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以埃博霉素B为先导化合物,用不同分子量的聚乙二醇衍生物(PEG-NH_2或PEG-SH)对其进行修饰,合成了11个水溶性埃博霉素B衍生物,并通过NMR和MS确证了其结构。采用MTT法考察了目标化合物对人体肝癌细胞HepG2的抑制作用,并通过考察其对人体原代肝细胞的半数致死率评价了目标化合物的毒性。结果表明,目标化合物对HepG2均表现出较好的抑制作用,对人体原代肝细胞毒性明显下降,水溶性也得到明显改善。
Epothilone B as the lead compound was modified with polyethylene glycol derivatives of different molecular weights (PEG-NH 2 or PEG-SH) to synthesize 11 water-soluble epothilone B derivatives by NMR and MS confirmed its structure. The inhibitory effect of the target compound on HepG2 human hepatocellular carcinoma cell line was investigated by MTT assay. The toxicity of the target compound was evaluated by investigating its half-lethality on human primary hepatocytes. The results showed that the target compounds showed good inhibitory effect on HepG2, significantly reduced the toxicity of human primary hepatocytes, and significantly improved water solubility.