Resveratrol Sensitizes Selectively Thyroid Cancer Cell to 131-Iodine Toxicity

Background. In this study, the radiosensitizing effect of resveratrol as a natural product was investigated on cell toxicity induced by 131I in thyroid cancer cell. Methods. Human thyroid cancer cell and human nonmalignant fibroblast cell (HFFF2) were treated with 131I and/or resveratrol at different concentrations for 48 h. The cell proliferation was measured by determination of the percent of the survival cells using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. Results. Findings of this study show that resveratrol enhanced the cell death induced by 131I on thyroid cancer cell. Also, resveratrol exhibited a protective effect on normal cells against 131I toxicity. Conclusion. This result indicates a promising effect of resveratrol on improvement of cellular toxicity during iodine therapy

The Effects of Punica granatum

Background. We compared the efficacy of P. granatum (P) flower extract with that of silver sulfadiazine (SSD) for treating thermal burn injuries in rats. Methods. Ten Wistar rats in each group were topically given base cream, normal saline, cream containing 1% SSD, or creams containing 5% or 10% Punica granatum flower extract. The treatments were administered once daily until complete wound healing was observed. The wound area and healing time were assessed. In addition, percentage wound contraction and histopathological characteristics such as neovascularization and collagen formation were determined. The tannin content in P. granatum extract was determined. Results. The decrease in the average size of wounds on day 15 of the treatment was higher in rats treated with creams containing P. granatum extract than in rats treated with cream containing SSD (2.8±0.9 cm2 versus 8.4±3.2 cm2). The wounds completely healed on day 25 of the treatment in rats treated with creams containing P. granatum flower extract compared with those in rats treated with the other agents. Conclusion. These results indicated that P. granatum flower extract promoted wound healing in rats and could be used for managing burn injuries

Discovery of novel 1,2,4-triazolo-1,2,4-triazines with thiomethylpyridine hinge binders as potent c-Met kinase inhibitors

Mesenchymal-epithelial transition factor HGF/c-Met overactivation is involved in diverse human cancers. Herein, we report the synthesis and biological evaluation of thiomethylpyridine-linked triazolotriazines as c-Met kinase inhibitors

Optimizing Labeling Conditions for Cysteine-Based Peptides with 99m

Radiolabelled peptides have attracted a great deal of attention due to their wide applicability in the development of target-specific radiopharmaceuticals. They can easily be used in diagnostic imaging as carriers for the delivery of radionuclides to tumors as well as for therapy. Previous investigations revealed that technetium(V) could form stable complexes with peptide-based ligands of N3S type such as Cys-Gly-Gly-Gly. Herein, a targeting HER-2 receptor peptide was labeled with technetium-99m (99mTc) with two different types of tetrapeptide-based ligands, Cys-Gly-Gly-Gly and Cys-Ser-Ser-Ser. The effect of experimental parameters in the labeling procedure such as type of buffer solutions, pH of media, and type of exchange ligands were optimized toward obtaining maximum labeling yield. The optimum labeling conditions were different for two peptides. Shelf life of both labeled peptides was determined by analytical reversed-phase high-performance liquid chromatography (RP-HPLC) and thin layer chromatography (TLC) that showed radiochemical yield up to 95% even after 4 h

The use of 99mTc-phytate for assessment the protective effect of vitamin E against hepatotoxicity induced by methotrexat in rat

In this study, we investigated the protective effect of vitamin E against methotrexate (MTX)-induced hepatotoxicity by quantitative liver 99mTc-phytate uptake and liver imaging and to compare its effect with histopathology in rat. Rats were divided into five groups as control, solvent, Vit E (100 mg/kg), MTX (20 mg/kg), Vit E + MTX and. Vit E was intraperitoneally administrated for 17 days before MTX injection and continued for 4 days. 99mTc-phytate was injected through the tail of rats after the drug administration. The percentage of the injected dose per gram of liver and spleen tissues (%ID/g) was calculated. Liver imaging was obtained with gamma camera. In other experiment, liver of treated rats were assessed for histopathology. 99mTc-phytate uptake per gram tissue of the livers as %ID/g in control, solvent, MTX, Vit E, Vit E + MTX and MTX groups were 8.99% ± 1.37, 8.53% ± 2.91, 8.65% ± 3.84, 3.22% ± 1.09 and 8.38% ± 2.68. Vit E administration with MTX resulted in a significant increasing in the level of %ID/g. Vit E treatment improved the shape of live in planner image. Histophatological examinations showed a protective effect of Vit E against MTX-induced hepatoxicity in rats. The results showed that Vit E significantly attenuates the MTX-induced hepatotoxicity in rats, and 99mTc-phytate uptake in liver as well as liver image to be acceptable techniques for assessment of liver and spleen damages and/or their tissues protective effects in animal model.Hepatotoxicity is one of the most common side effects of methotrexate (MTX) therapy in patients. The aim of this study was to evaluate the protective effect of vitamin E against MTX-induced hepatotoxicity using 99mTc-phytate as a radiopharmaceutical agent in animals. Rats were divided into five groups as follows: control, solvent, Vit E (100 mg/kg), MTX (20 mg/kg) and Vit E + MTX. Animals were intraperitoneally injected with Vit E for 17 days before MTX injection and continued for 4 days. 99mTc-phytate was injected into the tail of rats after the 21 days of Vit E administration. Percentage of the injected dose per gram of liver and spleen tissues (%ID/g) was calculated in treated rats. Liver imaging was obtained with gamma camera. In other experiment, liver of treated rats was assessed for histopathology. 99mTc-phytate uptake (%ID/g) of livers in control, solvent, Vit E, MTX and Vit E + MTX groups were 8.99% ± 1.37, 8.53% ± 2.91, 8.65% ± 3.84, 3.22% ± 1.09 and 8.38% ± 2.68. Vit E administration resulted in a significant increase of the level of %ID/g in MTX-injected animal. Vit E pre-treatment improved the shape of liver in MTX-treated rat which was seen abnormal view in planar imaging. Histophatological examinations approved the protective effect of Vit E against MTX-induced hepatotoxicity in rats. The results of this study show that Vit E significantly attenuates the MTX-induced hepatotoxicity in rats, and 99mTc-phytate is an acceptable radiopharmaceutical agent for assessment of liver and spleen damages in the animal model

