Anthraquinones are a major class of compounds naturally occurring in Asphodelus microcarpus. The pharmacological actions of anthraquinones in cancer cells are known to induce apoptosis or autophagy, and revert multidrug resistance. In this study, five anthraquinone-type analogs were isolated from the methanol extract of A. microcarpus leaves and identified as, emodin, rhein, physcion, aloe-emodin, and emodic acid. Among them, aloe-emodin and emodic-acid strongly inhibited the proliferation, cells-intrinsic NF-κB activity and metastatic ability of breast cancer. Although aloe-emodin inhibited p38 and ERK phosphorylation, emodic-acid more markedly inhibited JNK, in addition to p38 and ERK phosphorylation. Both aloe-emodin and emodic-acid inhibited the secretion of the pro-tumorigenic cytokines IL-1β and IL-6, and VEGF and MMP expression, and subsequently inhibited the invasive and migratory potential of 4T1 cells. Thus, our study demonstrated the effects of aloe-emodin and emodin-acid in controlling the migratory and invasive ability of 4T1 breast cancer cells, in addition to inhibiting NF-κB activity and the expression of its downstream target molecules.

蒽醌是天然存在于小果油菜中的一大类化合物。已知蒽醌在癌细胞中的药理作用可诱导细胞凋亡或自噬，并恢复多药耐药性。在本研究中，从A. microcarpus的甲醇提取物中分离出五种蒽醌类类似物叶并鉴定为大黄素、大黄酸、大黄素、芦荟大黄素和大黄素。其中，芦荟大黄素和大黄素酸对乳腺癌的增殖、细胞内源性NF-κB活性和转移能力有很强的抑制作用。尽管芦荟大黄素抑制 p38 和 ERK 磷酸化，但除 p38 和 ERK 磷酸化外，大黄素还能更显着地抑制 JNK。芦荟大黄素和大黄素酸均抑制促肿瘤细胞因子 IL-1β 和 IL-6 的分泌，以及 VEGF 和 MMP 的表达，进而抑制 4T1 细胞的侵袭和迁移潜能。因此，我们的研究证明了芦荟大黄素和大黄素酸除了抑制 NF-κB 活性及其下游靶分子的表达外，还可以控制 4T1 乳腺癌细胞的迁移和侵袭能力。