Enantioselective Synthesis of Spirooxindole Derivatives through Lewis Acid-Catalyzed Michael Addition/Cyclization Cascade.

A Mg(OTf)-catalyzed asymmetric Michael addition/cyclization cascade reaction between 3-isothiocyanato oxindoles and 2-arylidene-1,3-indanediones has been developed. This transformation provides an efficient and concise approach to biologically important bispiro[indanedione-oxindole-pyrrolidinyl]s under mild conditions in good to excellent yields (70-99% yields) with moderate to good stereoselectivities (up to 99% and >95:5 d.r.

Inhibitory effects of flavonoids and alkaloids from the traditional antihyperglycemic herb var. on α-glucosidase activity.

The rhizome of var. (commercially used as ) yielded three new compounds: 8-methylaromadendrin (), --coumaroyl-7-butoxytyramine (), and ---coumaroyl-7-ethoxytyramine (), alongside 23 known compounds (). Specifically, compound was separated into four isomers (ad) with / and 7 /7 configurations confirmed by coupling constants and Cotton effects, and compounds -, , , and were identified in this herb for the first time.

Molecular characterization of a teleost-specific toll-like receptor 22 (tlr22) gene from yellow catfish (Pelteobagrus fulvidraco) and its transcriptional change in response to poly I:C and Aeromonas hydrophila stimuli.

Toll-like receptors (TLRs) are a class of pattern recognition receptors (PRRs) that can recognize pathogen-associated molecular patterns (PMPs) and play important roles in the innate immune system in vertebrates. In this study, we identified a teleost-specific tlr22 gene from yellow catfish (Pelteobagrus fulvidraco) and its immune roles in response to different pathogens were also determined. The open reading frame (ORF) of the tlr22 was 2892 bp in length, encoding a protein of 963 amino acids.

Untargeted and targeted gingival metabolome in rodents reveal metabolic links between high-fat diet-induced obesity and periodontitis.

Aim: To characterize gingival metabolome in high-fat diet (HFD)-induced obesity in mice with/without periodontitis.

Methods: HFD-induced obesity mouse model was established by 16-week feeding, and a lean control group was fed with low-fat diet (n = 21/group). Both models were induced for periodontitis on the left sides by molar ligation for 10 days, whereas the right sides were used as controls.

The complete mitochondrial genome of (Teleostei, Cypriniformes) in Nujiang River: characterization and phylogenetic position.

is an endemic species found in Nujiang River and Lantsang. In this study, the complete mitochondrial genome of was determined. The circular mitochondrial genome was 16,576 bp long, containing 13 protein-coding genes, two ribosomal genes (rRNA), 22 transfer RNA () genes, an origin of light-strand replication (OL), and one displacement loop locus (D-loop).

Biodistribution and Toxicity Assessment of Superparamagnetic Iron Oxide Nanoparticles In Vitro and In Vivo.

Biodistribution and toxicity assessment are critical for safe clinical use of newly developed medicines. Superparamagnetic iron oxide nanoparticles (SPION) are effective carriers for targeted drug delivery. This study aimed to examine the toxicity and biodistribution of SPION coated with polyethylenimine (PEI) (SPION-PEI) designed for small interfering RNA (siRNA) delivery both in vitro and in vivo.

Genetic variants in DNA repair pathway genes and risk of esophageal squamous cell carcinoma and gastric adenocarcinoma in a Chinese population.

The DNA repair pathways help to maintain genomic integrity and therefore genetic variation in the pathways could affect the propensity to develop cancer. Selected germline single nucleotide polymorphisms (SNPs) in the pathways have been associated with esophageal cancer and gastric cancer (GC) but few studies have comprehensively examined the pathway genes. We aimed to investigate associations between DNA repair pathway genes and risk of esophageal squamous cell carcinoma (ESCC) and GC, using data from a genome-wide association study in a Han Chinese population where ESCC and GC are the predominant cancers.

Three-dimensional nanographene based on triptycene: synthesis and its application in fluorescence imaging.

A novel kind of three-dimensional (3D) nanographene based on a triptycene structure bearing three hexa-peri-hexabenzocoronene (HBC) moieties was synthesized efficiently from triiodotriptycene. With the characteristic of intrinsic fluorescence, the 3D nanographene was used as a fluorescent agent for in vitro and in vivo fluorescence imaging with good antiphotobleaching ability and little toxicity.

Novel electrochemical sensor based on functionalized graphene for simultaneous determination of adenine and guanine in DNA.

A nano-material carboxylic acid functionalized graphene (graphene-COOH) was prepared and used to construct a novel biosensor for the simultaneous detection of adenine and guanine. The direct electrooxidation behaviors of adenine and guanine on the graphene-COOH modified glassy carbon electrode (graphene-COOH/GCE) were carefully investigated by cyclic voltammetry and differential pulse voltammetry. The results indicated that both adenine and guanine showed the increase of the oxidation peak currents with the negative shift of the oxidation peak potentials in contrast to that on the bare glassy carbon electrode.

Transcription-inhibition and antitumor activities of N-alkylated tetraazacyclododecanes.

A series of alkyl-substituted tetraazacyclododecane congeners were synthesized, and their antitumor activities towards human HeLa cells as well as their effect on the in vitro transcription with T7 RNA polymerase were investigated. A structure-activity-relationship (SAR) study identified the most-active congeners as those with medium alkyl-chain lengths. Three compounds, 5-7, were found to exhibit significant biological activities, with IC50 values towards HeLa cells in the low-micromolar range.

A water-soluble, octacationic zinc phthalocyanine as molecular probe for nucleic acid secondary structure.

The interaction between CT-DNA and the zinc phthalocyanine ZnPc (1) was studied by UV/VIS and fluorescence titration, as well as by thermal denaturation. ZnPc was found to strongly bind to CT-DNA (K(app)=7.35 x 10(5) M(-1)) in a non-intercalative mode.

Synthesis and biological studies of N-alkylated cyclic diamines.

Several alkyl-substituted mesocyclic diamines were synthesized, and their interaction with DNA were studied by melting-temperature measurements and the ethidium bromide (EB)-fluorescence competitive method. The supercoiled DNA hydrolytic cleavage by 1,4-dioctyl-1,4-diazepan-6-ol (4) was supported by the evidence from free-radical quenching and T4-ligase ligation. Preliminary pharmacological tests showed that only 1,4-dioctyl-1,4-diazepan-6-ol (4) had antitumor activity against HeLa cell lines in vitro.

DNA hydrolysis promoted by 1,7-dimethyl-1,4,7,10-tetraazacyclododecane.

Several acyclic and macrocyclic polyamines were evaluated for their ability to cleave DNA. 1,7-Dimethyl-1,4,7,10-tetraazacyclododecane (DMC) could hydrolyze double-strand DNA at a concentration of 25microM. pH 7.