Romanian Society of Pharmaceutical Sciences

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EVALUATION OF THE CYTOTOXIC EFFECTS INDUCED BY 68Ga-NODAGA-c(RGDfK) AND 68Ga-DOTA-c(RGDfK) IN MURINE MALIGNANT MELANOMA

MARIETA ELENA PANAIT 1#, MARIA IULIANA GRUIA 1, ANTONELA BUȘCĂ 1*, MARIAN AUGUSTIN MARINCAȘ 1,2#

1Institute of Oncology Prof. Dr. Al. Trestioreanu, 252 Fundeni Street, 022328, Bucharest, Romania
2“Carol Davila” University of Medicine and Pharmacy, 37 Dionisie Lupu Street, 020021, Bucharest, Romania

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Targeting alpha(v)beta(3) integrin receptors cells using 68Ga-labelled RGD peptides could be a promising approach for Positron Emission Tomography (PET). Data shows that this medical investigation causes minimal damage to adjacent tissues. However, little information is available concerning the effects that may occur in tumour tissue after 68Ga exposure. Therefore, in this paper we investigated some of the biological effects induced by 68Ga-NODAGA-c(RGDfK) and 68GaDOTA-c(RGDfK) in melanoma bearing mice, evaluating different parameters underlying melanoma progression such as: (1) apoptotic activity, (2) cell cycle phases and (3) oxidative stress levels evaluated by lipid peroxidation and total thiols concentrations in cell lysates. The two radiolabelled compounds induced increases of apoptotic events as well as G2/M cell cycle blockage, in tumour cells. Conversely, the two radiolabelled compounds induced no significant changes in the oxidative stress. The results demonstrated the ability of 68Ga-labelled compounds to exert inhibitory effects on tumour cells, manifested both by apoptosis induction and cell cycle blockage. We consider that the results will help to a better understanding of radiation biology revealing some of the cellular changes associated with medical imaging procedures. These results are also promising for further in vitro and in vivo evaluation of Peptide Receptor Radionuclide Therapy.