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In this study, a continuous flow microchannel reactor was designed and constructed for continuous and efficient fatty acid chain modification (FACylation) of polypeptides to achieve higher production capacity than that obtained in a batch reactor. In this microreactor, loxenatide (LOX) was site-specifically modified by N-tetradecylmaleimide (C 14 -MAL) to continuously synthesize the target product, N-tetradecyl-loxenatide (C 14 -LOX). Based on the experimental data under different conditions, a kinetic model of FACylation was established to describe the initial stage of the continuous reaction in the microreactor. Under the optimal conditions obtained by the kinetic model, the reaction time in the microreactor could be reduced to 1/3 that of the batch reactor at the same yield, and the production capacity of the microreactor was at least 3.78 times that of the batch reactor within the same time (40 h). These results would contribute to the development of microreactors in the biopharmaceutical industry. [Display omitted] • Loxenatide (LOX) was specifically modified by a fatty acid chain. • Continuous and efficient synthesis of the product C 14 -LOX by a microchannel reactor. • The optimal reaction conditions obtained by the reaction kinetics. [ABSTRACT FROM AUTHOR]

Hydrocarbon source rocks, as a main geologic factor of petroliferous systems in a sedimentary basin, play a key role in the accumulation of oil and gas and the formation of hydrocarbon accumulations. This study, which focuses on difficulties in prediction of hydrocarbon source rocks in basins or sags with low exploration degree and insufficient hydrocarbon source rock indicators, taking the Wenchang Formation of northern Zhu I Depression, Pearl River Mouth Basin as an example, proposed a hypothesis of "finding lakes and hydrocarbon source rocks". Detailed steps include, first , determination of the lacustrine basin boundary according to analysis of seismic foreset facies, determination of the depositional area based on the compilation of strata residual thickness maps, determination of the lacustrine basin shape according to deciphering slope break belt system, determination of the fluctuation of paleo-water depth according to biogeochemical indicators of mature exploration areas, determination of the lacustrine basin scale based on analyses of tectonics intensity and accommodation space, which prove the existence of the lacustrine basin and identify the range of semi deep-deep lake; second , further analyses of tectonopalaeogeomorphology, paleo-provenance, palaeoclimate and paleo-water depth to reconstruct the geologic background of the original basin and semi-deep-deep lacustrine facies, to determine the distribution of semi-deep/deep lacustrine sediments in combination with studies of logging facies, core facies, seismic facies and sedimentary facies, and to rank the sags' potential of developing hydrocarbon source rocks from controlling factors of source-to-sink system development; third , on the basis of regional sedimentary facies analysis, through identification and assessment of seismic facies types of semi-deep/deep lacustrine basins in mature areas, establishing "hydrocarbon source rock facies" in mature areas to instruct the identification and depicting of hydrocarbon source rocks in semi-deep/deep lacustrine basins with low exploration degree; fourth , through systematical summary of hydrocarbon-rich geological factors and lower limit index of hydrocarbon formation of the sags already revealed by drilling wells (e.g., sag area, tectonic subsidence amount, accommodation space, provenance characteristic, mudstone thickness, water body environment, sedimentary facies types of hydrocarbon source rocks), in correlation with corresponding indexes of sags with low exploration degree, then the evaluation and sorting of high-quality source rocks in areas with sparsely distributed or no drilling wells can be conducted with multi-factors and multiple dimensions. It is concluded that LF22 sag, HZ10 sag and HZ8 sag are II-order hydrocarbon rich sags; whereas HZS, HZ11 and HZ24 are the III-order hydrocarbon-generating sags. [ABSTRACT FROM AUTHOR]

Microbial-induced calcium carbonate precipitation (MICP) is utilized to effectively seal microcracks in concrete. In this study, coconut shell charcoal was used as a carrier for adsorbed bacteria to act as a biomass self-healing agent, and the healing effect of microbial mortar was enhanced by the addition of basalt fibers. The effect of the combined action of biomass self-healing agents and fibers on the mechanical properties and healing ability of mortars has been investigated. The complete process of microbial metabolism in the cement matrix was firstly revealed by microscopic experiments. Optical microscopy was used observed the deposition paths of the fillers under multifiber conditions at different depths. The results showed that a large number of fibers changed the healing products that transformed from two-dimensional to three-dimensional due to the bridging effect between the calcium carbonate grown on the neighboring fibers, which enhanced the healing ability of the cracks. • A first work about the complete process of bacterial metabolism is found by SEM test. • Reveal the microcosmic mechanism of MICP technology. • Multiple numbers of fibers change deposition of CaCO 3 from two to three-dimensional to enhance the healing ability. • A new test device is designed to quantitatively measure the depth of healed cracks. • Mortar specimens mixed with biomass self-healing agents and basalt fibers have greater mechanical properties. [ABSTRACT FROM AUTHOR]

