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Öğe Bioavailability of 99mTc-paclitaxel-glucuronide ( 99mTc-PAC-G)(2011) Muftuler F.Z.B.; Demir I.; Ünak P.; Içhedef Ç.; Kilçar A.Y.An 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 99mTc and the radiochemical yield of radiolabeled compound (99mTc-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 99mTc-PAC-G may potentially be used in breast tissue as an imaging agent. © by Oldenbourg Wissenschaftsverlag, München.Öğe Effect of rosemary (Rosmarinus officinalis) extract on the biodistribution of 99mTc sulphur colloid and on the radiolabeled blood constituents(Sociedade Brasileira de Farmacognosia, 2013) Uçar E.; Teksöz S.; Içhedef C.; Kilçar A.Y.; Ünak P.With this study we evaluated the effects of the herb rosemary (Rosmarinus officinalis L. Lamiaceae) extract on the labeling of blood constituents with technetium-99m (99mTc) labeled sulphur colloid and on the biodistribution of 99mTc-Sulphur Colloid in Wistar albino rats. For this purpose, two groups of animals (male wistar rats, 130-140 g) were treated (1 mL) with a rosemary extract (750 mg/kg body wt.,n=9) and water (control, n=9) separately by gavage for five days. 99mTc-Sulphur Colloid was administrated by intravenous injection; organs/tissues were withdrawn and weighted. Blood was centrifuged, plasma and blood cells were isolated. The radioactivity was counted to calculate the percentage of activity per gram for each organ/tissue and percentage of activity in blood cells and plasma. A signifi cant increase (p<0.05) in the uptake of 99mTc-Sulphur Colloid in the liver after the treatment with rosemary extract was observed. These results indicate that the substances or metabolites of the rosemary extract would change the biodistribution of 99mTc-Sulphur Colloid.Öğe Synthesis, radiolabeling and in vivo biodistribution of diethylstilbestrol phosphate derivative (DES-P)(2012) Ünak P.; Biber Müftüler F.Z.; Içhedef Ç.; Medine E.I.; Özmen K.; Ünak T.; Kilçar A.Y.; Gümüşer F.G.; Parlak Y.; Bilgin E.S.Diethylstilbestrol (DES) is a well known, nonsteroidal estrogen with high affinity for the estrogen receptor (ER). Today DES is used to treat breast and prostate cancers. A phosphate derivative of DES [Diethylstilbestrol diphosphate (DES-P)] which is specific to tumor cells consisting alkaline phosphatase enzyme was synthesized and labeled with 99mTc using tin chloride as reducing agent. In vivo biological activity of 99mTc labeled diethylstilbestrol phosphate compound ( 99mTc-DES-P) was examined by biodistribution studies on Wistar Albino rats. Statistical evaluation was performed using SPSS 13 program. The percentage (%) radiolabeling yield of 99mTc-DES-P and quality control studies were done by Thin Layer Radio Chromatography (TLRC). Results showed that, 99mTc-DES-P may be proposed as an imaging agent for ER enriched tumors such as uterus and prostate and their metastases in bones. © 2012 Akadémiai Kiadó.Öğe Thymidine kinase enzyme selective imaging radiopharmaceutical: 99mTc(CO)3-Ganciclovir(2013) Gedik B.; Teksöz S.; Içhedef Ç.; Kilçar A.Y.; Medine E.I.; Uçar E.The aim of this study is to radiolabel ganciclovir, known as having selective antiviral properties against thymidine kinase, with technetium tricarbonylcore (99mTc(CO)3 + and to investigate the biological behavior of this complex in vitro and in vivo. Commercially provided Ganciclovir (GCV) was radiolabeled with 99mTc(CO)3-. Initially, optimum radiolabeling conditions were determined by analyzing factors such as temperature, pH and time. Quality control of the radiolabeled compound was performed. The radiolabeling yield was found to be 97%. The 99mTc(CO)3 -GCV complex also displayed good in vitro stability during the 24 h period. In vitro cell uptake studies showed that the 99mTc(CO)3-GCV complex is highly uptaken in A-549, PC-3, HeLa cell lines according to the control group 99mTc(I)-tricarbonyl core. The knowledge gained from in vivo and in vitro studies of 99mTc(CO)3-GCV could contribute to the development of a new HSV1-tk gene imaging agent. © by Oldenbourg Wissenschaftsverlag, München.