2-取代萘醌类衍生物对HepG2细胞的抑制作用

Inhibitory Effects of 2-Substituted Naphthoquinone Derivatives on HepG2

萘醌类衍生物具有包括抗癌活性在内的广泛生理活性。研究以1,5-二羟基萘为原料,经五步反应得到了3个环状及支链的氨基萘醌类衍生物(f1、f2、f3)和直链的亚砜类萘醌类衍生物(i),并通过质谱和1H NMR进行结构鉴定,采用噻唑蓝(MTT)法研究了对肝癌细胞系HepG2细胞的细胞毒性。结果显示化合物i的抗癌抑制活性最强IC50为17.46μmmol·mL-1,表明取代基含有直链及2位亲核试剂具有增强萘醌类衍生物对癌细胞杀伤能力的作用。

Naphthoquinones had extensive biological activity including anticancer. Three cyclic or branched chain amino naphthoquinone derivatives （f1, f2 and f3） and one linear chain sulfinyl naphthoquinone derivative （i） were synthesized starting from 1,5-dihydroxynaphthalene through a five-steps reaction. The structures of these compounds were determined by 1H NMR and Mass Spectrometry and the inhibition activities were evaluated on human hepatocarcinoma cell line （HepG2） by MTT assay. The results showed that the Compound i had the strongest inhibition effect with IC50 17.46 μmmol·mL-1, which demonstrated that naphthoquinones containing the linear chain and 2 position nucleophilic reagents could strengthen the anticancer effect.