Photo-induced Coupling Reaction of 1,1-Diphenyl-2,2-dicyanoethylene with 10-Methyl-9,10-dihydroacridine

Diphenyl-2, 2-dicyanoethylene reacts with 10-methyl-9, 10-dihydroacridine in deaerated acetonitrile under irradiation with l>320 nm to give the coupling product 1, 1-diphenyl-1-(10-methyl-9-acridinyl)-2, 2-dicyanoethane, which has been characterized by X-ray crystallographic, MS and NMR analyses.

SYNTHESIS OF 3,4-DIPHENYL-1.3,4-DIAZAPHOSPHOLID1N-2-ONE-4-OXIDE BY MANNICH-TYPE REACTION

Phenylurea reacted with dichlorophenylphosphine and aldehydes or ketones by Mannich-type reaction in anhydrous benzene to give five-mem- bered phosphorous heterocyclic compounds.However.derivatives of α-ureidoalkylphosphonic acids were obtained as the reaction performed in glacial acetic acid.

Genome-wide association mapping of vitamins B1 and B2 in common wheat

Vitamin B is essential for maintaining normal life activities in humans and animals who have to intake the microelement from the outside, especially from cereal products. In the present study 166 Chinese and foreign wheat cultivars planted in two environments were characterized for variation in vitamin B1 and B2 contents. A genome-wide association study(GWAS) using the wheat 90 K SNP assay identified 17 loci for vitamin B1 and 7 for vitamin B2 contents. Linear regression analysis showed a significantly positive correlation of the number of favorable alleles with vitamin B1 and B2 contents. Marker-trait associations(MTAs) at IWB43809(6AS, 0cM) and IWB69903(6AS, 13cM) were new and stable, and significantly associated with vitamin B1 content across two environments. The loci identified in this study and associated SNP markers could be used for improvement of vitamin B1 and B2 contents to obtain superior quality along with grain yield in wheat.

Synthesis and Crystal Structure of 1,2-Dis(1,3-diphenylpropan-2-yl)disulfane

A novel compound of 1,2-dis（1,3-diphenylpropan-2-yl）disulfane（C30H30S2,Mr=454.27）was synthesized in ethanol with 1,3-diphenyl-2-propanone as raw materials,giving high yield of product（90%）.Its structure was determined by IR,1H NMR,MS,elemental analysis and X-ray diffraction.The crystal belongs to monoclinic,space group C2 with a=18.727（3）,b=6.5179（9）,c=13.7576（18）,β=131.0610（10）o,V=1266.2（3）3,Z=2,Dc=2.136 g/cm3,μ=1.078 mm-1,F（000）=843,R=0.0490 and wR=0.1247 for 3211 observed reflections with I2（I）.X-ray analysis reveals that the molecule is not symmetrical.There exist no classical hydrogen bonds andπ-πstacking interactions.Moreover,the thermal stability of compound 3 was investigated.

Global hypomethylation in hepatocellular carcinoma and its relationship to aflatoxin B_1 exposure

AIM:To determine global DNA methylation in paired hepatocellular carcinoma(HCC) samples using several different assays and explore the correlations between hypomethylation and clinical parameters and biomarkers,including that of aflatoxin B 1 exposure.METHODS:Using the radio labeled methyl acceptance assay as a measure of global hypomethylation,as well as two repetitive elements,including satellite 2(Sat2) by MethyLight and long interspersed nucleotide elements(LINE1),by pyrosequencing.RESULTS:By all three assays,mean methylation levels in tumor tissues were significantly lower than that in adjacent tissues.Methyl acceptance assay log(mean ± SD) disintegrations/min/ng DNA are 70.0 ± 54.8 and 32.4 ± 15.6,respectively,P = 0.040;percent methylation of Sat2 42.2 ± 55.1 and 117.9 ± 88.8,respectively,P < 0.0001 and percent methylation LINE1 48.6 ± 14.8 and 71.7 ± 1.4,respectively,P < 0.0001.Aflatoxin B 1 albumin(AFB 1-Alb) adducts,a measure of exposure to this dietary carcinogen,were inversely correlated with LINE1 methylation(r =-0.36,P = 0.034).CONCLUSION:Consistent hypomethylation in tumor compared to adjacent tissue was found by the three different methods.AFB 1 exposure is associated with DNA global hypomethylation,suggesting that chemical carcinogens may influence epigenetic changes in humans.

