TY - JOUR

T1 - In Vitro and in Silico Investigation of Water-Soluble Fullerenol C60(OH)24

T2 - Bioactivity and Biocompatibility

AU - Sharoyko, Vladimir V.

AU - Iamalova, Nailia R.

AU - Ageev, Sergei V.

AU - Meshcheriakov, Anatolii A.

AU - Iurev, Gleb O.

AU - Petrov, Andrey V.

AU - Nerukh, Dmitry A.

AU - Farafonov, Vladimir S.

AU - Vasina, Lubov V.

AU - Penkova, Anastasia V.

AU - Semenov, Konstantin N.

N1 - Publisher Copyright: © 2021 American Chemical Society. All rights reserved.

PY - 2021/8/10

Y1 - 2021/8/10

N2 - Light fullerenes, C60 and C70, have significant potential in biomedical applications due to their ability to absorb reactive oxygen species, inhibit the development of tumors, inactivate viruses and bacteria, and as the basis for developing systems for targeted drug delivery. However, the hydrophobicity of individual fullerenes complicates their practical use; therefore, creating water-soluble derivatives of fullerenes is increasingly important. Currently, the most studied soluble adducts of fullerenes are polyhydroxy fullerenes or fullerenols. Unfortunately, investigations of fullerenol biocompatibility are fragmental. They often lack reproducibility both in the synthesis of the compounds and their biological action. We here investigate the biocompatibility of a well-defined fullerenol C60(OH)24 obtained using methods that minimize the content of impurities and quantitatively characterize the product's composition. We carry out comprehensive biochemical and biophysical investigations of C60(OH)24 that include photodynamic properties, cyto- and genotoxicity, hemocompatibility (spontaneous and photo-induced hemolysis, platelet aggregation), and the thermodynamic characteristics of C60(OH)24 binding to human serum albumin and DNA. The performed studies show good biocompatibility of fullerenol C60(OH)24, which makes it a promising object for potential use in biomedicine.

AB - Light fullerenes, C60 and C70, have significant potential in biomedical applications due to their ability to absorb reactive oxygen species, inhibit the development of tumors, inactivate viruses and bacteria, and as the basis for developing systems for targeted drug delivery. However, the hydrophobicity of individual fullerenes complicates their practical use; therefore, creating water-soluble derivatives of fullerenes is increasingly important. Currently, the most studied soluble adducts of fullerenes are polyhydroxy fullerenes or fullerenols. Unfortunately, investigations of fullerenol biocompatibility are fragmental. They often lack reproducibility both in the synthesis of the compounds and their biological action. We here investigate the biocompatibility of a well-defined fullerenol C60(OH)24 obtained using methods that minimize the content of impurities and quantitatively characterize the product's composition. We carry out comprehensive biochemical and biophysical investigations of C60(OH)24 that include photodynamic properties, cyto- and genotoxicity, hemocompatibility (spontaneous and photo-induced hemolysis, platelet aggregation), and the thermodynamic characteristics of C60(OH)24 binding to human serum albumin and DNA. The performed studies show good biocompatibility of fullerenol C60(OH)24, which makes it a promising object for potential use in biomedicine.

KW - Computer Simulation

KW - Fullerenes/pharmacology

KW - Humans

KW - Reproducibility of Results

KW - Water

KW - MICRONUCLEI

KW - ANTIOXIDANT PROPERTIES

KW - OXYGEN

KW - PHYSICOCHEMICAL PROPERTIES

KW - NANOPARTICLES

KW - DNA

KW - SCAVENGING ACTIVITY

KW - C-60

KW - HEPATOTOXICITY

KW - ABERRATIONS

UR - http://www.scopus.com/inward/record.url?scp=85113970570&partnerID=8YFLogxK

UR - https://www.mendeley.com/catalogue/a7d73dc4-dcf3-32fd-80ee-6e2382ce8801/

U2 - 10.1021/acs.jpcb.1c03332

DO - 10.1021/acs.jpcb.1c03332

M3 - Article

C2 - 34375109

AN - SCOPUS:85113970570

VL - 125

SP - 9197

EP - 9212

JO - Journal of Physical Chemistry B

JF - Journal of Physical Chemistry B

SN - 1520-6106

IS - 32

ER -