Uptake of Ga-curcumin Derivatives in Different Cancer Cell Lines: Toward the Development of New Potential 68 Ga-labelled Curcuminoids-Based Radiotracers for Tumour Imaging

J Inorg Biochem. 2017 Aug;173:113-119. doi: 10.1016/j.jinorgbio.2017.05.002. Epub 2017 May 10.

Abstract

Thanks to the ability to suppress the proliferation and to kill tumour cells, several studies have shown the anti-cancer effects of curcumin (CUR) and its derivatives, i.e. diacetylcurcumin (DAC) and bis-dehydroxycurcumin (bDHC). This study is focused onto the development of curcuminoid complexes with gallium-68 employed as potential new radio-labelled probes to detect neoplastic tissues through imaging techniques such as positron emission tomography. To this purpose, the uptake of three Ga-curcuminoid complexes, namely Ga(CUR)2+, Ga(DAC)2+, Ga(bDHC)2+, by various tumour cell lines was compared with the uptake of the same compounds by normal human lymphocytes by flow cytometry using the intrinsic fluorescence of the curcuminoids. Ga(CUR)2+, and particularly Ga(DAC)2+, showed a higher uptake by colorectal carcinoma (HT29) and lymphoma (K562) cell lines than lymphocytes, while the uptake of Ga(bDHC)2+ was higher in lymphocytes than in all the other cell lines. Based on the fluorescence data, Gallium-68 labelled complexes were then tested in HT29 cell line. 68Ga(DAC)2+ showed the highest uptake by HT29 cells (higher internalization with a lower externalization) and the highest affinity. The obtained results are promising and the findings foster further investigation on the development of curcumin-metal-based radiopharmaceuticals.

Keywords: Curcumin; Curcuminoid complexes; Gallium-68; PET radiotracers; Tumour cells.

MeSH terms

  • Cell Line, Tumor
  • Curcumin / analysis
  • Curcumin / chemistry*
  • Diagnostic Imaging / methods*
  • Gallium Radioisotopes / analysis
  • Gallium Radioisotopes / chemistry*
  • HT29 Cells
  • Humans
  • K562 Cells
  • Positron-Emission Tomography

Substances

  • Gallium Radioisotopes
  • Gallium-68
  • Curcumin