Quantification of thymol content in different extracts of Zataria multiflora by HPLC method

Zataria multiflora Boiss is used in traditional folk remedies as antiseptic, analgesic, carminative, anthelmintic medication. The main components of Z. multiflora are phenolic compounds such as thymol and carvacrol. The aim of this study was developed a simple and rapid method for determination of the thymol in different extracts of Z. multiflora by HPLC method. The dried aerial parts of Z. multiflora in the flowering stage was extracted with ethanol 34%, 42% and 70% for 48 hours. Several mobile phase systems were applied for development and separation of thymol and carvacrol that have close retention time in HPLC system. The peaks of thymol and carvacrol are successfully separated in acetonitrile-water-acetic acid mobile phase. Thymol and carvacrol were separated with a retention times 10.4 and 9.8 minutes respectively, in an isocratic solvent system with HPLC. Thymol content was 2.7 ± 0.06, 3.7 ± 0.07 and 6.0 ± 0.11 mg/g, in ethanol at concentration of 34%, 42% and 70%, respectively. Thymol content in different hydroalcoholic extract of Z. multiflora is dependent to ethanol concentration in extraction solvent

99mTc-HYNIC-(tricine/EDDA)-FROP peptide for MCF-7 breast tumor targeting and imaging

Abstract Background Breast cancer is the most common malignancy among women in the world. Development of novel tumor-specific radiopharmaceuticals for early breast tumor diagnosis is highly desirable. In this study we developed 99mTc-HYNIC-(tricine/EDDA)-Lys-FROP peptide with the ability of specific binding to MCF-7 breast tumor. Methods The FROP-1 peptide was conjugated with the bifunctional chelator hydrazinonicotinamide (HYNIC) and labeled with 99mTc using tricine/EDDA co-ligand. The cellular specific binding of 99mTc-HYNIC-FROP was evaluated on different cell lines as well as with blocking experiment on MCF-7 (human breast adenocarcinoma). The tumor targeting and imaging of this labeled peptide were performed on MCF-7 tumor bearing mice. Results Radiochemical purity for 99mTc-HYNIC-(tricine/EDDA)-FROP was 99% which was determined with ITLC method. This radiolabeled peptide showed high stability in normal saline and serum about 98% which was monitored with HPLC method. In saturation binding experiments, the binding constant (Kd) to MCF-7 cells was determined to be 158 nM. Biodistribution results revealed that the 99mTc-HYNIC-FROP was mainly exerted from urinary route. The maximum tumor uptake was found after 30 min post injection (p.i.); however maximum tumor/muscle ratio was seen at 15 min p.i. The tumor uptake of this labeled peptide was specific and blocked by co-injection of excess FROP. According to the planar gamma imaging result, tumor was clearly visible due to the tumor uptake of 99mTc-HYNIC-(tricine/EDDA)-FROP in mouse after 15 min p.i. Conclusions The 99mTc-HYNIC-(tricine/EDDA)-FROP is considered a promising probe with high specific binding to MCF-7 breast cancer cells

Epicatechin enhances anti-proliferative effect of bleomycin in ovarian cancer cell

Background: Bleomycin (BLM) is an anti-cancer drug widely used in the treatment of cancer. BLM causes several side effects related to DNA and cellular damage. The aim of this study was investigated the effects of tea polyphenol epicatechin on anti-proliferative effects induced by bleomycin in human normal skin and human ovarian cancer cells.Materials and Methods: Human ovarian cancer cell (SKOV-3) and human non-malignant fibroblast cell (HFFF2) were treated with epicatechin at various concentrations (10, 25 and 50 µM) and BLM alone and with their combinations, further their effects on cell viability were evaluated.Results: The combined treatment of epicatechin with BLM enhanced significantly inhibition of cell growth in comparison to BLM alone in cancer cell. Epicatechin enhanced significantly cytotoxicity induced by BLM with 83% at dose 50 µM, while it was 92% in BLM-treated cells. Epicatechin was not showed any cytotoxicity on HFFF2 cells. Conclusion: Study suggests that epicatechin chemosensitize the ovarian cancer cell to BLM-induced growth inhibition without any toxicity on normal cell