Bibracchial Lariat Ethers(Ⅰ)——The Synthesis and Crystal Structure of the N,N'-bis(2-Methoxy-1-Naphthylmethyl)-4,13-Diaza-18-Crown-6 Sodium Iodide Complex

Diaza Crown ethers are versatile complexing reagents, their complexing abilities are dramatically modified by the electron donating atoms on substituents attached to the nitrogen if they can give a three-dimensional cavity as in cryptates. Hence the synthesis and characterization of bibracchial lariat ethers (BIBLES) have received much attention. In the preparation of new BIBLES, a complex Ⅱ was unexpectedly obtained.

Baculovirus vector-mediated transfer of NIS gene into colon tumor cells for radionuclide therapy

AIM:To investigate the feasibility of radionuclide therapy of colon tumor cells by baculovirus vector-mediated transfer of the sodium/iodide symporter(NIS) gene.METHODS:A recombinant baculovirus plasmid carrying the NIS gene was constructed,and the viruses(BacNIS) were prepared using the Bac-to-Bac system.The infection efficiency in the colon cancer cell line SW1116 of a green fluorescent protein(GFP) expressing baculovirus(Bac-GFP) at different multiplicities of infection(MOI) with various concentrations of sodium butyrate was determined by flow cytometry.An in vitro cytotoxicity assay was also conducted after infection of SW1116 cells with Bac-NIS.Iodine uptake of Bac-NIS infected SW1116 cells and inhibition of this uptake by sodium perchlorate was examined,and the effect of Bac-NISmediated 131 I in killing tumor cells was evaluated by cell colony formation tests.RESULTS:Infection and transgene expression in SW1116with Bac-GFP were significantly enhanced by sodium butyrate,as up to 72% of SW1116 cells were infected with the virus at MOI of 400 and sodium butyrate at 0.5 mmol/L.No obvious cytotoxicity was observed under these conditions.Infection of SW1116 with Bac-NIS allowed uptake of 131 I in these tumor cells,which could be inhibited by sodium perchlorate.The viability of SW1116 cells infected with Bac-NIS was significantly lower than with Bac-GFP,suggesting that NIS gene-mediated 131 I uptake could specifically kill tumor cells.CONCLUSION:Baculovirus vector-mediated NIS gene therapy is a potential approach for treatment of colon cancer.

Study the Attenuation Coefficient of Granite to Use It as Shields against Gamma Ray

The present work investigates the linear and mass attenuation coefficients for gamma rays practically and theoretically by using spectroscopy gamma ray (UCS-20) and program (XCOM)) for various types of common use granite, and compares them with the lead because of its high blocking ability for this type of radiation. This paper concluded through linear and mass attenuation coefficients measurements that these coefficients decrease with increasing incident photons energy. Measurements also showed that the linear attenuation coefficients appropriate linearly with density while mass attenuation coefficients do not get affected.

Primary lung cancer with radioiodine avidity: A thyroid cancer cohort study

BACKGROUND A proportion of lung cancers show sodium/iodide symporter(NIS)expression.Lung cancers with NIS expression may uptake radioiodine(RAI)and show RAIavid lesions on RAI scan for differentiated thyroid cancer(DTC)surveillance.AIM To investigate the possibility of RAI uptake by lung cancer in a cohort with thyroid cancer.METHODS RAI-avid lung cancers were analyzed using a prospectively maintained database of patients with thyroid cancer who were registered at a medical center between December 1,1976 and May 28,2018.NIS expression in lung cancer was assessed using immunohistochemical staining.RESULTS Of the 5000 patients with thyroid cancer from the studied dataset,4602 had DTC.During follow-up,33 patients developed primary lung cancer.Of these patients,nine received an iodine-131(131I)scan within 1 year before the diagnosis of lung cancer.One of these nine lung cancers was RAI-avid.NIS expression was evaluated,and three of the eight available lung cancers revealed NIS expression.The proportions of lung cancer cells with NIS expression were 60%,15%,and 10%.The RAI-avid lung cancer had the highest level of expression(60%).The RAI-avid lung cancer had a spiculated border upon single-photon emission computed tomography/computed tomography,which led to an accurate diagnosis.CONCLUSION A proportion of lung cancer demonstrates NIS expression and is RAI-avid.Clinicians should be aware of this possibility in the interpretation of RAI scintigraphy.

