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Article

C60 Fullerene as an Effective Nanoplatform of Alkaloid Berberine Delivery into Leukemic Cells

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Division Molecular Biotechnology and Functional Genomics, Technical University of Applied Sciences Wildau, Hochschulring 1, 15745 Wildau, Germany
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Department of Bioinformatics, Biocenter, University of Würzburg, Am Hubland, 97074 Würzburg, Germany
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Taras Shevchenko National University of Kyiv, Volodymyrska 64, 01601 Kyiv, Ukraine
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Laboratory of Molecular and Cell Biophysics, Sevastopol State University, 299053 Sevastopol, Crimea
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Laboratory of Organic Synthesis and NMR Spectroscopy, Belgorod State University, 308015 Belgorod, Russia
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Palladin Institute of Biochemistry, NAS of Ukraine, Leontovicha Str. 9, 01030 Kyiv, Ukraine
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Institute of Physics, NAS of Ukraine, 46 av. Nauki, 03028 Kyiv, Ukraine
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Institute of Chemistry and Biotechnology, University of Technology Ilmenau, Weimarer Straße 25 (Curiebau), 98693 Ilmenau, Germany
*
Author to whom correspondence should be addressed.
Pharmaceutics 2019, 11(11), 586; https://doi.org/10.3390/pharmaceutics11110586
Received: 8 October 2019 / Revised: 4 November 2019 / Accepted: 5 November 2019 / Published: 8 November 2019
A herbal alkaloid Berberine (Ber), used for centuries in Ayurvedic, Chinese, Middle-Eastern, and native American folk medicines, is nowadays proved to function as a safe anticancer agent. Yet, its poor water solubility, stability, and bioavailability hinder clinical application. In this study, we have explored a nanosized carbon nanoparticle—C60 fullerene (C60)—for optimized Ber delivery into leukemic cells. Water dispersions of noncovalent C60-Ber nanocomplexes in the 1:2, 1:1, and 2:1 molar ratios were prepared. UV–Vis spectroscopy, dynamic light scattering (DLS), and atomic force microscopy (AFM) evidenced a complexation of the Ber cation with the negatively charged C60 molecule. The computer simulation showed that π-stacking dominates in Ber and C60 binding in an aqueous solution. Complexation with C60 was found to promote Ber intracellular uptake. By increasing C60 concentration, the C60-Ber nanocomplexes exhibited higher antiproliferative potential towards CCRF-CEM cells, in accordance with the following order: free Ber < 1:2 < 1:1 < 2:1 (the most toxic). The activation of caspase 3/7 and accumulation in the sub-G1 phase of CCRF-CEM cells treated with C60-Ber nanocomplexes evidenced apoptosis induction. Thus, this study indicates that the fast and easy noncovalent complexation of alkaloid Ber with C60 improved its in vitro efficiency against cancer cells. View Full-Text
Keywords: C60 fullerene; Berberine; noncovalent nanocomplex; UV–Vis; DLS and AFM measurements; drug release; leukemic cells; uptake; cytotoxicity; apoptosis C60 fullerene; Berberine; noncovalent nanocomplex; UV–Vis; DLS and AFM measurements; drug release; leukemic cells; uptake; cytotoxicity; apoptosis
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MDPI and ACS Style

Grebinyk, A.; Prylutska, S.; Buchelnikov, A.; Tverdokhleb, N.; Grebinyk, S.; Evstigneev, M.; Matyshevska, O.; Cherepanov, V.; Prylutskyy, Y.; Yashchuk, V.; Naumovets, A.; Ritter, U.; Dandekar, T.; Frohme, M. C60 Fullerene as an Effective Nanoplatform of Alkaloid Berberine Delivery into Leukemic Cells. Pharmaceutics 2019, 11, 586. https://doi.org/10.3390/pharmaceutics11110586

AMA Style

Grebinyk A, Prylutska S, Buchelnikov A, Tverdokhleb N, Grebinyk S, Evstigneev M, Matyshevska O, Cherepanov V, Prylutskyy Y, Yashchuk V, Naumovets A, Ritter U, Dandekar T, Frohme M. C60 Fullerene as an Effective Nanoplatform of Alkaloid Berberine Delivery into Leukemic Cells. Pharmaceutics. 2019; 11(11):586. https://doi.org/10.3390/pharmaceutics11110586

Chicago/Turabian Style

Grebinyk, Anna, Svitlana Prylutska, Anatoliy Buchelnikov, Nina Tverdokhleb, Sergii Grebinyk, Maxim Evstigneev, Olga Matyshevska, Vsevolod Cherepanov, Yuriy Prylutskyy, Valeriy Yashchuk, Anton Naumovets, Uwe Ritter, Thomas Dandekar, and Marcus Frohme. 2019. "C60 Fullerene as an Effective Nanoplatform of Alkaloid Berberine Delivery into Leukemic Cells" Pharmaceutics 11, no. 11: 586. https://doi.org/10.3390/pharmaceutics11110586

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