A methoxyflavanone derivative, 2′,3′,4′-trimethoxy-5,6-naphthoflavanone, inhibits proliferation of HCT116 human colon cancer cells by inducing G2/M cell cycle arrest and apoptosis

被引：1
|
作者：
Lee, Kyungho [1 ]
Lee, Da Hyun [1 ]
Jung, You Jung [2 ]
Shin, Soon Young [1 ,2 ]
Koh, Dongsoo [3 ]
Lee, Young Han [1 ,2 ]
机构：
[1] Konkuk Univ, Coll Biol Sci & Biotechnol, Dept Biol Sci, Seoul 05029, South Korea
[2] Konkuk Univ, Canc & Metab Inst, Seoul 05029, South Korea
[3] Dongduk Womens Univ, Dept Appl Chem, Seoul 02748, South Korea
来源：
APPLIED BIOLOGICAL CHEMISTRY | 2016年 / 59卷 / 02期
关键词：
2 ',3 ',4 '-Trimethoxy-5,6-naphthoflavanone; Apoptosis; Cell cycle arrest; Flavonoids; HCT116 human colon cancer cells; FLAVONOIDS; FLAVANONES; EXPRESSION; ALPHA; BAX;
D O I：
10.1007/s13765-016-0164-9
中图分类号：
TS2 [食品工业];
学科分类号：
0832 ;
摘要：
A methoxylated flavanone derivative, 2',3',4'-trimethoxy-5,6-naphthoflavanone (TMNF), was synthesized, and its anti-proliferative activity was evaluated. In HCT116 colon cancer cells, TMNF inhibited cellular proliferation and triggered cytotoxicity. A flow cytometry assay showed that TMNF caused cell cycle arrest at the G2/M phase with a concomitant decrease in the population of G1 phase cells. Furthermore, TMNF caused accumulation of p53 and its downstream target, Bax, and stimulated cleavage of caspase-7 and poly(ADP-ribose) polymerase. These data suggest that methoxylated naphthoflavanone can be an attractive pharmacophore for further development of therapeutic adjuvants.
引用
收藏
页码：249 / 253
页数：5
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