• Have an evaluation of weather resistance of different sticky rice paste modified soil including freeze-thaw, temperature and humidity, and Na 2 SO 4 corrosion, and explain the traditional method of adding sticky rice paste into in-situ soil. • Reveal the adhesive and wrapping action between starch molecules of traditional gelatinous sticky rice paste and soil particles. • The gelatinized sticky rice paste compared with other preparation methods of sticky rice paste, has the characteristics of nano-materials and the fluidity quality of colloid and solution, and its modified soil has the superior weather resistance. Effective restoration measures are required to protect earthen sites in historical heritage locations. In this study, sticky rice paste was added to in situ site soils and the water resistance and disintegration of the modified soils were investigated. Further, the influences of freeze–thaw, dry–wet, and Na 2 SO 4 -corrosion cycles on the compressive strength of the modified soil and its morphology were assessed. The results obtained indicate that the modified soil exhibited the highest water resistance and strength after 30 freeze–thaw and dry–wet cycles and 20 Na 2 SO 4 -corrosion cycles. This work is expected to provide future guidance on improved restoration and protection of earthen sites. [ABSTRACT FROM AUTHOR]

Unconventionally high amount of atomic vacancies up to more than 10% are known to form in Ge-Sb-Te crystals upon rapid crystallization from the amorphous phase. Upon thermal annealing, an ordering process of these atomic vacancies is observed, triggering a structural transition from the recrystallized rocksalt structure to a stable layered trigonal structure and a transition from insulator to metal. In this work, we demonstrate an opposite vacancy disordering process upon extensive electron beam irradiation, which is accompanied by the reverse transition from the stable trigonal phase to the metastable cubic phase. The combined in situ transmission electron microscopy experiments and density functional theory nudged elastic band calculations reveal three transition stages, including (I) the vacancy diffusion in the trigonal phase, (II) the change in atomic stacking, and (III) the disappearance of vacancy-rich planes. The mechanism of vacancy disordering is attributed to kinetic knock-on collision effects of the high-energy electron beam, which prevail over the heating effects. Image, graphical abstract [ABSTRACT FROM AUTHOR]

According to the characteristics of earthen sites' erosion and the existing environments of arid and semi-arid zones, this work comes up with the conception of sacrificial layer. Covering the surface of the earthen site with a mud coating layer, similar to the natural materials found at the site, it would provide a protective layer for exogenic forces to destroy, while preserving the earthen site. Experiments were carried out to separately test the shrinkage rate, heat sensitivity, color difference, mechanical properties, vapor permeability, wetting–drying cycle, and rainfall erosion by adding wheat chaff and hemp fibers with different proportions. Experimental results show that wheat chaff and hemp fibers are ideal modified materials for the sacrificial layer with good performance. The optimum proportion of hemp fiber, wheat chaff, and soil was 0.5:1.25:100. The sacrificial layer has broad application prospects to the surfaces of earthen sites in arid and semi-arid zones. [ABSTRACT FROM AUTHOR]

• Properties of rammed interface layers of earthen structures were analyzed. • Tensile and shear strengths of these layers were lower than compressive strength. • The rammed pit interface showed superior properties compared to other types. Layer interfaces are the weakest parts of traditional rammed earthen structures. Different ramming technologies for the interfaces between layers were found to have a significant effect on the level of destruction. Accordingly, four interface treatment methods were simulated to reveal the mechanism and damage mode for the interfaces between different layers: no interface, fine interface, coarse interface and rammed pit interface. Moreover, elastic wave velocity, tensile strength, compressive strength and shear strength tests were performed to explore the effects of different interface treatment technologies on different layers. The results showed that the tensile and shear strengths of the rammed earthen layer interfaces were much lower than the compressive strength. The tensile strength was only 1/30 of the compressive strength, which was the decisive factor in the ultimate destruction of such sites. An effective measure to improve the shear strength of rammed earthen sites is to increase the depth and uniform area of friction of the layer interface, and the roughness of the contact surface between layers. The interface treatment with the rammed pit layer provided superior results to the coarse and fine layers. The abovementioned results provide a theoretical basis for the scientific cognition of traditional ramming and consolidation technologies of earthen sites. [ABSTRACT FROM AUTHOR]

