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The photocatalyzed water splitting reaction in aqueous methanol solution is an efficient preparation method for hydrogen and methanal under mild conditions. In this work, metal sulfide-loaded TiO2 photocatalysts for hydrogen and methanol production were synthesized by hydrothermal method (180°C/12 h) and characterized by X-ray diffraction (XRD), UV-visible diffuse reflectance spectroscopy (DRS), scanning electron microscopy (SEM), and energy-dispersive X-ray spectroscopy (EDX). The crystal structures of the samples are the typical anatase phase of TiO2 and exhibit a spherical morphology. When TiO2 was loaded with CoS, ZnS, and Bi2S3, respectively, the resulting catalysts showed photocatalytic activities for water decomposition to hydrogen in aqueous methanol solution under 300 W Xe lamp irradiation. Among the photocatalysts with various compositions, the 20 wt% CoS/TiO2 sample with a 2.1 eV band gap showed the maximum photocatalytic activity for the photocatalytic reaction, which indicated that CoS improved the separation ratio of photoexcited electrons and holes. The enhanced activity can be attributed to the intimate junctions that are formed between CoS and TiO2, which can reduce the electron-hole recombination. The production rate of hydrogen with 20 wt% CoS/TiO2 photocatalyst was about 5.6 mmol/g/h, which was 67 times higher than that of pure TiO2. The formation rate of HCHO was 1.9 mmol/g/h with 98.7% selectivity. Moreover, the CoS/TiO2 photocatalyst demonstrated good reusability and stability. In the present study, it is demonstrated that CoS can act as an effective cocatalyst to enhance the photocatalytic hydrogen and methanal production activity of TiO2. The highly improved performance of the CoS/TiO2 composite was mainly ascribed to the efficient charge separation.

Various types of eosinophilic neurons (ENs) are found in the post-ischemic brain. The aim of the present study was to elucidate the temporal and spatial profile of ENs, the expression of TUNEL staining and ultrastructural characteristics in the core and peripheral regions of the cortex post-ischemia. Unilateral forebrain ischemia was induced in Mongolian gerbils by transient common carotid artery occlusions, and the brains from 3 h to 2 weeks post-ischemia were prepared for morphometric, electron microscopy (EM) and TUNEL staining of the ENs. Light microscopy showed that ENs with minimally abnormal nuclei and swollen cell bodies appeared at 3 h in the ischemic core and at 12 h in the periphery. Thereafter, ENs with pyknosis and irregular atrophic cytoplasm peaked at 12 h, pyknosis with scant cytoplasm peaked at 4 days, and TUNEL-positive staining was observed in the ischemic core. In the ischemic periphery, ENs had slightly atrophic cytoplasm and sequentially developed pyknosis, karyorrhexis and karyolysis over 1 week. These cells were also positive for TUNEL. In EM, severe organelle dilation and vacuolization preceded chromatin fragmentation in the ischemic core, while chromatin fragmentation and homogenization were the vital characteristics in the ischemic periphery. There might be two region-dependent pathways for EN changes in the post-ischemic brain: pyknosis with cytoplasmic shrinkage in the core and nuclear disintegration with slightly atrophic cytoplasm in the periphery. These pathways were comparable to necrosis and proceeded from non-classical apoptosis to necrosis, respectively.

Ideal anticancer nano drug delivery systems (NDDSs) need to overcome a series of physiological barriers including blood circulation, tumor accumulation, tumor penetration, internalization by cancer cells, lysosomal escape, and on-demand intracellular drug release following systemic administration. However, it remains a big challenge to construct NDDSs that can overcome all the barriers at the same time. Here, we develop zwitterionic temperature/redox-sensitive nanogels loaded with near-infrared (NIR) dye Indocyanine green (ICG) and anticancer drug doxorubicin (I/D@NG). I/D@NG exhibits enhanced photothermal effects, and NIR irradiation markedly decreases its diameter. NIR irradiation at tumor sites significantly enhances tumor accumulation, tumor penetration, and cellular uptake of I/D@NG with prolonged blood circulation time. Furthermore, I/D@NG can effectively escape from lysosomes by singlet oxygen-induced lysosomal disruption, and DOX is then sufficiently released from the nanogels to the nucleus in response to high intracellular GSH and photothermal effects. This nanoplatform for thermo-chemotherapy not only efficiently exerts synergistic cytotoxicity but also overcomes all the physiological barriers of therapeutic agent, thereby providing a substantial in vivo anticancer effect. The multiple functions of I/D@NG provide new insights into designing nanoplatforms for synergistic cancer therapy.

Novel synthetic compounds similar to heroin and its major active metabolites, 6-acetylmorphine and morphine, were examined as potential surrogate haptens for the ability to interface with the immune system for a heroin vaccine. Recent studies have suggested that heroin-like haptens must degrade hydrolytically to induce independent immune responses both to heroin and to the metabolites, resulting in antisera containing mixtures of antibodies (type 2 cross-reactivity). To test this concept, two unique hydrolytically stable haptens were created based on presumed structural facial similarities to heroin or to its active metabolites. After conjugation of a heroin-like hapten (DiAmHap) to tetanus toxoid and mixing with liposomes containing monophosphoryl lipid A, high titers of antibodies after two injections in mice had complementary binding sites that exhibited strong type 1 ("true") specific cross-reactivity with heroin and with both of its physiologically active metabolites. Mice immunized with each surrogate hapten exhibited reduced antinociceptive effects caused by injection of heroin. This approach obviates the need to create hydrolytically unstable synthetic heroin-like compounds to induce independent immune responses to heroin and its active metabolites for vaccine development. Facial recognition of hydrolytically stable surrogate haptens by antibodies together with type 1 cross-reactivities with heroin and its metabolites can help to guide synthetic chemical strategies for efficient development of a heroin vaccine.