Estrogen affects neuropathic pain through upregulating N-methyl-D-aspartate acid receptor 1 expression in the dorsal root ganglion of rats

Estrogen affects the generation and transmission of neuropathic pain,but the specific regulatory mechanism is still unclear.Activation of the N-methyl-D-aspartate acid receptor 1（NMDAR1） plays an important role in the production and maintenance of hyperalgesia and allodynia.The present study was conducted to determine whether a relationship exists between estrogen and NMDAR1 in peripheral nerve pain.A chronic sciatic nerve constriction injury model of chronic neuropathic pain was established in rats.These rats were then subcutaneously injected with 17β-estradiol,the NMDAR1 antagonist D（-）-2-amino-5-phosphonopentanoic acid（AP-5）,or both once daily for 15 days.Compared with injured drug na？ve rats,rats with chronic sciatic nerve injury that were administered estradiol showed a lower paw withdrawal mechanical threshold and a shorter paw withdrawal thermal latency,indicating increased sensitivity to mechanical and thermal pain.Estrogen administration was also associated with increased expression of NMDAR1 immunoreactivity（as assessed by immunohistochemistry） and protein（as determined by western blot assay） in spinal dorsal root ganglia.This 17β-estradiol-induced increase in NMDAR1 expression was blocked by co-administration with AP-5,whereas AP-5 alone did not affect NMDAR1 expression.These results suggest that 17β-estradiol administration significantly reduced mechanical and thermal pain thresholds in rats with chronic constriction of the sciatic nerve,and that the mechanism for this increased sensitivity may be related to the upregulation of NMDAR1 expression in dorsal root ganglia.

Effect of sericin on diabetic hippocampal growth hormone/insulin-like growth factor 1 axis

Previous studies have shown that sericin extracted from silk cocoon significantly reduces blood glucose levels and protects the nervous system against diabetes mellitus. In this study, a rat type 2 diabetes mellitus model was established by intraperitoneal injection of 25 mg/kg streptozotocin for 3 successive days, following which the rats were treated with sericin for 35 days. After treatment, the blood glucose levels of the diabetic rats decreased significantly, the growth hormone level in serum and its expression in the hippocampus decreased significantly, while the insulin-like growth factor-1 level in serum and insulin-like growth factor-1 and growth hormone receptor expression in the hippocampus increased significantly. The experimental findings indicate that sericin improves disorders of the growth hormone/insulin-like growth factor 1 axis to alleviate hippocampal damage in diabetic rats.

Imbalance of matrix metalloproteinase-9 and matrix metalloproteinase tissue inhibitor-1 may contribute to hemorrhage in cerebellar arteriovenous malformations

In this study, we determined the expression levels of matrix metalloproteinase-2 and -9 and matrix metalloproteinase tissue inhibitor-1 and -2 in brain tissues and blood plasma of patients undergoing surgery for cerebellar arteriovenous malformations or primary epilepsy （control group）. Immunohistochemistry and enzyme-linked immunosorbent assay revealed that the expression of matrix metalloproteinase-9 and matrix metalloproteinase tissue inhibitor-1 was significantly higher in patients with cerebellar arteriovenous malformations than in patients with primary epilepsy. The ratio of matrix metalloproteinase-9 to matrix metalloproteinase tissue inhibitor-1 was significantly higher in patients with hemorrhagic cerebellar arteriovenous malformations compared with those with non-hemorrhagic malformations. Matrix metalloproteinase-2 and matrix metalloproteinase tissue inhibitor-2 levels were not significantly changed. These findings indicate that an imbalance of matrix metalloproteinase-9 and matrix metalloproteinase tissue inhibitor-I, resulting in a relative overabundance of matrix metalloproteinase-9, might be the underlying mechanism of hemorrhage of cerebellar arteriovenous malformations.

Antioxidant Activity Evaluation in a Series of Heterocyclic Compounds Derived from 1,8-Diaminonaphthalene

From (2,3-dihydro-1H-perimidin-2-yl)-phenyl, the substitution of OH group in ortho or para position on the phenyl ring, allows us to synthesize the studied compounds. These three compounds have been characterized by conventional spectroscopic methods (NMR and MS). The interest of this work is to review the antioxidant activity of our compounds. The antioxidant activity screening carried out according to FRAP and DPPH methods revealed significant anti-free radical properties for compounds 1 and 2 even at low concentrations. In contrast to the compound 2, compound 3 for which the OH group is substituted in para position has the lowest activity in both cases. Therefore the para position seems to be the least sensitive position to increase the antioxidant activity of this pharmacophore.

