Advanced Radiation Technology Institute (ARTI), Korea Atomic Energy Research Institute (KAERI), Jeongeup-si, Jeollabuk-do 580-185, Republic of Korea.
BMC Complement Altern Med. 2013 Dec 11;13:350. doi: 10.1186/1472-6882-13-350.
Centipedegrass extract (CGE) is mainly composed of maysin and its derivatives, which are recognized internationally as natural compounds. Compared to other flavonoids, maysin has a unique structure in that mannose is bound to the flavonoid backbone. CGE exhibits some biological properties in that it can function as an anti-oxidant, anti-inflammatory, anti-adipogenic, and insecticidal. Whether CGE has other biological functions, such as anti-cancer activity, is unknown.
B16F1 (mouse) and SKMEL-5 (human) cells were treated with CGE, and their subsequent survival was determined using MTT assay. We performed a cell cycle analysis using propidium iodide (PI), and detected apoptosis using double staining with annexin V-FITC/PI. In addition, we examined mitochondrial membrane potentials using flow cytometry, as well as signaling mechanisms with an immunoblotting analysis.
CGE inhibited skin cancer cell growth by arresting the cell cycle in the G2/M phase, and increased both early and late apoptotic cell populations without affecting normal cells. Furthermore, we observed mitochondrial transmembrane depolarization, increased cytochrome-c release, caspase-3 and caspase-7 activation, and increased poly ADP-ribose polymerase degradation. CGE also downregulated activation of p-AKT, p-glycogen synthase kinase-3β (GSK-3β), and p-BAD in a time-dependent manner. LY294002 inhibition of phosphoinositide 3-kinase (PI3K) significantly sensitized skin cancer cells, which led to an increase in CGE-induced apoptosis.
CGE controlled skin cancer cell growth by inhibiting the PI3K/AKT/GSK-3β signaling pathway and activating the effector caspases. This study is the first to demonstrate anti-cancer properties for CGE, and that CGE may be an effective therapeutic agent for treating skin cancer.
蜈蚣草提取物（CGE）主要由穗花杉双黄酮及其衍生物组成，这些物质已被国际公认为天然化合物。与其他类黄酮相比，穗花杉双黄酮的结构独特，其黄酮骨架上连接有甘露糖。CGE 具有抗氧化、抗炎、抗脂肪生成和杀虫等生物特性。目前尚不清楚 CGE 是否具有其他生物功能，如抗癌活性。
用 CGE 处理 B16F1（小鼠）和 SKMEL-5（人）细胞，用 MTT 法测定细胞存活率。我们用碘化丙啶（PI）进行细胞周期分析，用 annexin V-FITC/PI 双重染色检测细胞凋亡。此外，我们还通过流式细胞术检测线粒体膜电位，通过免疫印迹分析检测信号转导机制。
CGE 通过将细胞周期阻滞在 G2/M 期来抑制皮肤癌细胞生长，并增加早期和晚期凋亡细胞群体，而不影响正常细胞。此外，我们观察到线粒体跨膜去极化、细胞色素 c 释放增加、caspase-3 和 caspase-7 激活以及多聚 ADP-核糖聚合酶降解增加。CGE 还呈时间依赖性地下调 p-AKT、p-糖原合酶激酶-3β（GSK-3β）和 p-BAD 的激活。PI3K 抑制剂 LY294002 显著增强了皮肤癌细胞对 CGE 的敏感性，导致 CGE 诱导的细胞凋亡增加。
CGE 通过抑制 PI3K/AKT/GSK-3β 信号通路和激活效应 caspase 来控制皮肤癌细胞的生长。本研究首次证明 CGE 具有抗癌特性，CGE 可能是治疗皮肤癌的有效治疗剂。
