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Succinobucol’s New Coat - Conjugation with Steroids to Alter Its Drug Effect and Bioavailability
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SYSNO ASEP 0368252 Document Type J - Journal Article R&D Document Type Journal Article Subsidiary J Článek ve WOS Title Succinobucol’s New Coat - Conjugation with Steroids to Alter Its Drug Effect and Bioavailability Author(s) Jurček, Ondřej (UEB-Q)
Ikonen, S. (FI)
Buřičová, Lucie (UEB-Q)
Wimmerová, Martina (UEB-Q)
Wimmer, Zdeněk (UEB-Q) RID, ORCID
Drašar, P. (CZ)
Horníček, Jan (UOCHB-X)
Galandáková, A. (CZ)
Ulrichová, J. (CZ)
Kolehmainen, E. T. (FI)Source Title Molecules. - : MDPI
Roč. 16, č. 11 (2011), s. 9404-9420Number of pages 17 s. Language eng - English Country CH - Switzerland Keywords succinobucol ; phytosterol ; atherosclerosis Subject RIV CC - Organic Chemistry R&D Projects 2B06024 GA MŠMT - Ministry of Education, Youth and Sports (MEYS) OC10001 GA MŠMT - Ministry of Education, Youth and Sports (MEYS) GA203/09/2037 GA ČR - Czech Science Foundation (CSF) CEZ AV0Z50380511 - UEB-Q (2005-2011) AV0Z40550506 - UOCHB-X (2005-2011) UT WOS 000297697200038 DOI 10.3390/molecules16119404 Annotation Synthesis, detailed structural characterization (X-ray, NMR, MS, IR, elemental analysis), and studies of toxicity, antioxidant activity and bioavailability of unique potent anti-atherosclerotic succinobucol-steroid conjugates are reported. The conjugates consist of, on one side, the therapeutically important drug succinobucol ([4-{2,6-di-tert-butyl-4-[(1-{[3-tert-butyl-4-hydroxy-5-(propan-2-yl)phenyl]sulfanyl}ethyl)sulfanyl]phenoxy}-4-oxo-butanoic acid]) possessing an antioxidant and anti-inflammatory activity, and on the other side, plant stanol/sterols (stigmastanol, β-sitosterol and stigmasterol) possessing an ability to lower the blood cholesterol level. A cholesterol-succinobucol prodrug was also prepared in order to enhance the absorption of succinobucol through the intestinal membrane into the organism and to target the drug into the place of lipid metabolism—The enterohepatic circulation system. Workplace Institute of Experimental Botany Contact David Klier, knihovna@ueb.cas.cz, Tel.: 220 390 469 Year of Publishing 2012
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