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Published on: May 27, 2016
Magnolol and Honokiol Inhibited the Function and Expression of BCRP with Mechanism Exploration
Chung-Ping Yu1,2, Pei-Ying Li1, Szu-Yu Chen1
1School of Pharmacy, College of Pharmacy, China Medical University, Taichung 406040, Taiwan.
Abstract:
Breast cancer resistance protein (BCRP), one of the ATP-binding cassette (ABC) transporters, was associated with the multidrug resistance (MDR) of chemotherapy. Magnolol (MN) and honokiol (HK) are major bioactive polyphenols of Magnolia officinalis. This study investigated the effects of MN and HK on the function and expression of BCRP for the purpose of developing BCRP inhibitor to overcome MDR. Cell lines including MDCKII-BCRP and MDCKII-WT were used for evaluating the function and expression of BCRP. The results showed that MN (100-12.5 µM) and HK (100-12.5 µM) significantly decreased the function of BCRP by 80~12% and 67~14%, respectively. In addition, MN and HK were verified as substrates of BCRP. Furthermore, MN and HK reduced the protein expression of BCRP, and inhibited the phosphorylation of epidermal growth factor receptor (EGFR) and phosphatidylinositol 3-kinase (PI3K). In conclusion, both MN and HK decreased the function and expression of BCRP via EGFR/PI3K signaling pathway. Therefore, both compounds were promising candidates for reversing the MDR of chemotherapy.
Insights
Magnolol and honokiol inhibit breast cancer resistance protein (BCRP) function and expression, offering potential to overcome chemotherapy multidrug resistance (MDR). These natural compounds may reverse MDR by targeting the EGFR/PI3K pathway.
Area of Science:
- Pharmacology
- Biochemistry
- Molecular Biology
Background:
- Breast cancer resistance protein (BCRP) is an ABC transporter linked to chemotherapy multidrug resistance (MDR).
- Magnolol (MN) and honokiol (HK) are bioactive polyphenols from *Magnolia officinalis*.
Purpose of the Study:
- To investigate the effects of MN and HK on BCRP function and expression.
- To explore the potential of MN and HK as BCRP inhibitors to overcome MDR.
Main Methods:
- Utilized MDCKII-BCRP and MDCKII-WT cell lines to assess BCRP function and expression.
- Evaluated the impact of MN and HK on BCRP activity, expression, and related signaling pathways (EGFR/PI3K).
Main Results:
- MN and HK significantly decreased BCRP function (80-12% and 67-14%, respectively) and were identified as BCRP substrates.
- Both compounds reduced BCRP protein expression and inhibited EGFR and PI3K phosphorylation.
- MN and HK modulate BCRP via the EGFR/PI3K signaling pathway.
Conclusions:
- MN and HK effectively decrease BCRP function and expression.
- These polyphenols show promise in reversing chemotherapy-induced MDR by targeting the EGFR/PI3K pathway.
