Antibacterial and cytotoxic metabolites of termite-associated Streptomyces sp. BYF63.

Four anthraquinone derivatives, termstrin A, B, C and D (1-4), were isolated and purified from termite-associated Streptomyces sp. BYF63. Their structures were elucidated on the basis of extensive spectroscopic analyses (HR-ESI-MS, 1D and 2D NMR).

Screening novel drug candidates for Alzheimer's disease by an integrated network and transcriptome analysis.

Motivation: Alzheimer's disease (AD) is a serious degenerative brain disease and the most common cause of dementia. The current available drugs for AD provide symptomatic benefit, but there is no effective drug to cure the disease. The emergence of large-scale genomic, pharmacological data provides new opportunities for drug discovery and drug repositioning as a promising strategy in searching novel drug for AD.

Targeting JMJD3 histone demethylase mediates cardiac fibrosis and cardiac function following myocardial infarction.

Myocardial fibrosis is the pathological consequence of injury-induced fibroblastto-myofibroblast transition, resulting in increased stiffness and diminished cardiac function. Histone modification has been shown to play an important role in the pathogenesis of cardiac fibrosis. Here, we identified H3K27me3 demethylase JMJD3/KDM6B promotes cardiac fibrosis via regulation of fibrogenic pathways.

Depletion of the diabetic gut microbiota resistance enhances stem cells therapy in type 1 diabetes mellitus.

Microbiome, considered as the "second genome" of the host, is altered in type 1 diabetes mellitus (T1DM) patients to a state of dysbiosis. Mesenchymal stem cell (MSC) transplantation is a promising treatment for T1DM but is limited by several factors in the diabetic host. In this study, we tested the hypothesis that dysbiotic gut microbiota may limit MSC therapy, and modulating gut microbiota may help to improve the effects of MSC transplantation.

Integrative analysis of DNA methylation and gene expression profiles identified potential breast cancer-specific diagnostic markers.

Breast cancer is a common malignant tumor among women whose prognosis is largely determined by the period and accuracy of diagnosis. We here propose to identify a robust DNA methylation-based breast cancer-specific diagnostic signature. Genome-wide DNA methylation and gene expression profiles of breast cancer patients along with their adjacent normal tissues from the Cancer Genome Atlas (TCGA) were obtained as the training set.

Morphological and molecular characterization of a new freshwater microsporidium, Jirovecia sinensis sp. n. (Microsporidia) infecting the coelomocytes of Branchiura sowerbyi (Oligochaeta: Naididae) in China.

We report a new microsporidium Jirovecia sinensis sp. n. from a freshwater oligochaete, Branchiura sowerbyi collected in Hongze city, Jiangsu province, East China.

Design, synthesis and anticancer activity of naphthoquinone derivatives.

Basis on molecular docking and pharmacophore analysis of naphthoquinone moiety, a total of 23 compounds were designed and synthesised. With the help of reverse targets searching, anti-cancer activity was preliminarily evaluated, most of them are effective against some tumour cells, especially compound : 1-(5,8-dihydroxy-1,4-dioxo-1,4-dihydronaphthalen-2-yl)-4-methylpent-3-en-1-yl-4-oxo-4-((4-phenoxyphenyl)amino) butanoate whose IC against SGC-7901 was 4.1 ± 2.

A validated surrogate analyte UPLC-MS/MS assay for quantitation of TUDCA, TCDCA, UDCA and CDCA in rat plasma: Application in a pharmacokinetic study of cultured bear bile powder.

Bear bile is a valuable medicinal material used in traditional Chinese medicine for over 2000 years. However, developing a substitute has become necessary because of protection measures for this endangered species. The ingredients of in vitro cultured bear bile powder (CBBP) include tauroursodeoxycholic acid (TUDCA), taurochenodeoxycholic acid (TCDCA), ursodeoxycholic acid (UDCA) and chenodeoxycholic acid (CDCA, and it has pharmacological properties that are similar to those of natural bear bile powder (NBBP).

Involvement of the JNK signaling in granular corneal dystrophy by modulating TGF-β-induced TGFBI expression and corneal fibroblast apoptosis.

Granular corneal dystrophy (GCD) is featured by corneal deposits of transforming growth factor beta-induced gene (TGFBI) mediated by the TGF-β (transforming growth factor-β)/Smad signaling. However, the roles of c-Jun amino-terminal kinase (JNK) pathway in GCD pathogenesis remains unexplored, which was investigated in this study. JNK signaling activation and inhibition in primary corneal fibroblasts were obtained by treatments with anisomycin and SP600125, respectively.

Discovery and SARs of 5-Chloro--phenyl--(pyridin-2-yl)pyrimidine-2,4-diamine Derivatives as Oral Available and Dual CDK 6 and 9 Inhibitors with Potent Antitumor Activity.

Cyclin-dependent kinases (CDKs) are promising therapeutic targets for cancer therapy. Herein, we describe our efforts toward the discovery of a series of 5-chloro--phenyl--(pyridin-2-yl)pyrimidine-2,4-diamine derivatives as dual CDK6 and 9 inhibitors. Intensive structural modifications lead to the identification of compound as the most active dual CDK6/9 inhibitor with balancing potency against these two targets and good selectivity over CDK2.

Bio-inspired fabrication of nacre-mimetic hybrid nanocoating for eco-friendly fire-resistant precious cellulosic Chinese Xuan paper.

Nacre-mimetic materials possess excellent thermostability and barrier performance which provide novel idea for high efficient flame retardant strategy. In this study, we propose an eco-friendly approach to fabricate fire-resistant cellulosic Chinese Xuan paper by layer-by-layer (LBL) assembly chitosan (CH) and montmorillonite (MMT). The flame retardancy of Xuan paper was greatly improved after the LBL assembly coated CH/MMT, it achieved excellent flame retardancy when the CH/MMT bilayer was over 10 BL with the LOI value higher than of 35 %.

