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目的合成具有抗炎活性的天然三萜皂苷——齐墩果酸3-O-β-D葡萄糖(1→3α)--L-鼠李糖(1→2)α--L-吡喃阿拉伯糖苷(1)。方法以齐墩果酸为起始原料,采用逐步糖苷化策略,应用苄基、异丙亚甲基、乙酰氧基、过原酸酯等保护基方法,合成目标产物。以三萜皂苷β-hederin为阳性对照,采用MTT法测试目标物对肿瘤细胞的抑制活性。结果与结论经13步反应合成目标化合物,总收率23.7%,目标化合物结构经M S和1H-NMR确证。初步的体外药理实验结果表明,合成的皂苷产物仍然具有较强的肿瘤细胞毒活性。
OBJECTIVE To synthesize natural triterpene saponin-oleanolic acid 3-O-β-D glucose (1 → 3α) -L-rhamnose (1 → 2) α-L-arabinopyranoside Glycoside (1). Methods Using oleanolic acid as the starting material, the target product was synthesized by a stepwise glycosylation strategy using benzyl, isopropylethylene, acetoxy, peroxyester and other protecting groups. Triterpene saponin β-hederin as a positive control, the use of MTT assay of the target inhibitory activity of tumor cells. Results and Conclusion The target compounds were synthesized in 13 steps with the total yield of 23.7%. The structures of target compounds were confirmed by M S and 1H-NMR. Preliminary pharmacological experiments in vitro showed that the synthesized saponin products still have strong tumor cytotoxic activity.