Počet záznamů: 1

Succinobucol’s New Coat - Conjugation with Steroids to Alter Its Drug Effect and Bioavailability

  1. 1.
    0368252 - UEB-Q 2012 RIV CH eng J - Článek v odborném periodiku
    Jurček, Ondřej - Ikonen, S. - Buřičová, Lucie - Wimmerová, Martina - Wimmer, Zdeněk - Drašar, P. - Horníček, Jan - Galandáková, A. - Ulrichová, J. - Kolehmainen, E. T.
    Succinobucol’s New Coat - Conjugation with Steroids to Alter Its Drug Effect and Bioavailability.
    Molecules. Roč. 16, č. 11 (2011), s. 9404-9420 ISSN 1420-3049
    Grant CEP: GA MŠk 2B06024; GA MŠk(CZ) OC10001; GA ČR GA203/09/2037
    Výzkumný záměr: CEZ:AV0Z50380511; CEZ:AV0Z40550506
    Klíčová slova: succinobucol * phytosterol * atherosclerosis
    Kód oboru RIV: CC - Organická chemie
    Impakt faktor: 2.386, rok: 2011

    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.
    Trvalý link: http://hdl.handle.net/11104/0202647