肿瘤药学2018，Vol.8Issue(6)：856-861,866,7.DOI:10.3969/j.issn.2095-1264.2018.06.05
黄酮衍生物的合成与抗肿瘤活性评价
Synthesis and Anti-tumor in vitro Evaluation of Flavonoid Derivatives ★
摘要
Abstract
Objective To synthesize a series of flavonoid derivatives with anti-tumor activity. Methods Trimethoxy flavonoids 2 and 4 were prepared by a Friedel-Crafts reaction and an improved Baker-Venkatarama rearrangement reaction, followed by esterification with salicylic acid derivatives 6a and 6b to obtain target compounds 7a, 7b, 8a, 8b, 9a and 9b. MTT colorimetric assay was used to detect the anti-proliferative activity of target compounds on MGC-803 cells, MFC cells, HepG2 cells and MCF-7 cells. Flow cytometry investigated MFC cells apoptosis after treatment with compound 7b at different concentrations for 24 h. Results The target compound was confirmed by 1H NMR and ESI-MS which were in full accordance with their depicted structures. On the whole, compound 7b showed the most po-tent anti-proliferative activity than other compounds and 5-Fu. It also showed low toxicity on normal liver cells L-02. What’s more, compound 7b showed obvious inhibition against MFC cells with IC50 values of (13.73±2.04) μM. It induced apoptosis of MFC cells in a dose-dependent manner. Conclusion Compound 7b is expected to become a new type of highly effective, low-toxic anti-tumor candidate drug, and its anti-tumor activity and its mechanism still need further exploration.关键词
黄酮/水杨酸/合成/体外/抗肿瘤Key words
Flavonoids/Salicylic acid/Synthesis/In vitro/Anti-tumor分类
医药卫生引用本文复制引用
朱志敏,邓湘萍,王哲,熊润德,刘仁波,曹轩,唐国涛..黄酮衍生物的合成与抗肿瘤活性评价[J].肿瘤药学,2018,8(6):856-861,866,7.基金项目
国家自然科学基金资助项目(30672042). （30672042）
