摘要
小檗碱、和厚朴酚、槲皮素都是具有良好抗肿瘤活性的先导化合物,以其为原料合成了三个新型化合物,通过~1H NMR、^(13)C NMR、2D NMR、HRMS、IR和UV等方法对目标化合物进行结构确证;体外抗HepG2肝癌细胞活性结果显示,两个化合物对Hep G2肝癌细胞的抑制作用远远优于原料药和厚朴酚与盐酸小檗碱,且活性与阳性对照药顺铂相当,有望成为潜在的抗肿瘤药物.
Berberine, honokiol, quercetin are the lead compounds with outstanding anti-tumor activities. Three novel products were synthesized from honokiol, quercetin and berberine. The structures of the products were firstly confirmed by 1H NMR, 13C NMR, 2D NMR, HRMS, IR and UV. All products were evaluated for their anti-tumor activities against HepG2 cell in vitro and the results showed that the inhibitory effects of two compounds on HepG2 cell were far superior to honokiol and berberine hydrochloride, and the anti-tumor activities were similar to the reference drug cisplatin. It means that compounds 1 and 2 are expected to be the potential anti-tumor drugs.
作者
廖世莉
张国改
曹涵
陈碧莹
李卫民
吴霞
冯毅凡
Liao Shili;Zhang Guogai;Cao Han;Chen Biying;Li Weimin;Wu Xia;Feng Yifan(Central Laboratory, Guangdong Pharmaceutical University, Guangzhou 510000;College of Chinese Materia Medica, Guangzhou University of Chinese Medicine, Guangzhou 510000)
出处
《有机化学》
SCIE
CAS
CSCD
北大核心
2018年第6期1549-1555,共7页
Chinese Journal of Organic Chemistry
基金
Project supported by the National Natural Science Foundation of China(Nos.21275036,81202429)~~
关键词
小檗碱
和厚朴酚
槲皮素
抗癌活性
berberine
honokiol
quercetin
anti-tumor activity