Synthesis and investigation of anticancer potential of radiolabeled naphthalene monoimide bearing imidazolium salt.

Imidazolium salts and derivatives have antitumor efficacy and toxic effects in different micro-organisms. In this study, an imidazolium bromide salt (NMI) was synthesized, and its antitumor potential was investigated by in vitro studies. Radiolabeling of synthesized NMI was carried out by iodogen method using I radionuclide.

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

Topoisomerase 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 (131)I 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).

Dual Nuclear/Fluorescence Imaging Potantial of Zinc(II) Phthalocyanine in MIA PaCa-2 Cell Line.

Background And Objective: Pancreatic cancer is very common and difficult to diagnose in early stage. Imaging systems for diagnosing cancer have many disadvantages. However, combining different imaging modalities offers synergistic advantages.

Intracellular uptake and fluorescence imaging potential in tumor cell of zinc phthalocyanine.

A near IR absorbing phthalocyanine bearing four binaphtyl group has been synthesized in order to investigate its cytotoxicity and intracellular uptake of sensitizer on MCF-7 (human breast cancer), MDAH (ovarian cancer), HeLa (human epitheloid cervix carcinoma), EMT-6 (mouse breast cancer) and WI-38 (human fibroblast lung) cell lines. ZnPc showed four time higher intracellular uptake in carcinoma cells (MCF-7) than normal (WI-38) cell lines. With the aim of studying in detail the biodistribution feature and tumor nuclear imaging capacity, ZnPc was also labeled with I-131.

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

Photodynamic 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 (131) I using an iodogen method with high efficiency (93.

Synthesis, Radiolabeling, and Bioevaluation of Bis(Trifluoromethanesulfonyl) Imide.

Imidazolium salts have antitumor potential and toxicological effects on various microorganisms. The authors' aim is to synthesize a new imidazolium salt and to assess its pharmacokinetic and antitumor potentials by in vitro and in vivo studies. In this study, bis(trifluoromethanesulfonyl) imide (ITFSI) was synthesized and labeled with (131)I using the iodogen method.

Investigation of In vitro PDT Activities and In vivo Biopotential of Zinc Phthalocyanines Using (131)I Radioisotope.

Novel octylthio-containing asymmetrically substituted Zn(II) phthalocyanine (Zn(II)Pc1) and a symmetric derivative (Zn(II)Pc2) have been prepared to investigate the biological potential and ability to photosensitize singlet oxygen for photodynamic therapy applications. In this study, the singlet oxygen generation potential and in vitro photodynamic activities of these compounds have been tested. Both ZnPcs reveal to be very efficient singlet oxygen generators and promising PSs for PDT applications.

131I-Zn-Chlorophyll derivative photosensitizer for tumor imaging and photodynamic therapy.

In recent years, the photodynamic therapy studies have gained considerable attention as an alternative method to surgery, chemotherapy and radiotherapy which is commonly used to fight cancer. In this study, biological potentials of a benzyloxy bearing zinc(II) pheophorbide-a (Zn-PH-A) were investigated via in vivo and in vitro experiments. Zn-PH-A was labeled with (131)I with high efficiency (95.

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

The 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 (131)I with high efficiency (92.9 ± 4.

Design of radiolabeled gelatinase inhibitor peptide ((99m)Tc-CLP) and evaluation in rats.

In malignant tissues, MMP-9 (gelatinase B, 92 kDa type IV collagenase) and MMP-2 (gelatinase A, 72 kDa type IV collagenase) are the most prevalent matrix metalloproteinases related to the tumor aggressiveness and metastatic potential. Since elevated levels of gelatinases are associated with poor prognosis in cancer patients, these enzymes are potential targets for tumor imaging to possibly predict metastases. In the present study, a cyclic decapeptide, CLP (Cys-Leu-Pro-Gly-His-Trp-Gly-Phe-Pro-Ser-Cys), was selected as a basic peptide because of its selective inhibitory activity toward gelatinases.

Evaluation of (131)I-pentamidine for scintigraphy of experimentally Leishmania tropica-infected hamsters.

We aimed to assess the ability of (131)I-Pentamidine scintigraphy to detect the lesions of Leishmania tropica infection. An experimental model of cutaneous leishmaniasis was developed. The presence of cutaneous leishmaniasis was confirmed.

In vitro evaluation of (99m)Tc-EDDA/tricine-HYNIC-Q-Litorin in gastrin-releasing peptide receptor positive tumor cell lines.

Bombesin and its derivatives exhibit a high affinity for gastrin-releasing peptide receptor (GRPr), which is over-expressed in a variety of human cancers (prostate, pancreatic, lung, etc.). The aim of this study was to investigate the in vitro potential of the hydrazinonicotinamide (HYNIC)-Q-Litorin.

Influence of uracil on bacterial translocation in an intestinal obstruction model in rats.

Introduction: Bacterial translocation occurs when intestinal mucosa and the intestinal wall lose their barrier properties against bacteria such as in the case of intestinal obstruction. Enteral nutrition with immunonutrients strengthens the immune system and thickens the intestinal barrier thus preventing bacterial translocation.

