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目的:设计并合成积雪草酸A环、C-23位羟基以及C-28位羧基衍生物,并对其体外抗肿瘤活性进行测试。方法:以天然产物积雪草酸为先导化合物,经氧化、酰化等反应对其A环、C-23位羟基以及C-28位羧基进行结构修饰,合成2,3-二氧代-2,3-开环-23-羟基(乙酰基)-乌苏烷型-12-烯-28-酯类衍生物。结果:经MS及1H-NMR谱图解析得到确证。结论:采用MTT法,选用人癌细胞SGC-7901和A549对它们进行初步的体外抗肿瘤活性测试。目标化合物对2种细胞株的抑制率均明显高于母体化合物,且化合物g和k的抑制效果高于吉非替尼,值得进一步研究。
OBJECTIVE: To design and synthesize Centella asiatica A-ring, C-23 hydroxyl group and C-28 carboxyl derivative, and to test the antitumor activity in vitro. Methods: The natural product Asiatic acid was used as the lead compound, and its A ring, C-23 hydroxyl group and C-28 carboxyl group were modified by oxidation and acylation to synthesize 2,3-dioxo-2, 3-Ring-opened-23-hydroxy (acetyl) -sursuchen-12-en-28-ester derivatives. Results: confirmed by MS and 1H-NMR spectral analysis. Conclusion: MTT assay was used to test the anti-tumor activity of SGC-7901 and A549 in vitro. The inhibitory rates of the target compounds on the two cell lines were significantly higher than that of the parent compound, and the inhibitory effect of the compounds g and k was higher than that of gefitinib, which deserved further study.