Three haptens have been synthesized with linkers for attachment to carrier macromolecules at either the piperidino-nitrogen or via an introduced 3-amino group. Two of the haptens, with a 2-oxopropyl functionality at either C6, or at both the C3 and C6 positions on the 4,5-epoxymorphinan framework, as well as the third hapten (DiAmHap) with diamido moieties at both the C3 and C6 positions, should be much more stable in solution, or in vivo in a vaccine, than a hapten with an ester in one of those positions, as found in many heroin-based haptens. A “classical” opioid synthetic scheme enabled the formation of a 3-amino-4,5-epoxymorphinan which could not be obtained using palladium chemistry. Our vaccines are aimed at the reduction of the abuse of heroin and, as well, at the reduction of the effects of its predominant metabolites, 6-acetylmorphine and morphine. One of the haptens, DiAmHap, has given interesting results in a heroin vaccine and is clearly more suited for the purpose than the other two haptens.

In this work, Co1-xZnxIn2S4 nanocomposites photocatalysts were synthesized by hydrothermal method, and characterized by UV-visible DRS. The prepared Co0.5Zn0.5In2S4 nanocomposites, which exhibits the highest H2 production rate, the value is 36.08 umolh−1g−1, exceeding more than 8 times compared with the pure ZnIn2S4 and CoIn2S4. Co0.5Zn0.5In2S4 nanocomposites also has good reuse and stability. Two reasons lead to higher photocatalytic H2 production activity are enough visible-light absorption capacity and suitable conduction band potential of the Co0.5Zn0.5In2S4. In this research, it is proven that Co0.5Zn0.5In2S4nanocompositesphotocatalystscan enhance the photocatalytic H2 production activity. The significant improvement in the performance of Co0.5Zn0.5In2S4 nanocomposites is mainly due to effective charge separation.

In order to create an effective immunization approach for a potential vaccine to heroin, liposomes containing monophosphoryl lipid A [L(MPLA)] were tested as an adjuvant system to induce antibodies to heroin hapten analogs. Four synthetic haptens and two immunization strategies were employed. In the first strategy, a hydrophobic 23 amino acid immunogenic peptide derived from the membrane proximal external region of gp41 from HIV-1 envelope protein was embedded as a carrier in the outer surface of L(MPLA), to which was conjugated a 15 amino acid universal T cell epitope and a terminal heroin hapten analog. In the second strategy, tetanus toxoid (TT) carrier protein was decorated with haptens by conjugation, and the hapten-conjugated protein was mixed with L(MPLA). After immunization of mice, each of the immunization strategies was effective for induction of IgG anti-hapten antibodies. The first immunization strategy induced a mean end-point IgG titer against one of two haptens tested of approximately 12,800; however, no detectable antibodies were induced against the liposome-associated HIV-1 carrier peptide. In the second immunization strategy, depending on the hapten used for decorating the TT, end-point IgG titers ranged from 100,000 to 6,500,000. In this strategy, in which hapten was conjugated to the TT, end-point IgG titers of 400,000 to the TT carrier were observed with each conjugate. However, upon mixing unconjugated TT with L(MPLA), anti-TT titers of 6,500,000 were observed. We conclude that L(MPLA) serves as a potent adjuvant for inducing antibodies to candidate heroin haptens. However, antibodies to the carrier peptide or protein were partly or completed inhibited by the presence of conjugated hapten.

TiO2has been widely used as a key catalyst in photocatalytic reactions; it also shows good catalytic activity for esterification reactions. Different sulfated M-TiO2nanoparticles (M = Ag, Au, Rh, and Pt) were prepared by photodeposition and ultrasonic methods. The results show that the noble metal nanoparticles, which were loaded onto a TiO2surface, slightly affected the crystal phase and particle size of TiO2. Among all the catalysts,SO42-/Au-TiO2exhibited the best catalytic activity in the esterification reaction for the synthesis of citric acidn-butyl acetate and in the decomposition of methyl orange, as confirmed by a high conversion rate of up to 98.2% and 100% degradation rate, respectively. This can be attributed to an increase in the Lewis acidity of the catalyst and increased separation efficiency of electron-hole pairs. This superior catalyst has great potential applications in esterification reactions and wastewater treatments.

RuCl3/NaIO4-initiated oxidation of oxiranemethanols was investigated, and two products, oxirane-2-carboxylic acid and (5′-oxotetrahydrofuran-3-yl)acetic acid, were obtained in variant ratios. The product structures were determined and a tentative mechanism involving oxidation-rearrangement-oxidation process was proposed. Glucokinase enzymatic assay revealed that oxiranecarboxamides 4a–c retained moderate GK activation potency with amide 4a showing an EC50 value of 584 nM and a high activation fold of 3.14. However, (5′-oxotetrahydrofuran-3-yl)acetamide 11a is inactive. This study not only provided an alternative protocol to access (5′-oxotetrahydrofuran-3-yl)acetic acid analogs, but also yielded nanomolar GA activators (esp. 4a) for further structure–activity relationship study.

