Yeon Park Jun, Young Kim Hyun, Shibamoto Takayuki, Su Jang Tae, Cheon Lee Sang, Suk Shim Jae, Hahm Dae-Hyun, Lee Hae-Jeung, Lee Sanghyun, Sung Kang Ki
College of Korean Medicine, Gachon University, Seongnam 13120, Republic of Korea.
Department of Food Science, Gyeongnam National University of Science and Technology, Jinju 52725, Republic of Korea.
Bioorg Med Chem Lett. 2017 Sep 1;27(17):3968-3973. doi: 10.1016/j.bmcl.2017.07.070. Epub 2017 Jul 29.
The biological activities of the ethanol extract from Cirsium japonicum var. maackii (ICF-1) and its major component, polyphenol cirsimaritin, were investigated as part of the search for possible alternative drugs for breast cancer. Three in vitro cell-based assays were used: the cell proliferation assay, tube-formation assay, and Western blot analysis. Both the ICF-1 extract and cirsimaritin inhibited the viability of HUVECs in a dose-dependent manner. The inhibition achieved was 36.89% at a level of 200μg/ml by the ICF-1 extract and 62.04% at a level of 100μM by cirsimaritin. The ICF-1 extract and cirsimaritin reduced tube formation by 12.69% at level of 25μg/ml and 32.18% at the levels of 6.25μM, respectively. Cirsimaritin inhibited angiogenesis by downregulation of VEGF, p-Akt and p-ERK in MDA-MB-231 cells, suggesting that cirsimaritin is potentially useful as an anti-metastatic agent. The present study demonstrated that Cirsium japonicum extract and its active component cirsimaritin is an excellent candidate as an alternative anti-breast cancer drug.
作为寻找乳腺癌替代药物的一部分，对大蓟（ICF-1）乙醇提取物及其主要成分多酚刺囊酸的生物活性进行了研究。使用了三种基于细胞的体外试验：细胞增殖试验、管形成试验和蛋白质印迹分析。ICF-1提取物和刺囊酸均以剂量依赖性方式抑制人脐静脉内皮细胞（HUVECs）的活力。ICF-1提取物在200μg/ml水平时抑制率为36.89%，刺囊酸在100μM水平时抑制率为62.04%。ICF-1提取物和刺囊酸分别在25μg/ml水平时使管形成减少12.69%，在6.25μM水平时使管形成减少32.18%。刺囊酸通过下调MDA-MB-231细胞中的血管内皮生长因子（VEGF）、磷酸化蛋白激酶B（p-Akt）和磷酸化细胞外信号调节激酶（p-ERK）来抑制血管生成，这表明刺囊酸可能作为一种抗转移剂。本研究表明，大蓟提取物及其活性成分刺囊酸是一种优秀的乳腺癌替代药物候选物。
