Xia Yi-Qun, Wei Xiao-Yan, Li Wu-Lan, Kanchana Karvannan, Xu Chao-Chao, Chen Da-Hui, Chou Pei-Hong, Jin Rong, Wu Jian-Zhang, Liang Guang
Chemical Biology Research Center, College of Pharmaceutical Sciences, Wenzhou Medical University, Wenzhou, Zhejiang, China E-mail :
Asian Pac J Cancer Prev. 2014;15(16):6893-8. doi: 10.7314/apjcp.2014.15.16.6893.
Curcumin and its analogues have been reported to exert anti-cancer activity against a variety of tumors. Here, we reported A501, a new curcumin analogue. The effect of A501 on cell viability was detected by MTT assay, the result showed that A501 had a better inhibiting effect on the four non-small cell lung cancer (NSCLC) cells than that of curcumin. Moreover, Colony forming experiment showed A501 significant restrained cell proliferation. Flow cytometry displayed A501 can cause G2/M arrest and induce apoptosis. Western blotting showed that A501 decreased the expression of cyclinB1, cdc-2, bcl-2, while increased the expression of p53, cleaved caspase-3 and bax. In conclusion, curcumin analogues A501 played antitumor activity by inhibiting cell proliferation and inducing apoptosis of NSCLC cells. And it was likely to be a promising starting point for the development of curcumin-based anticancer drugs.
据报道,姜黄素及其类似物对多种肿瘤具有抗癌活性。在此,我们报道了一种新的姜黄素类似物A501。通过MTT法检测A501对细胞活力的影响,结果表明A501对四种非小细胞肺癌(NSCLC)细胞的抑制作用优于姜黄素。此外,集落形成实验表明A501显著抑制细胞增殖。流式细胞术显示A501可导致G2/M期阻滞并诱导凋亡。蛋白质免疫印迹法表明,A501降低了细胞周期蛋白B1、细胞周期蛋白依赖性激酶2(cdc-2)、凋亡抑制蛋白(bcl-2)的表达,同时增加了抑癌基因p53、裂解的半胱天冬酶-3和促凋亡蛋白(bax)的表达。总之,姜黄素类似物A501通过抑制NSCLC细胞增殖和诱导凋亡发挥抗肿瘤活性。它可能是开发基于姜黄素的抗癌药物的一个有前景的起点。