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Zavisnost lipofilnosti i vezivanja za proteine plazme inhibitora angiotenzin konvertujućeg enzima

dc.creatorOdović, Jadranka
dc.creatorTrbojević-Stanković, Jasna
dc.date.accessioned2019-09-02T11:31:59Z
dc.date.available2019-09-02T11:31:59Z
dc.date.issued2012
dc.identifier.issn0365-4478
dc.identifier.urihttp://farfar.pharmacy.bg.ac.rs/handle/123456789/1826
dc.description.abstractAngiotensin-converting enzyme (ACE) inhibitors represent a significant group of drugs primarily used in the treatment of hypertension and congestive heart failure. In this research, seven ACE inhibitors (enalapril, quinapril, fosinopril, lisinopril, cilazapril, ramipril, benazepril) were studied to evaluate the relationship between their protein binding and calculated (logP values) or ultra-high performance liquid chromatography-tandem mass spectrometry (UHPLC-MS) and reversed-phase thin-layer chromatography (RP-TLC) lipophilicity data (φ0, CHI or C0 parameters, respectively). Their protein binding data varied from negligible (lisinopril) to 99% (fosinopril), while calculated logPKOWWIN values ranged from -0.94 (lisinopril) to 6.61 (fosinopril). The good correlations were established between protein binding values and logPKOWWIN data (R2=0.7520) as well as between protein binding and chromatographic hydrophobicity data, φ0, CHI or C0 parameters (R2 were 0.6160, 0.6242 and 0.6547, respectively). The possible application of hydrophobicity data in drugs protein binding evaluation can be of great importance in drug bioavailability.en
dc.description.abstractInhibitori angiotenzin konvertujućeg enzima (ACE inhibitori) predstavljaju veliku grupu lekova koji nalaze primenu u lečenju hipertenzije. U ovom radu analizirano je sedam ACE inhibitora (enalapril, kvinapril, fosinopril, lizinopril, cilazapril, ramipril i benazepril) kako bi se ispitala zavisnost između njihovog vezivanja za proteine plazme i lipofilnosti. Korelisane su vrednosti izračunatih (logPKOWWIN) ili hromatografski (UHPLC-MS i RP-TLC) dobijenih (φ0, CHI ili C0) hidrofobnih parametara. Procenat vezivanja za proteine plazme ispitivanih ACE inhibitora kretao se u opsegu od 0% do 99%, dok su vrednosti izračunatih logPKOWWIN vrednosti iznosile od -0.94 do 6.61. Dobijene su zadovoljavajuće korelacije između vrednosti vezivanja ACE inhibitora za proteine plazme i izračunatih logPKOWWIN vrednosti (R2=0,7520) kao i hromatografski dobijenih parametara hidrofobnosti, φ0, CHI, C0 (R2: 0,6160; 0,6242; 0,6547). PR Projekat Ministarstva nauke Republike Srbije, br. TR 34031.sr
dc.publisherUniverzitet u Nišu - Medicinski fakultet, Niš
dc.relationinfo:eu-repo/grantAgreement/MESTD/Technological Development (TD or TR)/34031/RS//
dc.rightsopenAccess
dc.sourceActa medica Medianae
dc.subjectangiotensin-converting enzyme inhibitors (ACE inhibitors)en
dc.subjectprotein bindingen
dc.subjectlipophilicityen
dc.subjectinhibitori angiotenzin-konvertujućeg enzima (ACE inhibitori)sr
dc.subjectvezivanje za proteine plazmesr
dc.subjectlipofilnostsr
dc.titleCorrelation between angiotensin-converting enzyme inhibitors lipophilicity and protein binding dataen
dc.titleZavisnost lipofilnosti i vezivanja za proteine plazme inhibitora angiotenzin konvertujućeg enzimasr
dc.typearticle
dc.rights.licenseBY
dcterms.abstractОдовић, Јадранка; Трбојевић-Станковић, Јасна; Зависност липофилности и везивања за протеине плазме инхибитора ангиотензин конвертујућег ензима; Зависност липофилности и везивања за протеине плазме инхибитора ангиотензин конвертујућег ензима;
dc.citation.volume51
dc.citation.issue4
dc.citation.spage13
dc.citation.epage18
dc.citation.other51(4): 13-18
dc.citation.rankM24
dc.identifier.fulltexthttp://farfar.pharmacy.bg.ac.rs//bitstream/id/626/1824.pdf
dc.identifier.rcubconv_902
dc.type.versionpublishedVersion


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