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In order to investigate the feasibility of in vitro screening the antitumor activity of natural compounds by trypsin, porcine trypsin was used to for screening test, which is marked by inhibition of enzyme activity. Four compounds, namely daidzin, genistin, matrine and oxymatrine, were selected as test subjects. The natural antitumor drug camptothecin was used as the control. The inhibitory effect was detected by two experimental methods: direct detection of trypsin activity inhibition and hydrolysis of bovine serum albumin by trypsin. The results showed the inhibitory effects of the four natural compounds on trypsin, and the inhibition rates of the four natural compounds were significantly different. The enzyme activity assay showed that the inhibitory effect of matrine was better than that of oxymatrine, indicating that trypsin had a good screening resolution. The inhibitory effect was significantly increased with the increased ratio of sample to trypsin, suggesting the structure-activity correlation and dose-effect correlation of the screening methods. Altogether, the experimental method of screening antitumor activity of natural compounds by trypsin has good application values. Since porcine trypsin is similar to human trypsin in terms of molecular structure and performance, it is more applicable for screening of antitumor efficacy of natural pharmacodynamic compounds.

The response of laterally loaded piles installed near the crest of clay slopes is analysed. Three-dimensional finite element analyses are presented for piles at various distances from a slope crest...

Objective To explore the related influencing mechanism of miR-384 and miR-134-5p acting on Yin Yang 1 (YY1) signaling transduction on the biological function of gastric cancer (GC) cells. Methods miR-384, miR-134-5p and YY1 levels in human GC cell lines KATO III, MKN-45, SNU-1 and normal gastric cell line GES-1 were measured by polymerase chain reaction (PCR). Dual luciferase reporter (DLR) gene assay and Western blot (WB) were employed for correlation analysis between miR-384, miR-134-5p and YY1. miR-384-inhibitor, miR-384-mimics, empty plasmid (miRNA-NC) and sh-YY1 were transfected into KATO III cells. Cell proliferation was determined by 3-(4,5-Dimethylthiazolyl-2)-2,5-Diphenyl Tetrazolium Bromide (MTT), cell invasion was measured by Transwell, and apoptosis was analyzed by flow cytometry (FC). Results In KATO III, MKN-45 and SNU-1 cell lines, YY1 was upregulated while miR-384 and miR-134-5p were downregulated (P

Five new Zn(II) coordination polymers, {[Zn2(HBPO)2(phen)2(H2O)2]·H2O}n (1), [Zn2(BPO)(H2BPO)(phen)4]·2(H2BPO)·4H2O (2), {[Zn(HBPO)(4,4′-bipy)0.5]·H2O}n (3), [Zn(HBPO)(dpe)0.5]n (4) and {[Zn2(HBPO)2(dpp)]·H2O}n (5), constructed from mixed ligand; bis(4-carboxylphenyl)phosphinic acid (H3BPO) and N-donor pyridine ligands (phen, 4,4′-bipy, dpe and dpp), have been synthesized and characterized by single crystal X-ray diffraction, IR spectroscopy and elemental analyses. Intermolecular hydrogen bonds, π- π interaction and other intermolecular interaction are effective in stabilization of the crystal structure of these supramolecular complexes. The thermal stability and luminescence properties of compounds 1–5 in the solid state were studied too.

This study aimed at understanding the differences in traits of functional twigs and leaves of a typical alpine shrub species,本研究分析了岷江源区卡卡山典型高山灌丛植物陇蜀杜鹃不同发育阶段(花芽期和开花期)及不同海拔(3600 m低海拔和3800 m高海拔)下功能小枝和叶片性状的差异,以及空间异质性对花芽期和开花期小枝功能性状相关性及其权衡作用的影响。结果表明: 低海拔同一生长期陇蜀杜鹃小枝长度显著大于高海拔,高海拔开花期小枝的花数量和花质量显著高于低海拔。同一海拔花芽期的小枝质量、叶片数量、总叶质量、总叶面积和总叶柄质量均显著大于开花期,单叶质量和单叶柄质量均显著小于开花期。与花芽期相比,开花期叶生物量占比减少了13%,而小枝质量占比显著增加。小枝的生物量权衡表明,花芽期性状倾向于小枝质量,开花期倾向于总叶质量;花芽期的叶偏好分配于单叶质量,低海拔和高海拔开花期叶片分别偏好分配到单叶柄质量和单叶质量。低海拔开花期小枝质量与总叶面积、总叶质量均为异速生长,单叶柄质量和单叶面积为异速生长。海拔和发育阶段共同影响了陇蜀杜鹃功能小枝和叶片的性状。.