Aim: To investigate the effects of ATPM-ET ((-)-3-N-Ethylaminothiazolo (5,4-b)-N-cyclopropylmethylmorphinan hydrochloride) on physical dependence and behavioral sensitization to morphine in mice. Methods: The pharmacological profile of ATPM-ET was characterized using competitive binding and GTPγS binding assays. We then examined the antinociceptive effects of ATPM-ET in the hot plate test. Morphine dependence assay and behavioral sensitization assay were used to determine the effect of ATPM-ET on physical dependence and behavior sensitization to morphine in mice. Results: The binding assay indicated that ATPM-ET ATPM-ET exhibited a high affinity to both κ- and µ-opioid receptors with K i values of 0.15 nmol/L and 4.7 nmol/L, respectively, indicating it was a full κ-opioid receptor agonist and a partial μ-opioid receptor agonist. In the hot plate test, ATPM-ET produced a dose-dependent antinociceptive effect, with an ED50 value of 2.68 (2.34-3.07) mg/kg. Administration of ATPM-ET (1 and 2 mg/kg, sc) prior to naloxone (3.0 mg/kg, sc) injection significantly inhibited withdrawal jumping of mice. In addition, ATPM-ET (1 and 2 mg/kg, sc) also showed a trend toward decreasing morphine withdrawal-induced weight loss. ATPM-ET (1.5 and 3 mg/kg, sc) 15 min before the morphine challenge significantly inhibited the morphine-induced behavior sensitiza- tion (P

A series of new 14-hydroxymorphinan analogues with a thiazole or imidazo[2,1-b]thiazole fragment as the heterocyclic function fused to ring C were designed and synthesized. These compounds can be viewed as the result of a direct modification at ring C of the 14-hydroxymorphinan scaffold. Among these compounds, three were identified as having potent binding affinity (approximately 1 nM) at both kappa and mu receptors, and acting as agonists at kappa and partial agonists or antagonists at mu receptors. In view of the promising results from studies on compounds with mixed kappa and mu receptor activities, these new compounds warrant further investigation.

Total synthesis of natural product marmycin A was studied. An expeditious synthetic strategy for the key fragment 8-amino-3-methylbenz[a]anthraquinone (1) was established with decarboxylative alkylation, Pd(OAc)(2)-catalyzed cyclization, aromatization, and C-N coupling as the key steps. However, final assembly of marmycin A was hampered by the failure to obtain the carbohydrate fragment 2. Instead, a small library of desmethyl analogues of marmycin A was prepared in moderate yields by using the InBr(3)-catalyzed C- and N-glycosidation reaction. The absolute configuration of these compounds was confirmed by comparison of their spectroscopic data with that reported for marmycin A, and by X-ray analysis.

A series of skeletal rearranged indolomorphinans 7a–d were obtained by N-demethylation of 3-methoxy-N-methyl-14-hydroxymorphinan-6-one 12 followed by N-realkylation, reduction and Fischer indole cyclization. The structure of the novel skeleton was confirmed by X-ray analysis. These new indoles displayed moderate binding affinity and selectivity at the μ receptor, with compound 7b showing the highest affinity at this receptor with a Ki value of 40 nM, and 6- and 25-fold selectivity against δ and κ receptors, respectively. Function assays showed that indolopropellanes 7b and 7c possessed full agonistic activity at all the opioid receptors indicating a different interaction model existed.

ATPM [(-)-3-amino-thiazolo[5,4-b]-N-cyclopropylmethylmorphinan hydrochloride] was found to have mixed kappa- and mu-opioid activity and identified to act as a full kappa-agonist and a partial mu-agonist by in vitro binding assays. The present study was undertaken to characterize its in vivo effects on morphine antinociceptive tolerance in mice and heroin self-administration in rats. ATPM was demonstrated to yield more potent antinociceptive effects than (-)U50,488H (trans-3,4-dichloro-N-methyl-N-[2-(1-pyrrolidinyl)cyclohexyl]benzeneacetamide). It was further found that the antinociceptive effects of ATPM were mediated by kappa- and mu-, but not delta-opioid, receptors. In addition to its agonist profile on the mu-receptor, ATPM also acted as a mu-antagonist, as measured by its inhibition of morphine-induced antinociception. It is more important that ATPM had a greater ratio of the ED(50) value of sedation to that of antinociception than (-)U50,488 (11.8 versus 3.7), indicative of a less sedative effect than (-)U50,488H. In addition, ATPM showed less potential to develop antinociceptive tolerance relative to (-)U50,488H and morphine. Moreover, it dose-dependently inhibited morphine-induced antinociceptive tolerance. Furthermore, it was found that chronic treatment of rats for 8 consecutive days with ATPM (0.5 mg/kg s.c.) produced sustained decreases in heroin self-administration. (-)U50,488H (2 mg/kg s.c.) also produced similar inhibitory effect. Taken together, our findings demonstrated that ATPM, a novel mixed kappa-agonist and mu-agonist/-antagonist, could inhibit morphine-induced antinociceptive tolerance, with less potential to develop tolerance and reduce heroin self-administration with less sedative effect. kappa-Agonists with some mu-activity appear to offer some advantages over selective kappa-agonists for the treatment of heroin abuse.

Herein, we reported a octahedral Cd3(C3N3S3)2 coordination polymer as a new noble metal-free photocatalyst for robust photocatalytic H2O2 production from methanol/water solution. The coordination polymer can give an unprecedented H2O2 yield of ca. 110.0 mmol • L−1 • g−1 at pH = 2.8 under visible light illumination. The characterization results clearly revealed that the photocatalytic H2O2 production proceeds by a pathway of two-electron reduction of O2 on the catalyst surface. This work showed the potential perspective of Mx(C3N3S3)y (M = transitional metals) coordination polymers as a series of new materials for solar energy storage and conversion.

