Design of Tc-99m-DTPA-CLP and Preliminary Evaluation in Rats

WOS: 000331795800013PubMed ID: 24148110Radiopharmaceuticals are localized in (malignant) tumor tissues by different mechanisms. One of these mechanisms, gelatinase enzyme activity, is associated with poor prognosis in cancer patients and potential targets for tumor imaging. There are some gelatinases to be associated with metastatic potential for tumor imaging to possibly predict metastases. In this study, a cyclic decapeptide conjugate, DTPA-CLP (DTPA-Cys-Leu-Pro-Gly-His-Trp-Gly-Phe-Pro-Ser-Cys), was selected as a peptide conjugate because of its selective inhibitory activity toward gelatinases. Peptide-conjugated DTPA-CLP was labeled with Tc-99m with a radiolabeling efficiency of 97.0 +/- 2.8%. After determining optimization conditions for radiolabeling, a biodistribution study of radiolabeled peptide in albino Wistar rats was performed. According to biodistribution data, Tc-99m-DTPA-CLP showed high uptake in the lung, liver, uterus, and spleen. These results show that Tc-99m-DTPA-CLP may be used for the imaging of gelatinase activity in metastatic tumors.Department of Scientific Projects at Ege University, Izmir, TurkeyEge University; Scientific and Technological Research Council of TurkeyTurkiye Bilimsel ve Teknolojik Arastirma Kurumu (TUBITAK) [111S253]The authors gratefully acknowledge the financial support received from the Department of Scientific Projects at Ege University, Izmir, Turkey, and the Scientific and Technological Research Council of Turkey, Scientific Project (111S253)

Intracellular uptake study of radiolabeled anticancer drug and impedimetric detection of its interaction with DNA

WOS: 000383524400021PubMed ID: 27591600Topoisomerase I inhibitor topotecan (TPT) is the only single-agent therapy certified for the remedy of repetitive small cell lung cancer (SCLC). In this study, TPT was labeled with I-131 via iodogen method and its quality control was determined using thin layer radiochromatography and paper electrophoresis methods. Intracellular uptake study was carried out with human lung adenocarcinoma cell line (A-549) and human lung fibroblast cell line (WI-38). The interaction of I-131-TPT with healthy DNA and cancer DNA was also investigated using single-use sensor technology combined with electrochemical impedance spectroscopy (EIS). The change at the charge transfer resistance (R-ct) obtained before/after interaction was evaluated. Similar to the results of intracellular uptake study, it was found that I-131-TPT could more interact with the cancer DNA than healthy DNA according to the impedimetric results. I-131-TPT is promising in terms of a new nuclear imaging agent for lung cancer. (C) 2016 Elsevier B.V. All rights reserved.Ege University, Scientific Research Project (BAP Project) [14FBE009]; TUBITAKTurkiye Bilimsel ve Teknolojik Arastirma Kurumu (TUBITAK) [2210-C]This research was supported by the Ege University, Scientific Research Project (BAP Project No. 14FBE009). M.T. also acknowledges the master scholarship Granted by TUBITAK (2210-C National Scholarship Programme for MSc Students)

A Solid Phase Extraction Application of Hybrid Nano B2O3/ZrO2 for Separation and Determination of Trace Indium in Environmental Samples

WOS: 000430996100049Hybrid nanomaterials have attracted considerable interest in environmental science, analytical chemistry and atomic spectroscopy. In the present study, a column solid phase extractioo procedure was developed for the separation and preconcentration of indium in various matrixes by using hybrid nanomaterial B2O3/ZrO2 (HNMBZ). Various experimental and analytical parameters such as sample solution pH, sample solution volume, flow rate of sample solution and eluent, volume and concentration of eluent and amount of HNMBZ, effect of common matrix ions and capacity of sorbent were investigated. The adsorbed metal ions on HNMBZ were eluted with 6 mL of 1 mol . L-1 HNO3 solutions and their concentrations were determined by high-resolution continuum source flame atomic absorption spectrometry (HR-CS FAAS). Under the optimized conditions, detection limits for indium for 3 pixels and 5 pixels were found as 0. 20 and 0. 16 mu g . L-1, respectively. The accuracy of the procedure was checked by spiked water samples. The developed procedure was successfully applied to real samples for the separation and determination of indium.Scientific and Technological Research Council of Turkey (TUBITAK)Turkiye Bilimsel ve Teknolojik Arastirma Kurumu (TUBITAK) [110T111, 214Z221]the Scientific and Technological Research Council of Turkey (TUBITAK Grants no. 110T111, 214Z221

