Deng Xiangping, Zhao Zihao, Xiong Shujuan, Xiong Runde, Liu Juan, Wang Zhe, Zou Liu, Lei Xiaoyong, Cao Xuan, Xie Zhizhong, Chen Yanming, Zheng Xing, Liu Yunmei, Tang Guotao
a Hunan Province Cooperative Innovation Center for Molecular Target New Drug Study, Institute of Pharmacy and Pharmacology , University of South China , Hengyang , China.
b Pharmacy Department , Xiangtan Central Hospital , Xiangtan , China.
Nat Prod Res. 2018 Sep;32(18):2178-2186. doi: 10.1080/14786419.2017.1371159. Epub 2017 Sep 5.
A series of chrysin salicylate derivatives as potential antitumour agents were synthesised and evaluated their antitumour activities in vitro and in vivo. Most of the compounds exhibited moderate to good activities against MCF-7 cells, HepG2 cells, MGC-803cells and MFC cells. Among them, compound 3f showed the most potent activity against MGC-803 cells and MFC cells with IC values of 23.83 ± 3.68 and 27.34 ± 5.21 μM, respectively. The flow cytometry assay reconfirmed that compound 3f promoted the occurrence of tumour cells' G1/S block under the inhibiting effect of compound 3f. Compound 3f possessed higher antitumour efficacy in tumour-bearing mice, compared with the positive control 5-Fu and the blank control saline.
合成了一系列白杨素水杨酸酯衍生物作为潜在的抗肿瘤剂，并对其体外和体内抗肿瘤活性进行了评估。大多数化合物对MCF-7细胞、HepG2细胞、MGC-803细胞和MFC细胞表现出中等至良好的活性。其中，化合物3f对MGC-803细胞和MFC细胞表现出最强的活性，IC值分别为23.83±3.68和27.34±5.21μM。流式细胞术分析再次证实，在化合物3f的抑制作用下，化合物3f促进了肿瘤细胞G1/S期阻滞的发生。与阳性对照5-氟尿嘧啶和空白对照生理盐水相比，化合物3f在荷瘤小鼠中具有更高的抗肿瘤疗效。