Highlights • Spy1, a unique cell cycle regulator, was decreased in ALS motor neurons. • DNA damage response was activated in SOD1G93A-transfected cells. • Decreased Spy1 expression activated the DNA damage response in SOD1G93A-transfected cells. • Increased Spy1 expression inhibited the DNA damage response in SOD1G93A-transfected cells. • Spy1 played a protective role in ALS motor neurons. Abstract Increasing evidence indicates that DNA damage and p53 activation play major roles in the pathological process of motor neuron death in amyotrophic lateral sclerosis (ALS). Human SpeedyA1 (Spy1), a member of the Speedy/Ringo family, enhances cell proliferation and promotes tumorigenesis. Further studies have demonstrated that Spy1 promotes cell survival and inhibits DNA damage-induced apoptosis. We showed that the Spy1 expression levels were substantially decreased in ALS motor neurons compared with wild-type controls both in vivo and in vitro by qRT-PCR, western blotting, and Immunoassay tests. In addition, we established that over-expression of human SOD1 mutant G93A led to a decreased expression of Spy1. Furthermore, DNA damage response was activated in SOD1G93A-transfected cells (mSOD1 cells). Moreover, decreased Spy1 expression reduced cell viability and further activated the DNA damage response in mSOD1 cells. In contrast, increased Spy1 expression improved cell viability and inhibited the DNA damage response in mSOD1 cells. These results suggest that Spy1 plays a protective role in ALS motor neurons. Importantly, these findings provide a novel direction for therapeutic options for patients with ALS as well as for trial designs, such as investigating the role of oncogenic proteins in ALS. [ABSTRACT FROM AUTHOR]

Graphical abstract Highlights • Recombinant hirudin variant-2 (HV2) was conjugated with palmitic acid (PAL). • The selectivity of this reaction was improved in mixed aqueous-DMSO solution. • Three mono-PAL-HV2 isomers was efficiently separated by prep-HPLC. • Mono-PAL-HV2-3 showed the highest selectivity and the highest in vitro bioactivity. • The modification site of mono-PAL-HV2-3 was identified as Lys 27 of HV2. Abstract In this study, chemical modification of recombinant hirudin variant-2 (HV2) with palmitic acid (PAL) was proposed as an alternative approach to circumvent the limitations of PEGylation. To facilitate a sufficient contact of the hydrophilic HV2 to the hydrophobic PAL, thereby improving the reaction specificity to achieve the desired mono-PAL-HV2 with high retained bioactivity, the reaction was developed in mixed aqueous-organic solutions. Compared with HV2 conjugation with PAL-benzotriazole (PAL-BTA) in mixed aqueous-NMP solution, the conjugation of HV2 with PAL- N -hydroxysuccinimide (PAL-NHS) in mixed aqueous-DMSO solution could improve the site-specific conjugation of one PAL molecule to a particular lysine residue. Furthermore, the reaction mixture of the latter was further purified by preparative liquid chromatography. Three mono-PAL-HV2 isomers were obtained and retained 36%, 4% and 89% of the in vitro anticoagulant activity of unmodified HV2, respectively. One of the mono-PAL-HV2 isomers, namely, mono-PAL-HV2-3, was isolated with the highest selectivity and exhibited the highest in vitro anticoagulant bioactivity. Modification site analysis of mono-PAL-HV2-3 revealed that a single PAL molecule was conjugated at Lys27 of HV2. This study presented a successful PAL modification in which site-specific reaction was improved to achieve the desired mono-PAL-HV2 with highly retained bioactivity in mixed aqueous-organic solutions. [ABSTRACT FROM AUTHOR]

This paper proposes a new design method employed for a practical integration of multistage compression osculating cones waverider and Busemann inlet. The singularity based on Taylor–Maccoll equations for Busemann inlet is vertified to result in the failure to directly integrate mutistage waverider and Busemann inlet. In order to avoid this limitation, a revised transition portion is incorporated into the integration, which achieves the objective to integrate multistage compression waverider with Busemann inlet in geometrical configuration. Aerodynamic characteristics of the integration and a compared three-stage compression osculating cones waverider are compared and analyzed in the same design conditions with the same leading edge of the forebody. The research results show that the integration with a Busemann inlet as its third-stage compression surface has greater lift-to-drag ratio, more uniform airbreathing inflow at the inlet entrance, and greater total pressure recovery coefficient with the same mass flowrate. And the performance can satisfy the requirements of the forebody-inlet compression for hypersonic vehicles. [ABSTRACT FROM AUTHOR]