Aim: The purpose of this study is to investigate the effect of uracil which is an immunonutrient on bacterial translocation using rats with intestinal obstruction as a model.

Radiolabeling of folate targeted multifunctional conjugate with Technetium-99m and biodistribution studies in rats.

Despite the progress in the diagnosis and management of early stage disease, the management of advanced prostate cancer remains an important problem. Prostate tissue expresses folate receptor (FR) which binds both folic acid and folate-linked drugs or imaging agents. Doxorubicin is the best known and most widely used member of the anthracycline antibiotic group of anticancer agents.

Synthesis and biological evaluation of radiolabeled photosensitizer linked bovine serum albumin nanoparticles as a tumor imaging agent.

In this study, we reported on the synthesis and biological evaluation of radiolabeled fluorescent dye conjugated bovine serum albumin nanoparticles within the size range 190-210 nm. The bovine serum albumin nanoparticles (BSANPs) were prepared using a desolvation method, and chemical cross-linking was performed using gluteraldehyde. Furthermore, pheophorbide-a (PH-A) was loaded on the BSANPs.

Synthesis and biological evaluation of receptor-based tumor imaging agent: (99m)Tc-folate-glucaric acid.

The aim of the present study was to prepare (99m)Tc-folate-glucaric acid and investigate the radiopharmaceutical potential for tumors imaging that over express folate receptor. Folate-glucaric acid was synthesized and the synthesized folate conjugate was confirmed with (1)H NMR and LC-MS/MS methods. Folate-glucaric acid was labeled with (99m)Tc, and its radiolabelling efficiency was found as 96 ± 2.

Evaluation of 99mTc-Pheophorbide-a use in infection imaging: a rat model.

This study aims to prepare (99m)Technetium Pheophorbide-a ((99m)Tc-PH-A) complex and evaluate its efficiency as an infection imaging agent. First, PH-A was obtained from Spirulina maxima algae, and the product compound was confirmed using (1)H NMR and MS (ESI) methods. The PH-A was then labeled with (99m)Tc using the tin chloride method and its biological efficacy as a potential radiotracer for Staphylococcus aureus (S.

In vitro evaluation of apoptosis with 99mTc-glucoheptonate.

Radiopharmaceuticals are useful to evaluate effectiveness of cancer treatments as well as diagnosis of diseases. (99m)Tc-Glucoheptonate has high sensitivity for imaging lung cancer tissues. In this study, the potential use of (99m)Tc-glucoheptonate for monitoring apoptosis related to chemotherapeutic agents is investigated in vitro using A549 lung cancer cell line.

Evaluation of ⁹⁹(m)Tc-labeled antibiotics for infection detection.

One of the fields of research in nuclear medicine is the development of new radiopharmaceuticals for imaging infection and inflammation in humans. For this development, several antimicrobial peptides, antibiotics, antibiotic peptide and chemotactic peptides, etc., have been radiolabeled with different radionuclides (⁶⁷Ga, ⁹⁹(m)Tc, ¹¹¹In, ¹⁸F, ¹³¹I, etc.

Radiolabeling of morphine with (131)i and its biodistribution in rats.

This study was conducted to determine the possible radiopharmaceutical potential of morphin labeled with (131)I. Morphine was extracted from dry capsules of the opium poppy (Papaver somniferum L.), purified by high-performance liquid chromatography, and characterized with nuclear magnetic resonance and infrared spectroscopy.

Design and synthesis of 99mTc-citro-folate for use as a tumor-targeted radiopharmaceutical.

Folate conjugates exhibit high affinity for folate receptor (FR) positive cells and tissues, such as those in tumors, making them attractive candidates and of interest in diagnostic tumor imaging. The aim of study was to synthesize a novel radiopharmaceutical based folate conjugate, (99m)Tc-citro-folate, and to evaluate its efficiency as a targeted agent for imaging tumors that over express FR. TLC, HPLC (1)H NMR and LC-MS/MS methods were used to check and confirm the synthesized citro-folate.

In vitro evaluation, biodistribution in rats of radiolabeled raloxifene.

Raloxifene is a selective estrogen receptor modulator that produces both estrogen agonistic effects on bone and lipid metabolism and estrogen-antagonistic effects on uterine endometrium and breast tissue. In the present study, raloxifene was labeled with I-131 by iodogen method and investigated for its radiopharmaceutical potential. Radiolabeling yield is 91+/-0.

Synthesis and biodistribution studies of two novel radiolabeled estrone derivatives.

Background: Two 99mTc-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, 99mTc-2,2',2"2"'-(2,2'-(2-(3-methoxy-13-methyl-17-oxo-7, 8, 9, 11, 12, 13, 14, 15, 16, 7-decahydro-6H- cyclopenta[a]phenanthren-2-ylamino)-2- oxoethylazanediyl) bis(ethane-2,1-diyl)) bis(azanetriyl) tetraacetic acid (99mTc-2-DTPA-3-methoxy estrone) and 9mTc-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-diyl))bis(azanetriyl)tetraacetic acid (99mTc-4-DTPA-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).