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

5 years ago

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

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.

Publisher URL: www.sciencedirect.com/science

DOI: S0162013417300211