Baicalein and baicalin inhibit colon cancer using two distinct fashions of apoptosis and senescence.
Baicalein and baicalin inhibit colon cancer using two distinct fashions of apoptosis and senescence.
复制标题
黄芩素和黄芩苷通过两种不同的细胞凋亡和衰老方式抑制结肠癌
DOI：
10.18632/oncotarget.24015
复制
发表时间：
2018-04-13
期刊：
影响因子：
--
通讯作者：
Peng G
中科院分区：
文献类型：
--
作者：
Dou J;Wang Z;Ma L;Peng B;Mao K;Li C;Su M;Zhou C;Peng G
黄芩素和黄芩苷是黄芩的活性成分，具有广泛的抗肿瘤活性。然而，黄芩素和黄芩苷如何以及是否抑制结肠癌尚不清楚。在这里，我们证明黄芩素和黄芩苷可以显着抑制人结肠癌细胞的生长和增殖。此外，两者都可以诱导细胞周期停滞，并抑制癌细胞集落形成和迁移。黄芩素和黄芩苷分别通过诱导结肠癌细胞凋亡和衰老而发挥抑制作用。此外，我们还发现黄芩苷诱导肿瘤细胞衰老是由于其抑制肿瘤细胞端粒酶逆转录酶的表达，MAPK、ERK和p38信号通路参与了黄芩素和黄芩苷介导的结肠癌细胞凋亡和衰老的调节。此外，我们在人源化小鼠异种移植模型中使用人结肠癌细胞的体内研究进一步证明了黄芩素和黄芩苷可以诱导肿瘤细胞凋亡和衰老，从而抑制体内肿瘤发生和结肠癌生长。这些数据清楚地表明黄芩素和黄芩苷对人结肠癌具有有效的抗癌作用，可能成为潜在的新型有效的肿瘤治疗靶向药物。
Baicalein and baicalin are active components of the Scutellaria baicalensis Georgi and both have broad anti-tumor activity. However, how and whether baicalein and baicalin inhibit colon cancer is unclear. Here we demonstrate that baicalein and baicalin can significantly inhibit human colon cancer cell growth and proliferation. Furthermore, both can induce cell cycle arrest, and suppress cancer cell colony formation and migration. The suppressive effects are mechanistically due to the induction of colon cancer cell apoptosis and senescence mediated by baicalein and baicalin, respectively. Furthermore, we revealed that baicalin-induced senescence in tumor cells is due to its inhibition of telomerase reverse transcriptase expression in tumor cells, and that MAPK ERK and p38 signaling pathways are causatively involved in the regulation of colon cancer cell apoptosis and senescence mediated by baicalein and baicalin. In addition, our in vivo studies using human colon cancer cells in humanized mouse xenograft models, further demonstrated that baicalein and baicalin can induce tumor cell apoptosis and senescence, resulting in inhibition of tumorigenesis and growth of colon cancer in vivo. These data clearly suggest that baicalein and baicalin have potent anti-cancer effects against human colon cancer and could be potential novel and effective target drugs for cancer therapy.