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Article

Palmatine, a Bioactive Protoberberine Alkaloid Isolated from Berberis cretica, Inhibits the Growth of Human Estrogen Receptor-Positive Breast Cancer Cells and Acts Synergistically and Additively with Doxorubicin

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Department of Biochemistry and Molecular Biology, Medical University of Lublin, Chodzki 1, 20-093 Lublin, Poland
2
Department of Pathophysiology, Medical University of Lublin, Jaczewskiego 8b, 20-090 Lublin, Poland
3
Department of Pharmacognosy with Medicinal Plants Garden, Medical University of Lublin, Chodzki 1, 20-093 Lublin, Poland
4
Laboratory of Pharmacognosy and Natural Products Chemistry, School of Pharmacy, National and Kapodistrian University of Athens, Panepistimioupoli Zografou, 15771 Athens, Greece
5
Independent Medical Biology Unit, Medical University of Lublin, Jaczewskiego 8b, 20-090 Lublin, Poland
*
Author to whom correspondence should be addressed.
Academic Editors: Anna Stochmal, Jerzy Żuchowski, Solomiia Kozachok, Andy J. Pérez and Łukasz Pecio
Molecules 2021, 26(20), 6253; https://doi.org/10.3390/molecules26206253
Received: 2 September 2021 / Revised: 1 October 2021 / Accepted: 8 October 2021 / Published: 15 October 2021
Palmatine (PLT) is a natural isoquinoline alkaloid that belongs to the class of protoberberines and exhibits a wide spectrum of pharmacological and biological properties, including anti-cancer activity. The aim of our study was to isolate PLT from the roots of Berberis cretica and investigate its cytotoxic and anti-proliferative effects in vitro alone and in combination with doxorubicine (DOX) using human ER+/HER2 breast cancer cell lines. The alkaloid was purified by column chromatography filled with silica gel NP and Sephadex LH-20 resin developed in the mixture of methanol: water (50:50 v/v) that provided high-purity alkaloid for bioactivity studies. The purity of the alkaloid was confirmed by high resolution mass measurement and MS/MS fragmentation analysis in the HPLC-ESI-QTOF-MS/MS-based analysis. It was found that PLT treatment inhibited the viability and proliferation of breast cancer cells in a dose-dependent manner as demonstrated by MTT and BrdU assays. PLT showed a quite similar growth inhibition on breast cancer cells with IC50 values ranging from 5.126 to 5.805 µg/mL. In contrast, growth of normal human breast epithelial cells was not affected by PLT. The growth inhibitory activity of PLT was related to the induction of apoptosis, as determined by Annexin V/PI staining. Moreover, PLT sensitized breast cancer cells to DOX. Isobolographic analysis revealed synergistic and additive interactions between studied agents. Our studies suggest that PLT can be a potential candidate agent for preventing and treating breast cancer. View Full-Text
Keywords: palmatine; isoquinoline alkaloids; Berberis cretica; Berberidaceae; breast cancer; isobolographic analysis; natural products; HPLC-MS palmatine; isoquinoline alkaloids; Berberis cretica; Berberidaceae; breast cancer; isobolographic analysis; natural products; HPLC-MS
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MDPI and ACS Style

Grabarska, A.; Wróblewska-Łuczka, P.; Kukula-Koch, W.; Łuszczki, J.J.; Kalpoutzakis, E.; Adamczuk, G.; Skaltsounis, A.L.; Stepulak, A. Palmatine, a Bioactive Protoberberine Alkaloid Isolated from Berberis cretica, Inhibits the Growth of Human Estrogen Receptor-Positive Breast Cancer Cells and Acts Synergistically and Additively with Doxorubicin. Molecules 2021, 26, 6253. https://doi.org/10.3390/molecules26206253

AMA Style

Grabarska A, Wróblewska-Łuczka P, Kukula-Koch W, Łuszczki JJ, Kalpoutzakis E, Adamczuk G, Skaltsounis AL, Stepulak A. Palmatine, a Bioactive Protoberberine Alkaloid Isolated from Berberis cretica, Inhibits the Growth of Human Estrogen Receptor-Positive Breast Cancer Cells and Acts Synergistically and Additively with Doxorubicin. Molecules. 2021; 26(20):6253. https://doi.org/10.3390/molecules26206253

Chicago/Turabian Style

Grabarska, Aneta, Paula Wróblewska-Łuczka, Wirginia Kukula-Koch, Jarogniew J. Łuszczki, Eleftherios Kalpoutzakis, Grzegorz Adamczuk, Alexios L. Skaltsounis, and Andrzej Stepulak. 2021. "Palmatine, a Bioactive Protoberberine Alkaloid Isolated from Berberis cretica, Inhibits the Growth of Human Estrogen Receptor-Positive Breast Cancer Cells and Acts Synergistically and Additively with Doxorubicin" Molecules 26, no. 20: 6253. https://doi.org/10.3390/molecules26206253

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