Subphthalocyanine as a fluorescence imaging agent for breast tumor

WOS: 000474330400061PubMed ID: 31026614Tri-tert-butyl-carboxyl subphthalocyanine (SubPc) was synthesized and evaluated as a fluorescence agent. Fluorescence imaging for breast tumor in vivo was performed using nude mice as models. Results indicate high uptake in tumor at 20 h. Tumor-non tumor ratio was determined as 2.25. The imaging results demonstrate the potential of this fluorescence-imaging agent in the diagnosis of breast tumor. In the future, subphthalocyanine is also developing as a dual functional, which is fluorescence imaging and as a photodynamic therapeutic agent for the treatment and diagnosis of cancer

Nuclear imaging potential and in vitro photodynamic activity of symmetrical and asymmetrical zinc phthalocyanines

WOS: 000374698900005PubMed ID: 27059543Photodynamic therapy (PDT) is based on exposing a light-sensitive material that has been localized in target tissues with visible light. In the current study, symmetric Zn(II) octaoctadodecylphthalocyanine (1) and the asymmetrically substituted hydroxyhexyloxy derivative (2) were examined as a multifunctional agent for tumour nuclear imaging and for PDT potential. Zn(II)Pc 1 and Zn(II)Pc 2 were radiolabelled with I-131 using an iodogen method with high efficiency (93.5 +/- 3.5% and 93.0 +/- 2.8%, respectively) under the optimum conditions. Biodistribution study results showed that radiolabelled Zn(II)Pc 1 had a high uptake in the large intestine and unchanging uptake in the ovary. However, radiolabelled Zn(II)Pc 2 uptake was statically significant in the large intestine, pancreas, ovary and lung. For the PDT studies, EMT6/P (mouse mammary cell line) and HeLa (cervical adenocarcinoma cell line) with Zn(II)Pc 1 and Zn(II)Pc 2 were exposed to red light (650nm) at 10-30J/cm(2). Zn(II)Pc 1 and Zn(II)Pc 2 had a good PDT efficacy in the EMT6/P cell line. In conclusion, radiolabelled Zn(II)Pc 1 might be a promising imaging agent for pancreas, ovary and colon tumours. However, the radiolabelled Zn(II)Pc 2 might be a promising nuclear imaging and PDT agent for colon, lung, pancreas and ovary tumours

Investigation of Vipera Anatolica Venom Disintegrin via Intracellular Uptake with Radiolabeling Study and Cell-Based Electrochemical Biosensing Assay

WOS: 000464733200028PubMed ID: 30276529Snake venoms are a natural biological source that has potential therapeutic value with various protein compounds. Disintegrins originally were discovered as a family of proteins from snake venoms composed of cysteine rich low molecular weight polypeptides. Disintegrins exhibit specific binding and higher affinity toward integrin with potential inhibition of function. Trans-membrane receptors of the integrin family may involve in many pathological conditions such as inflammation and tumor progression with important processes related to invasion and migration. Since disintegrins have the ability to bind to integrins, they could be used for cancer detection and treatment, and in monitoring of therapy in select cancer types. The main purpose of the study is to investigate disintegrin containing Vipera anatolica (VAT) crude venom potential for radiolabeling and intracellular uptake as well as electrochemical biosensing assay against U87MG human brain glioblastoma cells. For this purpose, VAT crude venom containing U87MG cell-specific disintegrin was investigated in terms of radiolabeling and intracellular uptake as well as electrochemical biosensing assay in comparison with echistatin (ECT) disintegrin in cells. The interaction between VAT crude venom and ECT with HEK293 human non-tumorigenic embryonic kidney cells and glioblastoma U87MG cells was electrochemically investigated using pencil graphite electrodes (PGEs). The interaction of the VAT crude venom and ECT with HEK293 and U87MG cells was detected according to the changes in oxidation signals. Then, VAT crude venom and echistatin were labeled with I-131 via iodogen method. Intracellular uptakes of radiolabeled molecules were investigated in U87MG cell line. I-131-VAT can be an agent for imaging of glioblastoma cancer. Further work will focus on the production of large quantities of pure VAT disintegrin with a biotechnological approach to improving imaging agent

