7-[4-(5,7-Dimethyl-1,8-naphthyridin-2-yl­oxy)phen­oxy]-2,4-dimethyl-1,8-naphthyridine methanol disolvate

The title compound, C26H22N4O2·2CH3OH, was synthesized and characterized by 1H NMR spectroscopy and X-ray structure analysis. There is one half-mol­ecule in the asymmetric unit with a centre of symmetry located at the centre of the benzene ring. The two bridged naphthyridine ring systems are in an anti­parallel orientation. In the crystal structure, O—H⋯N, C—H⋯O and C—H⋯N inter­actions define the packing

A comparison about the inhibitory effect of curcunmin and Avastin on the rat corneal neovascularization

AIM: To compare the inhibitory effect of curcunmin and Avastin on the rat corneal neovascularization(CNV), and approach the mechanism of the curcunmin's inhibition. METHODS: CNV was established in thirty SD rats by alkaline burning. Rats were divided equally to group A and group B at random. In group A, right eyes were experimental group A1, treated by 40μmol/L curcunmin solution, and left eyes were control group A2, treated by 0.09% sodium chloride. In group B, right eyes were experimental group group B1, treated by 5g/L avastin, and left eyes were control group B2, treated by 0.09% sodium chloride. Cornea and aqueous humor were collected by time spot. The capillary vessels were study, and the expressions of VEGF were detected by Enzyme-Linked immunosorbnent Assay(ELISA). RESULTS: No toxic effects of the drugs were found. The capillary vessels in experimental group were less than those of control group(P<0.01). No statistical different of the capillary vessels between two drugs were found. The expressions of VEGF in experimental group were less than those in control group(P<0.01). The expressions of VEGF in B1 group were less than in group A1. CONCLUSION: The inhibitory effect to CNV of curcunmin and avastin have no statistical different in the experiment, but curcunmin has the less inhibitory effect to the expressions of VEGF than avastin. Curcunmin may have other mechanism in the inhibitory action on CNV

Oxonium picrate

The title compound, H3O+·C6H2N3O7 −, consists of one picrate anion and one oxonium cation. The oxonium cation is located on a crystallographic twofold axis and both its H atoms are disordered, each over two symmetry-equivalent positions with occupancy ratios of 0.75. The picrate anions are also located on twofold axes bis­ecting the phenolate and p-nitro groups. π–π inter­actions between the rings of the picrates [centroid-to-centroid distances of 3.324 (2) Å] connect the anions to form stacks along the a-axis direction. The stacks are further joined together by the protonated water mol­ecules through hydrogen bonds to form two-dimensional sheets extending parallel to the ab plane. The sheets are stacked on top of each other along the c-axis direction and connected through C—H⋯O inter­actions between the CH groups of the benzene rings and the picrate nitro groups, with C⋯O distances of 3.450 (2) Å

Bis(7-amino-2,4-dimethyl-1,8-naphthyridine)dinitratocadmium(II)

In the title compound, [Cd(NO3)2(C10H11N3)2], two naph­thyridine ring systems are coordinated to the Cd ion through the two N atoms in a bidentate chelating mode, whereas the remaining coordination sites are occupied by two O atoms from two different nitrate groups to complete the octahedral geometry. Inter­moleular N—H⋯O hydrogen bonds link the mol­ecules to form a one-dimensionnal sheet parallel to the ac plane. Weak slipped π–π stacking involving the naphthyridine ring systems stabilizes the structure

Edge-Termination and Core-Modification Effects of Hexagonal Nanosheet Graphene

[[abstract]]Optimized geometries and electronic structures of two different hexagonal grapheme nanosheets (HGNSs), with armchair (n-A-HGNS, n = 3–11) and zigzag (n-Z-HGNS, n = 1–8) edges have been calculated by using the GGA/PBE method implemented in the SIESTA package, with the DZP basis set, where n represents the number of peripheral rings. The computed HOMO-LUMO energy gap (Eg = ELUMO − EHOMO) decreases for fully H-terminated A- and Z-HGNSs with increasing n, i.e., with increasing nanosheet size and pπ-orbitals being widely delocalized over the sheet surface. The full terminations, calculated with various functional groups, including the electron-withdrawing (F-, Cl-, and CN-) and -donating (OH-, and SH-) substitutions, were addressed. Significant lowering of EHOMO and ELUMO was obtained for CN-terminated HGNS as compared to those for H-terminated ones due to the mesomeric effect. The calculated Eg value decreases with increasing n for all terminations, whereby for the SH-termination in HGNS, the termination effect becomes less significant with increasing n. Further, the calculation results for stabilities of HGNS oxides support the tendency toward the oxidative reactivity at the edge site of the sheet, which shows most pronounced C-C bond length alternation, by chemical modification. Physical properties of HGNSs with various numbers of the core-defects, which can be obtained by strong oxidation, were also investigated. Their structures can change drastically from planar to saddle-like shapes. These conformations could be used as stationary phases with controlled interaction in the separation methods such as HPLC and the other chemical analysis techniques.[[notice]]補正完畢[[incitationindex]]SCI[[booktype]]電子