We report on the use of a sprayable and thermogelating biomaterial (Poloxamer™; a.k.a. Pluronic™) in optical imaging of pH values, local oxygen and temperature. The material is highly biocompatible and easy to handle. We also show that the material is well permeable to oxygen (thus making it a good choice for use in oxygen sensors), and is stable in liquid solution and at elevated temperature. We demonstrate its applicability in optical sensors for oxygen, pH and temperature. This was accomplished by incorporating appropriate luminescent probes in various kinds of microparticles (which act as hosts for the probes and prevent dye leaching and aggregation), and then dispersing the microparticles in the thermogelating polymer. The resulting sensor gels were deposited on the surface of interest via spraying at temperatures of <20 °C. At these temperatures, the gels adhere well to the target, even on uneven surfaces such as skin, wounds, and bacterial cultures. If temperature is risen to above 25 °C, the gels form a thin and soft but solid sensing layer which, however, can be simply removed from surface of interest by cooling and wiping it off, or by washing with water. Sprayable thermogelating sensors present obvious advantages over other sensors by not causing damage to the surface of interest. In our perception, the sensing materials also have wide further applicability in sensors for other species including clinically relevant gases, enzyme substrates (such as glucose or lactate) and ions. [ABSTRACT FROM AUTHOR]

3-Arylfuran-2(5 H )-one derivatives show good antibacterial activity and were determined as tyrosyl-tRNA synthetase (TyrRS) inhibitors. In a systematic medicinal chemistry exploration, we demonstrated chemical opportunities to treat infections caused by Helicobacter pylori . Twenty 3-arylfuran-2(5 H )-ones were synthesized and evaluated for anti- H. pylori , antioxidant and anti-urease activities which are closely interconnected with H. pylori infection. The results displayed that some of the compounds show excellent antioxidant activity, and good anti- H. pylori and urease inhibitory activities. Out of these compounds, 3-(3-methylphenyl)furan-2(5 H )-one ( b9 ) showed the most potent antioxidant activity (IC 50 = 8.2 μM) and good anti- H. pylori activity (MIC 50 = 2.6 μg/mL), and it can be used as a good candidate for discovering novel anti-gastric ulcer agent. [ABSTRACT FROM AUTHOR]

Novel structured triacylglycerols (STAGs) enriched with unsaturated fatty acids (UFAs) and low palmitic acid (PA) content were firstly synthesized from Schizochytrium sp. oil and oleic acid (OA) via solvent-free acidolysis catalyzed by Lipozyme RM IM. The results indicated that, the PA content decreased from 24.49% to 6.95%, while the UFAs content increased from 70.20% to 90.9% at the sn -1,3 positions in the STAGs under the optimal condition (i.e., lipase load of 7%, molar ratio of microalgae oil TAGs to OA of 1:3, and temperature of 65 °C). The lipase Lipozyme RM IM could be reused 16 times without significant loss of activity. The improved plastic and storage ranges of STAGs are useful for infant formula formulations, by which a possible method is blending of this product and 1,3-dioleoyl-2-palmitoylglycerol enriched fats and minor lipids based on the corresponding chemical compositions of human milk fat. [ABSTRACT FROM AUTHOR]

