Uptake of Ga-curcumin derivatives in different cancer cell lines: Toward the development of new potential Ga-68-labelled curcuminoids-based radiotracers for tumour imaging

作者：Rubagotti Sara; Croci Stefania; Ferrari Erika^*; Orteca Giulia; Iori Michele; Capponi Pier C; Versari Annibale; Asti Mattia

来源：Journal of Inorganic Biochemistry, 2017, 173: 113-119.

DOI：10.1016/j.jinorgbio.2017.05.002

• Gallium-68
• Curcumin
• Curcuminoid complexes
• Tumour cells
• PET radiotracers

Thanks to the ability to suppress the proliferation and to kill tumour cells, several studies have shown the anticancer 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. Ga-68 (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.

• 出版日期2017-8