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Öğe Bioavailability of Tc-99m-paclitaxel-glucuronide (Tc-99m-PAC-G)(Walter De Gruyter Gmbh, 2011) Muftuler, F. Z. Biber; Demir, I.; Unak, P.; Ichedef, C.; Kilcar, A. YurtAn antitumor agent paclitaxel (PAC) has been proved to be efficient in the treatment of breast and ovarian cancer. Glucuronic acid-derived paclitaxel compound (paclitaxel-glucuronide (PAC-G)) was enzymatically synthesized using microsome preparate separated from rat livers. The biodistribution mechanism of PAC-G in healthy female Albino Wistar rats has been investigated. The expected structure is confirmed according to LC/MS results, and the possible attachment is to C2-hydroxyl group. PAC-G was labeled with Tc-99m and the radiochemical yield of radiolabeled compound (Tc-99m-PAC-G) was 98.00 +/- 2.74% (n = 9). The range of the breast/blood and breast/muscle ratios is approximately between 3 and 35 in 240 min. All these experimental studies indicate that Tc-99m-PAC-G may potentially be used in breast tissue as an imaging agent.Öğe Design Of A Radiolabeled Polymeric Drug Carrier System (99)mTc(CO)(3)-Oxaliplatin-PEG-PLA(Springer, 2017) Senocak, K.; Teksoz, S.; Kilcar, A. Yurt; Ucar, E.; Aydin, B.Öğe In vivo biological evaluation of I-131 radiolabeled-paclitaxel glucuronide (I-131-PAC-G)(Walter De Gruyter Gmbh, 2012) Aslan, O.; Muftuler, F. Z. Biber; Kilcar, A. Yurt; Ichedef, C.; Unak, P.Paclitaxel (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 beta-glucuronides 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 I-131 and to perform its in vivo biological evaluation. Glucuronic acid derived paclitaxel compound [paclitaxel-glucuronide (PAC-G)] was labeled with I-131 using iodogen method. According to thin layer radio chromatography (TLRC) method, the radio-chemical yield of I-131-PAC-G was 84.30 +/- 7.40% (n = 10). The biodistribution of I-131-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 I-131-PAC-G may potentially be used in breast, ovary and prostate tissues as an imaging agent. Also it is thought that (131)-PAC-G bears a theraphy potential because of the I-131 radionuclide and can be improved with further investigations.Öğe Isolation of hydroxytyrosol from olive leaves extract, radioiodination and investigation of bioaffinity using in vivo/in vitro methods(Walter De Gruyter Gmbh, 2013) Ozkan, M.; Muftuler, F. Z. Biber; Kilcar, A. Yurt; Medine, E. I.; Unak, P.It is known that medicinal plants like olive have biological activities due to their flavonoid content such as olueropein, tyrosol, hydroxytyrosol etc. In current study, hydroxytrosol (HT) which is one of the major phenolic compounds in olive, olive leaves and olive oil, was isolated after methanol extraction and purification of olive leaves which are grown in the northern Anatolia region of Turkey. The isolated HT was radiolabeled with I-131 (I-131-HT) and the bioaffinity of this radiolabeled component of olive leaves extract was investigated by using in vivo/in vitro methods. It was found that HT could be radiolabeled with I-131 in yields of 95.6 +/- 4.4% (n = 8), and in vivo studies showed that I-131-HT is taken up by urinary bladder, stomach, small intestine, large intestine, breast and prostate. Significant incorporation of activity was observed in cell lines via in vitro studies.Öğe Superparamagnetic Iron Oxide Nanoparticle Mediated Radiosensitization at Megavoltage Radiation(Elsevier Ireland Ltd, 2019) Kirakli, E. Korkmaz; Takan, G.; Hoca, S.; Muftuler, F. Z. Biber; Kilcar, A. Yurt; Kamer, S. Arun; Anacak, Y.Öğe Synthesis and radiolabeling of PLGA encapsulated everolimus nanoparticles(Wiley, 2019) Bilgi, A.; Gedik, F.; Gokulu, S. G.; Kilcar, A. Yurt; Yildirim, N.; Akman, L.; Ozsaran, A. A.