Numerous wolframite–quartz vein type tungsten deposits are present in the Gannan metallogenic belt, South China, including the Piaotang and Dangping deposits in the Chong-You-Yu ore cluster, the Dajishan deposit in the Jiulianshan ore cluster, and the Pangushan deposit in the Yushan ore cluster. The ores generally consist of quartz and wolframite, with variable amounts of base metal sulfides. Wolframite and quartz are intergrown, but the genetic relationships between them are still ambiguous. Quartz contains two-phase aqueous inclusions (type I) and two- or three-phase CO 2 -bearing inclusions (type II), but wolframite only contains two-phase aqueous inclusions (type Iw). The homogenization temperatures for primary inclusions in wolframite are generally 40 to 100 °C higher than those in quartz in a single deposit. Moreover, there are variable amounts of CO 2 in inclusions in quartz, but no CO 2 -rich inclusions are identified in coexisting wolframite. Type I fluid inclusions in quartz from the Piaotang deposit show that fluid mixing is predominant in the formation of quartz veins, whereas fluid inclusions from the Dangping deposit suggest that simple cooling is the primary factor. Quartz from the Dajishan and Pangushan deposits contains both type I and coexisting type II inclusions, indicating a process of fluid immiscibility. The homogenization temperatures of two-phase aqueous inclusions (type Iw) in wolframite from all of these deposits show a clearly decreasing trend with constant salinities, implying a simple cooling process. Hence, simple cooling, fluid mixing, and fluid immiscibility take place in quartz but only simple cooling happens in wolframite. Our results show that the gangue and ore minerals from the Late Mesozoic tungsten deposits in the Gannan metallogenic belt have different homogenization temperatures, volatile compositions, and fluid processes. The gangue minerals do not provide reasonable estimates of the depositional conditions of the ore minerals even though they are intimately intergrown. [ABSTRACT FROM AUTHOR]

Serious loss of polyethylene glycol (PEG) reagent is confronted during PEGylation of proteins in mildly acidic aqueous solution. In this study, a novel approach of PEGylation of recombinant hirudin variant-2 (HV2) with monomethoxy-PEG-succinimidyl carbonate (mPEG-SC) was developed in six mixed aqueous–organic solutions. The PEGylation efficiency in each mixed solutions was greater than that in pure aqueous solution. Structure analysis of HV2, hydrolysis kinetics of mPEG-SC, and PEGylation kinetics of HV2 in different solutions revealed that solvent effects occurred in mixed aqueous–organic solutions. According to the dominant solvent effect of PEGylation acceleration and mPEG-SC hydrolysis inhibition, the selected mixed aqueous–organic solutions could be divided into different types (PEGylation-driven, mPEG-SC hydrolysis-driven, both PEGylation and mPEG-SC hydrolysis-driven). In aqueous-DMSO solutions, the desired yield (approximately 50%) of mono-PEG-HV2 was achieved under the optimized reaction conditions. The optimal usage of PEG reagent could decrease 3–5 fold compared with that of PEGylation in pure aqueous solution. The mono-PEG-HV2 could restore its structure and bioactivity after being purified into aqueous solution. This study demonstrated that PEGylation of proteins in mixed aqueous–organic solutions could be used as an alternative method to PEGylation in pure aqueous solution. [ABSTRACT FROM AUTHOR]

Abstract: 3-Arylfuran-2(5H)-one, a novel antibacterial pharmacophore targeting tyrosyl-tRNA synthetase (TyrRS), was hybridized with the clinically used fluoroquinolones to give a series of novel multi-target antimicrobial agents. Thus, twenty seven 3-arylfuran-2(5H)-one-fluoroquinolone hybrids were synthesized and evaluated for their antimicrobial activities. Some of the hybrids exhibited merits from both parents, displaying a broad spectrum of activity against resistant strains including both Gram-negative and Gram-positive bacteria. The most potent compound (11) in antibacterial assay shows MIC50 of 0.11μg/mL against Multiple drug resistant Escherichia coli, being about 51-fold more potent than ciprofloxacin. The enzyme assays reveal that 11 is a potent multi-target inhibitor with IC50 of 1.15±0.07μM against DNA gyrase and 0.12±0.04μM against TyrRS, respectively. Its excellent inhibitory activities against isolated enzymes and intact cells strongly suggest that 11 deserves to further research as a novel antibiotic. [Copyright &y& Elsevier]

Abstract: Based on a rationally conceived pharmacophore model to build a multi-target bacterial topoisomerase inhibitor, twenty-one fluoroquinolone–flavonoid hybrids were synthesized. Some obtained hybrids show excellent antibacterial activity against drug-resistant microorganisms with narigenin–ciprofloxacin being the most active, showing 8, 43, 23 and 88 times better activity than ciprofloxacin against Escherichia coli ATCC 35218, Bacillus subtilis ATCC 6633, Staphylococcus aureus ATCC 25923 and Candida albicans ATCC 90873, respectively. Drug accumulation and DNA supercoiling assays of two active analogues revealed potent inhibition of both the DNA gyrase and efflux pump, confirming the desired dual mode of action. Molecular docking study disclosed that the introduced flavonoid moiety not only provides several additional interactions but also does not disturb the binding mode of the floxacin moiety. Our data also demonstrated that development of antifungals is possible from fluoroquinolones modified at C-7 position. [Copyright &y& Elsevier]

