Metabolic Stability of New Mito-Protective Short-Chain Naphthoquinones.
HepG2 cell culture
idebenone
metabolic stability
mitochondrial dysfunction
reverse-phase liquid chromatography
short-chain quinone
Journal
Pharmaceuticals (Basel, Switzerland)
ISSN: 1424-8247
Titre abrégé: Pharmaceuticals (Basel)
Pays: Switzerland
ID NLM: 101238453
Informations de publication
Date de publication:
12 Feb 2020
12 Feb 2020
Historique:
received:
04
12
2019
revised:
30
12
2019
accepted:
08
02
2020
entrez:
16
2
2020
pubmed:
16
2
2020
medline:
16
2
2020
Statut:
epublish
Résumé
Short-chain quinones (SCQs) have been identified as potential drug candidates against mitochondrial dysfunction, which is largely dependent on their reversible redox characteristics of the active quinone core. We recently synthesized a SCQ library of > 148 naphthoquinone derivatives and identified 16 compounds with enhanced cytoprotection compared to the clinically used benzoquinone idebenone. One of the major drawbacks of idebenone is its high metabolic conversion in the liver, which significantly restricts is therapeutic activity. Therefore, this study assessed the metabolic stability of the 16 identified naphthoquinone derivatives
Identifiants
pubmed: 32059451
pii: ph13020029
doi: 10.3390/ph13020029
pmc: PMC7169385
pii:
doi:
Types de publication
Journal Article
Langues
eng
Déclaration de conflit d'intérêts
The authors declare no conflict of interest.
Références
Biol Pharm Bull. 2018 May 1;41(5):722-732
pubmed: 29445054
Medchemcomm. 2019 Jan 16;10(3):399-412
pubmed: 30996858
J Endocrinol. 2018 Mar;236(3):R145-R159
pubmed: 29431147
Cell Biol Toxicol. 2012 Apr;28(2):69-87
pubmed: 22258563
Brain. 2011 Sep;134(Pt 9):2677-86
pubmed: 21788663
Brain. 2013 Feb;136(Pt 2):e230
pubmed: 23388409
Expert Opin Drug Metab Toxicol. 2010 Nov;6(11):1437-44
pubmed: 20955109
Pharmacol Res. 2018 Nov;137:89-103
pubmed: 30290222
Curr Med Chem. 2019 Feb 12;:
pubmed: 30747057
Toxicol Appl Pharmacol. 2010 May 1;244(3):336-43
pubmed: 20132835
Redox Biol. 2015;4:289-95
pubmed: 25625583
Eur J Clin Pharmacol. 2009 May;65(5):493-501
pubmed: 19125241
PLoS One. 2011 Mar 31;6(3):e17963
pubmed: 21483849
J Neuroophthalmol. 2013 Mar;33(1):30-6
pubmed: 23263355
PLoS One. 2012;7(4):e36153
pubmed: 22558363
J Neurol. 2009 Mar;256 Suppl 1:31-5
pubmed: 19283348
Curr Drug Targets. 2016;17(12):1341-9
pubmed: 26212267
Arch Neurol. 2007 Jun;64(6):803-8
pubmed: 17562928