Antigout Effects of Plantago asiatica

The XOD inhibitory effects of Plantaginis Semen, that is, the seeds of P. asiatisca, and its representative four single compounds, acteoside, 1H-indolo-3-carbaldehyde, isoacteoside, and myristic acid, were evaluated by electron transfer signal blocking activities (ETSBA), which is based on the electron transfer signal of XOD enzymatic reaction. The blocking activities were detected using an electrochemical biosensing method. Compared with control, significant effects were observed after the addition of P. asiatica extract, acteoside, and 1H-indolo-3-carbaldehyde (all p<0.05). The IC50 values of the extract and acteoside are 89.14 and 7.55 μg·mL−1, respectively. The IC20 values of the extract, acteoside, and 1H-indolo-3-carbaldehyde are 24.28, 3.88, and 16.16 μg·mL−1, respectively. Due to the relatively lower inhibitory potential of 1H-indolo-3-carbaldehyde, its IC50 was not obtained. In addition, isoacteoside and myristic acid did not show any XOD inhibitory effects. Our data demonstrated that the XOD inhibitory effects of the extract, acteoside, and 1H-indolo-3-carbaldehyde can be accurately evaluated by the ETSBA method. The results from this study indicated that Plantaginis Semen significantly inhibited XOD activities to reduce hyperuricemia and treat gout. The study also proves that measuring the electron transfer signal blocking activities is a simple, sensitive, and accurate method to evaluate the XOD inhibitory effects

INTERVENTION EFFECT AND DOSE-DEPENDENT RESPONSE OF TANREQING INJECTION ON AIRWAY MUCUS HYPERSECRETION IN LIPOPOLYSACCHARIDE-INDUCED RATS

Background: Tanreqing injection, a Chinese herbal formulation comprising Radix Scutellariae, Fructus Forsythiae, Flos Lonicerae, Antelope horn, and Bear bile powder, has been used to treat bronchitis and pneumonia for many years in China. However, its anti-mucus-hypersecretion mechanism has yet not been fully interpreted. We aim to assess the effect and dose-response relationships of Tanreqing injection on lipopolysacchaide (LPS) induced airway mucus hypersecretion in rats. Material and methods: Forty-eight male rats were randomly divided into four groups (12 per group). A rat model of airway mucus hypersecretion was generated with LPS. Tanreqing injection was given by intratracheal instillation, and bronchoalveolar lavage fluid (BALF) from the right lung was collected. BALF total protein was determined by bicinchoninic acid disodium assay (BCA). Muc5ac was measured using enzyme linked immunosorbent assay (ELISA) and immunohistochemistry. The expression of muc5ac mRNA was detected by real-time polyermase chain reaction (RT-PCR). The middle lobe of the right lung was stained with alcian blue-periodic acid sthiff (AB-PAS) and positive staining relative shading area examined. Results: LPS caused airway mucus hypersecretion, The LPS-induced airway mucus hypersecretion increased beginning at 24 hr, and peaked at 96 hr. Tanreqing injection could inhibit airway mucus hypersecretion, and suppress the expression of muc5ac mRNA. Conclusion: Tanreqing injection inhibits airway mucus hypersecretion in a certain dose-dependent trend

Soybean GmPHD-Type Transcription Regulators Improve Stress Tolerance in Transgenic Arabidopsis Plants

Soybean [Glycine max (L.) Merr.] is one of the most important crops for oil and protein resource. Improvement of stress tolerance will be beneficial for soybean seed production.Six GmPHD genes encoding Alfin1-type PHD finger protein were identified and their expressions differentially responded to drought, salt, cold and ABA treatments. The six GmPHDs were nuclear proteins and showed ability to bind the cis-element "GTGGAG". The N-terminal domain of GmPHD played a major role in DNA binding. Using a protoplast assay system, we find that GmPHD1 to GmPHD5 had transcriptional suppression activity whereas GmPHD6 did not have. In yeast assay, the GmPHD6 can form homodimer and heterodimer with the other GmPHDs except GmPHD2. The N-terminal plus the variable regions but not the PHD-finger is required for the dimerization. Transgenic Arabidopsis plants overexpressing the GmPHD2 showed salt tolerance when compared with the wild type plants. This tolerance was likely achieved by diminishing the oxidative stress through regulation of downstream genes.These results provide important clues for soybean stress tolerance through manipulation of PHD-type transcription regulator

Host A-to-I RNA editing signatures in intracellular bacterial and single-strand RNA viral infections

BackgroundMicrobial infection is accompanied by remodeling of the host transcriptome. Involvement of A-to-I RNA editing has been reported during viral infection but remains to be elucidated during intracellular bacterial infections.ResultsHerein we analyzed A-to-I RNA editing during intracellular bacterial infections based on 18 RNA-Seq datasets of 210 mouse samples involving 7 tissue types and 8 intracellular bacterial pathogens (IBPs), and identified a consensus signature of RNA editing for IBP infections, mainly involving neutrophil-mediated innate immunity and lipid metabolism. Further comparison of host RNA editing patterns revealed remarkable similarities between pneumonia caused by IBPs and single-strand RNA (ssRNA) viruses, such as altered editing enzyme expression, editing site numbers, and levels. In addition, functional enrichment analysis of genes with RNA editing highlighted that the Rab GTPase family played a common and vital role in the host immune response to IBP and ssRNA viral infections, which was indicated by the consistent up-regulated RNA editing of Ras-related protein Rab27a. Nevertheless, dramatic differences between IBP and viral infections were also observed, and clearly distinguished the two types of intracellular infections.ConclusionOur study showed transcriptome-wide host A-to-I RNA editing alteration during IBP and ssRNA viral infections. By identifying and comparing consensus signatures of host A-to-I RNA editing, our analysis implicates the importance of host A-to-I RNA editing during these infections and provides new insights into the diagnosis and treatment of infectious diseases