Article Publish Status: FREE
Abstract Title:

Berberine Reverses Breast Cancer Multidrug Resistance Based on Fluorescence Pharmacokineticsand.

Abstract Source:

ACS Omega. 2021 Apr 27 ;6(16):10645-10654. Epub 2021 Apr 13. PMID: 34056218

Abstract Author(s):

Ke Qian, Chao-Yuan Tang, Li-Ying Chen, Shuang Zheng, Yue Zhao, Li-Sha Ma, Li Xu, Lu-Hui Fan, Jian-Dong Yu, Hong-Sheng Tan, Ya-Lan Sun, Li-Li Shen, Yang Lu, Qi Liu, Yun Liu, Yang Xiong

Article Affiliation:

Ke Qian


Exploring the mechanism through which berberine (Ber) reverses the multidrug resistance (MDR) of breast cancer is of great importance. Herein, we used the methyl thiazolyl tetrazolium assay to determine the drug resistance and cytotoxicity of Ber and doxorubicin (DOX) alone or in combination on the breast cancer cell line MCF-7/DOX. The results showed that Ber could synergistically enhance the inhibitory effect of DOX on tumor cell proliferation, and the optimal combination ratio was Ber/DOX = 2:1. Using a luciferase reporter assay system combined with the bioluminescence imaging technology, the efflux kinetics of d-luciferin potassium salt in MCF-7/DOXcells treated with Berwas investigated. The results showed that Ber could significantly reduce the efflux of d-luciferin potassium salt in MCF-7/DOXcells. In addition, western blot and immunohistochemistry experiments showed that the expression of P-glycoprotein (P-gp/ABCB1) and multidrug resistance protein 1 (MRP1/ABCC1) in MCF-7/DOXcells was downregulated upon Ber treatment. Finally, high-performance liquid chromatography was used to investigate the effect of Ber on DOX tissue distribution, and the results showed that the uptake of DOX in tumor tissues increased significantly when combined with Ber (<0.05). Thus, the results illustrated that Ber can reverse MDR by inhibiting the efflux function of ATP-binding cassette transporters and downregulating their expression levels.

Study Type : Animal Study, In Vitro Study

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