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.
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|Data di pubblicazione:||2017|
|Titolo:||Uptake of Ga-curcumin derivatives in different cancer cell lines: toward the development of new potential 68Ga-labelled curcuminoids-based radiotracers for tumour imaging.|
|Autori:||Rubagotti, Sara; Croci, Stefania; Ferrari, Erika; Orteca,Giulia; Iori, Michele; Capponi, Pier C.; Versari, Annibale; Asti, Mattia|
|Digital Object Identifier (DOI):||10.1016/j.jinorgbio.2017.05.002|
|Appare nelle tipologie:||Articolo su rivista|
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