In vivo biological evaluation of 131I radiolabeled-paclitaxel glucuronide ( 131I-PAC-G)

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dc.contributor.authorAslan O.
dc.contributor.authorBiber Muftuler F.Z.
dc.contributor.authorYurt Kilcar A.
dc.contributor.authorIchedef C.
dc.contributor.authorUnak P.
dc.date.accessioned2019-10-27T08:33:05Z
dc.date.available2019-10-27T08:33:05Z
dc.date.issued2012
dc.departmentEge Üniversitesien_US
dc.description.abstractPaclitaxel (PAC) is a natural occurring diterpene alkoloid originally isolated from the bark of Taxus Brevifolia. It is one of the most important antitumor agents for clinical treatment of ovarian, breast non-small cell lung and prostate cancers. It is known that these types of cancer cells have high ß-glucuronidase enzyme which can catalyze the hydrolysis of glucuronides. This is why the synthesis compounds which undergo glucuronidation come into question in the imaging and therapy of these cancer cells. The aim of current study is conjugation of glucuronic acid (G) to the starting substance PAC, labeling with 131I and to perform its in vivo biological evaluation. Glucuronic acid derived paclitaxel compound [paclitaxel-glucuronide (PAC-G)] was labeled with 131I using iodogen method. According to thin layer radio chromatography (TLRC) method, the radiochemical yield of 131I-PAC-G was 84.30 ±7.40% (n = 10). The biodistribution of 131I-PAC-G in healthy female and male Wistar Albino rats has been investigated. Imaging studies on male Balb-C mice were performed by using the Kodak FX PRO in vivo Imaging System. The range of the breast/blood, breast/muscle; ovary/blood, ovary/muscle ratios is approximately between 1.29 and 11.34 in 240 min, and between 0.71 and 8.24 in 240 min for female rats. The prostate/blood and prostate/muscle ratio is between 1.94 and 6.95 in 30 min for male rats. All these experimental studies indicate that 131I-PAC-G may potentially be used in breast, ovary and prostate tissues as an imaging agent. Also it is thought that 131I-PAC-G bears a theraphy potential because of the 131I radionuclide and can be improved with further investigations. © by Oldenbourg Wissenschaftsverlag, München.en_US
dc.identifier.doi10.1524/ract.2012.1922
dc.identifier.endpage345en_US
dc.identifier.issn0033-8230
dc.identifier.issn0033-8230en_US
dc.identifier.issue5en_US
dc.identifier.scopusqualityQ3en_US
dc.identifier.startpage339en_US
dc.identifier.urihttps://doi.org/10.1524/ract.2012.1922
dc.identifier.urihttps://hdl.handle.net/11454/26646
dc.identifier.volume100en_US
dc.indekslendigikaynakScopusen_US
dc.language.isoenen_US
dc.relation.ispartofRadiochimica Actaen_US
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanıen_US
dc.rightsinfo:eu-repo/semantics/closedAccessen_US
dc.subject131I-paclitaxel- glucuronide ( 131I-PAC-G)en_US
dc.subjectPaclitaxel (PAC)en_US
dc.subjectPaclitaxel-glucuronideen_US
dc.titleIn vivo biological evaluation of 131I radiolabeled-paclitaxel glucuronide ( 131I-PAC-G)en_US
dc.typeArticleen_US

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