Journal
BIOORGANIC CHEMISTRY
Volume 117, Issue -, Pages -Publisher
ACADEMIC PRESS INC ELSEVIER SCIENCE
DOI: 10.1016/j.bioorg.2021.105415
Keywords
Pillar[5]arene; Binase; Bleomycin; Lysozyme; A549 cells; Macrocyclic receptors
Funding
- Russian Science Foundation [17-13-01208]
- Russian Science Foundation [20-13-18010] Funding Source: Russian Science Foundation
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The supramolecular complexes formed by pillar[5]arenes containing sulfonate fragments with therapeutic proteins can penetrate tumor cells and exhibit significant cytotoxicity towards them, while maintaining the enzymatic activity of the proteins.
Pillar[5]arenes containing sulfonate fragments have been shown to form supramolecular complexes with therapeutic proteins to facilitate targeted transport with an increased duration of action and enhanced bioavailability. Regioselective synthesis was used to obtain a water-soluble pillar[5]arene containing the fluorescent label FITC and nine sulfoethoxy fragments. The pillar[5]arene formed complexes with the therapeutic proteins binase, bleomycin, and lysozyme in a 1:2 ratio as demonstrated by UV-vis and fluorescence spectroscopy. The formation of stable spherical nanosized macrocycle/binase complexes with an average particle size of 200 nm was established by dynamic light scattering and transmission electron microscopy. Flow cytometry demonstrated the ability of macrocycle/binase complexes to penetrate into tumor cells where they exhibited significant cytotoxicity towards A549 cells at 10- 5-10-6 M while maintaining the enzymatic activity of binase.
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