Magnolol and Honokiol Inhibited the Function and Expression of BCRP with Mechanism Exploration
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 <i>Magnolia officinalis</i>. This study investigated the eff...
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| Format: | Article |
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MDPI AG
2021-12-01
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| Series: | Molecules |
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| Online Access: | https://www.mdpi.com/1420-3049/26/23/7390 |
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| author | Chung-Ping Yu Pei-Ying Li Szu-Yu Chen Shiuan-Pey Lin Yu-Chi Hou |
| author_facet | Chung-Ping Yu Pei-Ying Li Szu-Yu Chen Shiuan-Pey Lin Yu-Chi Hou |
| author_sort | Chung-Ping Yu |
| collection | DOAJ |
| description | 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 <i>Magnolia officinalis</i>. 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. |
| first_indexed | 2024-03-10T04:47:37Z |
| format | Article |
| id | doaj.art-b149fca58dfb446bbb4c7c7f78dcc210 |
| institution | Directory Open Access Journal |
| issn | 1420-3049 |
| language | English |
| last_indexed | 2024-03-10T04:47:37Z |
| publishDate | 2021-12-01 |
| publisher | MDPI AG |
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| series | Molecules |
| spelling | doaj.art-b149fca58dfb446bbb4c7c7f78dcc2102023-11-23T02:51:50ZengMDPI AGMolecules1420-30492021-12-012623739010.3390/molecules26237390Magnolol and Honokiol Inhibited the Function and Expression of BCRP with Mechanism ExplorationChung-Ping Yu0Pei-Ying Li1Szu-Yu Chen2Shiuan-Pey Lin3Yu-Chi Hou4School of Pharmacy, College of Pharmacy, China Medical University, Taichung 406040, TaiwanSchool of Pharmacy, College of Pharmacy, China Medical University, Taichung 406040, TaiwanSchool of Pharmacy, College of Pharmacy, China Medical University, Taichung 406040, TaiwanSchool of Pharmacy, College of Pharmacy, China Medical University, Taichung 406040, TaiwanSchool of Pharmacy, College of Pharmacy, China Medical University, Taichung 406040, TaiwanBreast 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 <i>Magnolia officinalis</i>. 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.https://www.mdpi.com/1420-3049/26/23/7390magnololhonokiolBCRPEGFRMDR |
| spellingShingle | Chung-Ping Yu Pei-Ying Li Szu-Yu Chen Shiuan-Pey Lin Yu-Chi Hou Magnolol and Honokiol Inhibited the Function and Expression of BCRP with Mechanism Exploration Molecules magnolol honokiol BCRP EGFR MDR |
| title | Magnolol and Honokiol Inhibited the Function and Expression of BCRP with Mechanism Exploration |
| title_full | Magnolol and Honokiol Inhibited the Function and Expression of BCRP with Mechanism Exploration |
| title_fullStr | Magnolol and Honokiol Inhibited the Function and Expression of BCRP with Mechanism Exploration |
| title_full_unstemmed | Magnolol and Honokiol Inhibited the Function and Expression of BCRP with Mechanism Exploration |
| title_short | Magnolol and Honokiol Inhibited the Function and Expression of BCRP with Mechanism Exploration |
| title_sort | magnolol and honokiol inhibited the function and expression of bcrp with mechanism exploration |
| topic | magnolol honokiol BCRP EGFR MDR |
| url | https://www.mdpi.com/1420-3049/26/23/7390 |
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