The effects of thyroid-stimulating hormone,estradiol and prolactin on sodium/iodide symporter mRNA expression in mouse lactating mammary gland cells under different iodine levels

Objective The present study investigated the sodium/iodide symporter mRNA expression in mouse lactating mammary gland cells under different iodine levels and the effects of thyroid-stimulating hormone(TSH),estradiol(E2)and prolactin(PRL)on NIS mRNA expression in mouse lactating mammary gland cells.

Studies on sulfinatodehalogenation XVI.Sodium dithionite-initiated addition of perfluoroalkyl iodides to terminal alkynes

Reaction of perfluoroalkyl iodides with a series of alkynes under sulfinatodehalogenation condition gave a mixture of E/Z adducts very readily in high yield, thus constituted a mild, convenient and effective new method for the addition of perfluoroalkyl iodides to alkynes. Under the same con- dition, in the presence of 1-hexyne perfluoroalkyl bromide and 1,1,1-trichlorotrifluoroethane reacted only to give sulfinates as the major products. A radical mechanism was proposed for the addition reaction.

Studies on sulfinatodehalogenation ⅩⅩⅧ.The addition of polyfluoroalkyl iodides to olefins initiated by sodium disulfite

Polyfluoroalkyl iodides reacted with olefins in aqueous DMF solution of sodium disulfite under mild conditions to give the corresponding 1:1 adducts in good yields,providing a convenient polyfluoroalkylation method.This indicated that R_F radicals were formed in the reaction of polyfluoroalkyl iodides and sodium disulfite.A SET mechanism is proposed for the sulfinatodehalogenation reaction of sodium disulfite.

A convenient catalytic oxidative 1,2-shift of arylalkenes for preparation of α-aryl ketones mediated by NaI

Using a catalytic amount of Nal and a stoichiometric oxidant Oxone-@,a convenient procedure has been developed for the catalytic oxidative 1,2-shift of arylalkenes in CH3CN/H2O at room temperature,which provides the corresponding α-aryl ketones in moderate to good yields.In this protocol,sodium iodide is first oxidized into hypoiodous acid,which reacts with arylalkene to afford iodohydrin.Then,the iodohydrin is transformed into the α-aryl ketone via an oxidative 1,2-shift rearrangement.

NES1/KLK10 and hNIS gene therapy enhanced iodine-131 internal radiation in PC3 proliferation inhibition

NES1 gene is thought to be a tumor-suppressor gene.Our previous study found that overexpression of NES1 gene in PC3 cell line could slow down the tumor proliferation rate,associated with a mild decrease in BCL-2 expression.The BCL-2 decrease could increase the sensitivity of radiotherapy to tumors.Thus,we supposed to have an“enhanced firepower”effect by combining overexpressed NES1 gene therapy and 131I radiation therapy uptake by overexpressed hNIS protein.We found a weak endogenous expression of hNIS protein in PC3 cells and demonstrated that the low expression of hNIS protein in PC3 cells might be the reason for the low iodine uptake.By overexpressing hNIS in PC3,the radioactive iodine uptake ability was significantly increased.Results of in vitro and in vivo tumor proliferation experiments and 18F-fluorothymidine(18F-FLT)micro-positron emission tomography/computed tomography(micro-PET/CT)imaging showed that the combined NES1 gene therapy and 131I radiation therapy mediated by overexpressed hNIS protein had the best tumor proliferative inhibition effect.Immunohistochemistry showed an obvious decrease of Ki-67 expression and the lowest BCL-2 expression.These data suggest that via inhibition of BCL-2 expression,overexpressed NES1 might enhance the effect of radiation therapy of 131I uptake in hNIS overexpressed PC3 cells.