Εξειδίκευση τύπου :	Άρθρο σε επιστημονικό περιοδικό
Τίτλος:	Oil-in-water microemulsions as hosts for benzothiophene-based cytotoxic compounds: An effective combination
Δημιουργός/Συγγραφέας:	Theochari I. [EL] Παπαδημητρίου, Βασιλική[EN] Papadimitriou, Vassiliki [EL] Παπαχατζής, Δημήτρης Π.[EN] Papahatjis, Demetris P. Assimomytis N. Pappou E. Pratsinis H. [EL] Ξενάκης, Αριστοτέλης[EN] Xenakis, Aristotelis [EL] Πλέτσα, Βασιλική[EN] Pletsa, Vassiliki
Εκδότης:	MDPI Multidisciplinary Digital Publishing Institute
Ημερομηνία:	2018
Γλώσσα:	Αγγλικά
ISSN:	2313-7673
DOI:	10.3390/biomimetics3020013
Περίληψη:	Targeted delivery of chemotherapeutics in order to overcome side effects and enhance chemosensitivity remains a major issue in cancer research. In this context, biocompatible oil-in-water (O/W) microemulsions were developed as matrices for the encapsulation of DPS-2 a benzothiophene analogue, exhibiting high cytotoxicity in various cancer cell lines, among them the MW 164 skin melanoma and Caco-2 human epithelial colorectal adenocarcinoma cell lines. The microemulsion delivery system was structurally characterized by dynamic light scattering (DLS) and electron paramagnetic resonance (EPR) spectroscopy. The effective release of a lipophilic encapsulated compound was evaluated via confocal microscopy. The cytotoxic effect, in the presence and absence of DPS-2, was examined through the thiazolyl blue tetrazolium bromide (MTT) cell proliferation assay. When encapsulated, DPS-2 was as cytotoxic as when dissolved in dimethyl sulfoxide (DMSO). Hence, the oil cores of O/W microemulsions were proven effective biocompatible carriers of lipophilic bioactive molecules in biological assessment experiments. Further investigation through fluorescence-activated cell sorting (FACS) analysis, comet assay, and Western blotting, revealed that DPS-2, although non-genotoxic, induced S phase delay accompanied by cdc25A degradation and a nonapoptotic cell death in both cell lines, which implies that this benzothiophene analogue is a deoxyribonucleic acid (DNA) replication inhibitor.
Τίτλος πηγής δημοσίευσης:	Biomimetics
Τόμος/Κεφάλαιο:	3
Τεύχος:	2
Θεματική Κατηγορία:	[EL] Βιολογία (Γενικά)[EN] Biology (General)
Λέξεις-Κλειδιά:	Chemotherapy DNA replication fork Drug delivery Electron paramagnetic resonance Mechanisms of cell death Microemulsions
Αξιολόγηση από ομότιμους (peer reviewed):	Ναι
Κάτοχος πνευματικών δικαιωμάτων:	© 2018 by the authors.
Όροι και προϋποθέσεις δικαιωμάτων:	All Open Access, Gold, Green
Σημειώσεις:	Εθνικό 'Ίδρυμα Ερευνών, EIE; European Commission, EC; European Regional Development Fund, FEDER. This work was supported by the Greece and the European Regional Development Fund of the European Union under the Operational Program "Competitiveness, Entrepreneurship and Innovation" (NSRF 2007-2013) and the Regional Operational Program of Attica (STHENOS project within GSRT'S KRIPIS). We also acknowledge support of this work by the project "STHENOS-b: Targeted therapeutic approaches against degenerative diseases with special focus on cancer and ageing-optimisation of the targeted bioactive molecules" (MIS 5002398) which is implemented under the Action "Action for the Strategic Development on the Research and Technological Sector", funded by the Operational Program "Competitiveness, Entrepreneurship and Innovation" (NSRF 2014-2020) and co-financed by the Greece and the European Regional Development Fund of the European Union.
Εμφανίζεται στις συλλογές:	Ινστιτούτο Χημικής Βιολογίας - Επιστημονικό έργο