Design, synthesis and biological evaluation of thieno[3,2-c]pyrazol-urea derivatives as potent glycogen synthase kinase 3β inhibitors based on the DFG-out conformation.

Glycogen synthase kinase 3β (GSK-3β) is a potential therapeutic target for the treatment of a variety of human diseases. Here, we report the design and synthesis of a series of thieno[3,2-c]pyrazol-urea derivatives and evaluation of their GSK-3β inhibitory activity. Among these analogues, the compound without substitution on terminal phenyl ring (3a) was found to be the most potent GSK-3β inhibitor with an IC of 74.

Sensitive Organic Vapor Sensors Based on Flexible Porous Conductive Composites with Multilevel Pores and Thin, Rough, Hollow-Wall Structure.

Advanced organic vapor sensors that simultaneously have high sensitivity, fast response, and good reproducibility are required. Herein, flexible, robust, and conductive vapor-grown carbon fibers (VGCFs)-filled polydimethylsiloxane (PDMS) porous composites (VGCFs/PDMS sponge (CPS)) with multilevel pores and thin, rough, and hollows wall were prepared based on the sacrificial template method and a simple dip-spin-coating process. The optimized material showed outstanding mechanical elasticity and durability, good electrical conductivity and hydrophobicity, as well as excellent acid and alkali tolerance.

[Moxibustion combined with acupoint catgut embedding promotes recovery of injured colonic mucosa by suppressing inflammation in ulcerative colitis rats].

Objective: To observe the effect of moxibustion and acupoint catgut embedding (ACE) at "Tianshu"(ST25) "Dachangshu"(BL25) and "Shangjuxu"(ST37) on changes of body mass, stool property, histopathological conditions and expression levels of interleukin 6 (IL-6) in colonic mucosa of ulcerative colitis (UC) rats, so as to reveal its anti-inflammatory mechanisms underlying improvement of UC.

Methods: SD rats were randomized into normal, model, moxibustion, ACE and moxibustion＋ACE groups (＝6 in each group). The UC model was established by enema of trinitro-benzene-sulfonic acid and ethanol.

Ancestry informative DIP loci for dissecting genetic structure and ancestry proportions of Qinghai Tibetan and Tibet Tibetan groups.

Tibetans living in the Qing-Tibet plateau show unique genetic features since they are exposed to the high altitude environment. Accordingly, it is necessary for us to analyze genetic components of the Tibetan groups. Here, genetic structure and ancestry proportions of Tibet Tibetan and Qinghai Tibetan groups are dissected by using a previously published ancestral deletion/insertion polymorphisms (DIPs) panel.

Biogeographic origin prediction of three continental populations through 42 ancestry informative SNPs.

A biogeographic estimate of a certain population can not only discern population substructure in the whole genome association study, but also provide informative clues for forensic investigations when obtained DNA genotypes do not find a match in the available forensic DNA database. In this study, 100 ancestry informative single nucleotide polymorphisms (AISNPs) were first presented to differentiate three continental ancestries (African, East Asian and European). Ultimately, forty-two AISNPs were chosen from the 100 AISNPs.

Synthesis and Optimization of Ti/Li/Al Ternary Layered Double Hydroxides for Efficient Photocatalytic Reduction of CO to CH.

A series of Ti/Li/Al ternary layered double hydroxides (TiLiAl-LDHs) with different Ti:Li:Al molar ratios were prepared by a coprecipitation method for photocatalytic CO reduction. It was demonstrated that the contents of anions between the layers of Ti/Li/Al-LDHs greatly determined the photocatalytic activity for CO reduction. With Ti:Li:Al molar ratios optimized to be 1:3:2, the largest contents of [Formula: see text] anion and hydroxyl group were obtained for the TiLiAl-LDHs sample, which exhibited the highest photocatalytic activity for CO reduction, with CH production rate achieving 1.

Genetic distribution and forensic evaluation of multiplex autosomal short tandem repeats in the Chinese Xinjiang Mongolian group.

To further enrich the genetic data of the Chinese Xinjiang Mongolian group, the genetic distribution and forensic parameters of 19 autosomal short tandem repeats (STRs) were investigated. Altogether, 249 alleles were observed in these 19 STRs. The mean values of the polymorphism information content (PIC), match probability (MP), discrimination power (DP), and probability of exclusion (PE) for these 19 STRs were 0.

Detecting live bacteria instantly utilizing AIE strategies.

A new class of biosensor molecules evoking fluorescent emission by rotation-restricted binding with bacteria was examined for its applicability in detecting live bacteria instantly. The fluorogens possessed multiple tetraphenylethene (TPE)-cored boronic acids to oligomerize through complexation with cis-diols on bacterial surfaces, resulting in aggregation-induced emission (AIE). The fluorogen having two boronic acid units discriminated between live and dead bacteria by showing AIE activity only with the latter.

Heat Transfer Behavior across the Dentino-Enamel Junction in the Human Tooth.

During eating, the teeth usually endure the sharply temperature changes because of different foods. It is of importance to investigate the heat transfer and heat dissipation behavior of the dentino-enamel junction (DEJ) of human tooth since dentine and enamel have different thermophysical properties. The spatial and temporal temperature distributions on the enamel, dentine, and pulpal chamber of both the human tooth and its discontinuous boundaries, were measured using infrared thermography using a stepped temperature increase on the outer boundary of enamel crowns.

Preparation of S14161 and its analogues and the discovery of 6-bromo-8-ethoxy-3-nitro-2H-chromene as a more potent antitumor agent in vitro.

The small chemical compound 8-ethoxy-2-(4-fluorophenyl)-3-nitro-2H-chromene (S14161) was recently identified as an inhibitor of the phosphoinositide 3-kinase (PI3K). In the present study, we designed a novel synthesis of S14161 and prepared a series of its analogues via the oxa-Michael-Henry reaction in the presence of catalytic amounts of l-proline and triethylamine. Further structural simplification led to the identification of 6-bromo-8-ethoxy-3-nitro-2H-chromene (BENC-511) that exhibited potent antiproliferative activities against a panel of 12 tumor cell lines.

Recent developments of p38α MAP kinase inhibitors as antiinflammatory agents based on the imidazole scaffolds.

Rheumatoid arthritis (RA) and other chronic inflammatory diseases are always the major therapeutic challenges. Recent research efforts provided new insights into the molecular basis of these diseases and new opportunities for developing improved anti-inflammatory drugs. The p38 mitogen-activated protein (MAP) kinase plays a central role in the regulation of the biosynthesis and release of several proinflammatory cytokines including tumor necrosis factor alpha (TNF-α) and interleukin-1 beta (IL-1β).