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Molecules 2017, 22(11), 1847; doi:10.3390/molecules22111847

Berberine Activates Aryl Hydrocarbon Receptor but Suppresses CYP1A1 Induction through miR-21-3p Stimulation in MCF-7 Breast Cancer Cells

1
Division of Basic Chinese Medicine, National Research Institute of Chinese Medicine, Taipei 112, Taiwan
2
Institute of Biopharmaceutical Sciences, School of Pharmacy, National Yang-Ming University, Taipei 112, Taiwan
3
Department of Chemistry, National Cheng-Kung University, Tainen 701, Taiwan
4
National Institute of Environmental Health Sciences, National Health Research Institutes, Zhunan, Miaoli 350, Taiwan
5
Division of Chinese Materia Medica Development, National Research Institute of Chinese Medicine, Taipei 112, Taiwan
6
Institute of Medical Sciences, Taipei Medical University, Taipei 101, Taiwan
7
Department and Institute of Pharmacology, School of Medicine, National Yang-Ming University, Taipei 112, Taiwan
*
Author to whom correspondence should be addressed.
Received: 4 October 2017 / Revised: 19 October 2017 / Accepted: 25 October 2017 / Published: 28 October 2017
View Full-Text   |   Download PDF [1745 KB, uploaded 31 October 2017]   |  

Abstract

Berberine and the methylenedioxy ring-opening derivatives palmatine and jatrorrhizine are active ingredients in immunomodulatory plants, such as goldenseal. This study aimed to illustrate the effects of protoberberines on aryl hydrocarbon receptor (AhR) activation and cytochrome P450 (CYP) 1 in the estrogen receptor (ER)α(+) MCF-7 breast cancer cells. Among protoberberines at non-cytotoxic concentrations (≤10 μM), berberine had the most potent and statistically significant effects on AhR activation and CYP1A1/1A2/1B1 mRNA induction. The 24-h exposure to 10 μM berberine did not change CYP1A1 mRNA stability, protein level and function. Berberine significantly increased micro RNA (miR)-21-3p by 36% and the transfection of an inhibitor of miR-21-3p restored the induction of CYP1A1 protein with a 50% increase. These findings demonstrate that the ring opening of the methylenedioxyl moiety in berberine decreased AhR activation in MCF-7 cells. While CYP1A1 mRNA was elevated, berberine-induced miR-21-3p suppressed the increase of functional CYP1A1 protein expression. View Full-Text
Keywords: berberine; aryl hydrocarbon receptor; CYP1A1; miR-21-3p; breast cancer cells berberine; aryl hydrocarbon receptor; CYP1A1; miR-21-3p; breast cancer cells
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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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MDPI and ACS Style

Lo, S.-N.; Wang, C.-W.; Chen, Y.-S.; Huang, C.-C.; Wu, T.-S.; Li, L.-A.; Lee, I.-J.; Ueng, Y.-F. Berberine Activates Aryl Hydrocarbon Receptor but Suppresses CYP1A1 Induction through miR-21-3p Stimulation in MCF-7 Breast Cancer Cells. Molecules 2017, 22, 1847.

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