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Peer-reviewedCC BY 4.0Journal of Biochemical and Molecular Toxicology

PEGylated Chrysin: In Vitro Biological Activity and Mechanistic Insights in HepG2 Cells

  • Fátima Belén Gasser1
  • Julia Oggero2
  • María Sol Renna1
  • María Florencia Beltramino1
  • Candela Simonetto1
  • Lucía Dominguez3
  • Hugo Héctor Ortega1
  • Santiago Eduardo Vaillard2
  • Victoria Anahí Vaillard2
  • María Eugenia Baravalle1,4
4 affiliations
  1. 1Centro de Medicina Comparada, Instituto de Ciencias Veterinarias del Litoral (ICIVET) Universidad Nacional del Litoral and Consejo Nacional de Investigaciones Científicas y Técnicas (CONICET). Esperanza Santa Fe Argentina
  2. 2Instituto de Desarrollo Tecnológico para la Industria Química (INTEC) Universidad Nacional del Litoral and Consejo Nacional de Investigaciones Científicas y Técnicas (CONICET) Santa Fe Argentina
  3. 3Laboratorio de Microscopia Aplicada a Estudios Moleculares y Celulares (LAMAE) Instituto de Investigación y Desarrollo en Bioingeniería y Bioinformática (IBB), UNER. Oro Verde Entre Ríos Argentina
  4. 4Centro Universitario Gálvez Universidad Nacional del Litoral (UNL), Gálvez Santa Fe Argentina
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Abstract

PEGylated chrysin, a natural flavonoid conjugated with methoxypolyethylene glycol, exhibits in vitro cytotoxic properties, likely through apoptosis induction. In this study, we investigated its biological effects on HepG2 hepatocellular carcinoma cells, comparing its activity with the chemotherapeutic agent paclitaxel. We evaluated reactive oxygen species (ROS) production, membrane integrity, DNA damage, and wound closure using the scratch assay. At equivalent concentrations, PEGylated chrysin induced higher cell membrane damage but generated lower ROS levels compared to paclitaxel. Both compounds exhibited similar efficacy to reduce wound closure under the evaluated experimental conditions. Additionally, PEGylated chrysin significantly increased the frequency of micronuclei in binucleated cells, indicating genotoxic potential. To assess cellular uptake, a novel fluorescein−tagged conjugate (fluorescein−PEG−chrysin) was synthesized which demonstrated that the PEGylated drug is accumulated in the cytoplasm of HepG2 cells. These results highlight PEGylated chrysin as a promising candidate with antiproliferative potential, capable of inducing diverse cellular damage pathways in liver cancer cells while showing a distinct cytotoxic profile compared with Paclitaxel.

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Cite

BibTeXRIS
BibTeX
@article{gasser2026pegylated,
  title = {{PEGylated Chrysin: In Vitro Biological Activity and Mechanistic Insights in HepG2 Cells}},
  author = {Fátima Belén Gasser and Julia Oggero and María Sol Renna and María Florencia Beltramino and Candela Simonetto and Lucía Dominguez and Hugo Héctor Ortega and Santiago Eduardo Vaillard and Victoria Anahí Vaillard and María Eugenia Baravalle},
  journal = {Journal of Biochemical and Molecular Toxicology},
  year = {2026},
  month = nov,
  doi = {10.1002/jbt.71169},
  url = {https://doi.org/10.1002/jbt.71169},
  note = {CC BY 4.0},
}
RIS
TY  - JOUR
TI  - PEGylated Chrysin: In Vitro Biological Activity and Mechanistic Insights in HepG2 Cells
AU  - Fátima Belén Gasser
AU  - Julia Oggero
AU  - María Sol Renna
AU  - María Florencia Beltramino
AU  - Candela Simonetto
AU  - Lucía Dominguez
AU  - Hugo Héctor Ortega
AU  - Santiago Eduardo Vaillard
AU  - Victoria Anahí Vaillard
AU  - María Eugenia Baravalle
PY  - 2026
DA  - 2026/11/04
JO  - Journal of Biochemical and Molecular Toxicology
DO  - 10.1002/jbt.71169
UR  - https://doi.org/10.1002/jbt.71169
AB  - PEGylated chrysin, a natural flavonoid conjugated with methoxypolyethylene glycol, exhibits in vitro cytotoxic properties, likely through apoptosis induction. In this study, we investigated its biological effects on HepG2 hepatocellular carcinoma cells, comparing its activity with the chemotherapeutic agent paclitaxel. We evaluated reactive oxygen species (ROS) production, membrane integrity, DNA damage, and wound closure using the scratch assay. At equivalent concentrations, PEGylated chrysin induced higher cell membrane damage but generated lower ROS levels compared to paclitaxel. Both compounds exhibited similar efficacy to reduce wound closure under the evaluated experimental conditions. Additionally, PEGylated chrysin significantly increased the frequency of micronuclei in binucleated cells, indicating genotoxic potential. To assess cellular uptake, a novel fluorescein−tagged conjugate (fluorescein−PEG−chrysin) was synthesized which demonstrated that the PEGylated drug is accumulated in the cytoplasm of HepG2 cells. These results highlight PEGylated chrysin as a promising candidate with antiproliferative potential, capable of inducing diverse cellular damage pathways in liver cancer cells while showing a distinct cytotoxic profile compared with Paclitaxel.
SN  - 1095-6670
SN  - 1099-0461
ER  -