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C60 fullerene as an effective nanoplatform of alkaloid Berberine delivery into leukemic cells

Please always quote using this URN: urn:nbn:de:bvb:20-opus-193216
  • 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, dynamicA 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 C\(_{60}\) binding in an aqueous solution. Complexation with C\(_{60}\) was found to promote Ber intracellular uptake. By increasing C\(_{60}\) concentration, the C\(_{60}\)-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 C\(_{60}\)-Ber nanocomplexes evidenced apoptosis induction. Thus, this study indicates that the fast and easy noncovalent complexation of alkaloid Ber with C\(_{60}\) improved its in vitro efficiency against cancer cells.show moreshow less

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Metadaten
Author: Anna Grebinyk, Svitlana Prylutska, Anatoliy Buchelnikov, Nina Tverdokhleb, Sergii Grebinyk, Maxim Evstigneev, Olga Matyshevska, Vsevolod Cherepanov, Yuriy Prylutskyy, Valeriy Yashchuk, Anton Naumovets, Uwe Ritter, Thomas Dandekar, Marcus Frohme
URN:urn:nbn:de:bvb:20-opus-193216
Document Type:Journal article
Faculties:Fakultät für Biologie / Theodor-Boveri-Institut für Biowissenschaften
Language:English
Parent Title (English):Pharmaceutics
ISSN:1999-4923
Year of Completion:2019
Volume:11
Issue:11
Pagenumber:586
Source:Pharmaceutics 2019, 11(11), 586; https://doi.org/10.3390/pharmaceutics11110586
DOI:https://doi.org/10.3390/pharmaceutics11110586
Dewey Decimal Classification:5 Naturwissenschaften und Mathematik / 57 Biowissenschaften; Biologie / 570 Biowissenschaften; Biologie
Tag:Berberine; C60 fullerene; DLS and AFM measurements; UV–Vis; apoptosis; cytotoxicity; drug release; leukemic cells; noncovalent nanocomplex; uptake
Release Date:2020/08/18
Date of first Publication:2019/11/08
Licence (German):License LogoCC BY: Creative-Commons-Lizenz: Namensnennung 4.0 International