芹菜素衍生物的合成及其抗癌活性

Synthesis and anti-cancer activities of apigenin derivatives.

作者信息

Zheng Xing, Yu Liuying, Yang Jing, Yao Xu, Yan Wenna, Bo Shaowei, Liu Ya, Wei Yun, Wu Zhiyi, Wang Guan

机构信息

Institute of Pharmacy & Pharmacology, University of South China, Hengyang, 421001, China.

出版信息

Med Chem. 2014;10(7):747-52. doi: 10.2174/1573406410666140307152557.

DOI:10.2174/1573406410666140307152557

PMID:24605779

Abstract

A novel series of apigenin derivatives with phloroglucinol or resorcinol as raw materials were synthesized according to Baker-Venaktaraman reaction and their in vitro inhibitory activities on colorectal adenocarcinoma (HT-29) and leucocythemia (HL-60) cell lines were evaluated by the standard methyl thiazole tetrazolium (MTT) method. The results of biological test showed that some of apigenin derivatives possessed stronger anti-cancer activities than apigenin. Compound 6 showed the strongest activity against colorectal adenocarcinoma (HT-29) and leucocythemia (HL-60) cell lines with IC50 valure of 2.03±0.22 µM, 2.25±0.42 µM, it was better than 5-FU (12.92±0.61 µM, 9.56±0.16 µM), which shows a potential compound for colorectal adenocarcinoma and leucocythemia.

摘要

以间苯三酚或间苯二酚为原料，根据贝克-维纳卡拉曼反应合成了一系列新型芹菜素衍生物，并采用标准甲基噻唑四氮唑（MTT）法评价了它们对结肠腺癌（HT-29）和白血病（HL-60）细胞系的体外抑制活性。生物学试验结果表明，部分芹菜素衍生物具有比芹菜素更强的抗癌活性。化合物6对结肠腺癌（HT-29）和白血病（HL-60）细胞系表现出最强的活性，IC50值分别为2.03±0.22 µM、2.25±0.42 µM，优于5-氟尿嘧啶（12.92±0.61 µM、9.56±0.16 µM），是一种有潜力用于治疗结肠腺癌和白血病的化合物。