Despite the broad anticancer activity, whereas the clinical application of luteolin is hindered by unsatisfactory water solubility and non-targeting. Herein, targeted inhibitory effects of luteolin-loading HER2 nanospheres (Her-2-NPs) were successfully prepared by thin film ultrasonic method. In comparison with the non-targeted nanospheres, Her-2 nanospheres could significantly boost the intake of luteolin in SK-BR-3 cells. The proliferation and apoptosis of breast cancer cells were detected by MTT testing and flow cytometry examination, respectively. Consequently, the expressions of FOXO1 mRNA level was detected using qPCR assay and protein level was detected using Westernblot. We discovered that Luteolin-loading Her-2 nanospheres could significantly hinder the proliferation of breast cancer cells, down-regulation their migration, and up-regulation FOXO1 expression at mRNA and protein levels, reveal a mechanism whereby luteolin interferes with breast cancer. Collectively, these results suggest Her-2-modified nanospheres increases the efficiency of luteolin uptake and thus improves the treatment benefit of breast cancer.

中文翻译：

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装载木犀草素的 Her-2 纳米球增强了乳腺癌的靶向和治疗效果。

尽管具有广泛的抗癌活性，但木犀草素的临床应用受到不令人满意的水溶性和非靶向性的阻碍。在此，通过薄膜超声法成功制备了负载木犀草素的HER2纳米球（Her-2-NPs）的靶向抑制作用。与非靶向纳米球相比，Her-2 纳米球可以显着提高 SK-BR-3 细胞中木犀草素的摄入量。分别采用MTT法和流式细胞术检测乳腺癌细胞的增殖和凋亡情况。因此，使用qPCR测定法检测FOXO1 mRNA水平的表达，使用Westernblot检测蛋白质水平。我们发现装载木犀草素的 Her-2 纳米球可以显着阻碍乳腺癌细胞的增殖，下调它们的迁移，在 mRNA 和蛋白质水平上调 FOXO1 表达，揭示木犀草素干扰乳腺癌的机制。总的来说，这些结果表明 Her-2 修饰的纳米球提高了木犀草素的吸收效率，从而提高了乳腺癌的治疗效果。