Pseudonocardians A–C, New Diazaanthraquinone Derivatives from a Deap-Sea Actinomycete Pseudonocardia sp. SCSIO 01299

Pseudonocardians A–C (2–4), three new diazaanthraquinone derivatives, along with a previously synthesized compound deoxynyboquinone (1), were produced by the strain SCSIO 01299, a marine actinomycete member of the genus Pseudonocardia, isolated from deep-sea sediment of the South China Sea. The structures of compounds 1–4 were determined by mass spectrometry and NMR experiments (1H, 13C, HSQC, and HMBC). The structure of compound 1, which was obtained for the first time from a natural source, was confirmed by X-ray analysis. Compounds 1–3 exhibited potent cytotoxic activities against three tumor cell lines of SF-268, MCF-7 and NCI-H460 with IC50 values between 0.01 and 0.21 μm, and also showed antibacterial activities on Staphylococcus aureus ATCC 29213, Enterococcus faecalis ATCC 29212 and Bacillus thuringensis SCSIO BT01, with MIC values of 1–4 μg mL−1

Microarray-Based Approach Identifies Differentially Expressed MicroRNAs in Porcine Sexually Immature and Mature Testes

MicroRNAs (miRNAs) are short non-coding RNA molecules which are proved to be involved in mammalian spermatogenesis. Their expression and function in the porcine germ cells are not fully understood.We employed a miRNA microarray containing 1260 unique miRNA probes to evaluate the miRNA expression patterns between sexually immature (60-day) and mature (180-day) pig testes. One hundred and twenty nine miRNAs representing 164 reporter miRNAs were expressed differently (p<0.1). Fifty one miRNAs were significantly up-regulated and 78 miRNAs were down-regulated in mature testes. Nine of these differentially expressed miRNAs were validated using quantitative RT-PCR assay. Totally 15,919 putative miRNA-target sites were detected by using RNA22 method to align 445 NCBI pig cDNA sequences with these 129 differentially expressed miRNAs, and seven putative target genes involved in spermatogenesis including DAZL, RNF4 gene were simply confirmed by quantitative RT-PCR.Overall, the results of this study indicated specific miRNAs expression in porcine testes and suggested that miRNAs had a role in regulating spermatogenesis

New Polyphenols from a Deep Sea Spiromastix sp. Fungus, and Their Antibacterial Activities

Eleven new polyphenols namely spiromastols A–K (1–11) were isolated from the fermentation broth of a deep sea-derived fungus Spiromastix sp. MCCC 3A00308. Their structures were determined by extensive NMR data and mass spectroscopic analysis in association with chemical conversion. The structures are classified as diphenyl ethers, diphenyl esters and isocoumarin derivatives, while the n-propyl group in the analogues is rarely found in natural products. Compounds 1–3 exhibited potent inhibitory effects against a panel of bacterial strains, including Xanthomanes vesicatoria, Pseudomonas lachrymans, Agrobacterium tumefaciens, Ralstonia solanacearum, Bacillus thuringensis, Staphylococcus aureus and Bacillus subtilis, with minimal inhibitory concentration (MIC) values ranging from 0.25 to 4 µg/mL. The structure-activity relationships are discussed, while the polychlorinated analogues 1–3 are assumed to be a promising structural model for further development as antibacterial agents

New Polyphenols from a Deep Sea Spiromastix sp. Fungus, and Their Antibacterial Activities

Eleven new polyphenols namely spiromastols A–K (1–11) were isolated from the fermentation broth of a deep sea-derived fungus Spiromastix sp. MCCC 3A00308. Their structures were determined by extensive NMR data and mass spectroscopic analysis in association with chemical conversion. The structures are classified as diphenyl ethers, diphenyl esters and isocoumarin derivatives, while the n-propyl group in the analogues is rarely found in natural products. Compounds 1–3 exhibited potent inhibitory effects against a panel of bacterial strains, including Xanthomanes vesicatoria, Pseudomonas lachrymans, Agrobacterium tumefaciens, Ralstonia solanacearum, Bacillus thuringensis, Staphylococcus aureus and Bacillus subtilis, with minimal inhibitory concentration (MIC) values ranging from 0.25 to 4 µg/mL. The structure-activity relationships are discussed, while the polychlorinated analogues 1–3 are assumed to be a promising structural model for further development as antibacterial agents

Microstructure, mechanical and tribological properties of multilayer graphene reinforced WC-10Ni3Al prepared by microwave sintering

The multilayer graphene (MLG) reinforced WC-10Ni3Al cemented carbide was prepared by microwave sintering. The effects of the sintering temperature and MLG content on the microstructure and mechanical properties of the WC-10Ni3Al cemented carbide were investigated. The promotion effect and strengthening mechanism of MLG on WC-10Ni3Al by microwave sintering were explored. The tribological properties of WC-10Ni3Al and Ti6Al4V(TC4) were studied, and the wear mechanism of WC-10Ni3Al was revealed. The experiment result show that the WC-10Ni3Al-0.5 wt.% MLG sample sintered at 1450 °C had its greatest mechanical properties with a relative density of 96.9%, hardness of 1430 HV, flexural strength of 1410 MPa and fracture toughness of 15.7 MPa mm1/2, which were 4.2%, 12.2%, 24.4%, and 29.6% greater than those of the sample without MLG added, respectively. The reinforcing and toughening mechanisms of adding MLG in WC-10Ni3Al samples consist of fine crystal strengthening, crack bridging and deflection, MLG pulling out and bridging. The results of friction experiment show that the friction coefficient and wear rate of the WC-10Ni3Al samples were lower than those of YG8 (WC-8 wt. % Co cemented carbide). The WC-10 Ni3Al-0.5 wt.% MLG sample obtained the lowest friction coefficient of 0.35 and the lowest wear rate of 1.69 × 10−5 mm3N−1m−1. A stable solid lubrication film was produced on the friction surface of the WC-10Ni3Al samples, which was conducive to reducing the breakage and wear of WC grains. MLG can enhance the stability of solid lubrication film and reduce its friction coefficient

