Discovery of vanadium complexes bearing tridentate schiff base ligands as novel LSD1 inhibitors

Lysine specific demethylase (LSD1) plays a pivotal role in epigenetic modulation of gene expression. Abberrant expression of LSD1 was associated with the progress and oncogenesis of multiple human cancers. Herein, we report the preliminary anti-LSD1 evaluation of the synthetic vanadium (V) complexes. Among them, complex 2 showed a moderate inhibitory effect against LSD1 with IC₅₀ value of 19.0?μM, as well as good selectivity over MAO-A/B. Complex 2 is the first vanadium based LSD1 inhibitor, which provides a novel scaffold for the development of LSD1 inhibitor.     

The Inner Nuclear Membrane Protein Bqt4 in Fission Yeast Contains a DNA-Binding Domain Essential for Telomere Association with the Nuclear Envelope

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Molecular Identification and Diversity of ‘Candidatus Phytoplasma solani’ Associated with Red‐leaf Disease of Salvia miltiorrhiza in China

Reddening disease has recently been threatening Salvia miltiorrhiza in China, ranging from 30 to 50%. The main symptoms observed, such as plant stunting, inflorescence malformation, leaf reddening, fibrous roots browning, skin blackening and eventually root rot, are typically associated with phytoplasma infection. The presence of phytoplasmas was demonstrated through phytoplasma‐specific PCR, with the expected amplification (1.8 kb) from symptomatic S. miltiorrhiza plants from Shangluo, Shangzhou and Luonan fields in Shaanxi Province of China. The sequences of 16S rRNA, tuf, secY and vmp1 genes amplified from LN‐1 phytoplasma shared the closest homologies of 99%, 100%, 99% and 98% with those of the reference strain Candidatus Phytoplasma solani (subgroup 16SrXII‐A), respectively. The phylogenetic trees showed that LN‐1 phytoplasma clustered with the members of 16SrXII‐A group, including Ca. P. solani. Computer‐simulated restriction fragment length polymorphism analysis further supported this classification. Diversity analysis showed that all ‘Ca. P. solani’ strains identified from the three different regions examined shared 100% identical 16S rRNA, tuf, secY and vmp1 nucleotide sequences. To the best of our knowledge, this is the first report of phytoplasma infecting the medicinal plant of S. miltiorrhiza. The results demonstrate that ‘Ca. P. solani’ is the presumptive aetiological agent of S. miltiorrhiza reddening disease in China.     

Disporum sinovietnamicum sp. nov. (Colchicaceae) from southwestern Guangxi,China

Disporum sinovietnamicum R. C. Hu & Y. Feng Huang sp. nov. is described and from southwestern Guangxi, China. It is morphologically closest to D. jinfoshanense X. Z. Li, D. M. Zhang & D. Y. Hong, but differs by having stems that are 35–90 cm tall, narrowly lanceolate and thinly leathery leaves, and ovate and glabrous tepals.     

Effects of simulated nitrogen deposition on soil respiration in a Bambusa pervariabilis x Dendrocala mopsi plantation in rainy area of West China

From January 2008 to February 2009, a field experiment was conducted in Rainy Area of West China to understand the effects of nitrogen (N) deposition on the soil respiration in a Bambusa pervariabilis x Dendrocala mopsi plantation. Four treatments were installed, i. e., no N added (control), 5 g N m(-2) a(-1) (low-N), 15 g N m(-2) a(-1) (medium-N), and 30 g N m(-2) a(-1) (high-N), and soil respiration rate was determined by infra-red CO2 analyzer. In the plantation, soil respiration rate had an obvious seasonal change, with the maximum in July and the minimum in January. In control plot, the annual cumulative soil respiration was (389 +/- 34) g m(-2) a(-1). Soil respiration rate had significant positive exponential relationships with soil temperature at 10 cm depth and air temperature, and significant positive linear relationships with soil microbial biomass carbon (MBC) and nitrogen (MBN). Simulated N deposition promoted soil respiration significantly, with significant differences between the low- and medium-N and the control but no significant difference between high-N and the control. In control plot, surface soil (0-20 cm) MBC and MBN were 0.460 and 0.020 mg g(-1), respectively. In N-added plots, both the MBC and the MBN had significant increase. The fine root density in surface soil was 388 g m(-2), which was less affected by simulated N deposition. The soil respiration Q10 value calculated from soil temperature at 10 cm depth and air temperature was 2.66 and 1.87, respectively, and short-term N deposition had lesser effects on the Q10 value. The variation of soil respiration in the plantation was mainly controlled by temperature and soil microbial biomass, and simulated N deposition could increase the CO2 emission via increasing soil microbial biomass.     

