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

  • 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.

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Metadaten
URN:urn:nbn:de:kobv:526-opus4-12932
Publisher DOI:https://doi.org/10.3390/pharmaceutics11110586
Author:Anna GrebinykORCiD, Svitlana PrylutskaORCiD, Anatoliy Buchelnikov, Nina Tverdokhleb, Sergii GrebinykORCiD, Maxim Evstigneev, Olga Matyshevska, Vsevolod Cherepanov, Yuriy PrylutskyyORCiD, Valeriy YashchukORCiD, Anton Naumovets, Uwe RitterORCiD, Thomas DandekarORCiDGND, Marcus FrohmeORCiDGND
ISSN:1999-4923
Parent Title (English):Pharmaceutics
Document Type:Article
Language:English
Year of Publication:2019
Volume:11
Issue:11
Publisher:MDPI
Faculties an central facilities:Fachbereich Ingenieur- und Naturwissenschaften
Date of first Publication:2019/11/08
Publishing Institution:Technische Hochschule Wildau
Tag:C60 fullerene; DLS and AFM measurements; UV–Vis; apoptosis; berberine; cytotoxicity; drug release; leukemic cell; noncovalent nanocomplex; uptake
Source:Grebinyk, A., Prylutska, S., Buchelnikov, A., Tverdokhleb, N., Grebinyk, S., Evstigneev, M., et al. (2019). C60 Fullerene as an Effective Nanoplatform of Alkaloid Berberine Delivery into Leukemic Cells Pharmaceutics. 11 (11), 586.
Dewey Decimal Classification:5 Naturwissenschaften und Mathematik / 57 Biowissenschaften; Biologie / 570 Biowissenschaften; Biologie
Funding:DFG-geförderter Publikationsfonds
Licence (German):Creative Commons - CC BY - Namensnennung 4.0 International
Release Date:2019/12/18
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