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Abstract <p>The interaction of Dp44mT and DpC thiosemicarbazones with a model lipid membrane and the effect of cholesterol on their localization are studied by NMR spectroscopy and molecular dynamics. It is shown that Dp44mT is mainly localized at the membrane surface, while DpC can penetrate deeper into the hydrophobic region. Cholesterol pushes both compounds out to the bilayer surface. Interestingly, DpC and Dp44mT have similar antiproliferative activities, even though the former exhibits better penetration ability. This fact indicates the absence of any direct correlation between lipophilicity and activity in this case. Redox activity of iron-containing complexes in the reaction of linoleic acid peroxidation is studied: [Fe(Dp44mT)2]<sup>+</sup> is active only in the presence of ascorbic acid, [Fe(DpC)2]<sup>+</sup> is most active, and [Fe(AOBP)2]<sup>+</sup> is not active, apparently due to the steric factor. Weak redox activity of the [Fe(AOBP)2]<sup>+</sup> complex correlates with its low antiproliferative activity. The obtained results demonstrate an important role of cholesterol for the distribution of ligands in the membrane, a complex relation between lipophilicity and biological activity, and an essential role of redox properties of iron complexes in their anticancer activity.</p>

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Interaction of Thiosemicarbazones and Their Iron Containing Complexes with Model Lipid Membranes

  • 期刊论文

  • 发表日期：

    2025年11月1日

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  • V. E. Koshman,
  • O. Y. Selyutina,
  • A. A. Stepanov,
  • S. F. Vasilevsky,
  • N. E. Polyakov

摘要

Abstract

The interaction of Dp44mT and DpC thiosemicarbazones with a model lipid membrane and the effect of cholesterol on their localization are studied by NMR spectroscopy and molecular dynamics. It is shown that Dp44mT is mainly localized at the membrane surface, while DpC can penetrate deeper into the hydrophobic region. Cholesterol pushes both compounds out to the bilayer surface. Interestingly, DpC and Dp44mT have similar antiproliferative activities, even though the former exhibits better penetration ability. This fact indicates the absence of any direct correlation between lipophilicity and activity in this case. Redox activity of iron-containing complexes in the reaction of linoleic acid peroxidation is studied: [Fe(Dp44mT)2]+ is active only in the presence of ascorbic acid, [Fe(DpC)2]+ is most active, and [Fe(AOBP)2]+ is not active, apparently due to the steric factor. Weak redox activity of the [Fe(AOBP)2]+ complex correlates with its low antiproliferative activity. The obtained results demonstrate an important role of cholesterol for the distribution of ligands in the membrane, a complex relation between lipophilicity and biological activity, and an essential role of redox properties of iron complexes in their anticancer activity.