Näytä suppeat kuvailutiedot

dc.contributor.authorJurcek, Ondrej
dc.contributor.authorIkonen, Satu
dc.contributor.authorBuricova, Lucie
dc.contributor.authorWimmerova, Martina
dc.contributor.authorWimmer, Zdenek
dc.contributor.authorDrasar, Pavel
dc.contributor.authorHornicek, Jan
dc.contributor.authorGalandakova, Adela
dc.contributor.authorUlrichova, Jitka
dc.contributor.authorKolehmainen, Erkki
dc.date.accessioned2012-11-05T12:36:33Z
dc.date.available2012-11-05T12:36:33Z
dc.date.issued2011
dc.identifier.citationJurcek, O., Ikonen, S., Buricova, L., Wimmerova, M., Wimmer, Z., Drasar, P., Hornicek, J., Galandakova, A., Ulrichova, J. & Kolehmainen, E. (2011). Succinobucol's New Coat -Conjugation with Steroids to Alter Its Drug Effect and Bioavailability. Molecules, 16 (11), 9404-9420. doi:10.3390/molecules16119404 Retrieved from http://www.mdpi.com//1420-3049/16/11/9404/
dc.identifier.urihttps://jyx.jyu.fi/handle/123456789/40162
dc.description.abstractSynthesis, 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. Their low toxicity towards mice fibroblasts at maximal concentrations, their antioxidant activity, comparable or even higher than that of ascorbic acid as determined by direct quenching of the DPPH radical, and their potential for significantly altering total and LDL cholesterol levels, suggest that these conjugates merit further studies in the treatment of cardiovascular or other related diseases. A brief discussion of succinobucol’s ability to quench the radicals, supported with a computational model of the electrostatic potential mapped on the electron density surface of the drug, is also presented.fi
dc.language.isoeng
dc.publisherMDPI publishing
dc.relation.ispartofseriesMolecules
dc.relation.urihttp://www.mdpi.com/journal/molecules
dc.subject.othersuccinobucolen
dc.subject.otherprobucolen
dc.subject.otherkasvisterolifi
dc.subject.otherateroskleroosifi
dc.subject.otherkolesterolifi
dc.titleSuccinobucol's New Coat - Conjugation with Steroids to Alter Its Drug Effect and Bioavailability
dc.typeArticle
dc.identifier.urnURN:NBN:fi:jyu-201211052851
dc.contributor.laitosKemian laitosfi
dc.contributor.laitosDepartment of Chemistryen
dc.type.urihttp://purl.org/eprint/type/JournalArticle
dc.identifier.doi10.3390/molecules16119404
dc.type.coarjournal article
dc.description.reviewstatuspeerReviewed
dc.relation.issn1420-3049
dc.type.versionpublishedVersion
dc.rights.copyright© 2011 by the authors; licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution license.
dc.rights.accesslevelopenAccessfi
dc.rights.urlhttp://creativecommons.org/licenses/by/3.0/)


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Näytä suppeat kuvailutiedot

© 2011 by the authors; licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution license.
Ellei muuten mainita, aineiston lisenssi on © 2011 by the authors; licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution license.