Εξειδίκευση τύπου :	Άρθρο σε επιστημονικό περιοδικό
Τίτλος:	Design and Synthesis of Novel Antioxidant 2-Substituted-5,7,8-Trimethyl-1,4-Benzoxazine Hybrids: Effects on Young and Senescent Fibroblasts
Δημιουργός/Συγγραφέας:	Fotopoulou, Theano Papadopoulou, Adamantia Tzani, Andromachi Mamais, Michail Mavrogonatou, Eleni Pratsinis, Harris [EL] Κουφάκη, Μαρία[EN] Koufaki, Maria Kletsas, Dimitris [EL] Καλογεροπούλου, Θεοδώρα[EN] Calogeropoulou, Theodora
Ημερομηνία:	2024-06-29
Γλώσσα:	Αγγλικά
ISSN:	2076-3921
DOI:	10.3390/antiox13070798
Άλλο:	39061867
Περίληψη:	The exponential growth of the aged population worldwide is followed by an increase in the prevalence of age-related disorders. Oxidative stress plays central role in damage accumulation during ageing and cell senescence. Thus, a major target of today's anti-ageing research has been focused on antioxidants counteracting senescence. In the current work, six novel 5,7,8-trimethyl-1,4-benzoxazine/catechol or resorcinol hybrids were synthesized connected through a methoxymethyl-1,2,3-triazolyl or a 1,2,3-triazoly linker. The compounds were evaluated for their antioxidant capacity in a cell-free system and for their ability to reduce intracellular ROS levels in human skin fibroblasts, both young (early-passage) and senescent. The most efficient compounds were further tested in these cells for their ability to induce the expression of the gene heme oxygenase-1 (ho-1), known to regulate redox homeostasis, and cellular glutathione (GSH) levels. Overall, the two catechol derivatives were found to be more potent than the resorcinol analogues. Furthermore, these two derivatives were shown to act coordinately as radical scavengers, ROS inhibitors, ho-1 gene expression inducers, and GSH enhancers. Interestingly, one of the two catechol derivatives was also found to enhance human skin fibroblast viability. The properties of the synthesized compounds support their potential use in cosmetic applications, especially in products targeting skin ageing.
Τίτλος πηγής δημοσίευσης:	Antioxidants (Basel, Switzerland)
Τόμος/Κεφάλαιο:	13
Τεύχος:	7
Θεματική Κατηγορία:	[EL] Χημική Βιολογία[EN] Chemical Biology [EL] Οργανική χημεία[EN] Organic chemistry [EL] Βιοχημεία[EN] Biochemistry [EL] Θεραπευτική. Φαρμακολογία[EN] Therapeutics.Pharmacology
Λέξεις-Κλειδιά:	1,4-benzoxazines GSH enhancers anti-ageing antioxidant catechol heme oxygenase-1 gene hybrids resorcinol young and senescent skin fibroblasts
EU Grant:	OPENSCREEN-GR: An Open-Access Research Infrastructure of Chemical Biology and Target-Based Screening Technologies for Human and Animal Health Agriculture and the Environment” “(2018–2020)
EU Grant identifier:	(MIS) 5002691
Κάτοχος πνευματικών δικαιωμάτων:	© 2024 by the authors. Licensee MDPI, Basel, Switzerland.
Όροι και προϋποθέσεις δικαιωμάτων:	This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https:// creativecommons.org/licenses/by/ 4.0/).
Ηλεκτρονική διεύθυνση στον εκδότη (link):	https://doi.org/10.3390/antiox13070798
Εμφανίζεται στις συλλογές:	Ινστιτούτο Χημικής Βιολογίας - Επιστημονικό έργο