Prevalent use and evolution of exonic regulatory sequences in the human genome

Abstract It has long been known that exons can serve as cis‐regulatory sequences, such as enhancers. However, the prevalence of such dual‐use of exons and how they evolve remain elusive. Based on our recently predicted, highly accurate large sets of cis‐regulatory module candidates (CRMCs) and non‐CRMCs in the human genome, we find that exonic transcription factor binding sites (TFBSs) occupy at least a third of the total exon lengths, and 96.7% of genes have exonic TFBSs. Both A/T and C/G in exonic TFBSs are more likely under evolutionary constraints than those in non‐CRMC exons. Exonic TFBSs in codons tend to encode loops rather than more critical helices and strands in protein structures, while exonic TFBSs in untranslated regions (UTRs) tend to avoid positions where known UTR‐related functions are located. Moreover, active exonic TFBSs tend to be in close physical proximity to distal promoters whose genes have elevated transcription levels. These results suggest that exonic TFBSs might be more prevalent than originally thought and likely in dual‐use. We proposed a parsimonious model that well explains the observed evolutionary behaviors of exonic TFBS as well as how a stretch of codons evolve into a TFBS. Key points There are more exonic regulatory sequences in the human genome than originally thought. Exonic transcription factor binding sites are more likely under negative selection or positive selection than counterpart nonregulatory sequences. Exonic transcription factor binding sites tend to be located in genome sequences that encode less critical loops in protein structures, or in less critical parts in 5′ and 3′ untranslated regions

Preparation of WC-TiC-Ni3Al-CaF2 functionally graded self-lubricating tool material by microwave sintering and its cutting performance

With the concern of the environment, green dry cutting technology is getting more and more attention and self-lubricating tool technology plays an important role in dry cutting. Due to the demand for high temperature performance of tools during dry cutting process, cemented carbide with Ni3Al as the binder phase has received extensive attention due to its excellent high temperature strength and high temperature oxidation resistance. In this paper, WC-TiC-Ni3Al-CaF2 graded self-lubricating material and tools were prepared by microwave heating method, and its microstructure, mechanical properties and cutting performance were studied. Results show that gradient self-lubricating material can be quickly prepared by microwave heating technology, and the strength is equivalent to that of conventional heating technology. CaF2 not only plays a role in self-lubrication, but also refines the grain of the material. A reasonable gradient design can improve the mechanical properties of the material. When the gradient distribution exponent is n1 = 2, the material has high mechanical properties. Cutting experiments show that the WC-TiC-Ni3Al-CaF2 functional gradient self-lubricating tool has better cutting performance than the homogeneous WC-TiC-Ni3Al hard alloys

New Monoterpenoids and Polyketides from the Deep-Sea Sediment-Derived Fungus Aspergillus sydowii MCCC 3A00324

Chemical study of the secondary metabolites of a deep-sea-derived fungus Aspergillus sydowii MCCC 3A00324 led to the isolation of eleven compounds (1&ndash;11), including one novel (1) and one new (2) osmane-related monoterpenoids and two undescribed polyketides (3 and 4). The structures of the metabolites were determined by comprehensive analyses of the NMR and HRESIMS spectra, in association with quantum chemical calculations of the 13C NMR, ECD, and specific rotation data for the configurational assignment. Compound 1 possessed a novel monoterpenoid skeleton, biogenetically probably derived from the osmane-type monoperpenoid after the cyclopentane ring cleavage and oxidation reactions. Additionally, compound 3 was the first example of the &alpha;-pyrone derivatives bearing two phenyl units at C-3 and C-5, respectively. The anti-inflammatory activities of 1&ndash;11 were tested. As a result, compound 6 showed potent inhibitory nitric oxide production in lipopolysaccharide (LPS)-activated BV-2 microglia cells with an inhibition rate of 94.4% at the concentration of 10 &micro;M. In addition, a plausible biosynthetic pathway for 1 and 2 was also proposed

Microindolinone A, a Novel 4,5,6,7-Tetrahydroindole, from the Deep-Sea-Derived Actinomycete Microbacterium sp. MCCC 1A11207

A novel indole, microindolinone A (1), was isolated from a deep-sea-derived actinomycete Microbacterium sp. MCCC 1A11207, together with 18 known compounds (2–19). By detailed analysis of the 1H, 13C, HSQC, COSY, HMBC, high resolution electron spray ionization mass spectrum (HRESIMS), and circular dichroism (CD) data, the absolute configuration of 1 was elucidated as 5R-hydroxy-4,5,6,7-tetrahydroindole-4-one. It is noteworthy that 1 is the second example of a saturated indole isolated from nature