[No abstract available]Öğe Synthesis And Radiolabeling Of Temozolomide Loaded Solid Lipid Nanoparticles(Springer, 2017) An, K.; Teksoz, S.; Ichedef, C.; Ucar, E.; Kilcar, A. YurtÖğe SYNTHESIS OF A THERANOSTIC AGENT: RADIOIODINATED PEGYLATED PLGA-INDOCYANINE CAPSULES AND IN VITRO DETERMINATION OF THEIR BIOAFFINITY ON OVARIAN, CERVICAL AND BREAST CANCER CELLS(Lippincott Williams & Wilkins, 2017) Akman, L.; Muftuler, F. Z. Biber; Bilgi, A.; Kilcar, A. Yurt; Gokulu, S. G.; Medine, E. I.; Terek, M. C.Öğe SYNTHESIS OF A THERANOSTIC AGENT: RADIOIODINATED PEGYLATED PLGA-INDOCYANINE CAPSULES AND IN VITRO DETERMINATION OF THEIR BIOAFFINITY ON OVARIAN, CERVICAL AND BREAST CANCER CELLS(Lippincott Williams & Wilkins, 2017) Akman, L.; Muftuler, F. Z. Biber; Bilgi, A.; Kilcar, A. Yurt; Gokulu, S. G.; Medine, E. I.; Terek, M. C.Öğe Synthesis of I-131/125 Labelled Diethylstilbestrol (DES) Glucuronide Conjugated Magnetic Nanoparticles and Investigation of Biological Affinities(Springer, 2011) Unak, P.; Yilmaz, T.; Muftuler, F. Z. Biber; Medine, E.; Ichedef, C.; Kilcar, A. Yurt; Unak, T.Öğe Synthesis, radiolabeling and biodistribution of morphine glucuronide (mor-glu)(Springer, 2012) Enginar, H.; Unak, P.; Muftuler, F. Z. Biber; Lambrecht, F. Y.; Medine, E. I.; Yolcular, S.; Kilcar, A. Yurt; Seyitoglu, B.; Bulduk, I.The aim of this study was to synthesize a glucuronide conjugated morphine derivative which could be labeled with I-131, as a radiopharmaceutical, and to investigate its radiopharmaceutical potential using biodistribution studies in male Albino Wistar rats. Morphine was extracted from dry capsules of the opium poppy (Papaver somniferum L.). It was conjugated with UDP-glucuronic acid by using UDP-glucuronyl transferase (UDPGT) enzyme rich microsomes, purified by high performance liquid chromatography (HPLC) and characterized by nuclear magnetic resonance (NMR), infrared (IR) spectroscopy and liquid chromatography mass spectroscopy (LC-MS/MS). Normal and receptor blockage biodistribution studies were performed in male Albino Wistar rats. The results of the tissue distribution studies showed that I-131 labeled morphine glucuronide (I-131-mor-glu) uptake in the small intestine, large intestine and urinary bladder was higher than in the other tissues of the rats in the blocked receptor and unblocked receptor. A greater uptake of the radio labeled substance was observed in the hypothalamus and mid brain than in the other branches of the rats' brains.Öğe Synthesis, Radiolabeling and In Vivo Tissue Distribution of an Anti-Oestrogen Glucuronide Compound, Tc-99m-TOR-G(Int Inst Anticancer Research, 2010) Muftuler, F. Z. Biber; Unak, P.; Yolcular, S.; Kilcar, A. Yurt; Ichedef, C.; Enginar, H.; Sakarya, S.Toremifene (TOR) has been used as an anti-oestrogen drug for the treatment and prevention of human breast cancer. The aim of this study was the addition of the hydrophilic groups diethylenetriamine pentaacetic acid (DTPA) and glucuronic acid to the starting substance TOR and to label it with technetium-99m (Tc-99m) radionuclide and to investigate radiopharmaceutical potential of the new compound. The synthesis reactions are completed in four steps, including enzymatic reaction, with the following sub-steps; preparation of microsomal fraction from Hutu 80 cell line and subsequent purification of UDP-glucuronyl transferase (UDPGT), estimation of protein quantity in microsomal samples and glucuronidation reaction. The results indicate that Tc-99m-TOR-G may be proposed as a new anti-oestrogen glucuronide imaging agent for ovarian tumours.