Assessment of antioxidant activity, redox behavior, and human serum albumin binding of pyrogallol-coumarin hybrids

The antioxidant activity of the compounds, two pyrogallol-coumarin hybrids (PCH-1 and PCH-2), was evaluated using DPPH, ABTS, and FRAP assays. The obtained results indicate the excellent antioxidant potential of both compounds. Quantitative evaluation showed that PCH-2 exhibits antioxidant capacity comparable to or better than standard compounds (NDGA, gallic acid, and trolox). In addition, PCH-1 and PCH-2 showed significant cytotoxic activity against HCT-116 colon cancer cells, and the cytotoxicity was achieved by their pro-oxidant activity. UV–Vis and fluorescence spectroscopy show that strong and specific interactions between HSA and the synthesized compounds result in ground-state complex formation and temperature-dependent binding. Thermodynamic analysis showed that PCH-1 binding is primarily driven by hydrophobic interactions, while PCH-2 associates with HSA mainly through hydrogen bonding and van der Waals interactions. Molecular binding studies revealed a strong binding affinity of PCH for HSA, especially at site I. Rigid docking of PCHs gave negative binding free energies (ΔG ≈ −27.9 to −35.9 kJ/mol) and binding constants (Kb = 0.5–12.6 μmol/L), indicating enhanced ligand-protein interactions via hydrogen bonds and hydrophobic contacts. These results suggest stable HSA-ligand complexes and support the potential of HSA as a carrier for the compounds under study.

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Publication Details

Journal
Results in Chemistry
Published
2026-04-21
DOI
https://doi.org/10.1016/j.rechem.2026.103350
Primary Topic
Protein Interaction Studies and Fluorescence Analysis
Type
article
Field-Weighted Citation Impact
0.00

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article

Assessment of antioxidant activity, redox behavior, and human serum albumin binding of pyrogallol-coumarin hybrids

Dušica Simijonović, Danijela Nikodijević, Danijela Cvetković, Dejan Milenković et al.
Results in Chemistry
Protein Interaction Studies and Fluorescence Analysis
article

Assessment of antioxidant activity, redox behavior, and human serum albumin binding of pyrogallol-coumarin hybrids

Dušica Simijonović, Danijela Nikodijević, Danijela Cvetković, Dejan Milenković, Tamara Mladenović, Milena Milutinović, Zoran Marković, Edina Avdović
article en

Abstract

The antioxidant activity of the compounds, two pyrogallol-coumarin hybrids (PCH-1 and PCH-2), was evaluated using DPPH, ABTS, and FRAP assays. The obtained results indicate the excellent antioxidant potential of both compounds. Quantitative evaluation showed that PCH-2 exhibits antioxidant capacity comparable to or better than standard compounds (NDGA, gallic acid, and trolox). In addition, PCH-1 and PCH-2 showed significant cytotoxic activity against HCT-116 colon cancer cells, and the cytotoxicity was achieved by their pro-oxidant activity. UV–Vis and fluorescence spectroscopy show that strong and specific interactions between HSA and the synthesized compounds result in ground-state complex formation and temperature-dependent binding. Thermodynamic analysis showed that PCH-1 binding is primarily driven by hydrophobic interactions, while PCH-2 associates with HSA mainly through hydrogen bonding and van der Waals interactions. Molecular binding studies revealed a strong binding affinity of PCH for HSA, especially at site I. Rigid docking of PCHs gave negative binding free energies (ΔG ≈ −27.9 to −35.9 kJ/mol) and binding constants (Kb = 0.5–12.6 μmol/L), indicating enhanced ligand-protein interactions via hydrogen bonds and hydrophobic contacts. These results suggest stable HSA-ligand complexes and support the potential of HSA as a carrier for the compounds under study.

Results in ChemistryVol. 26
Science Fund of the Republic of Serbia
Zero hunger
Openalex Percentile: Top 17%
Protein Interaction Studies and Fluorescence Analysis
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