Conjugate of chlorin е6 with iron bis(dicarbollide) nanocluster: synthesis and biological properties

Future Med Chem. 2020 Jun;12(11):1015-1023. doi: 10.4155/fmc-2020-0029. Epub 2020 Apr 22.

Abstract

Background: Efficiency of both photodynamic and boron-neutron capture anticancer therapies (BNCT) depends on the properties of the used photo- and neutronsensitizer. We report on the synthesis and properties of the advanced photo- and neutronsensitizer designed as a conjugate of chlorin e6 with iron bis(dicarbollide) nanocluster. Results: The conjugate is shown to accumulate efficiently in rat glioblastoma C6 cells delivering >109 boron atoms per cell and thus meeting requirements for BNCT agents, to provide photoinduced 50% death of C6 cells at 35 ± 3 nM, to be not toxic for cells without activating stimulus. Conclusions: The conjugate is a prospective theranostic agent for photodynamic, BNCT and fluorescent diagnostics of tumors.

Keywords: anticancer; boron-neutron capture; nanoconjugate; neutronsensitizer; photodynamic; photosensitizer; theranostic.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents / chemical synthesis
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacology*
  • Cell Proliferation / drug effects
  • Chlorophyllides
  • Drug Screening Assays, Antitumor
  • Ferric Compounds / chemistry
  • Ferric Compounds / pharmacology*
  • Humans
  • Molecular Conformation
  • Nanostructures / chemistry*
  • Photosensitizing Agents / chemical synthesis
  • Photosensitizing Agents / chemistry
  • Photosensitizing Agents / pharmacology*
  • Porphyrins / chemistry
  • Porphyrins / pharmacology*
  • Tumor Cells, Cultured

Substances

  • Antineoplastic Agents
  • Chlorophyllides
  • Ferric Compounds
  • Photosensitizing Agents
  • Porphyrins
  • phytochlorin