An In Vitro and In Vivo Study of Thyroid Disruption of 1,2-Bis(2,4,6-tribromophenoxy)ethane(BTBPE)�A Novel Brominated Flame Retardant

The novel brominated flame retardant,1,2-bis-(2,4,6-tribromophenoxy)ethane(BTBPE),is an emerging environ-mental pollutant with undetermined toxicity.We investigated how BTBPE causes thyroid endocrine disruption with integrated in silico,in vitro,and in vivo assays.In yeast two-hybrid and T-Screen assays,BTBPE interacted with zebrafish thyroid hormone receptors with binding energies weaker than the TR agonist-3,3′,5-Triiodo-L-thyronine(T3),and disrupted thyroid function as a thyroid receptor(TR)agonist.We examined the bioconcentra-tion,developmental toxicity,and thyroid endocrine disruption in zebrafish after a 14-day exposure to BTBPE(1,3,10μg/L).Thyroxine(T4)was lower in BTBPE-treated larvae,whereas corticotropin-releasing hormone(CRH)and thyroid-stimulating hormone(TSH)were higher.The gene transcription alterations along the hypothalamic-pituitary-thyroid(HPT)axis were observed.Furthermore,reduced locomotion suggested that BTBPE imparts developmental neurotoxicity at zebrafish early developmental stage.Establishing that BTBPE has thyroid endocrine-disrupting effects is an important step for understanding and managing BTBPE toxicity.

Morphology Control over the Organic Nanoparticles of 1,3-Diphenyl-5-(9-anthryl)-2-pyrazoline

The organic nanoparticles of a blue-light-emitting molecule,1,3-diphenyl-5-(9-anthryl)-2-pyrazoline,were prepared by reprecipitation method using acetonitrile as the solvent for the molecular precursor. Three morphologies,spherical,doughnut-shaped and cubic,could be observed on the silicon substrate for the nanoparticles by the volume-controlled addition of acetonitrile. The evolution of particle morphology as a function of acetonitrile addition was attributed to the variation of the growth habits of the particles in the different environment. The nanoparticles exhibit the novel photoluminescence spectra as compared to those of monomer and the bulk crystals.

Rat cardiomyocyte H9c2(2-1)-based sulforhodamine B assay as a promising in vitro method to assess the biological component of effluent toxicity

The treatment of wastewaters is crucial to maintain the ecological status of receiving waters,and thereby guarantee the protection of aquatic life and human health.Wastewater quality evaluation is conventionally based on physicochemical parameters,but increasing attention has been paid to integrate physicochemical and biological data.Nevertheless,the regulatory use of fish in biological testing methods has been subject to various ethical and cost concerns,and in vitro cell-based assays have thus become an important topic of interest.Hence,the present study intends:(a) to evaluate the efficiency of two different sample pre-concentration techniques (lyophilisation and solid phase extraction) to assess the toxicity of municipal effluents on rat cardiomyoblast H9c2(2-1) cells,and (b) maximizing the use of the effluent sample collected,to estimate the environmental condition of the receiving environment.The gathered results demonstrate that the H9c2(2-1) sulforhodamine B-based assay is an appropriate in vitro method to assess biological effluent toxicity,and the best results were attained by lyophilising the sample as pre-treatment.Due to its response,the H9c2(2-1) cell line might be a possible alternative in vitro model for fish lethal testing to assess the toxicity of municipal effluents.The physicochemical status of the sample suggests a high potential for eutrophication,and iron exceeded the permissible level for wastewater discharge,possibly due to the addition of ferric chloride for wastewater treatment.In general,the levels of carbamazepine and sulfamethoxazole are higher than those reported for other countries,and both surpassed the aquatic protective values for long-term exposure.

