1. Academic Validation
  2. The investigation of the interaction of warangalone with transferrin as a therapeutic biological macromolecule and the formation of a protein-ligand nanocomplex with superior anticancer activity against lung cancer cells

The investigation of the interaction of warangalone with transferrin as a therapeutic biological macromolecule and the formation of a protein-ligand nanocomplex with superior anticancer activity against lung cancer cells

  • Int J Biol Macromol. 2025 Apr:302:139951. doi: 10.1016/j.ijbiomac.2025.139951.
Jian-Qiao Cai 1 Si-Qiang Zheng 1 Bo Tao 1 Wen-Qiang Zhang 2 Chao Ma 3 Zi-Ming Wang 4
Affiliations

Affiliations

  • 1 Department of Thoracic Surgery, Shanghai Pulmonary Hospital, School of Medicine, Tongji University, Shanghai 200443, China.
  • 2 Department of Thoracic Surgery, Klinikum Ernst von Bergmann, Academic Hospital of the Charité-Universitätsmedizin Humboldt University Berlin, Potsdam, Germany.
  • 3 Department of Thoracic Surgery, The First Affiliated Hospital of Zhengzhou University, Zhengzhou University, Zhengzhou 450052, Henan, China.
  • 4 Department of Thoracic Surgery, Shanghai Pulmonary Hospital, School of Medicine, Tongji University, Shanghai 200443, China. Electronic address: wangzm0123@163.com.
Abstract

Though warangalone has shown Anticancer properties against breast Cancer cells, its colloidal stability and therapeutic index ought to be improved using a potential strategy, especially via protein-based (nano)carriers. In this research, transferrin was used as a plasma protein for the development of the warangalone-transferrin NPs. To investigate the mechanism underlying the formation of this complex, the interaction between warangalone and transferrin, as well as transferrin NPs, was analyzed using spectroscopic methods. The Anticancer properties of warangalone and warangalone-transferrin NPs in lung Cancer were subsequently evaluated. The findings showed that the hydrodynamic size, PDI, and zeta potential values of transferrin NPs were 122.4 ± 12.38 nm, 0.210, and -23.40 ± 3.28 mV, respectively. The association between warangalone and transferrin NP showed a strong binding strength (log Kb = 5.44 ± 0.07), while this affinity was reduced for the warangalone and the transferrin protein (log Kb = 4.88 ± 0.04). Theoretical research indicated that hydrophobic interactions serve as the main driving forces for the interaction of warangalone and transferrin. Cellular assays showed that the warangalone-transferrin NPs significantly affected cell death in lung Cancer cells. This research, by offering promising data, could be highly beneficial for advancing warangalone-transferrin NPs as a promising Anticancer platform.

Keywords

Interaction; Nanoformulation; Transferrin; Warangalone.

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