Labeling of graphene oxide with [131I]AgI and its stability analysis.

To explore the new iodine labeling method of nanomaterials, graphene oxide (GO) was labeled by 131I with AgI nanoparticles. As a control, GO was also labeled by 131I with chloramine-T method. The stability of the two 131I labeling materials, viz. [131I]AgI-GO and [131I]I-GO was evaluated. The results show that [131I]AgI-GO is very stable in inorganic environment such as PBS and saline. However, it is not stable enough in serum. The instability of [131I]AgI-GO in serum can be attributed to the higher affinity of Ag to S of thiol group in cysteine than iodine ions and much more chance of interaction between thiol group and [131I]AgI nanoparticles on two-dimensional GO than in three-dimensional nanomaterials.

Comparison and Mechanism Study of Antibacterial Activity of Cationic and Neutral Oligo-Thiophene-Ethynylene.

Photodynamic therapy (PDT) is a potential approach to resolve antibiotic resistance, and phenylene/thiophene-ethynylene oligomers have been widely studied as effective antibacterial reagents. Oligomers with thiophene moieties usually exhibit good antibacterial activity under light irradiation and dark conditions. In the previous study, we verified that neutral oligo-p-phenylene-ethynylenes (OPEs) exhibit better antibacterial activity than the corresponding cationic ones; however, whether this regular pattern also operates in other kinds of oligomers such as oligo-thiophene-ethynylene (OTE) is unknown. Also, the antibacterial activity comparison of OTEs bearing cyclic and acyclic amino groups will offer useful information to further understand the role of amino groups in the antibacterial process and guide the antibacterial reagent design as amino groups affect the antibacterial activity a lot. We synthesized four OTEs bearing neutral or cationic, cyclic, or acyclic amino groups and studied their antibacterial activity in detail. The experimental results indicated that the OTEs exhibited better antibacterial activity than the OPEs, the neutral OTEs exhibited better antibacterial activity in most cases, and OTEs bearing cyclic amino groups exhibited better antibacterial activity than those bearing acyclic ones in most cases. This study provides useful guidelines for further antibacterial reagent design and investigations.

Investigating Antibacterial Efficiency and Mechanism of Oligo-thiophenes under White Light and Specific Biocidal Activity against E. coli in Dark.

More strategies are required to develop better photosensitizers for photodynamic therapy (PDT). As oligo(phenylene-ethynylene) electrolytes (OPE), oligo(thiophene)s with primary amine as pendant groups (P-OT), and oligo(thiophene ethynylene) (OTE) exhibit excellent light-induced biocidal activity, we desire to converge the molecular design principles of these three kinds of antibacterial agents to combine their advantages to obtain high efficiency and economic biocides. Thus, four oligo(thiophene)s (OTs) were designed and synthesized in this study. The light-induced and dark antibacterial efficacy of the four OTs against Gram-positive Staphylococcus aureus (S. aureus) and Gram-negative Escherichia coli (E. coli) were both evaluated. Notably, all the OTs present high biocidal efficacy in the broad spectrum at low (micromolar) concentrations after white-light irradiation. In particular, the low cell cytotoxicity of OTs exhibits their good biocompatibility. These results illustrate that the OTs could work as promising PDT biocides. Interestingly, OT-3 shows a strong and specific dark killing activity against E. coli. The higher biocidal efficacy of T-OTs compared with that of Q-OTs confirms the tertiary amine is a better pendant group for π-conjugated antibacterial agents against E. coli. Mechanistic investigation proves ROS is the necessary element for antibiosis under white light. The interacting efficacy of the OT to the cell membrane, involving synergistic effects between hydrophilic-hydrophobic interactions and electrostatic attractions, is also critical in the killing process. The membrane intercalating activity plays a more essential role, as indicated by the antibacterial activity of OTs. The results provide a unique insight into the relationship between molecular structure and antibacterial activities of this class of antibacterial agents.

Biocidal Activity and Mechanism Study of Unsymmetrical Oligo-Phenylene-Ethynylenes.