Objective To explore the related influencing mechanism of miR-384 and miR-134-5p acting on Yin Yang 1 (YY1) signaling transduction on the biological function of gastric cancer (GC) cells. Methods miR-384, miR-134-5p and YY1 levels in human GC cell lines KATO III, MKN-45, SNU-1 and normal gastric cell line GES-1 were measured by polymerase chain reaction (PCR). Dual luciferase reporter (DLR) gene assay and Western blot (WB) were employed for correlation analysis between miR-384, miR-134-5p and YY1. miR-384-inhibitor, miR-384-mimics, empty plasmid (miRNA-NC) and sh-YY1 were transfected into KATO III cells. Cell proliferation was determined by 3-(4,5-Dimethylthiazolyl-2)-2,5-Diphenyl Tetrazolium Bromide (MTT), cell invasion was measured by Transwell, and apoptosis was analyzed by flow cytometry (FC). Results In KATO III, MKN-45 and SNU-1 cell lines, YY1 was upregulated while miR-384 and miR-134-5p were downregulated (P

Three-dimensional (3D) finite element analysis is used to investigate the vertical and horizontal bearing capacity of internal skirted foundations in normally consolidated uniform clay under undrai...

Two Cd(II) coordination polymers constructed from tris(p-carboxylphenyl)phosphine oxide (H3TPO), [Cd(HTPO)(1,4-bix)·3H2O]n (1) and [Cd2(HTPO)(HBPO)(H2O)2]n (2) (1,4-bix = 1,4-bis(imidazol-1-ylmethy...

Post-traumatic stress disorder (PTSD) is the serious psychiatric disorder. Paeoniflorin (PF) produces the antidepressant-like properties. However, few studies are concerned about its anti-PTSD-like effects and mechanisms. To investigate these, the single prolonged stress (SPS) model was utilized. PTSD-like behavioral deficits in rats after exposure to SPS were improved by PF (10 and 20 mg/kg, i.p.), evidenced by blocking increased freezing time in contextual fear paradigm (CFP) and increased time and entries in open arms in elevated plus maze (EPM) test without affecting the locomotor activity in open field (OF) test. We also found that increased levels of corticosterone (Cort), corticotropin releasing hormone (CRH) and adrenocorticotropic hormone (ACTH) after exposure to SPS were reversed by PF (10 and 20 mg/kg, i.p.) in serum, respectively. Moreover, the decreased levels of serotonin (5-HT) and 5-Hydroxyindoleacetic acid (5-HIAA) in prefrontal cortex and hippocampus were reversed by PF (10 and 20 mg/kg, i.p.), respectively. In summary, the anti-PTSD-like activities of PF were associated with the modulation of HPA axis and 5-HT system activation.

Anxiety disorder is a serious and burdensome psychiatric illness that frequently turn into chronic clinical conditions. Puerarin have been shown to be effective in the therapy of depression. However, few studies are concerned about the anxiolytic-like effects of puerarin. The current study aimed to evaluate the anxiolytic-like effects of puerarin and its possible mechanism. To evaluate this, the behavioral tests, i.e. Vogel-type conflict test (VTCT), elevated plus-maze test (EPMT), and open-field test (OFT) were conducted. Data showed that similar to the positive-control drug sertraline (Ser) (15 mg/kg, i.g.), the anxiolytic-like effects were produced by puerarin (60 and 120 mg/kg, i.g.) in VTCT and EMPT respectively without affecting locomotor activity in OFT. Moreover, the present study also found that consistent with Ser, the levels of allopregnanolone and serotonin (5-HT) in the prefrontal cortex and hippocampus were increased by puerarin (60 and 120 mg/kg, i.g.), respectively. In summary, the present study indicated that puerarin exerted the anxiolytic-like effects, which maybe associated with normalization of 5-HT levels and biosynthesis of allopregnanolone in brain.

Based on the hyperbolic curve tangent modulus method and the wedge stress theory, this paper proposes a calculation method for the settlement of a vertically loaded single pile in sloping ground. By establishing the relationship between the initial tangent modulus and the compression modulus of the slope soil, the tangent modulus of the slope soil is obtained combining with Mindlin-Geddes solution and Hansen formula, and the solution of the pile settlement in sloping ground is derived. Then, a series of numerical analyses are carried out to examine the feasibility of the proposed method. Finally, the effect of parameters is discussed in detail, including the slope angle, the distance of the pile from the slope crest, and the soil properties around the pile. The results show that the pile settlement will increase by increasing the slope angle or decreasing the distance of the pile from the slope crest, and the effect of the two parameters on the pile settlement is coupling-related. Besides, the compression modulus, cohesion, and internal friction angle of the soil around the pile are negatively related to the pile settlement and it is found that the compression modulus of the soil is the more influential parameter.

Histone positioning and modifications on viral genomes are important factors regulating virus replication. To investigate the dynamics of modified histones on the viral genome and their potential roles in antiviral response, we studied the dynamic changes of histone modifications across the HSV-1 genome in THP-1 cells. Histone modifications were detected on the HSV-1 genome soon after infection, including H3K9me3, H3K27me3, H3K4me3 and H3K27ac. These modifications emerged on the viral genome soon after infection and changed rapidly along with virus life cycle progression. The transcription repression marks, H3K9me3 and H3K27me3, decreased on the viral genome during the infection process; the transcription activation mark H3K27ac increased. Treatment with C646, an inhibitor of H3K27ac transferase p300, significantly repressed virus replication and viral gene expression. Our study reveals the relationship between histone modifications and viral gene expression and provides potential novel strategies for antiviral treatment.

