Mechanisms of an anti-cancer effect of a novel marine natural compound, exiguolide.

本实验旨在阐明新型海洋天然化合物甜菜内酯的抗癌作用机制。甜菜内酯作用于体外培养的癌细胞后，细胞周期受阻，出现凋亡细胞死亡。在小鼠体内异种移植模型中，甜菜内酯也能抑制肿瘤的生长。几种激酶参与了这种抗癌作用。然后，我们合成了结构修饰的甜菜内酯类似物。其中一些类似物在体外和体内都有类似的抗癌作用。这些结果将为开发可临床应用的抗癌新药提供依据。

The aim of this experiment is to elucidate the mechanisms of an anti-cancer effect of a novel marine natural compound, exiguolide. The cell cycle of cultured cancer cells was arrested with apoptotic cells death under incubation with exiguolide. Tumor growth was also attenuated by the treatment with exiguolide in the in vivo xenograft model in mice. Several kinases were involved in this anti-cancer effect. Then, we synthesized exiguolide analogues with modified structures. Some of the analogues had a similar anti-cancer effect in both in vitro and in vivo. These results will bring the basis for developing a new anti-cancer drug, which can be clinically applicable.