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以brartemicin为先导化合物设计合成了15个新型海藻糖衍生物,并通过1H NMR、MS及元素分析确证了其结构。采用MTT法考察目标化合物对肿瘤细胞Hep G2、A549和正常细胞HUVEC增殖的影响;采用Matrigel黏附实验,Transwell小室法考察目标化合物对Hep G2和A549细胞黏附、侵袭与迁移能力的影响。结果表明,在1~32μmol·L-1浓度内,15个目标物对Hep G2、A549和HUVEC细胞均无显著细胞毒性(P>0.05)。在上述浓度范围内,化合物79和82对A549细胞黏附、侵袭与迁移的抑制作用以及对Hep G2细胞的黏附与侵袭抑制作用,均优于阳性对照brartemicin。
Fifteen novel trehalose derivatives were designed and synthesized with brartemicin as the lead compound. Their structures were confirmed by 1H NMR, MS and elemental analysis. The effects of the target compounds on the proliferation of Hep G2 and A549 tumor cells and normal human HUVECs were investigated by MTT assay. The effects of the target compounds on the adhesion, invasion and migration of Hep G2 and A549 cells were investigated by Matrigel adhesion assay and Transwell chamber assay. The results showed that 15 target cells showed no significant cytotoxicity on Hep G2, A549 and HUVEC cells at a concentration of 1 ~ 32 μmol·L-1 (P> 0.05). In the above concentration range, the inhibitory effect of compounds 79 and 82 on the adhesion, invasion and migration of A549 cells and the adhesion and invasion inhibition of Hep G2 cells were better than the positive control brartemicin.