To investigate the current cognition of occupational exposure to human immunodeficiency virus (HIV) and the personal occupational protection awareness in healthcare workers in Liuzhou, China.A total of 270 healthcare workers were selected from 10 hospitals in Liuzhou by stratified random sampling for a cross-sectional study. And a self-administered questionnaire of occupational exposure to HIV was designed to conduct a survey. The descriptive analysis of data was carried out by Excel. And a logistic regression analysis was done to analyze the effects of different factors on healthcare workers' cognition of occupational exposure to HIV using the statistical analysis software SPSS 19.0.A total of 260 usable questionnaires (96.3%) were returned. Among them, 220 healthcare workers (84.6%) had received the trainings on occupational exposure to HIV; 223 healthcare wofkers (85.8%) were aware of the rules and regulations on prevention of occupational exposure to HIV and the operation procedures in their hospitals. The healthcare workers who had not received the trainings or had not known the rules and regulations and the operation procedures were mainly from primary or secondary hospitals. A total of 106 healthcare workers (40.8%) had directly contacted patients' blood or body fluids; 154 healthcare workers (59.2%) were injured by sharp instruments, and most were hollow needle stick injuries (98/154, 63.6%). A total of 168 healthcare workers (68.08%) had better cognitive awareness of occupational exposure to HIV, and 76 healthcare workers (29.2%) had moderate cognitive awareness. Some healthcare workers had poor knowledge in the common sense of AIDS/HIV and occupational exposure to HIV, the personal protection awareness of occupational exposure, or the disposal measures after occupational exposure. The univariate analysis using chi-square test showed that occupation and professional title were significantly correlated with the cognition (P0.05). The multivariate logistic regression analysis showed that the doctors (OR3.8; P0.05), nurses (OR3.04, P0.05), and laboratory technicians (OR=9.51, P0.05) had better awareness compared with the others. The healthcare workers with a primary or lower professional title had poorer awareness compared with the healthcare workers with a higher professional title (OR=0.47, P0.05).Healthcare workers have the risk of occupational exposure to HIT. They do not have comprehensive and systematic knowledge related to occupational exposure to HIV, and they have a high demand for training.

Vaccines against drugs of abuse have induced antibodies in animals that blocked the biological effects of the drug by sequestering the drug in the blood and preventing it from crossing the blood-brain barrier. Drugs of abuse are too small to induce antibodies and, therefore, require conjugation of drug hapten analogs to a carrier protein. The efficacy of these conjugate vaccines depends on several factors including hapten design, coupling strategy, hapten density, carrier protein selection, and vaccine adjuvant. Previously, we have shown that 1 (MorHap), a heroin/morphine hapten, conjugated to tetanus toxoid (TT) and mixed with liposomes containing monophosphoryl lipid A [L(MPLA)] as adjuvant, partially blocked the antinociceptive effects of heroin in mice. Herein, we extended those findings; demonstrating greatly improved vaccine induced antinociceptive effects up to 3% mean maximal potential effect (%MPE). This was obtained by evaluating the effects of vaccine efficacy of hapten 1 vaccine conjugates with varying hapten densities using two different commonly used carrier proteins, TT and cross-reactive material 197 (CRM197). Immunization of mice with these conjugates mixed with L(MPLA) induced very high anti-1 IgG peak levels of 400 – 1,500 µg/mL that bound to both heroin and its metabolites, 6-acetylmorphine and morphine. Except for the lowest hapten density for each carrier, the antibody titers and affinity were independent of hapten density. The TT carrier based vaccines induced long-lived inhibition of heroin-induced antinociception that correlated with increasing hapten density. The best formulation contained TT with the highest hapten density of ≥30 haptens/TT molecule and induced %MPE of approximately 3% after heroin challenge. In contrast, the best formulation using CRM197 was with intermediate 1 densities (10–15 haptens/ CRM197 molecule), but the %MPE was approximately 13%. In addition, the chemical synthesis of 1; the optimization of the conjugation method; and the methods for the accurate quantification of hapten density are described.

This paper presented an improved analytical method for calculating the stator end-winding leakage inductance of water filling induction motor equipped with concentric twoplane end-winding. The improved analytical method was derived based on the stored magnetic energy. The physical model of the end region was established for calculating the end winding leakage inductance. In the improved analytical method, the active axial permeance factor was introduced for considering the leakage distributed in the active end region. Then three dimensional (3-D) time harmonic finite element analysis (FEA) was performed on a model with all end structures. The magnetic field distribution in the end region was explored and the distribution of the end-winding leakage inductances of the inner plane end windings and outer plane end windings was analyzed. The results of the analysis show that the end-winding leakage inductance decreases when the excitation frequency increases and the changes are nonlinear. Finally, the results obtained by the improved analytical method are compared with the results obtained by the 3-D time harmonic FEA.

Dopamine is a key regulator in the CNS, contributing importantly to functions of arousal and attention, initiation of movement, perception, motivation and emotion. Its imbalance has been implicated in the pathophysiology, and more clearly in the pharmacology, of a number of neurobehavioural disorders, including Parkinson’s disease, schizophrenia, mania and depression, alcohol and drug abuse, as well as attention and eating disorders. Five major dopamine receptor subtypes (D1 – D5) have been identified, with distinct differences in their genes and peptide composition, molecular functions and neuropharmacology. These receptors represent the rational targets for the treatment of a large number of neurological and psychiatric disorders. In recent years, substantial efforts have addressed the most recently described dopamine receptor types, particularly types D3, D4 and D5, although most research involves the longer-known D1 and D2 dopamine receptors. Current pharmacological efforts in medicinal chemistry and ...

