染料木素
芒柄花素
类黄酮
柚皮素
芹菜素
细胞凋亡
传统医学
化学
药理学
生物化学
生物
医学
抗氧化剂
大豆黄酮
内分泌学
作者
Song‐Chwan Fang,Chin‐Lin Hsu,Hsin-Tang Lin,Gow‐Chin Yen
摘要
Millettia reticulata Benth is cultivated in Asian countries. M. reticulata Benth has multiple biological functions and is one of the oldest tonic herbs in traditional Chinese medicine. It has been elevated to one of the most commonly used herbs in modern Chinese medicine. The aims of this work were to study the in vitro anticancer activity of flavonoid derivatives isolated from the stems of M. reticulata Benth. Six flavonoid derivatives including (−)-epicatechin (1), naringenin (2), 5,7,3′,5′-tetrahydroxyflavanone (3), formononetin (4), isoliquiritigenin (5), and genistein (6) were isolated from the stems of M. reticulata Benth. The structures of 1−6 were determined by spectroscopic methods. The effects of flavonoid derivatives (1−6) on the viability of human cancer cells (including HepG2, SK-Hep-1, Huh7, PLC5, COLO 205, HT-29, and SW 872 cells) were investigated. The results indicated that genistein (6) had the strongest inhibitory activity with an IC50 value of 16.23 μM in SK-Hep-1 human hepatocellular carcinoma cells. Treatment of SK-Hep-1 cells with genistein (6) caused loss of mitochondrial membrane potential. Western blot data revealed that genistein (6) stimulated an increase in the protein expression of Fas, FasL, and p53. Additionally, treatment with genistein (6) changed the ratio of expression levels of pro- and anti-apoptotic Bcl-2 family members and subsequently induced the activation of caspase-9 and caspase-3, which was followed by cleavage of poly(ADP-ribose) polymerase (PARP). These results demonstrate that genistein (6) induces apoptosis in SK-Hep-1 cells via both Fas- and mitochondria-mediated pathways.
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