Abstract: Polystyrene nanoparticles (PSNPs) with an average size of 85nm and loaded with an oxygen-quenchable luminescent ruthenium complex were used to sense and image oxygen inside cells following 2-photon excitation (2-PE). The ruthenium probe possesses a large two-photon absorption cross-section, and 2-PE is achieved by irradiation in the near infrared with commercially available fs-pulsed laser systems. The luminescence of the dye-loaded PSNPs is strongly quenched by oxygen, and Stern–Volmer plots are linear for both conventional single-photon excitation (1-PE) and for 2-PE. The particles do not show any significant cytotoxicity below a threshold concentration of 5μg/mL and are readily taken up by mammalian cells (MCF-7), presumably via membrane mediated pathways. Thus, the PSNPs promise to be well suited to image the oxygen distribution in living cells and tissues. The 2-PE is considered to be advantageous over conventional imaging techniques because it works in the near-infrared where background absorption and luminescence of biomatter is much weaker than at excitation wavelengths below 600nm. [Copyright &y& Elsevier]

Abstract: Total generalized variation (TGV) regularization model is one of the most effective methods for denoising and eliminating staircase effect. However, the TGV regularization model tends to blur edges as the existence of high-order derivative. In order to avoid the staircase effect while alleviating the edge blurring, an iterative reweighted TGV based Poisson noise removal model is presented under the assumption that each pixel of noisy image follows a Poisson distribution. The weight function incorporated in the TGV regularization term is derived from the expectation maximization (EM) algorithm. We design a new iterative weighted primal–dual algorithm, which is an improvement of the classic iterative reweighted algorithm. Numerical experimental results show the better performance of our model in removing noise effectively while preserving edges and eliminating staircase effect. [Copyright &y& Elsevier]

Summary: Lateral thoracic (LT) flaps are primarily used as pedicle flaps for reconstructing limb and chest wall defects and have rarely been applied for head and neck reconstruction. We aimed to present our surgical techniques and experience using free LT cutaneous, myocutaneous and conjoint flaps for oral and maxillofacial reconstruction. From 2006 to 2010, we reconstructed 28 cases of oral and maxillofacial soft tissue defects using LT flaps. Controls were 54 cases reconstructed with anterior forearm flaps during same period. Flap size and pedicle length were recorded intraoperatively. Patients were monitored for flap survival in hospital until discharge and then followed regularly for 3–38 months, assessing for tumor recurrence, flap appearance, donor site function and cosmesis. All patients had free flaps except for one LT pedicle flap. LT flap patients were significantly younger than controls (45.5 vs. 54.8 years, p = 0.004) and had greater flap size than controls (55.2 cm2 vs. 40.3 cm2, p = 0.001). Of 28 LT flaps transferred, 26 survived completely; 1 failed (total necrosis due to venous insufficiency), and 1 suffered tip necrosis. No significant differences were observed in flap survival between groups. Follow-up was shorter in LT flap patients than in controls (20.3 months vs. 26.9 months, p = 0.02). Application of the LT flap is a reliable technique for reconstruction of maxillofacial defects with minimal donor site morbidity and favorable aesthetic outcomes. [Copyright &y& Elsevier]

Abstract: Thirty-eight 3-aryl-4-acyloxyethoxyfuran-2(5H)-ones were designed, prepared and tested for antibacterial activities. Some of them showed significant antibacterial activity against Gram-positive organism, Gram-negative organism and fungus. Out of these compounds, 4-(2-(3-chlorophenylformyloxy)ethoxy)-3-(4-chlorophenyl)furan-2(5H)-one (d40) showed the widest spectrum of activity with MIC50 of 2.0μg/mL against Staphylococcus aureus, 4.3μg/mL against Escherichia coli, 1.5μg/mL against Pseudomonas aeruginosa and 1.2μg/mL against Candida albicans. Our data disclosed that MIC50 values against whole cell bacteria are positive correlation with MIC50 values against tyrosyl-tRNA synthetase. Meanwhile, molecular docking of d40 into S. aureus tyrosyl-tRNA synthetase active site was also performed, and the inhibitor tightly fitting the active site might be an important reason why it has high antimicrobial activity. [Copyright &y& Elsevier]