論文 - 詳細
RRC ID | 62039 |
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著者 | Yamauchi K, Mitsunaga T, Afroze SH, Uddin MN. |
タイトル | Structure-Activity Relationships of Methylquercetin on Anti-migration and Anti-proliferation Activity in B16 Melanoma Cells. |
ジャーナル | Anticancer Res |
Abstract |
BACKGROUND:Melanoma is a malignant skin tumor and quercetin has been reported to inhibit metastasis. A quercetin glycoside and 7 methylquercetins were synthesized from rutin to investigate structure-activity relationships. MATERIALS AND METHODS:We evaluated the anti-proliferative and anti-migration activity of quercetin glycoside and 7 methylquercetins in murine B16 melanoma cells by commercially available kits. We also examined the effect of these compounds on growth of human fibroblast cells to evaluate cytotoxicity. RESULTS:3-O-methylquercetin (2) exhibited 30, 38, 45% migration activity at 25, 12.5, 6.25 μM respectively. Furthermore, 3,4',7-O-trimethylquercetin (5) and 3,4'-O-dimethylquercetin (3) inhibited migration more potent than 2 with no cytotoxicity. 3-hydroxymethylquercetin and quercetin glycoside exhibited no anti-migration activity. Furthermore, the 3 and 4 inhibited melanoma proliferation with no cytotoxicity. CONCLUSION:The methoxyl group at the C-3 position plays an important role in inhibiting the migration of B16 melanoma cells. |
巻・号 | 37(4) |
ページ | 1575-1579 |
公開日 | 2017-4-1 |
DOI | 10.21873/anticanres.11487 |
PII | 37/4/1575 |
PMID | 28373417 |
MeSH | Animals Antineoplastic Agents / pharmacology* Antioxidants / chemistry Antioxidants / pharmacology* Apoptosis / drug effects* Cell Movement / drug effects* Cell Proliferation / drug effects* Cells, Cultured Dose-Response Relationship, Drug Fibroblasts / drug effects Fibroblasts / pathology Humans Melanoma, Experimental / drug therapy Melanoma, Experimental / pathology* Mice Quercetin / chemistry Quercetin / pharmacology* Structure-Activity Relationship |
IF | 1.994 |
リソース情報 | |
ヒト・動物細胞 | NB1RGB(RCB0222) |