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姜黄素类似物 JZ534 的体外抗肺癌活性。

Anti-Lung Cancer Activity of the Curcumin Analog JZ534 In Vitro.

机构信息

Chemical Biology Research Center, School of Pharmaceutical Sciences, Wenzhou Medical University, Wenzhou, Zhejiang 325035, China.

Chemical Biology Research Center, School of Pharmaceutical Sciences, Wenzhou Medical University, Wenzhou, Zhejiang 325035, China ; Department of Pharmacy, The First Affiliated Hospital of Wenzhou Medical University, Wenzhou, Zhejiang 325000, China.

出版信息

Biomed Res Int. 2015;2015:504529. doi: 10.1155/2015/504529. Epub 2015 Apr 21.

Abstract

This study investigated the anticancer effect of the curcumin analog JZ534 on lung cancer cell lines H460, A549, H1975, and HCC827. The antiproliferation effect of JZ534 was measured through the methylthiazoletetrazolium assay, and cell colony formation was observed. Cell cycle and apoptosis were determined by flow cytometry, and the preliminary mechanism was studied by Western blot. Results showed that JZ534 significantly inhibited the vitality and colony formation of lung cancer cells. JZ534 induced the G2/M cell cycle arrest of the cancer cells and suppressed the expression of cycle-related proteins, including cyclin B1 and Cdc2. Meanwhile, JZ534 induced cell apoptosis and upregulated the expression of apoptosis-related proteins, including cleaved caspase-3, Bax, and p53. At the same dose, JZ534 showed better antitumor activity than curcumin. These results suggest that JZ534 exhibits excellent anti-lung cancer activity by inhibiting the growth and inducing the apoptosis of lung cancer cells. Therefore, JZ534 is a promising lead compound for cancer treatment.

摘要

本研究探讨了姜黄素类似物 JZ534 对肺癌细胞系 H460、A549、H1975 和 HCC827 的抗癌作用。通过噻唑蓝比色法测量 JZ534 的增殖抑制作用,并观察细胞集落形成情况。通过流式细胞术检测细胞周期和凋亡,并用 Western blot 初步研究其作用机制。结果表明,JZ534 显著抑制肺癌细胞活力和集落形成。JZ534 诱导癌细胞 G2/M 细胞周期阻滞,并抑制周期相关蛋白(包括细胞周期蛋白 B1 和 Cdc2)的表达。同时,JZ534 诱导细胞凋亡,并上调凋亡相关蛋白(包括 cleaved caspase-3、Bax 和 p53)的表达。在相同剂量下,JZ534 对肿瘤的抑制活性优于姜黄素。这些结果表明,JZ534 通过抑制肺癌细胞生长和诱导细胞凋亡发挥优异的抗癌活性。因此,JZ534 是一种很有前途的癌症治疗先导化合物。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bb00/4419220/9e79ade02300/BMRI2015-504529.001.jpg

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