Jmjd3 regulates inflammasome activation and aggravates DSS-induced colitis in mice.

The intracellular NOD-like receptor nucleotide-binding domain-like receptors Family Pyrin Domain Containing 3 (NLRP3) is a pivotal regulator of intestinal homeostasis through regulating a variety of inflammatory and autoimmune diseases. The Jumonji domain-containing 3 (Jmjd3) plays important role in inflammatory responses and thus has been proposed as a novel attractive epigenetic target for the treatment of inflammatory diseases. We here investigated whether targeting Jmjd3 regulates NLRP3 inflammasome during experimental colitis.

Evaluation of Corneal Curvature and Astigmatism in Patients with Persistent Pupillary Membrane by Partial Coherence Interferometry Measurements.

Purpose: To evaluate and compare the corneal curvature and astigmatism in patients with persistent pupillary membrane (PPM) and healthy controls by partial coherence interferometry.

Methods: This study included 14 eyes (9 patients) with PPM and 16 eyes (16 subjects) without PPM or other ocular disease, which were age and gender matched. The horizontal corneal radius of curvature (hCRC), vertical CRC (vCRC), average CRC (aveCRC), corneal astigmatic vectors (CAV), and axis were recorded using partial coherence interferometry.

Perinatal phthalates exposure decreases fine-motor functions in 11-year-old girls: Results from weighted Quantile sum regression.

Introduction: Phthalates are a group of high production chemicals, generally used as plasticizers and odor enhancers. Phthalates cross the blood-placenta barrier and are associated with deficits in cognitive functions and behavior problems in offspring. We previously reported sex-specific associations with motor function when phthalates are considered singly.

Transcriptomic analysis of oligochaete immune responses to myxosporeans infection: Branchiura sowerbyi infected with Myxobolus cultus.

The Myxozoa are endoparasites characterized by a two-host life cycle that typically involves invertebrates and vertebrates as definitive and intermediate hosts, respectively. However, little is known about invertebrate-myxosporean interactions, particularly about patterns of host immune defense. We used RNA-sequencing to identify genes that are possibly involved in the immune responses of the oligochaete Branchiura sowerbyi naturally infected with Myxobolus cultus.

Development of a novel bio-inspired "cotton-like" collagen aggregate/chitin based biomaterial with a biomimetic 3D microstructure for efficient hemostasis and tissue repair.

Hemostatic materials based on collagen and chitin are commonly assessed with regard to their topical absorbability and bioactivity. However, their clinical application faces challenges such as relatively long hemostatic and wound healing times, single function, as well as wound bleeding in patients with blood diseases. Herein, a novel bio-inspired "cotton-like" collagen aggregate/chitin based biomaterial for rapid hemostatic and tissue repair (V-3D-Ag-col) was fabricated by a specific gradient-removal solvent approach.

5,7,3',4'-flavan-on-ol (taxifolin) protects against acetaminophen-induced liver injury by regulating the glutathione pathway.

Taxifolin (TAX) reportedly exerts protective and therapeutic effects in liver. Herein, the effects of TAX against acetaminophen (APAP)-induced hepatotoxicity were investigated. Pharmacodynamics, pharmacology and metabolomics analyses of TAX were assessed on C57 mice and L-02 cells.

The Relation of Birth Weight and Adiposity Across the Life Course to Semen Quality in Middle Age.

Background: Studies of body mass index and semen quality have reported mixed results, but almost all were cross-sectional and many were conducted in selected populations. Longitudinal studies in population-based cohorts are necessary to identify how timing and duration of excess adiposity may affect semen quality.

Methods: In 193 members of the Child Health and Development Studies birth cohort, we examined associations of birth weight and adiposity at six time points spanning early childhood and adulthood with sperm concentration, motility, and morphology at mean age 44 years, as well as with corresponding 2010 World Health Organization (WHO) subfertility reference levels.

Epigenetics-Based Tumor Cells Pyroptosis for Enhancing the Immunological Effect of Chemotherapeutic Nanocarriers.

Pyroptosis is a lytic and inflammatory form of programmed cell death and could be induced by chemotherapy drugs via caspase-3 mediation. However, the key protein gasdermin E (GSDME, translated by the gene) during the caspase-3-mediated pyroptosis process is absent in most tumor cells because of the hypermethylation of (deafness autosomal dominant 5) gene. Here, we develop a strategy of combining decitabine (DAC) with chemotherapy nanodrugs to trigger pyroptosis of tumor cells by epigenetics, further enhancing the immunological effect of chemotherapy.

Discovery of Novel Aryl Carboxamide Derivatives as Hypoxia-Inducible Factor 1α Signaling Inhibitors with Potent Activities of Anticancer Metastasis.

In order to discover novel hypoxia-inducible factor 1 (HIF-1) inhibitors for the cancer metastasis treatment, 68 new aryl carboxamide compounds were synthesized and evaluated for their inhibitory effect by dual luciferase-reporter assay. Based on five rounds of investigation on structure-activity relationships step by step, compound was discovered as the most active inhibitor (IC = 0.32 μM) with no obvious cytotoxicity (CC > 50 μM).

, a new species of (Gentianaceae) from Xinjiang, China.

Ma ex H.F. Cao, J.

Synthesis and and anti-inflammatory activity of novel 4-ferrocenylchroman-2-one derivatives.

A series of novel 4-ferrocenylchroman-2-one derivatives were designed and synthesised to discover potent anti-inflammatory agents for treatment of arthritis. All the target compounds had been screened for their anti-inflammatory activity by evaluating the inhibition effect of LPS-induced NO production in RAW 264.7 macrophages.