Cytotoxic and pro-apoptotic activities of medicarpin from Canavalia maritima(Aubl.) via the suppression of NF-κB activation in HeLa cells

海洋植物海刀豆紫檀素抑制人肿瘤细胞NF-κB活化所致细胞毒性和凋亡作用研究(英文)

Three known pterocarpin derivatives, （-）-medicarpin （PDI）, （-）-2-hydroxy-4,9-dimethoxypterocarpan （PD2）, and 4- hydroxy-3-methoxy-8,9-methylene-dioxypterocarpan （PD3） were isolated from Canavalia maritima, for the first time. The cytotoxic and pro-apoptotic activities of （-）-medicarpin in cutured human tumor HeLa cells and its effect on NF-r,B activation were investigated. We found that PD1 inhibited NF-r,B activation by high content screening analysis, and PD1 exhibited cytotoxicity by SRB assay. In addition, we found that PD1 induced nuclear condensation and increased membrane permeability and mitochondrial transmembrane potential in HeLa cells in a dose and time dependent manner. In conclusion, our data suggested that （- ）-medicarpin was capable of inhibiting tumor cell growth in vitro and inducing apoptosis, which might be via the suppression of NF-kB activation.

从海刀豆中首次分离得到三个已知化合物,(-)-medicarpin(PD1),(-)-2-hydroxy-4,9-dimethoxypterocarpan(PD2),4-hydroxy-3-methoxy-8,9-methylene-dioxy-pterocarpan(PD3),并探讨PD1对人肿瘤细胞的细胞毒性和诱导细胞凋亡作用。高内涵筛选分析结果表明,化合物PD1可以抑制NF-κB的活化,诱导细胞核固缩、改变细胞膜通透性与线粒体膜电势,抑制肿瘤细胞增殖。