F. Zumrut Biber Muftuler

A perspective on plant origin radiolabeled compounds, their biological affinities and interaction between plant extracts with radiopharmaceuticals

Plant origin products having anticancer properties come into prominence due to widespread of cancer. There is significant increase on the usage of plant origin products and their purification to investigate the potential use at the treatment and diagnosis. Plant origin radiolabeled compounds have been attracting more scientific attention since the achievement of earlier researches. Furthermore, plant extracts are consumed quite a lot with unknown side effects of their contents. Researchers focus on investigation of their interactions with radiopharmaceuticals. Current review is carried out to evaluate the contribution of plant extracts for the development of new plant origin radiolabeled (125/131I, 99mTc) compounds for imaging and/or therapy and to investigate the interaction of plant extracts with radiopharmaceuticals.

Synthesis, radiolabeling and in vivo biodistribution of diethylstilbestrol phosphate derivative (DES-P)

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.

Radioiodinated Magnetic Nanoparticles Conjugated With Moxifloxacin: Synthesis and In Vitro Biological Affinities

Magnetic nanoparticles (MNPs) were synthesized and coated with tetraethyl orthosilicate and aminosilane to create functional amino groups. Moxifloxacin (MXF) was conjugated to the modified MNPs using glutaraldehyde as crosslinker. Finally, MXF conjugated magnetic nanoparticles were radiolabeled and their biological affinities such as cell incorporation ratio, cytotoxicity, and their potential as cell imaging probe were investigated using A-549 cells. GRAPHICAL ABSTRACT

Extraction, radiolabeling, and biodistribution of thebaine in rats

The goal of this study was to determine the radiopharmaceutical potential of radioiodinated thebaine. Thebaine was extracted from dry capsules of opium poppy (Papaver somniferum L.), purified using high-performance liquid chromatography, and characterized with nuclear magnetic resonance and infrared spectroscopy. The purified thebaine was labeled with 131I using the iodogen method. Normal and receptor-blockage biodistribution studies were performed in male Albino Wistar rats. The results of the tissue distribution studies showed that the uptake of 131I-thebaine in the stomach, large intestine, spinal cord, and prostate was higher than in the other tissues. A greater uptake of radiolabeled thebaine in the rat brain was observed in the midbrain and hypothalamus. We concluded that (1) the labeling yield of 131I-thebaine was high, (2) a large amount of 131I-thebaine remained in the midbrain and hypothalamus, and (3) 131I-thebaine had enough stability for diagnostic scanning.

Diethylenetriamine Pentaacetic Acid Derivative of Toremifene and In Vitro Evaluation in Human Breast Cancer Cell Line MCF-7

Cytotoxic and apoptotic effects of toremifene-diethylenetriamine pentaacetic acid (TOR-DTPA), formed by conjugation of TOR and DTPA, on the MCF-7 cell line were evaluated. TOR-DTPA was synthesized and qualified via gas chromatography-mass spectrometry system, thin layer chromatography, and high performance liquid chromatography methods. To screen the biological properties of TOR-DTPA at determined concentrations, our ongoing effort was to evaluate apoptotic and cytotoxic effects on the MCF-7 cell line. Trypan blue dye exclusion test, XTT, ELISA, and TUNEL assays were utilized to evaluate cytotoxicity and apoptosis. TOR-DTPA has no cytotoxic and limited apoptotic effect on the MCF-7 cell line according to the results of in vitro studies. It is concluded that the lack of obvious apoptotic and cytotoxic effects allows the already proposed ligand, TOR-DTPA, to be improved as a novel hydrophilic ligand for breast imaging.

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

A 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 99mTc and 125/131I 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.

PLGA encapsulation effect on Bioquin-HMPAO: radiolabeling and in vitro behaviour on brain and lung cancer cells

Bioquin-HMPAO (BH) was previously investigated as a novel brain imaging agent by in vivo biodistribution studies. Present studies are carried out to explore radiolabeling and in vitro behaviour evaluation of poly (lactic-co-glycolic acid) (PLGA) encapsulated BH nanocapsules (BH-PLGA NCs). BH-PLGA NCs were characterized utilizing dynamic light scattering and scanning electron microscope. Encapsulation effect on radiolabeling with 99mTc was examined by stability and lipophilicity studies and effect on in vitro behaviour of 99mTc-BH was evaluated by incorporation studies on DAOY, U87-MG and A549 cells. It is observed that PLGA encapsulation has a positive and reinforcement effect.

PLGA encapsulation and radioiodination of indole-3-carbinol: investigation of anticancerogenic effects against MCF7, Caco2 and PC3 cells by in vitro assays

Encapsulation with PLGA of I3C and radioiodination have been performed. Anticancerogenic effects of I3C and I3C-PLGA have been investigated utilizing in vitro methods on breast adenocarcinoma epithelial (MCF7), colon adenocarcinoma epithelial (Caco2), prostate carcinoma epithelial (PC3) cells. Characterization of I3C-PLGA have been performed with DLS method and SEM analysis. I3C and I3C-PLGA compounds have been radiolabeled in high yields with 131I which is widely used for diagnosis and treatment in Nuclear Medicine. All experimental results demonstrated that radioiodinated compounds are promising in order to be used in Nuclear Medicine as well as present study contributed previously reported studies.