Bacterial contamination and the spread of antibiotic-resistant bacteria demand alternate methods to deal with bacterial infections. With particular advantages, photodynamic therapy (PDT) is a promising approach. As a kind of photosensitizer for PDT, light-induced antibacterial compounds like oligo-p-phenylene-ethynylenes (OPEs) have been widely investigated while these studies mainly focus on OPEs with quaternary ammonium salts. In our previous study, OPEs with tertiary amino groups (T-OPEs) were reported to exhibit a better antibacterial activity than the corresponding quaternary ammonium salts, which make it important to develop T-OPEs and further investigate their structure-activity relationship. Additionally, the terminal structure of the reported OPEs mainly consists of quaternary ammonium salts or tertiary amino groups, which could not be linked to other materials. Thus, to develop more effective and multifunctional antibacterial agents, we designed and synthesized four unsymmetrical OPEs having terminal amino groups, which could be linked to other functional units by covalent bonds. Their antibacterial activity against Gram-positive and Gram-negative bacteria and the mechanism have been investigated. The OPEs showed effective biocidal activity under fiber light irradiation, and no dark killing was observed. The mechanism study indicates that OPEs could penetrate and perturb the cell membrane and generate ROS under light irradiation, both of which could influence their antibacterial activity. The penetrating ability of OPEs is partly dependent on their lipophilicity and the structure and composition of the cell membrane.

Evaluating the Photodynamic Biocidal Activity and Investigating the Mechanism of Thiazolium Cyanine Dyes.

In order to develop ideal photosensitizers for photodynamic therapy (PDT), a thiazolium group was introduced in cyanine dyes to possess the advantages of intense absorption in the visible region and anti-microbial activity. We evaluated the anti-bacterial activity of the three thiazolium cyanine dyes against Staphylococcus aureus (Gram-positive bacteria) and Escherichia coli (Gram-negative bacteria) in vitro. This is the first time that such kinds of cyanine dyes are applied in the photodynamic antibiotic area. Cyanines display excellent anti-bacterial activity to S. aureus and E. coli exposed to white light irradiation, and the corresponding light-induced biocidal efficacy of cyanines increased with irradiation time and concentration. At the same time, there was no observation of dark anti-bacterial abilities. Especially, cyanines show low cell cytotoxicity and excellent biocompatibility. These results suggest that thiazolium cyanine could work as a photosensitizer in PDT with great promise and broad applications for killing bacteria. Mechanistic studies suggest that the reactive oxygen species (ROS) is the vital factor for combating bacteria exposure to white light conditions, whereas it is not the only determining factor of the biocidal activity. The interaction of the cyanine to the cell membrane also plays a critical role in killing bacteria, which has exhibited a synergic effect of electrostatic and hydrophobic interactions. It influences the cell uptake and the membrane perturbation activity of the cyanines, which indirectly affects the biocidal activity.

Visible light-induced biocidal activities and mechanistic study of neutral porphyrin derivatives against S. aureus and E. coli.

Positive charged porphyrins have long been regarded as effective biocidal agents, however neutral porphyrins have rarely been studied in their ability photoinactivating microbials, and the structure-activity relationship such as correlation of electronic effect and biocidal activity of porphyrins still remains unclear. Herein, four neutral porphyrins with various electronic effects were selected to undergo light-induced biocidal processes. It turned out that the TPPOH and TPPNH2 with electron-donating groups NH2 and OH, respectively, exhibited much more powerful light-induced biocidal activities against E. coli and S. aureus than TPP and TPPNO2 with electron-withdrawing group NO2. This phenomenon suggested that neutral porphyrins may be treated as a new class of biocidal agents and functional groups with various electronic effects on porphyrins can dramatically affect porphyrins' light-induced biocidal activities. Mechanistic studies demonstrate that despite a better light-induced antibacterial ability of TPPOH, its singlet oxygen generation efficacy is a little lower than that of TPPNH2, together with charge characteristics and lipophilicity, it is clear that (1) the oxidative species singlet oxygen and ROS played the key role in the photo-activated antimicrobial processes of porphyrins, and (2) higher singlet oxygen or ROS yields of TPPOH and TPPNH2 may originate from their structural characteristics, namely electron-donating groups OH or NH2, and (3) a synergistic effect of all other factors including the electrostatic and hydrophobic effects must involve in the process and cooperatively determine their biocidal activities.

A simple and convenient method for production of 89Zr with high purity.

A simple and convenient method for radiochemical separation 89Zr with no harmful substance was explored. The separated 89Zr was found to be [89Zr]Zr-chloride, and the recovery of the radioactivity was 85%±3% with high radionuclidic purity (99.99%). The yields of 89Zr via the reaction of (p, n) or (d, 2n) on Y target were also evaluated on CS-30 cyclotron, indicating the latter was more favorable for the production of 89Zr with a yield of 58±4 MBq/µA·h.

The radiation damage of crystalline silicon PN diode in tritium beta-voltaic battery.

