1. Αποθετήριο Παραδοτέων Υποτρόφων Δράσεων ΕΣΠΑ Τριτοβάθμιας Εκπαίδευσης 2017-2023
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3. Μεταδιδακτορικοί ερευνητές

Τύπος:	Άρθρο σε επιστημονικό περιοδικό
Τίτλος:	Organotin derivatives of cholic acid induce apoptosis into breast cancer cells and interfere with mitochondrion; synthesis, characterization and biological evaluation
Συγγραφέας:	[EL] Σταθοπούλου, Μαρία-Ελένη[EN] Stathopoulou, Maria-Eleni [EL] Ζουπάνου, Νικολέττα[EN] Zoupanou, Nikoletta [EL] Μπαντή, Χριστίνα[EN] Banti, Christina [EL] Δούβαλης, Αλέξιος[EN] Douvalis, Alexios [EL] Παπαχριστοδούλου, Χ.[EN] Papachristodoulou, Ch. [EL] Μαρούσης, Κωνσταντίνος[EN] Marousis, Konstantinos [EL] Σπυρούλιας, Γεώργιος[EN] Spyroulias, Georgios [EL] Μαυρομούστακος, Θωμάς[EN] Mavromoustakos, Thomas [EL] Χατζηκακού, Σωτήρης[EN] Hadjikakou, Sotirios
Ημερομηνία:	17/01/2021
Περίληψη:	Organotin(IV) derivatives of cholic acid (CAH) with the formulae R3Sn(CA) (R = Ph- (1), n-Bu- (2)) and R2Sn (CA)2 (R = Ph- (3), n-Bu- (4) and Me- (5)) were synthesized. The compounds were characterized in solid state by melting point, FT-IR, 119Sn M¨ossbauer, X-ray fluorescence (XRF) spectroscopy and in solution by 1H NMR, UV–Vis spectral data and by Electrospray Ionisation Mass spectrometry (ESI-MS), High Resolution Mass spectrometry (HRMS), and atomic absorption analysis. The in vitro bioactivity of 1–5 against human breast adenocarcinoma cancer cells MCF-7 (positive to hormone receptors) and MDA-MB-231 (negative to hormone receptors) reveal that triorganotin derivatives 1–2 exhibit significantly stronger activity than the corresponding diorganotin ones. Compound 5 is inactive against both cell lines at the concentrations tested. Triorganotins 1–2 inhibit selectively MCF-7 than MDA-MB-231 cells, suggesting hormone mimetic behavior of them. Organotins 1–4 inhibit both cancerous cell lines, stronger than cisplatin which rise up to 55-fold against MCF-7 and 170-fold against MDA-MB-231. The in vitro toxicity of 1–4 was evaluated on normal human fetal lung fibroblast cells (MRC-5), while their genotoxicity in vitro by micronucleus assay (MN). Moreover, the in vivo toxicity of 1–4 was tested by Artemia salina assay and their in vivo genotoxicity with Allium cepa test. The mechanism of action of 1–4 against MCF-7 was clarified in vitro by the means of cell morphology studies, cell cycle arrest, Acridine Orange/Ethidium Bromide (AO/EB) Staining, mitochondrial membrane permeabilization test and by their binding affinity toward the calf thymus (CT) DNA.
Γλώσσα:	Αγγλικά
Σελίδες:	16
DOI:	10.1016/j.steroids.2021.108798
EISSN:	1878-5867
Θεματική κατηγορία:	[EL] Ανόργανη και Πυρηνική χημεία[EN] Inorganic and Nuclear Chemistry [EL] Φαρμακευτική χημεία[EN] Medicinal chemistry
Λέξεις-κλειδιά:	βιοανόργανη χημεία; Bioinorganic chemistry; Organotins; Bile acids; Breast cancer; apoptosis; Mitochondrion
Κάτοχος πνευματικών δικαιωμάτων:	© 2021 Elsevier Inc. All rights reserved.
Ηλεκτρονική διεύθυνση του τεκμηρίου στον εκδότη:	https://www.sciencedirect.com/science/article/pii/S0039128X21000106
Ηλεκτρονική διεύθυνση περιοδικού:	https://www.sciencedirect.com/journal/steroids
Τίτλος πηγής δημοσίευσης:	Steroids
Τεύχος:	167
Σελίδες τεκμηρίου (στην πηγή):	Article no 108798
Σημειώσεις:	Acknowledgments (iii) C. N.B. has been financially supported by the State Scholarships Foundation (IKϒ) (Project No. 2019-050-0503-17816), through the Operational Programme “Human Resources Development, Education and Lifelong Learning” in the context of the project “Reinforcement of Postdoctoral Researchers - 2nd Cycle” (MIS-5033021), which is co financed by Greece and the European Union (European Social Fund- ESF).
Εμφανίζεται στις συλλογές:	Μεταδιδακτορικοί ερευνητές