Long circulation in blood, enhanced tumor accumulation and penetration, efficient cellular internalization and intracellular drug release are major challenges in the development of ideal anticancer drug delivery systems. Although several strategies have been reported to improve therapeutic efficacy, they mainly meet one or a few features which can not circumvent all the barriers. Here the stimuli-responsive zwitterionic nanogels were developed to overcome the sequential physiological barriers in cancer chemotherapy. The nanogels were constructed via a simple precipitation polymerization method by using temperature-sensitive monomer N-isopropylacrylamide (NIPAM) pH-responsive monomer methylallyl amine (MAA) and betaine-based zwitterionic monomer sulfobetaine methacrylate (SBMA) with in vivo anti-protein adsorption property as comonomers, and disulfide bonds-containing N, N'-bis(acryloyl) cystamine (BAC) as crosslinker. Volume phase transition temperature (VPTT) and surface charge of the prepared nanogels were precisely controlled by altering the feeding molar ratio of these comonomers. Remarkably, The nanogels possess ultra-pH sensitive hydrophilicity/hydrophobicity reversible property, in which the nanogels were hydrophilic in the blood (pH 7.4, 37 °C) for prolonged circulation, while they were rapidly switched to hydrophobic with similar size and surface charge at acidic tumor pH, resulting in enhanced tumor accumulation and penetration and strong internalization by normal cancer cells and CSCs. For efficient lysosomal escape and intracellular drug release, the nanogels were positively charged at lysosome pH, which allowed them to be transported into the cytosol where the loaded cargo DOX was released from the nanogels with the introduction of intracellular high GSH concentration to exert cytotoxicity. This study indicated that pH-dependent hydrophilicity/hydrophobicity-, surface charge-reversible and redox sensitive nanogels might be used as potential carriers for anticancer drugs, which provided a foundation for designing an effective drug delivery system for cancer therapy. Note: This abstract was not presented at the meeting. Citation Format: Hao Yang, Qin Wang, Fuying Li, Yanhong Zhu, Lu Gan, Xiangliang Yang. pH-regulated hydrophilicity/hydrophobicity-, surface charge-reversible and redox sensitive nanogels for anticancer drug delivery [abstract]. In: Proceedings of the American Association for Cancer Research Annual Meeting 2017; 2017 Apr 1-5; Washington, DC. Philadelphia (PA): AACR; Cancer Res 2017;77(13 Suppl):Abstract nr 3099. doi:10.1158/1538-7445.AM2017-3099

In this paper, a model of dry submersible motor with the static eccentricity was established to calculate the magnetic field and hysteresis loss. It is obvious that static eccentricity(SE) can affect the electromagnetic parameter. Therefore, the magnetic flux density of stator was researched based on Maxwell theory, including stator yoke and teeth. The faults of eccentricity can make the magnetic field intensity distorted according to the calculated results. Based on the iron loss separation model, the hysteresis loss was investigated both under normal and static eccentricity conditions. The comparison between the two conditions shows that hysteresis loss increased with the fault of static eccentricity. What's more, the conclusion can provide a method to detect the fault of air gap static eccentricity.

A taxonomic study was carried out on strain P73T, which was isolated from deep-sea sediment of the Indian Ocean by enrichment of polycyclic aromatic hydrocarbons. The strain was able to degrade biphenyl, naphthalene, 2-methylnaphthalene, 2,6-dimethylnaphthalene, acenaphthene, anthracene, phenanthrene, dibenzothiophene, dibenzofuran, fluorene, 4-methyldibenzothiophene and fluoranthene, but not pyrene or chrysene. Phylogenetic analysis based on 16S rRNA gene sequences showed that strain P73T formed a clade with the genera Celeribacter and Huaishuia within the family Rhodobacteraceae , with highest sequence similarity of 96.98 % to Celeribacter neptunius H 14T, followed by Huaishuia halophila ZXM137T (96.42 %). The bacterium was Gram-stain-negative, oxidase- and catalase-positive, rod-shaped and non-motile. Growth was observed at salinities from 0.5 to 12 % and at temperatures from 10 to 41 °C. The principal fatty acids (>10 %) of strain P73T were summed feature 8 (C18 : 1ω7c/ω6c) and C19 : 0ω8c cyclo. The sole respiratory quinone was Q-10. The major lipids were phosphatidylglycerol, one unknown aminolipid, one unknown phospholipid and one unknown lipid; a second unknown phospholipid and one unknown glycolipid were present as minor components. The G+C content of the chromosomal DNA was 66.0 mol%. The combined genotypic and phenotypic data show that strain P73T represents a novel species of the genus Celeribacter , for which the name Celeribacter indicus sp. nov. is proposed. The type strain is P73T ( = MCCC 1A01112T = LMG 27600T = DSM 27257T). Phylogenetic study and existing phenotypic information also show that Huaishuia halophila should be transferred to the genus Celeribacter as Celeribacter halophilus comb. nov. (type strain ZXM137T = MCCC 1A06432T = CGMCC 1.8891T = LMG 24854T).

We previously reported that the κ agonists with mixed μ activity could attenuate heroin self-administration with less potential to develop tolerance. The present study further investigated the effects of (-)-3-N-Ethylamino-thiazolo[5,4-b]-N-cyclopropylmethylmorphinan hydrochloride (ATPM-ET), a κ agonist and μ agonist/antagonist, on the acquisition and reinstatement of morphine-induced conditioned place preference (CPP), heroin self-administration and heroin-primed reinstatement of drug-seeking behavior. We found that ATPM-ET produced a longer duration of potent antinociceptive effects with less side effect of sedation. More importantly, ATPM-ET attenuated the acquisition of morphine-induced CPP, without affecting the reinstatement of morphine CPP. Furthermore, ATPM-ET significantly inhibited heroin self-administration and the reinstatement of heroin primed drug-seeking behavior. Taken together, ATPM-ET, a novel κ agonist and μ agonist/antagonist may have utility for the treatment of drug dependence.

