Baicalin inhibits breast cancer development via inhibiting IκB kinase activation in vitro and in vivo
Baicalin inhibits breast cancer development via inhibiting IκB kinase activation in vitro and in vivo
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黄芩苷通过抑制体外和体内 I kappa B 激酶激活来抑制乳腺癌的发展
DOI：
10.3892/ijo.2018.4594
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发表时间：
2018-12-01
影响因子：
5.2
通讯作者：
Wu, Qiong
中科院分区：
文献类型：
--
作者：
Gao, Yang;Liu, Hui;Wu, Qiong
本研究的目的是研究黄芩苷在乳腺癌中的作用和治疗潜力。黄芩苷用于治疗炎症性疾病。在乳腺癌 MCF-7 和 MDA-MB-231 细胞以及人乳腺癌异种移植小鼠中评估了黄芩苷的作用。用0、20或30μM黄芩苷处理细胞48小时，而异种移植小鼠则用0、100或200mg/kg黄芩苷腹腔注射处理30天。结果表明，黄芩苷治疗剂量依赖性地抑制乳腺癌细胞的侵袭、迁移和增殖，并在体外和体内诱导G1/S期细胞周期停滞。黄芩苷可减轻炎症损伤，抑制肿瘤坏死因子（TNF）-α和白细胞介素（IL）-1β的分泌，从而通过抑制I kappa B激酶来抑制核因子（NF）-kappa B-p65的激活。黄芩苷活性机制的研究表明，黄芩苷抑制NF-kappa B-p65蛋白表达，导致NF-kappa B诱导CCND1、BCL2、BIRC2和BIRC3表达增加，从而抑制细胞增殖、侵袭和迁移，并在体外和体内抑制抗凋亡因子。此外，黄芩苷不影响非致瘤性正常乳腺上皮细胞。这些结果表明黄芩苷可能对乳腺癌发挥治疗作用。
The aim of the present study was to investigate the effect and therapeutic potential of baicalin in breast cancer. Baicalin is used to treat inflammatory diseases. The effects of baicalin were assessed in breast cancer MCF-7 and MDA-MB-231 cells, and human breast cancer xenograft mice. Cells were treated with 0, 20 or 30 mu M baicalin for 48 h, while xenograft mice were treated with intraperitoneal injection of 0, 100 or 200 mg/kg baicalin for 30 days. The results demonstrated that treatment with baicalin dose-dependently suppressed breast cancer cell invasion, migration and proliferation, and also induced G1/S-phase cell cycle arrest in vitro and in vivo. Baicalin alleviated inflammation injury and inhibited the secretion of tumor necrosis factor (TNF)-alpha and interleukin (IL)-1 beta, thus suppressing nuclear factor (NF)-kappa B-p65 activation via inhibition of I kappa B kinase. Investigation of the mechanism underlying baicalin activity indicated that it inhibited protein expression of NF-kappa B-p65, leading to NF-kappa B-induced increased expression of CCND1, BCL2, BIRC2 and BIRC3, thus inhibiting cell proliferation, invasion and migration and suppressing anti-apoptotic factors in vitro and in vivo. In addition, baicalin did not affect non-tumorigenic normal breast epithelial cells. These results indicate that baicalin may exert therapeutic effects in breast cancer.