有机化学 ›› 2018, Vol. 38 ›› Issue (6): 1549-1555.DOI: 10.6023/cjoc201801023 上一篇    下一篇

研究简报

小檗碱与和厚朴酚及槲皮素缀合物的合成及其体外抗肝癌HepG2细胞活性评价

廖世莉a, 张国改a, 曹涵a, 陈碧莹a, 李卫民b, 吴霞a, 冯毅凡a   

  1. a 广东药科大学中心实验室 广州 510000;
    b 广州中医药大学中药学院 广州 510000
  • 收稿日期:2018-01-26 修回日期:2018-02-27 发布日期:2018-03-08
  • 通讯作者: 李卫民,E-mail:13925023915@139.com;吴霞,E-mail:wxiaxia@163.com;冯毅凡,E-mail:yffeng@139.com E-mail:13925023915@139.com;wxiaxia@163.com;yffeng@139.com
  • 基金资助:

    国家自然科学基金(Nos.21275036,81202429)资助项目.

Synthesis and Anti-tumor Activities against HepG2 Cell in vitro of the Conjugates of Honokiol, Quercetin and Berberine

Liao Shilia, Zhang Guogaia, Cao Hana, Chen Biyinga, Li Weiminb, Wu Xiaa, Feng Yifana   

  1. a Central Laboratory, Guangdong Pharmaceutical University, Guangzhou 510000;
    b College of Chinese Materia Medica, Guangzhou University of Chinese Medicine, Guangzhou 510000
  • Received:2018-01-26 Revised:2018-02-27 Published:2018-03-08
  • Contact: 10.6023/cjoc201801023 E-mail:13925023915@139.com;wxiaxia@163.com;yffeng@139.com
  • Supported by:

    Project supported by the National Natural Science Foundation of China (Nos. 21275036, 81202429).

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、13C 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HepG2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.

关键词: 小檗碱, 和厚朴酚, 槲皮素, 抗癌活性

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.

Key words: berberine, honokiol, quercetin, anti-tumor activity