A taxonomic study was carried out on strain D104(T), which was isolated from deep-sea subsurface sediment sample from the Arctic Ocean. The bacterium was found to be Gram-negative, oxidase negative and catalase weakly positive, rod shaped, motile by means of polar flagellum. The organism grows between 4 and 37 °C (optimum 25-28 °C) and 0.5-6 % NaCl (optimum 3 %). Phylogenetic analysis based on 16S rRNA gene sequences indicated that strain D104(T) belongs to the genus Marinomonas, with highest sequence similarities of 97.7 % to Marinomonas ushuaiensis DSM 15871(T), followed by M. dokdonensis DSW10-10(T) (96.9 %), M. arenicola KMM 3893(T) (96.7 %), M. arctica 328(T) (96.6 %) and other 18 species of the genus Marinomonas (94.4-96.5 %). The average nucleotide identity and estimated DNA-DNA hybridization values between strain D104(T) and M. ushuaiensis DSM 15871(T) were 84.24 % and 20.80 ± 2.33 % respectively. The principal fatty acids were C16:0, sum in feature 3 (C16:1 ω7c/C16:1 ω6c), sum in feature 8 (C18:1 ω7c/C18:1 ω6c) and C12:1 3OH. The G + C content of the chromosomal DNA was determined to be 44.8 mol%. The respiratory quinone was found to be Q8 (100 %). Polar lipids include phosphatidylglycerol and phosphatidylethanolamine as major phospholipids and aminolipid and phospholipid as minor components. The results of the genotypic and phenotypic analyses indicate that strain D104(T) represents a novel species of the genus Marinomonas, for which the name Marinomonas profundimaris sp. nov. is proposed, with the type strain D104(T) (=MCCC 1A07573(T) = LMG 27696(T)).

In rotor-bearing system of large submersible motor, many factors contribute to the generation of harmonics. This paper theoretically analyzes some factors and makes certain hypothesis. Rotor dynamics calculation model of large horizontal submersible motors is built. The phenomenon of harmonic resonance around the sub-critical speed is verified using finite element method, and the stress and displacement of bearing and rotor iron core are obtained. Finally, the resonance phenomenon which occurs at rated speed, due to the influence of harmonic and the change of sub-critical speed, can result in motor fault. The investigation in this paper supports references in the fault diagnosis and bearing selection in large horizontal submersible motors.

Oxide-bridged phenylmorphans were conceptualized as topologically distinct, structurally rigid ligands with 3-dimensional shapes that could not be appreciably modified on interaction with opioid receptors. An enantiomer of the N-phenethyl-substituted ortho-f isomer was found to have high affinity for the μ-receptor (Ki = 7 nM) and was about four times more potent than naloxone as an antagonist. In order to examine the effect of introduction of a small amount of flexibility into these molecules, we have replaced the rigid 5-membered oxide ring with a more flexible 6-membered carbon ring. Synthesis of the new N-phenethyl-substituted tricyclic N-substituted-2,3,4,9,10,10a-hexahydro-1H-1,4a-(epiminoethano)phenanthren-6- and 8-ols resulted in a two carbon-bridged relative of the f-isomers, the dihydrofuran ring was replaced by a cyclohexene ring. The carbocyclic compounds had much higher affinity and greater selectivity for the μ-receptor than the f-oxide-bridged phenylmorphans. They were also much more potent μ-antagonists, with activities comparable to naltrexone in the [35S]GTP-γ-S assay.

Both exogenous and endogenous cannabinoids can allosterically modulate glycine receptors (GlyRs). However, little is known about the molecular basis of cannabinoid-GlyR interactions. Here we report that sustained incubation with the endocannabinoid anandamide (AEA) substantially increased the amplitude of glycine-activated current in both rat cultured spinal neurons and in HEK-293 cells expressing human α1, rat α2 and α3 GlyRs. While the α1 and α3 subunits were highly sensitive to AEA-induced potentiation, the α2 subunit was relatively insensitive to AEA. Switching a serine at 296 and 307 in the TM3 (transmembrane domain 3) of the α1 and α3 subunits with an alanine (A) at the equivalent position in the α2 subunit converted the α1/α3 AEA-sensitive receptors to sensitivity resembling that of α2. The S296 residue is also critical for exogenous cannabinoid-induced potentiation ofIGly. The magnitude of AEA potentiation decreased with removal of either the hydroxyl or oxygen groups on AEA. While desoxy-AEA was significantly less efficacious in potentiatingIGly, desoxy-AEA inhibited potentiation produced by both Δ9-tetrahydrocannabinol (THC), a major psychoactive component of marijuana, and AEA. Similarly, didesoxy-THC, a modified THC with removal of both hydroxyl/oxygen groups, did not affectIGlywhen applied alone but inhibited the potentiation ofIGlyinduced by AEA and THC. These findings suggest that exogenous and endogenous cannabinoids potentiate GlyRs via a hydrogen bonding-like interaction. Such a specific interaction likely stems from a common molecular basis involving the S296 residue in the TM3 of the α1 and α3 subunits.

