4.7 Article

Myricetin 3-rhamnoside retards the proliferation of hormone-independent breast cancer cells by targeting hyaluronidase

出版社

TAYLOR & FRANCIS INC
DOI: 10.1080/07391102.2023.2256872

关键词

Myricetin 3-rhamnoside; breast cancer; hyaluronidase; ornithine decarboxylase; MD simulation; in silico molecular docking

向作者/读者索取更多资源

Myricetin 3-rhamnoside exhibits antiproliferative activity and regulates poor prognostic markers in breast cancer cell lines. The findings suggest that Myricetin 3-rhamnoside could serve as a pharmacophore for designing and synthesizing novel agents to manage hormone-independent breast cancer.
Breast cancer is the second-leading cause of cancer-related death in women and the most often diagnosed malignancy. As the majority of chemotherapeutic medications are associated with recurrence, drug resistance, and side effects, scientists are shifting to beneficial agents for prevention and treatment, such as natural molecules. Myricetin 3-rhamnoside, a natural flavonol glycoside is known for diverse pharmacological activities but fewer reports describe the antiproliferative ability. The study aims to investigate the antiproliferative efficacy and target [hyaluronidase (HYAL) and ornithine decarboxylase (ODC), two poor breast cancer prognostic markers] modulatory potential of myricetin 3-rhamnoside on breast cancer cell lines using cytotoxicity assays and in silico docking, molecular dynamics analysis, cell-free and cell-based test methods. Myricetin 3-rhamnoside significantly retard the growth of MDA-MB-231 cells in SRB (IC50 88.64 +/- 7.14 mu M) and MTT (56.26 +/- 8.50 mu M) assay. It suppressed the transition of cells to the S-phase by inducing arrest in the G0/G1 phase with a fold change of 1.10. It shows robust binding interaction with ODC (-7.90 kcal/mol) and HYAL (-9.46 kcal/mol) and inhibits ODC (15.22 +/- 2.61 mM) and HYAL (11.92 +/- 2.89 mM) activity, but in a cell-based assay, the prominent response was observed against HYAL (21.46 +/- 4.03 mM). Besides, it shows a 1.38 folddown regulation of HYAL and forms a stable complex with HYAL. The binding pocket for myricetin 3-rham noside and the simulation pocket during the simulation are identical, indicating that myricetin 3-rhamnoside is actively blocking hyaluronidase. The computational prediction suggests it is a safe molecule. These observations imply that myricetin 3-rhamnoside could be used as a pharmacophore to design and synthesize a novel and safe agent for managing hormone-independent breast cancer.

作者

我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。

评论

主要评分

4.7
评分不足

次要评分

新颖性
-
重要性
-
科学严谨性
-
评价这篇论文

推荐

暂无数据
暂无数据