derivatives to examine their anti-tumorigenic activities. In vitro inhibitory activity against phosphorylation of phospholipids promoted by tetradecanoylphorbol-13-acetate (TPA) in HeLa cells was adopted as a screening test for anti-tumor-promoting effect. In vivo experimental mouse skin tumors initiated by dimethylbenz[a]-anthracene (DMBA) and promoted by TPA were used to test the anti-tumor-promoting effect of chalcones. In the results, 3'- and 4'-methyl-3-hydroxychalcone showed the highest potency in inhibiting tumorigenesis. They also showed a remarkable inhibitory effect on the proliferation of HGC-27 cells derived from human gastric cancer. We discuss the structure-activity relationship, including stereo-chemical phototransformation, of some chalcone derivatives with reference to their ultraviolet (UV) and nuclear magnetic resonance (NMR) spectroscopic data.
Shibata
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Shibata Laboratory of Natural Medicinal Materials, Minophagen Pharmaceutical Company, Tokyo, Japan.
D000818:Animals; D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology*; D002599:Chalcone / Q000031:analogs & derivatives / Q000737:chemistry / Q000494:pharmacology*; D004354:Drug Screening Assays, Antitumor; D006367:HeLa Cells; D006801:Humans; D051379:Mice; D013997:Time Factors; D014407:Tumor Cells, Cultured
D000970:Antineoplastic Agents; D002599:Chalcone