A taxonomic study was carried out on strain P1T, which was isolated from mangrove sediment samples collected from Qinglan Port (Hainan, China). Cells were curved rods, that were motile, with a single polar flagellum. The strain was non-spore-forming with a cell size of 0.6×1.5–2.2 µm. Catalase and oxidase activities were not detected. Growth was observed in the temperature range 22–44 °C (optimum, 35–40 °C) and pH range 5.5–8.5 (optimum, pH 7.0). NaCl was required for growth and tolerated at up to 3.5 % (w/v) (optimum, 0.5 %). Strain P1Tutilized hydrogen, succinate,l-malate, citrate, oxalate,dl-lactate, pyruvate, or cysteine as electron donors, and sulfate or sulfite as electron acceptors. Fermentation products from pyruvate were acetate, H2and CO2. Phylogenetic analyses based on 16S rRNA gene sequences showed that strain P1Tformed a distinct evolutionary lineage within the familyDesulfovibrionaceae. Strain P1Twas most closely related to members of the generaDesulfovibrio(92.0–94.3 % 16S rRNA gene sequence similarity),Desulfocurvus(91.1 %),Bilophila(87.9 %) andLawsonia(86.0 %) of the familyDesulfovibrionaceae. The DNA G+C content of strain P1Twas 64.5 mol% and the major cellular fatty acids were iso-C15 : 0(18.8 %), anteiso-C15 : 0(5.0 %), C16 : 0(14.2 %) and iso-C17 : 1ω9c(24.4 %). The predominant menaquinone was MK-7 (97 %). Major polar lipids were phosphatidylcholine, phosphatidylethanolamine and phosphatidylglycerol. Strain P1Twas distinguishable from members of phylogenetically related genera by differences in several phenotypic properties. On the basis of the phenotypic and phylogenetic data, strain P1Trepresents a novel species of a new genus, for which the nameDesulfobaculum xiamenensisgen. nov., sp. nov. is proposed. The type strain ofDesulfobaculum xiamenensisis P1T( = CGMCC 1.5166T = DSM 24233T).

A novel alkylsulfatase gene, sdsAP, was cloned from a newly isolated bacterium Pseudomonas sp. S9. It encoded a protein of 675 amino acids with a calculated molecular mass of 74.9 kDa. The protein contained a typical N-terminal signal peptide of 41 amino acid residues, followed by a metallo-β-lactamase like domain at the N-terminus and a SCP-2-like domain at the C-terminus. This domain organization mode suggested that it belonged to the type III sulfatase. The mature alkylsulfatase was overexpressed in Escherichia coli. The optimal temperature and pH of the recombinant SdsAP were 70°C and 9.0, respectively. Notably, at optimal conditions, the purified recombinant SdsAP had a high specific activity of 23.25 μmol min(-1) mg(-1), a K(m (app)) of 264.3 μmol, and a V(max (app)) of 33.8 μmol min(-1) mg(-1) for SDS. Additionally, it still retained more than 90% activity after incubation at 65°C for 1 h, which was much different from other alkylsulfatases reported. The recombinant enzyme hydrolyzed the primary alkyl sulfate such as sodium octyl sulfate and sodium dodecyl sulfate (SDS). It was a Zn(2+)-containing and Ca(2+) activated alkylsulfatase. This is the first report to explore the various characteristics of the heterologous recombinant alkylsulfatase in details. These favorable properties could make SdsAP attractive to be useful in the degradation of SDS-containing waste.

The enantioselective hydrogenation of a series of challenging substrates, α-aryl-β-substituted acrylic acids, was realized with high efficiency and enantioselectivity (up to 96%) under the catalysis of Ir(I) complex of Spiro-based P,N ligand, SpinPHOX.

A series of N-thiazole substituted arylacetamides were designed on the basis of metabolic mechanism of the aminothiazole fragment as glucokinase (GK) activators for the treatment of type 2 diabetes. Instead of introducing a substituent to block the metabolic sensitive C-5 position on the thiazole core directly, a wide variety of C-4 or both C-4 and C-5 substitutions were explored. Compound R-9k bearing an iso-propyl group as the C-4 substituent was found possessing the highest GK activation potency with an EC(50) of 0.026microM. This compound significantly increased both glucose uptake and glycogen synthesis in rat primary cultured hepatocytes. Moreover, single oral administration of compound R-9k exerted significant reduction of blood glucose levels in both ICR and ob/ob mice. These promising results indicated that compound R-9k is a potent orally active GK activator, and is warranted for further investigation as a new anti-diabetic treatment.

A passive sub-ring was inserted into a semiconductor fiber-ring laser as the Vernier configuration to enable stable lasing spectrum. Wavelength tuning over 20 nm and fine tuning of less than 0.0001 nm were obtained by rotating the polarization controller and adjusting the voltage on the phase modulator, respectively. A narrow linewidth of less than 10 kHz and a sidemode suppression ratio of higher than 35 dB were demonstrated with single longitudinal-mode operation.

The enantioselective hydrogenation of a series of challenging substrates, alpha-aryl-beta-substituted acrylic acids, was realized with high efficiency and enantioselectivity (up to 96%) under the catalysis of Ir(i) complex of Spiro-based P,N ligand, SpinPHOX.

The 16S rRNA genes of Ruegeria pelagia NBRC 102038T and Ruegeria mobilis NBRC 101030T were resequenced and the results confirmed that they differ by only one base in their almost full-length sequences (1425 nt). The gyrB gene sequence similarity between the two strains was also high (97.7 %). The outcome of API 20NE, API ZYM and antibiotic susceptibility tests showed that the two strains show only one difference, in β-galactosidase activity, in API tests and five differences in susceptibility among 30 tested antibiotics. In addition, similar BOX-PCR fingerprints were obtained and the DNA–DNA relatedness between the two strains was 91±4 %. On the basis of these results, it is concluded that Ruegeria pelagia Lee et al. 2007 is a later heterotypic synonym of Ruegeria mobilis Muramatsu et al. 2007.

