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Molecules 2016, 21(2), 183;

Alisol F 24 Acetate Enhances Chemosensitivity and Apoptosis of MCF-7/DOX Cells by Inhibiting P-Glycoprotein-Mediated Drug Efflux

Tianjin State Key Laboratory of Modern Chinese Medicine, Tianjin University of Traditional Chinese Medicine, Tianjin 300193, China
Tianjin International Joint Academy of Biomedicine, Tianjin 300457, China
Author to whom correspondence should be addressed.
Academic Editor: Helena Vasconcelos
Received: 30 November 2015 / Revised: 26 January 2016 / Accepted: 28 January 2016 / Published: 4 February 2016
(This article belongs to the Special Issue New Approaches to Counteract Drug Resistance in Cancer)
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Multidrug resistance (MDR) is a prime reason for numerous failed oncotherapy approaches. In the present study, we investigated whether Alisol F 24 acetate (ALI) could reverse the MDR of MCF-7/DOX cells, a multidrug-resistant human breast cancer cell line. We found that ALI was a potent P-glycoprotein (P-gp) inhibitor, in the Caco-2-monolayer cell model. ALI showed a significant and concentration-dependent cytotoxic effect on MCF-7/DOX cells in combination with doxorubicin by increasing intracellular accumulation and inducing nuclear migration of doxorubicin. However, ALI had no such effect on MCF-7 cells. In addition, ALI also promoted doxorubicin-induced early apoptosis of MCF-7/DOX cells in a time-dependent manner. These results suggest that ALI can enhance chemosensitivity of doxorubicin and reinforce its anti-cancer effect by increasing its uptake, especially inducing its nuclear accumulation in MCF-7/DOX cells. Therefore, ALI could be developed as a potential MDR-reversing agent in cancer chemotherapy in further study. View Full-Text
Keywords: alisol F 24-acetate (ALI); multidrug resistance (MDR); doxorubicin; P-glycoprotein (P-gp) alisol F 24-acetate (ALI); multidrug resistance (MDR); doxorubicin; P-glycoprotein (P-gp)

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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).

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Pan, G.; Li, T.; Zeng, Q.; Wang, X.; Zhu, Y. Alisol F 24 Acetate Enhances Chemosensitivity and Apoptosis of MCF-7/DOX Cells by Inhibiting P-Glycoprotein-Mediated Drug Efflux. Molecules 2016, 21, 183.

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