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天然产物倍半萜内酯如青蒿素等具有重要的药用价值,Dehydrozaluzanin C是一种从兔耳风等药用植物根部提取分离的愈创木内酯类倍半萜内酯,为解决其生物含量的问题、了解其抗肿瘤活性,本研究设计出一种快速、高效的合成方法获得Dehydrozaluzanin C,探讨该化合物对膀胱癌T24细胞增殖、细胞凋亡的影响.实验结果表明,以去氢木香内酯为起始反应物,通过烯丙位氧化、戴斯-马丁氧化两步反应从而获得Dehydrozaluzanin C,总产率为73%.细胞增殖MTT实验结果表明该化合物能显著地制膀胱癌T24细胞的增殖,且该抑制作用呈现出明显的剂量依赖效应;DAPI染色结果表明该化合物能显著诱导T24细胞凋亡,Western Blot免疫印迹分析结果证实该化合物在分子水平上通过PARP的断裂从而诱导细胞凋亡.上述结果表明愈创木内酯Dehydrozaluzanin C对膀胱癌的预防与治疗具有潜在价值.
Natural products such as sesquiterpene lactones such as artemisinin has important medicinal value, Dehydrozaluzanin C is a kind of ligusticillin sesquiterpenoid lactones extracted from the roots of the rabbit ear wind and other medicinal plants, in order to solve its Biological content of the tumor to understand its anti-tumor activity, this study designed a rapid and efficient synthesis of Dehydrozaluzanin C, to explore the compound on bladder cancer T24 cell proliferation, apoptosis.Experimental results show that the dehydro Woody lactone as starting reactant, Dehydrozaluzanin C was obtained by allylic oxidation and Dess-Martin oxidation two-step reaction, the total yield was 73% .MTT assay showed that the compound could significantly inhibit bladder cancer T24 cells in a dose-dependent manner. The results of DAPI staining showed that the compound could significantly induce the apoptosis of T24 cells. Western blot analysis confirmed that the compound was induced by PARP cleavage at the molecular level Apoptosis.The above results show that guaiacolide Dehydrozaluzanin C has a potential value in the prevention and treatment of bladder cancer.