广东药科大学学报2017，Vol.33Issue(4)：488-492,508,6.DOI:10.16809/j.cnki.2096-3653.2017051801
木犀草素硝酸酯衍生物的合成及其体外活性研究
Synthesis and in vitro activities studies of luteolin nitrate derivatives
摘要
Abstract
Objective To design and synthesize new nitrates of luteolin. Methods Five target compounds were obtained by inserting an ether linkage between C-3′, C-4′of luteolin, then the C7-OH of luteolin was replaced by nitrate via nucleophilic substitution. IR and NMR were used for the structural characterization. NO release of the compounds in vitro was determined by Griess method, and the antitumor activity was measured by MTT method. Results The NO release of compounds 3a and 3b were quick and reached equilibrium rapidly and the release of 6a-6c series compounds were stable. The results showed that the protective structure of luteolin at the two phenolic hydroxyl groups affected the NO release in vitro. The MTT results showed the series of new compounds are non-toxic against HepG-2 and MCF-7 human cancer cell lines. Conclusion There is no correlation between the release of the nitric oxide and anti-tumor activity of luteolin nitrates. The activity could be improved by reasonable modification.关键词
木犀草素硝酸酯衍生物/NO供体/体外NO释放/抗肿瘤活性Key words
luteolin nitrate/NO donor/NO-release in vitro/antitumor activity分类
医药卫生引用本文复制引用
朱江华,肖敏捷,刘永谦,陈威连,郑佩玉,冯改丽,罗璟,王涛..木犀草素硝酸酯衍生物的合成及其体外活性研究[J].广东药科大学学报,2017,33(4):488-492,508,6.基金项目
广州中医药大学薪火计划( 20150103) （ 20150103）
广东省大学生创新实验项目( 201410572072) （ 201410572072）
