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鞣花酸通过诱导 G2/M 期阻滞抑制肝癌细胞增殖。

Corilagin inhibits hepatocellular carcinoma cell proliferation by inducing G2/M phase arrest.

机构信息

The Research and Development Center for Medicinal Plants and Plant Drugs, Xiamen Overseas Chinese Subtropical Plant Introduction Garden, Gusheng Road 4#, Xiamen, 361002, Fujian Province, China.

出版信息

Cell Biol Int. 2013 Oct;37(10):1046-54. doi: 10.1002/cbin.10132. Epub 2013 Jul 24.

Abstract

Hepatocellular carcinoma (HCC) is one of most common types of malignant tumours. Therefore, it is very important to identify powerful drugs and their antitumour mechanisms. Corilagin has a significant antitumour potential and lower toxicity in normal cells in vitro. The IC50 values of corilagin for normal Chang-liver cells and the HCC cell lines Bel7402 and SMMC7721 were 131.4, 24.5 and 23.4 µM, respectively, in the methyl thiazolyl tetrazolium (MTT) assay. MHCC97-H xenografts in Balb/c mice intraperitoneally injected with 30 mg/kg corilagin for 5 weeks showed a 47.3% inhibition of tumour growth in vivo. Furthermore, data from flow cytometry and Western blot analyses of cell cycle and cell cycle-related proteins suggest that corilagin arrests SMMC7721 cells at the G2/M phase by downregulating p-Akt and cyclin B1/cdc2 and upregulating p-p53 and p21(Cip1) . In conclusion, corilagin is a potential antitumour drug that is effective in retarding the growth of HCC, which is correlated with the activation of p-p53-p21(Cip1) -cdc2/cyclin B1.

摘要

肝细胞癌 (HCC) 是最常见的恶性肿瘤类型之一。因此,识别有效的药物及其抗肿瘤机制非常重要。柯里拉京在体外对正常细胞具有显著的抗肿瘤潜力和较低的毒性。MTT 法测定柯里拉京对正常 Chang-liver 细胞和 HCC 细胞系 Bel7402 和 SMMC7721 的 IC50 值分别为 131.4、24.5 和 23.4µM。在腹腔注射 30mg/kg 柯里拉京 5 周的 Balb/c 小鼠 MHCC97-H 异种移植瘤模型中,体内肿瘤生长抑制率为 47.3%。此外,细胞周期和细胞周期相关蛋白的流式细胞术和 Western blot 分析数据表明,柯里拉京通过下调 p-Akt 和 cyclin B1/cdc2 以及上调 p-p53 和 p21(Cip1) 使 SMMC7721 细胞停滞在 G2/M 期。综上所述,柯里拉京是一种有效的抗肿瘤药物,可延缓 HCC 的生长,这与 p-p53-p21(Cip1)-cdc2/cyclin B1 的激活有关。

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