ACTA Pharmaceutica Sciencia 2018 , Vol 56 , Num 2
Synthesis of Radioiodinated Thymoquinone Glucuronide Conjugated Magnetic Nanoparticle (125I-TQG-Fe3O4) and its Cytotoxicity and In Vitro Affinity
İskender İnce 1-2 Zümrüt Biber Müftüler 2 E. İlker Medine 2 Özge Kozguş Güldü 2 Volkan Tekin 2 Selin Aktar 3 Erdem Göker 4 Perihan Ünak 2
1 Ege University, Center for Drug R&D and Pharmacokinetic Applications (ARGEFAR), 35100
2 Ege University, Department of Nuclear Application, Institute of Nuclear Sciences, 35100
3 Ege University Faculty of Pharmacy, Department of Pharmaceutical Botany, Izmir 35100
4 Ege University School of Medicine, Division of Medical Oncology, Tulay Aktas Oncology Hospital, 35100
DOI : 10.23893/1307-2080.APS.05608 The aim of the current study is to develop solid, semisolid or liquid form of radionuclide labeled thymoquinone glucuronide conjugated magnetite nanoparticles those targets to the tumor for diagnosis and therapy of cancer.

For this purpose, thymoquinone (TQ), a molecule present in the seeds of Nigella (Nigella sativa) used to enhance the affinity of the drug to the tumor cells. TQ was isolated from its microsomes and an enzymatic method applied to synthesize beta glucuronic acid derivatized thymoquinone glucuronide (TQG). TQG attached magnetic nanoparticles (TQG-Fe3O4). TQG- Fe3O4 were radiolabeled with 125I and (125I-TQG- Fe3O4) its cytotoxic effect and in vitro affinity was investigated.

The IC50 values of TQG- Fe3O4 were found 27.31, 18.68, 11.88 (µg/mL) respectively 24, 48 and 72 hours against A549 cell line by WST-8 test as a colorimetric way. Incorporation ratios of TQG- Fe3O4 with A549 cells is the highest levels. It is seen that TQG-Fe3O4 could inhibit the apoptosis on A549 cells but, there is no apoptotic effect of the samples on BEAS-2B cells. Size distribution, cellular uptake and toxicity characteristics of TQG- Fe3O4 in this study maintains a useful targeted delivery system in lung cancer diagnosis and therapy. Keywords : Nigella thymoquinone (TQ), glucuronide derivative, beta glucuronidase, radiolabeling with 125I, magnetic nanoparticles, Fe3O4

Istanbul Medipol University