姜黄素衍生物EF24的抗肿瘤机制研究进展

Advances in understanding mechanisms underlying the antitumor activity of curcumin analogue EF24

姜黄素是最早由Vogel和Pelletier从草本植物姜黄的根茎中分离得到的一种酚性天然药物,因其抗肿瘤谱广,不良反应小,美国国立肿瘤研究所已将其列为第3代肿瘤化学预防药物.但是姜黄素的治疗效果却由于口服给药后吸收率低而受到阻碍,Ames等人已开发出一系列比姜黄素水溶性更好的衍生物,其中一种叫3,5-(E)-二(2-氟亚苄基)哌啶-4-酮醋酸盐(EF24),他在多种肿瘤细胞系中表现出比姜黄素更好的细胞毒性效能.

Curcumin, a natural polyphenol which was first extracted by Vogel and Pelletier from rhizomes of the plant Curcuma longa L, has potent anti- carcinogenic activity and low toxic side effects in a wide variety of tumor cells. It has been listed as a third-generation chemoprophylactic drug by the US National Cancer Institute. How- ever, the therapeutic benefit is hampered by its low absorption after transdermal or oral appli- cation. Ames et al. have developed a series of novel synthetic curcumin analogs that are more potent and have better water solubility than curcumin. One of these leading compounds, EF24, exhibits about 10-fold greater cytotoxic activity against various tion to curcumin. This cancer cell lines in rela- article will review the recent advances in understanding mechanisms underlying the antitumor activity of EF24.