Radiolabeling, in Vitro Cell Uptake, and in Vivo Photodynamic Therapy Potential of Targeted Mesoporous Silica Nanoparticles Containing Zinc Phthalocyanine

Kolatan, H Efsun/0000-0003-4761-2779; Tuncel, Ayca/0000-0003-0699-3309; , Fatma/0000-0002-9394-6908WOS: 000548455300035PubMed: 32412765Photodynamic therapy (PDT) is a noninvasive therapy based on the photodynamic effect. in this study, we sought to determine intracellular uptake and in vivo photodynamic therapy potential of Zn phthalocyanine-loaded mesoporous silica nanoparticles (MSNPS) against pancreatic cancer cells. MSNPS were labeled with I-131; the radiolabeling efficiency was found to 95.5 +/- 1.2% in pH 9 and 60 min reaction time. Besides, the highest intracellular uptake yields of I-131-MSNPS nanoparticles in MIA PaCa-2, AsPC-1, and PANC-1 cells were determined as 43.9 +/- 3.8%, 41.8 +/- 0.2%, and 37.9 +/- 1.3%, respectively, at 24 h incubation time. in vivo PDT studies were performed with subcutaneous xenograft cancer model nude mice with AsPC-1 pancreatic cancer cells. For photodynamic therapy, 685 nm red laser light 100 J/cm(2) light dose using and 5-20 mu M ZnPc containing MSNPS concentrations were applied. Histopathological studies revealed that the ratio of necrosis in tumor tissue was higher in the treatment group than the control groups.Scientific and Technological Research Council of Turkey (TUBITAK)Turkiye Bilimsel ve Teknolojik Arastirma Kurumu (TUBITAK) [2214/A]; Ege University, Scientific Research Project (BAP)Ege University [16 NBE 001]This research was funded by the Scientific and Technological Research Council of Turkey (TUBITAK; grant number2214/A), Ege University, Scientific Research Project (BAP; grant Number: 16 NBE 001)

Evaluation of cancer imaging potential and photodynamic therapy efficacy of copper (II) benzyloxypheophorbide-a

WOS: 000346915600008PubMed ID: 25230852The biological potential of a synthetic copper chlorophyll derivative was investigated via in vivo and in vitro experiments. The Cu-chlorophyll derivative photosensitizer (Cu-PH-A) was labeled with I-131 with high efficiency (92.9 +/- 4.2%) using the iodogen method. Cell culture studies were performed with the MCF-7 and MDAH-2774 cell lines after radiolabeling. The photosensitizing activity of Cu-PH-A was more effective in MDAH-2774 cells than in MCF-7 cells at a concentration of 50 mu M. When the biodistribution in female Albino Wistar rats was examined, uptake of the radiolabeled photosensitizer was maximal in the liver and ovaries after 60 min. It is concluded that radiolabeled Cu-chlorophyll derivative photosensitizer has high uptake in ovaries in normal rats. In addition, the intercellular uptake and PDT efficacy of the Cu-PH-A in MDAH-2774 were good compared with MCF-7 cells. This photosensitizer could be useful for both ovary tumour imaging and PDT.Scientific and Technological Research Council of Turkey, TUBITAKTurkiye Bilimsel ve Teknolojik Arastirma Kurumu (TUBITAK) [112T565]The authors declared no declaration of interest. The authors gratefully acknowledge financial support by The Scientific and Technological Research Council of Turkey, TUBITAK (Grant no: 112T565)