Abstract

Hyperoside (quercetin 3-o-β-d-galactopyranoside) is one of the flavonoid glycosides with anti-inflammatory, antidepressant, and anti-cancer effects. But it remains unknown whether it had effects on breast cancer. Here, different concentrations of hyperoside were used to explore its therapeutic potential in both breast cancer cells and subcutaneous homotransplant mouse model. CCK-8 and wound healing assays showed that the viability and migration capability of Michigan Cancer Foundation-7 (MCF-7) and 4T1 cells were inhibited by hyperoside, while the apoptosis of cells were increased. Real-time quantitative PCR (qRT-PCR) and western blot analysis were used to detect mRNA and the protein level, respectively, which showed decreased levels of B cell lymphoma-2 (Bcl-2) and X-linked inhibitor of apoptosis (XIAP), and increased levels of Bax and cleaved caspase-3. After exploration of the potential mechanism, we found that reactive oxygen species (ROS) production was reduced by the administration of hyperoside, which subsequently inhibited the activation of NF-κB signaling pathway. Tumor volume was significantly decreased in subcutaneous homotransplant mouse model in hyperoside-treated group, which was consistent with our study in vitro. These results indicated that hyperoside acted as an anticancer drug through ROS-related apoptosis and its mechanism included activation of the Bax–caspase-3 axis and the inhibition of the NF-κB signaling pathway.

Highlights

  • Breast cancer causes great concern for public health

  • In order to further explore the mechanism of hyperoside promoting apoptosis on breast cancer cells, we tested reactive oxygen species (ROS) levels after the stimulation of hyperoside

  • Results showed that the ROS level was decreased with the increased concentration of hyperoside (Figure 3a,b)

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Summary

Introduction

Breast cancer causes great concern for public health. According to a report about breast cancer published in 2018, the morbidity rate of breast cancer was almost equivalent to lung cancer (11.6%)and the mortality rate was the second among all cancers (6.6%) [1]. Breast cancer causes great concern for public health. Breast cancer is the leading cause for female death, followed by colorectal cancer and lung cancer [2]. Traditional therapies for breast cancer involve surgery, radiotherapy and chemotherapy [3,4], while there are many new methods like endocrine therapy, biological target therapy and traditional Chinese medicine therapy [5,6]. Chinese medicine has tremendous importance in chemotherapy as it has lesser side effects and toxicity [7], a great deal of studies has been devoted to identify novel drugs with potential for breast cancer treatment in recent years. We need to explore the molecular mechanism of the anti-breast cancer drugs for better treatment

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