Department of Gastrointestinal Surgery, Tongji Hospital, Huazhong University of Science and Technology, Wuhan, Hubei 430030, P.R. China.
Mol Med Rep. 2014 Mar;9(3):935-40. doi: 10.3892/mmr.2014.1886. Epub 2014 Jan 7.
Isorhamnetin, a flavonoid isolated from the fruits of herbal medicinal plants, such as Hippophae rhamnoides L., exerts anticancer effects similar to other flavonoids. However, the effect of isorhamnetin on colorectal cancer (CRC) and the underlying molecular mechanism are unclear. This study aimed to determine the effect of isorhamnetin on the proliferation of cells from the human CRC cell lines, HT‑29, HCT116 and SW480. It was demonstrated that isorhamnetin suppressed the proliferation of cells from all three cell lines, induced cell cycle arrest at the G2/M phase and suppressed cell proliferation by inhibiting the PI3K‑Akt‑mTOR pathway. Isorhamnetin also reduced the phosphorylation levels of Akt (ser473), phosph‑p70S6 kinase and phosph‑4E‑BP1 (t37/46) protein, and enhanced the expression of Cyclin B1 protein. Therefore, this compound was revealed to be a selective PI3K‑Akt‑mTOR pathway inhibitor, and may be a potent anticancer agent for the treatment of CRC, as it restrains the proliferation of CRC cells.
山柰酚是一种从药用植物果实中分离出来的类黄酮，其抗癌作用与其他类黄酮相似。然而，山柰酚对结直肠癌（CRC）的影响及其潜在的分子机制尚不清楚。本研究旨在确定山柰酚对人 CRC 细胞系 HT-29、HCT116 和 SW480 细胞增殖的影响。结果表明，山柰酚抑制了这三种细胞系的细胞增殖，诱导细胞周期停滞在 G2/M 期，并通过抑制 PI3K-Akt-mTOR 通路抑制细胞增殖。山奈酚还降低了 Akt（丝氨酸 473）、磷酸化 p70S6 激酶和磷酸化 4E-BP1（t37/46）蛋白的磷酸化水平，并增强了 Cyclin B1 蛋白的表达。因此，该化合物被证实是一种选择性的 PI3K-Akt-mTOR 通路抑制剂，可能是治疗 CRC 的有效抗癌药物，因为它可以抑制 CRC 细胞的增殖。
