有机化学 ›› 2012, Vol. 32 ›› Issue (05): 852-859.DOI: 10.6023/cjoc1107221 上一篇    下一篇

综述与进展

姜黄素前药的研究进展

涂永元a,b, 徐先祥a,b, 邱飞a,b   

  1. a 华侨大学分子药物学研究所 泉州 362021;
    b 分子药物教育部工程研究中心 泉州 362021
  • 收稿日期:2011-07-22 修回日期:2011-11-02 发布日期:2011-12-12
  • 通讯作者: 邱飞 E-mail:qiufei@hqu.edu.cn
  • 基金资助:

    国家自然科学基金(No. 30900351)、福建省自然科学基金(No. 2009J05029)、福建省生物医药工程研究生教育创新基地(No. 06070205)和华侨大学科研基金(No. 08BS412)资助项目.

Research Progress in the Prodrugs of Curcumin

Tu Yongyuana,b, Xu Xianxianga,b, Qiu Feia,b   

  1. a Institute of Molecular Medicine, Huaqiao University, Quanzhou 362021;
    b Engineering Research Center of Molecular Medicine, Ministry of Education, Quanzhou 362021
  • Received:2011-07-22 Revised:2011-11-02 Published:2011-12-12
  • Supported by:

    Project supported by the National Natural Science Foundation of China (No. 30900351), the Natural Science Foundation of Fujian Province of China (No. 2009J05029), the Fujian Biomedicial Engineering Graduate Student’s Educational Innovation Base (No. 06070205) and the Scientific Research Foundation of Huaqiao University (No. 08BS412).

近年来, 天然产物姜黄素因其显著的抗肿瘤等多种生物活性引起广泛关注. 然而姜黄素水溶性差、化学结构不稳定、生物利用度低, 限制了其在临床上的进一步应用. 用小分子或大分子载体对姜黄素的酚羟基进行修饰制备得到的姜黄素前药能较好地解决姜黄素上述的缺点, 也是改善姜黄素成药性的有效策略. 综述了近年来国内外姜黄素前药的研究进展.

关键词: 姜黄素, 前药, 药物化学, 抗肿瘤药物

In recent years, curcumin, a natural product, has been drawing attention from researchers for it has many kinds of significant bioactivities, such as antitumor activity. However, its clinical utility is limited due to a number of undesirable difficulties, such as its low aqueous solubility, instability and low bioavailability. Through conjugated the phenolic hydroxyl group of curcumin with low or high molecular weight carriers, various prodrugs of curcumin have been studied and developed to overcome its disadvantages. The development of prodrugs of curcumin was an effective method to improve the druggability of curcumin. In this paper, the research progresses in the prodrugs of curcumin in recent years are reviewed.

Key words: curcumin, prodrugs, medicinal chemistry, antitumor drug