Decline in the expression of IL-2 after trauma and changes in the nuclear transcription factors NFAT and AP-1

OBJECTIVE: To investigate whether the decrease in expression of interleukin-2 (IL-2) after trauma is associated with changes in DNA binding activity of nuclear factor of activated T cells (NFAT) and activator protein-1 (AP-1). METHODS: Mice with closed impact injury with fracture in both hind limbs were adopted as the trauma model. Spleen lymphocytes were isolated from traumatized mice and stimulated with Con-A. Culture supernatants were assayed for IL-2 activity, and total RNA was extracted from spleen lymphocytes and assayed for IL-2 mRNA. DNA binding activity of NFAT and AP-1 were measured by electrophoretic mobility shift assay (EMSA). The expression of c-Fos, c-Jun and JunB proteins was determined by the Western blot analysis. RESULTS: DNA binding activity of NFAT and AP-1 gradually decreased to a minimum of 41% and 49%, respectively, of the control on the 4th day after injury, which was closely followed by the decline in IL-2 activity and IL-2 mRNA. A decrease in the expression of c-Fos on the 1st and 4th day after trauma had no significant effect on c-Jun expression; the increase in expression of JunB was only on the 1st day after injury. CONCLUSION: Decreased IL-2 expression is, at least in part, due to a decline in the activation of NFAT and AP-1 in traumatized mice. The decline in DNA binding activity of NFAT and AP-1 is partly due to a trauma-induced block in the expression of c-Fos.

Synthesis of 3,3,5,5-tetrabenzyl-1,2,4-trithiol and 1,2-dis(1,3-arylpropan-2-yl)disulfane

Novel sulfur-containing compounds （3a-3c, 4a-4c） were obtained in ethanol with 1,3-diphenyl-2- propanone as the starting material. The advantages of this procedure were mild reaction conditions, simple protocol, and high yields. The structures of the products were characterized by IR, 1H NMR, MS and elementary analysis. The crystal of the new compound 4a belongs to monoclinic, space group C2 with a=18.727（3）, b=6.5179（9）, c=13.7576（18） A, fl=131.0610（10）°, V=I266.2（3）A3, Z=2, Dc=2.136g/cm3, μ=1.078mm 1, F（000）=843, R=0.0490 and wR=0.1247 for 3211 observed reflection with I 〉 2σ（I）. X-ray analysis reveals that the molecule is not symmetrical, the molecular structure is stabilized by weak π-π stacking interactions, and no classical hydrogen bonds can be observed.

The Application of Novel Electrochemical Approach to Antioxidant Activity Assay of Metal Porphyrins with Bulky 3,5-Diisobornyl-4-hydroxyphenyl Moieties

The complexes of biogenic metals (Zn2+,Cu2+,Co2+,Mn3+,Fe3+) based on meso-tetra(3,5-diisobor- nyl-4-hydroxyphenyl)porphyrin 1 were synthesized. The electrochemical behavior of these com-pounds was studied using cyclic voltammetry (CV) and rotating disk electrode (RDE) techniques. The antioxidant activity of complexes was estimated by means of the electrochemical assay based on the hydrogen atom transfer reaction to the stable radical 2,2’-diphenyl-1-picrylhydrazyl (DPPH). The RDE method was applied for this process monitoring. It was shown that the efficiency of the metal complexes (Cu2+,Co2+,Mn2+,Ni2+,Fe3+) is practically the same order as that of free base porphyrin 1. However the Zn2+ complex demonstrates significantly higher antioxidant activity, and the stoichiometry of the reaction was determined as σ = 4. The results demonstrate that porphyrin macrocycle can directly affect the antioxidant properties of 2,6-diisobornylphenol.

后发酵过程中乙醇对豆豉抗氧化能力的影响

以黄豆为原材料,接种米曲霉制作豆豉,在豆豉后发酵过程中设定了不同乙醇添加量,测定了不同乙醇添加量的豆豉样品清除DPPH(2,2-diphenyl-1-picrylhydrazyl hydrate)及ABTS[2,2-’azinobis-(3-ethylbenzthia-zoline-6-sulfonic acid)]自由基能力、Fe2+螯合能力、还原能力,评价了乙醇对豆豉抗氧化能力的影响。后发酵过程中,豆豉的抗氧化能力持续增大,醇对豆豉的抗氧化能力有影响,发酵相同时间的豆豉,抗氧化能力随乙醇含量的增大而下降。

Synthesis of a New β-Mercaptoalcohol

In this letter, (R)-1,1-diphenyl-2-mercapto-3-methyl-1-butanol was synthesized from L-valine and two synthetic routes have been tried.