Covalent layer-by-layer assembly of hyperbranched polyether and polyethyleneimine: multilayer films providing possibilities for surface functionalization and local drug delivery

A convenient and simple route to multifunctional surface coatings via the alternating covalent layer-by-layer (LBL) assembly of p-nitrophenyloxycarbonyl group-terminated hyperbranched polyether (HBPO-NO(2)) and polyethylenimine (PEI) is described. The in situ chemical reaction between HBPO-NO(2) and PEI onto aminolyzed substrates was rapid and mild. Results from ellipsometry measurements, contact angle measurements, and ATR-FTIR spectra confirmed the successful LBL assembly of the building blocks, and the surface reactivity of the multilayer films with HBPO-NO(2) as the outmost layer was demonstrated by the immobilization of an amine-functionalized fluorophore. Furthermore, a biomimetic surface was achieved by surface functionalization of the multilayer films with extracellular matrix protein collagen to promote the adhesion and growth of cells. The studies on the drug loading and in vitro release behaviors of the multilayer films demonstrated their application potentials in local delivery of hydrophilic and hydrophobic therapeutic agents.     

Characterization of amino acid residues essential for tetramer formation and DNA-binding activity of ssDNA-binding protein of <Emphasis Type="Italic">Mycobacterium tuberculosis</Emphasis>

Mycobacterium tuberculosis Rv0054 encodes a single-stranded DNA-binding protein (MtbSSB) that is essential for survival of the human pathogen and causative agent of tuberculosis. The function of MtbSSB has been proposed to be different from its E. coli homolog. However, the critical amino acid residues of MtbSSB and their regulatory effects on DNA-binding ability remain to be clearly characterized. In this study, using a frequency-controlled random mutagenesis method (FRM), mutant libraries of MtbSSB were successfully constructed. On the whole, 146 single, double, and triple MtbSSB mutants, which covered 89% of the amino acid residues along the whole MtbSSB gene, were isolated. Using bacterial two-hybrid assays in combination with native PAGE assays, four new mutants, E62G, D104N, E94G/T137N, and S130P/G153N were found to totally or partially lose their ability to form tetramer. Three novel mutants, E62G, D104N, and E94G/T134N, were characterized to have a much lower ssDNA-binding activity, while one mutant, F21L, was found to have a significantly higher activity through both electrophoretic mobility shift and surface plasmon resonance assays. Interestingly, three amino acid residues, E62, D104, and E94, were found to regulate both oligomerization and ssDNA-binding activity of MtbSSB. Our work provides an important resource and should help improve the understanding of the biochemical mechanisms and structure-function relationship of the DNA-binding protein in this important human pathogen.     

A Two-Year Surveillance of 2009 Pandemic Influenza A (H1N1) in Guangzhou,China: From Pandemic to Seasonal Influenza?

In this two-years surveillance of 2009 pandemic influenza A (H1N1) (pH1N1) in Guangzhou, China, we reported here that the scale and duration of pH1N1 outbreaks, severe disease and fatality rates of pH1N1 patients were significantly lower or shorter in the second epidemic year (May 2010-April 2011) than those in the first epidemic year (May 2009-April 2010) (P<0.05), but similar to those of seasonal influenza (P>0.05). Similar to seasonal influenza, pre-existing chronic pulmonary diseases was a risk factor associated with fatal cases of pH1N1 influenza. Different from seasonal influenza, which occurred in spring/summer seasons annually, pH1N1 influenza mainly occurred in autumn/winter seasons in the first epidemic year, but prolonged to winter/spring season in the second epidemic year. The information suggests a tendency that the epidemics of pH1N1 influenza may probably further shift to spring/summer seasons and become a predominant subtype of seasonal influenza in coming years in Guangzhou, China.