A perspective on Tc-99m and I-125/131 labeled receptor targeted compounds and their in vitro/in vivo affinities

WOS: 000412543600001A large number of radiolabeled compounds have been studied to identify their potential as diagnostic and therapeutic tools in different cancer types. We reviewed several of our studies to give a perspective on Tc-99m and I-125/131 labeled receptor targeted compounds which are estrogen receptor targeted, anti estrogen receptor targeted, opioid receptor targeted and receptor-binding peptide and their bioaffinities by using in vitro/in vivo methods

Radioiodination and biodistribution of isolated lawsone compound from Lawsonia inermis (henna) leaves extract

WOS: 000342134800027Lawsonia inermis (henna) is one of the most effective medicinal plants and it has been using for treatment of wounds and burns for centuries. The using of Henna leaves is very popular for cosmetic as well as medicine in many countries. Henna leaves contain lots of different compounds and lawsone (LW) is the main one. In current study, extraction with bidistillated water of henna leaves was performed and LW was isolated by using high performance liquid chromatography system. Chemical structure of LW was evaluated by nuclear magnetic resonance method. LW was radiolabeled with iodine-131 (I-131) radionuclide which is well known for nuclear imaging and therapy in nuclear medicine by utilizing iodogen method. The yield of radiolabeling of LW (I-131-LW) was calculated as 92.70 +/- A 4.312 % (n = 10) by thin layer radio chromatography. Its in vivo biological activity was investigated by biodistribution studies which were performed by using healthy female and male Balb/C mice. According to results of biodistribution, uptake of I-131 labeled LW compound in uterus, breast and ovary for female mice and prostate in male mice was higher than other organs in the body.Ege University Research FundEge University [2013 NBE 004]This study supported by Ege University Research Fund (contract no. 2013 NBE 004). The authors thank MSc student Emir Buyukok, MSc student Baris Yilmaz, PhD student Eser Ucar and MSc student Kadir Ari for the technical assistance during the animal experiments

Tc-99m labeled plumbagin: estrogen receptor dependent examination against breast cancer cells and comparison with PLGA encapsulated form

WOS: 000372268800003Plant origin products having anticancer properties come into prominence due to widespread of cancer. Plumbagin has various biological activities like anticancer activity. Estrogen receptor (ER) specificity of plumbagin (PL) and radiolabeled PL investigated by in vitro studies on ER+ and ER- adenocarcinoma cells. Additionally, PLGA encapsulation was carried out to reduce toxicity of plumbagin and encapsulation effect was investigated. Plumbagin radiolabeled with 100 % in yields and had ER specificity. Furthermore, PLGA encapsulation effected positively on properties of plumbagin; reduced toxicity, increased stability and ER specificity. A promising agent for the diagnosis of ER+ breast cancer is suggested.Ege UniversityEge University [2014 NBE 004]Current work is supported by Ege University Research Fund (contract no 2014 NBE 004). The authors thank to Busra Karatay and Gorkem Yildiz for the technical assistance during the assays

Somatostatin with Tc-99m and biodistribution studies in rats

WOS: 000252265700004PubMed ID: 18158765Somatostatin (SST) is a short-lived peptide hormone that regulates the endocrine system. The main use of the derivatives of SST is to diagnose diseases related to growth hormone and to use against some forms of cancer that involve growth hormone. Also, SST suppresses gastric acid secretion, gallbladder contractions, and pancreatic enzyme secretion. In this study, two different bifunctional chelating agents were used to examine the changes in the biologic half-life of SST. For this purpose, first D-penicillamine (DPA) and diethylene triaminepentaacetic acid (DTPA) were used to label SST with Tc-99m and then radiopharmaceutical potential of three Tc-99m-labeled complexes, Tc-99m-D-PA, (TC)-T-99m-D-PA-SST, and (99m)TcDTPA-SST, were compared with each other. Quality control for each labeled complex was established by using radiochromatographic methods. The radiolabeled complexes maintained their stabilities for 5 hours. Then, biodistribution studies were performed on Albino Wistar rats independently for three complexes. The results demonstrated that (TC)-T-99m-D-PA-SST exhibited long-term uptake in organs, and its clearance took longer than the Tc-99m-DTPA-SST complex

Synthesis and biodistribution studies of two novel radiolabeled estrone derivatives

WOS: 000253841300016PubMed ID: 18396789Background: Two Tc-99m-DTPA attached estrone derivatives were synthesized and their radiopharmaceutical potential was determined using female albino Wistar rats. Materials and Methods: Two novel radiolabeled estrone derivatives, Tc-99m-2,2',2 '',2'''-(2,2-(2-(3-methoxy-13-methyl-17-oxo- 7, 8, 9,11,12,13,14,15,16,17-decahydro-6H-cyclopenta[a]phenanthren-2-ylamino)-2-oxoethylazanediyl) bis(ethane-2,1-diyl))bis(azanettiyl) tetraacetic acid (Tc-99m-2-DTPA-3-methoxy estrone) and Tc-99m-2,2',2 '',2'''-(2,2'-(2-(3-methoxy-13-methyl-17-oxo-7,8,9,11,12,13,14,15,16,17-decahydro- 6H-cyclopenta[a]phenanthren-4-ylamino)-2-oxoethylazanediyl) bis(ethane-2,1-dlyl))bis(azanettiyl)tetraacetic acid (Tc-99m-4DTPA-3-methoxy estrone) were synthesized starting from estrone (3-hydroxy-13-methyl-7,8, 9,11,12,13,15,16-octahydro-6H-cyclopenta[a]phenanthren-17(14H)-one) and DTPA anhydride (2-(bis(2-(2,6-dioxomorpholino)ethyl)amino)acetic acid) as potential estrogen receptor imaging agents. The products were crystallized in ethyl alcohol (95%), purified by high performance liquid chromatography (HPLC) and characterized by nuclear magnetic resonance (NMR) and infrared spectroscopy (IR). The effect of the radiolabeled compounds on the biological behaviour of the molecules was evaluated through biodistribution studies in female albino Wistar rats. The rats were sacrificed at various time intervals, their organs were removed, and the activities of organs were counted using a gamma counter equipped with a Cd(Te) solid state detector. Results and Conclusion: Organ uptake was calculated as activity/gram tissue and time versus activity curves were generated. The tissue distribution studies exhibited a receptor-mediated uptake in the target organs of the rats for each compound. Both Tc-99m-2-DTPA-3-methoxy estrone and (99m)Tc4-DTPA-3-methoxy estrone were stable in vitro and were mainly excreted through the hepatobiliary pathway.. The biological data showed that the Tc-99m-2-DTPA-3-methoxy estrone had higher uptake in the target tissues than the Tc-99m-4-DTPA-3-methoxy estrone. The favourable in vitro/in vivo stability and biodistribution profiles suggest that these radioligands are good candidates for further exploration of their potential clinical applications