A Comparative Study of Antioxidant Activities between Fresh and Dry Mushrooms in the Genera <i>Cantharellus</i>and <i>Afrocantharellus</i>from Tanzania

Cantharellus and Afrocantharellus mushrooms are widely consumed in both fresh and dry forms. However, their antioxidant and whether their values changing with drying processes are not known. This study establishes their values and the effect of sun drying on their quality and quantity. Methanolic extracts of five Cantharellus and two Afrocantharellus species were investigated. The investigation used (1,1-diphenyl-2-picrylhydrazyl radical) DPPH as a substrate to determine radical scavenging abilities. Further quantitative analyses for carotenoids, flavonoid, total phenolic compounds and vitamin C content were done using spectrophotometric assay at 515 nm. Comparatively, fresh mushroom had higher vitamin C and Lycopene contents than their dry counterparts with β-carotene. Flavonoid and phenolic compounds were higher in dry forms than those in their fresh counterparts. Radical scavenging ability also varied with fresh forms depicting higher activity compared to dry forms. The variation was low in Afrocantharellus species (0.8% and 0.99%) while it was higher in Cantharellus species (24.12% and 7.52%). The highest ability was observed in fresh forms of Cantharellus pseudocibarius (EC50 50 = 0.4 mg/ml) was from dry form of Cantharellus rufopunctatus. This shows that studied mushrooms are rich in antioxidants and their quality and quantities are affected differently in both forms. Both dry and fresh mushrooms are potential sources of natural antioxidants. The portrayed high scavenging ability by these mushrooms envisages promoting them into potential nutraceutics.

Effect of Induced Mutation on Antioxidant Activity in Ocimum basilicum Linn

Five batches from the same stock of seeds of Ocimum basilicum were irradiated at 5, 10, 15, 20 and 25 Gy, respectively using 60C source. Methanolic leaf extracts of these samples and a control were evaluated for their antioxidant activity by the 1,1-diphenyl-2-picryl-hydrazyl (DPPH) free radical scavenging method using M2 plants. All the methanolic extracts showed antioxidant activity. The IC50 of the methanolic extracts of the six different treatments, control, 5 Gy, 10 Gy, 15 Gy, 20 Gy and 25 Gy, showed antioxidant activity with IC50 values of 100, 90, 86, 61, 71 and 70 μg/ml, respectively. Three individual mutants, M-15-5, M-20-6 and M-15-4, had IC50 values of 26, 30 and 40 μg/ml, respectively. These mutants were from the 15 Gy and 20 Gy treatments. From the results, it is confirmed that induced mutation can be employed to create variation in the levels of free radical scavenging activity in O. basilicum and can therefore serve as a tool for breeding for high levels of antioxidant activity in O. basilicum.

In vitro antioxidant activities of ethanol extract from Enhalus acoroides (L.F.) Royle

Objective:To search for new sources of safe and inexpensive antioxidants,the leaf,root and rhizome of Enhalus acoroides(E.acoroides) were screened for the first time for their antioxidant activities.Methods:Samples of leaf,root and rhizome from E.acoroides were tested for total phenolic content,proanthocyanidins and in vitro antioxidant activity in terms of total antioxidant assay,DPPH assay and FRAP assay.Results:The leaf sample was found to have high levels of phenolic(0.323±0.028 mg TAE/g) and proanthocyanidins(0.570 0±0.000 3 mg TAE/g) when compared to root and rhizome.The leaf samples exhibited higher total antioxidant activity (11.770±0.026 mg Ascorbic acid equivalent/g),higher percentage of DPPH radical scavenging activity(25.76±0.04) and higher reducing power(18.060±0.073) in terms of mg GAE/g.In addition, there was a significant correlation between total phenolic content and total antioxidant activity (R^2=0.923),DPPH assay(R^2=0.509).FRAP assay(R^2=0.994).Similarly,significant correlation was found between the proanthocyanidin and total antioxidant activity(R^2=0.977),DPPH assay (R^2=0.464) and the FRAP assay(R^2=0.998).Conclusions:These results suggested that E.acoroides have strong antioxidant potential.Further study is necessary for isolation and characterization of the active antioxidant agents,which can be used to treat various oxidative stress-related diseases.