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缬更昔洛韦诱导人乳腺癌细胞凋亡并抑制其迁移。

Valtrate from induces apoptosis and inhibits migration of human breast cancer cells .

机构信息

College of Pharmaceutical Science, Zhejiang Chinese Medical University, Hangzhou, Zhejiang, China.

出版信息

Nat Prod Res. 2020 Sep;34(18):2660-2663. doi: 10.1080/14786419.2018.1548454. Epub 2019 Jan 12.

Abstract

Valtrate is a principle compound isolated from , a traditional Chinese folk medicine originally used to treat various nervous disorders. Here, we found that valtrate exhibited significant anti-cancer activity , especially in human breast cancer cells, while displayed relatively low cytotoxicity to normal human breast epithelial cells (MCF 10A). Valtrate induced cell cycle arrest at G2/M stage and apoptosis in MDA-MB-231 and MCF-7 cells, with reduced expression of p-Akt (Ser 473), cyclin B1 and caspase 8, and increased expression of p21, p-cdc2, cleaved-caspase 3, cleaved-caspase 7 and poly (ADP-ribose) polymerase (PARP). In addition, valtrate inhibited cell migration through down-regulation of MMP-9 and MMP-2 expression. These results demonstrate that valtrate possesses anti-breast cancer activities via cell cycle arrest, apoptosis, and inhibition of cell migration, thus supporting valtrate as a potential antitumor agent.

摘要

缬草丙酯是从缬草中分离得到的主要化合物,缬草是一种传统的中药,最初用于治疗各种神经紊乱。在这里,我们发现缬草丙酯表现出显著的抗癌活性,特别是在人乳腺癌细胞中,而对正常的人乳腺上皮细胞(MCF10A)显示出相对较低的细胞毒性。缬草丙酯诱导 MDA-MB-231 和 MCF-7 细胞的细胞周期停滞在 G2/M 期并诱导细胞凋亡,降低了 p-Akt(Ser 473)、细胞周期蛋白 B1 和半胱天冬酶 8 的表达,增加了 p21、p-cdc2、cleaved-caspase 3、cleaved-caspase 7 和多聚(ADP-核糖)聚合酶(PARP)的表达。此外,缬草丙酯通过下调 MMP-9 和 MMP-2 的表达抑制细胞迁移。这些结果表明,缬草丙酯通过细胞周期停滞、细胞凋亡和抑制细胞迁移发挥抗乳腺癌活性,因此支持缬草丙酯作为一种潜在的抗肿瘤药物。

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