A tritium beta-voltaic battery using a crystalline silicon convertor composed of (100)Si/SiO2/Si3N4 film degrades remarkably with radiation from a high intensity titanium tritide film. Simulation and experiments were carried out to investigate the main factor causing the degradation. The radiation damages mainly comes from the x-ray emitted from the titanium tritide film and beta particle can relieve the damages. The x-ray radiation induced positive charges in the SiO2 film destroying the output property of the PN diode with the induction of an electric field.

Simulations about self-absorption of tritium in titanium tritide and the energy deposition in a silicon Schottky barrier diode.

Simulations on the self-absorption of tritium electrons in titanium tritide films and the energy deposition in a silicon Schottky barrier diode are carried out using the Geant4 radiation transport toolkit. Energy consumed in each part of the Schottky radiovoltaic battery is simulated to give a clue about how to make the battery work better. The power and energy-conversion efficiency of the tritium silicon Schottky radiovoltaic battery in an optimized design are simulated. Good consistency with experiments is obtained.

Investigation on a radiation tolerant betavoltaic battery based on Schottky barrier diode.

An Au-Si Schottky barrier diode was studied as the energy conversion device of betavoltaic batteries. Its electrical performance under radiation of Ni-63 and H-3 sources and radiation degradation under Am-241 were investigated and compared with those of the p-n junction. The results show that the Schottky diode had a higher I(sc) and harder radiation tolerance but lower V(oc) than the p-n junction. The results indicated that the Schottky diode can be a promising candidate for energy conversion of betavoltaic batteries.

The effect of temperature changes on electrical performance of the betavoltaic cell.

There is a significant relationship between temperature and electrical performance of a betavoltaic cell. Two silicon diodes used as energy conversion devices of betavoltaic cells were irradiated by Ni-63, and the relationships between the temperature and the electrical performance such as V(oc), I(sc), and P(max) were examined. I(sc) increased very little as temperature increased but V(oc) decreased considerably. The changing values of V(oc) were -3.1 and -3.0 mV/K, respectively, in the temperature range 233.15-333.15 K. As a result of this, P(max) and eta also decreased markedly.

DNA cleavage promoted by 2,9-dimethyl-4,7-diazadecane-2,9-dithiol (DDD) derivatives.

Three piperidine derivatives of 2,9-dimethyl-4,7-diazadecane-2,9-dithiol (DDD), NEPDDD, NEMPDDD, and NEMMPDDD, were synthesized and used as catalysts in DNA cleavage. Under physiological conditions, a series of experiments have been done. The effects of DNA cleavage with three ligands were studied under different concentrations, cleavage time, and pH values. The results strongly suggested that the plasmid DNA (pUC 19) can be cleaved efficiently by these ligands. For the cleavage reaction catalyzed by NEMPDDD, Form I DNA could convert to Form II completely, and the DNA-cleavage mechanism involved an oxidative pathway.

Labeling conditions, in vitro properties and biodistributions of various Sn-labeled complexes.

Conditions for preparing Sn-EDTMP, Sn-DTPMP, Sn-TTHMP, Sn-HEDTMP and Sn-DTPA in aqueous solution in open air environments, and their in vitro properties including adsorption on hydroxyapatite (HA) and collagen (I) and binding to bovine serum albumin (BSA) were studied using (117m)Sn and 113Sn as tracers. Biodistributions of SnO2.xH2O.yEDTMP, SnO2.xH2O.yDTPMP, SnO2.xH2O.yTTHMP, SnO2.xH2O.yHEDTMP, SnO2.xH2O.yDTPA in normal mice were also tested. Based on the above experiments, the relationship between in vitro biochemical properties and biodistributions of these SnO2.xH2O.yLigands was investigated. The results show that Sn(IV)-Ligands are prone to hydrolysis into SnO2.xH2O.yLigands in aqueous solutions in open air environments, especially when the ligand is DTPA, when the molar ratio of metal to ligand is higher than 1:200, or when the pH of the solution is higher than 10. The in vitro experiments show that all of the SnO2.xH2O.yLigands bind strongly to BSA, and the binding percentages of SnO2.xH2O.yLigands to BSA are much higher than those of the corresponding Sn(IV)-Ligands. The biodistribution data indicate that all of the SnO2.xH2O.yLigands locate mainly in bone with little uptake in liver. When the binding percentages of SnO2.xH2O.yLigands to BSA are similar, those SnO2.xH2O.yLigands with higher adsorption on HA and collagen (I) undergo lower liver uptake.