Mono- and bis-indolomorphinans were synthesized through a multi-step synthetic approach from the alkaloid, thebaine, to further explore the C-ring SAR (structure-activity relationship) of morphinan scaffold. Both mono-indoles displayed good binding affinity and selectivity for the delta receptor, with compound 6b possessed the highest K(i) value of 1.45 nm at this receptor. Bisindolomorphinans 7a,b did not have appreciable affinity for both delta and kappa receptors, but moderate binding at the mu receptor was observed. Functional assays indicated that the newly synthesized mono-indole 6b was delta-agonist, opposite to the delta-antagonist profile of naltrindole. Bisindoles 7a,b were mu-agonists. This work further confirms that the phenol component in opioids is essential for higher binding to the opioid receptors. The different binding ability, receptor selectivity, and the functional activity profiles of naltrindole 2, monoindole 6b, and bisindole 7b clearly indicated that they interact with the opioid receptors in different modes.

To further extend the structure-activity relationships of levorphanol, two series of novel morphinans were prepared by incorporation of an indole or aminothiazole fragment to the hexyl ring (ring C) in levorphanol. Such morphinans differed from previously reported ligands in that such indole- or aminothiazole-containing morphinans displayed enhanced binding affinity to the delta opioid receptor, while the affinity to kappa and micro receptors was slightly reduced.

s / Drug and Alcohol Dependence 156 (2015) e102–e182 e143 Hapten selection for heroin vaccines Gary R. Matyas2, Fuying Li1,3, Joshua Antoline1,3, Rashmi Jalah4, Oscar Torres4, Zoltan Beck4, Arthur Jacobson1,3, Carl Alving2, Kenner Rice1,3 1 Drug Design and Synthesis Section, National Institute on Drug Abuse, NIH, Bethesda, MD, United States 2 US Military HIV Research Program, Walter Reed Army Institute of Research, Silver Spring, MD, United States 3 National Institute on Alcohol Abuse and Alcoholism, NIH, Bethesda, MD, United States 4 US Military HIV Research Program, Herny M. Jackson Foundation for the Advancement of Military Medicine, Bethesda, MD, United States Aims: The aim of this study is to select a heroin hapten for a heroin vaccine. Heroin rapidly degrades to 6-acetylmophine and morphine after injection. We hypothesize that a heroin hapten can bedesigned that is chemically stable and can induce antibodies that bind to heroin and its metabolites. Methods: Seven different opioid haptens were synthesized. A mercaptopropanamide group was attached as the linker at the C3, C6or thebridgenitrogen. The acetyl groups of heroinwere replaced with acetamide or 2-oxypropyl groups. The haptens were attached to tetanus toxoid and mixed with liposomal lipid A. Mice were immunized with 3 doses every 3 weeks. The sera were assayed for hapten antibodies. The mice were challenged by the subcutaneous route with heroin (0.75–1mg/kg) and efficacy was assessed by nociception assays. Results: Anti-hapten titers ranged from 100,000 to 6,000,000. Mice immunizedwith haptens coupled at the bridge nitrogenwere only partially protected with a % maximal potential effect (%MPE) ≥50. Animals immunized with C3 position haptens were not challengeddue to lowantibody titers.Mice immunizedwith a C6 linked morphine hapten (MorHap) had a %MPE of 35. After optimization of the MorHap conjugation procedure, the %MPE was

To investigate the expression of interleukin 18 (IL-18) in intestinal mucosa of patients with inflammatory bowel disease (IBD) and its relation with disease active state.IL-18mRNA transcripts were evaluated by using a semiquantitative RT-PCR protocol. Specimens of 23 Crohn's disease (CD) and 20 ulcerative colitis (UC) patients and 20 controls were studied by immunohistochemical staining.Transcripts of IL-18 were found to be increased significantly in intestinal mucosa from active CD compared with UC and control. Immunohistochemical staining analysis localized the expression of IL-18 to intestinal epithelial cells and lamina propria (macrophages and dendritic cells, mainly). Staining was more intense in active CD compared with UC and control. Both transcriptions and staining of IL-18 in active UC were elevated, but there was no significant difference compared with control. Expression of IL-18 decreased in inactive CD (n = 9) or UC (n = 11) compared with active state of the same patients, and the difference in CD had significance.IL-18 may be involved in the pathogenesis of IBD and related with CD activity.

A re-entrant fiber optic gyro (RE-FOG) that utilizes a ring resonator (RR) and a low-coherence length light source is designed and demonstrated. A reflector is placed on one end of input/output directional coupler to realize light beams propagating in CW and CCW directions. RE-FOG promises a higher sensitivity than the conventional Sagnac interferometer fiber optic gyro (I-FOG) without the disadvantages of a resonant fiber optic gyro (R-FOG). Theoretical considerations of the sensitivity and the resolution of RE-FOG are discussed. Experimental results (the constant bias of 0.2 deg/h and the variance of random drift rate better than 0.1 deg/h) are also presented.

This paper reports the experimental results of PM-fiber ring resonator in resonator fiber optic gyroscope by our group in Tsinghua University. Adopting the PANDA-type and tied-type PM-fiber, the ring resonators about 12 meters length were fabricated according to the optimized parameters. Using a PZT modulator, the resonance curves and characteristics were recorded and analyzed. A Nd-YAG laser and a laser diode with fiber grating joined the system separately. Both of the lasers' linewidth is less than 200KHz and output power from fiber pigtail is more than 4 mW. We used two miniaturized bulked TiO2 crystal acousto-optical modulators as the frequency shifters of the clockwise wave and counterclockwise wave light. The experimental results were also presented.© (1998) COPYRIGHT SPIE--The International Society for Optical Engineering. Downloading of the abstract is permitted for personal use only.