In this paper, a method was developed to assess the vertical response of piles considering crushing characteristics. A load transfer model of a pile is built and the relationship between the crushing characteristics and load transfer function of a pile was analyzed. Based on the analysis results, the transfer equation of load function considering the crushing characteristics was derived using the finite difference method. The ideal side resistance and the load transfer mechanism of a pile can be obtained by the transfer equation of load function. The predicted response of piles with the proposed method is in good agreement with the response observed in some pile tests reported in the literature. Further study was conducted to discuss the effect of the parameters related to the load transfer model considering crushing characteristics on the load-settlement response of a single pile.

Post-traumatic stress disorder (PTSD) is a severe psychiatric condition. The allopregnanolone biosynthesis has been implicated as one of the possible contributors to PTSD. Inulin-type oligosaccharides of morinda officinalis (IOMO) had been shown to be effective in the therapy of depression. However, few studies concern the anti-PTSD-like effects of IOMO. To evaluate this, the single prolonged stress (SPS) model was used in the present study. It had been shown that the behavioral deficits of SPS-treated rats were reversed by IOMO (25.0 and 50.0 mg/kg, i.p.), which reversed the increased freezing time in contextual fear paradigm (CFP) and the decreased time and entries in open arms in the elevated plus maze (EPM) test without affecting the locomotor activity in the open field (OF) test. In addition, the decreased allopregnanolone in the prefrontal cortex, hippocampus, and amygdala was reversed by IOMO (25.0 and 50.0 mg/kg, i.p.), respectively. In summary, the present study indicated that the IOMO exert anti-PTSD-like behaviors, which maybe associated with the brain allopregnanolone biosynthesis.

This paper proposes a method for nonlinear analysis of a rigid pile under lateral load at the crest of clay slope. It is assumed that the ultimate soil resistance in front of the pile and behind the pile vary nonlinearly with depth. The modulus of horizontal subgrade reaction in front of the pile and behind the pile vary nonlinearly with the pile displacement at ground surface. The horizontal shear resistance at the pile base is considered and a bilinear relationship between the shear resistance and the displacement is used. Three distribution patterns of the soil resistance along a pile are also considered. Based on the force and moment equilibrium, the system equations are derived for a laterally loaded rigid pile in sloping ground with different soil resistance distribution patterns. The proposed method is validated by comparing its results with those from field tests, finite element analyses and a theoretical method. Finally, the method is used to analyze the effect of slope angle, pile-soil adhesion factor, height above ground surface of point of load application, pile diameter and embedded length on the lateral response of rigid piles.

Post-traumatic stress disorder (PTSD) is a severe psychiatric condition defined as a "trauma and stress-related disorder". Dampened allopregnanolone biosynthesis has been implicated as a possible contributor to PTSD aetiology. Free and Easy Wanderer Plus (FEWP) is a traditional Chinese medicine previously shown to be effective in PTSD treatment. However, little is known about the role of allopregnanolone in the anti-PTSD effects of FEWP. To evaluate this, the single prolonged stress (SPS) model was used in the present study. SPS-induced rats were administered FEWP (at doses of 2.5, 5.0 and 10.0 mg/kg, p.o.) after induction of SPS from days 2 through 15. After exposure to SPS, behavioral assessments were determined, including the open-field test, the contextual fear paradigm, and the elevated plus-maze test. The experimental model rats were decapitated at the end of the behavioral tests and the level of allopregnanolone in the prefrontal cortex, hippocampus and amygdala was measured by enzyme linked immunosorbent assay (ELISA). The behavioral deficits of the SPS-induced rats were significantly reversed by FEWP (at doses of 5.0 and 10.0 mg/kg, p.o.). The level of allopregnanolone was increased by administration of FEWP. In summary, this study indicated that the anti-PTSD effects of FEWP were associated with allopregnanolone biosynthesis.

“Solvent additives” process is a simple and efficient way to achieve high power conversion efficiency in bulk heterojunction organic solar cells. The morphology measurements at the nanoscale confirm that the addition of solvent additives may promote the 3′H-Cyclopropa[8, 25] [5, 6] fullerene-C70-D5 h(6)-3′ -butanoicacid, 3′-phenyl-, methyl ester (PCBM) aggregation in poly(3-hexylthiophene-2,5-diyl) (P3HT: PCBM) blend films. Larger phase separation between P3HT and PCBM caused by solvent additives facilitates the formation of bicontinuous network and therefore charge carriers can transport efficiently to the electrodes. Small angle X-ray scattering was applied to quantify the cluster size of PCBM and the interfacial area between P3HT and PCBM. The results demonstrate that the introduction of solvent additives may enlarge the size of PCBM clusters without decreasing interfacial area. Solvent additives could balance the large interfacial area for exciton dissociation and bicontinuous pathways for carrier transportation. The effect of thermal annealing on the nanomorphology of blend film is also investigated for comparison.

An analytical solution for the seepage field in water-filled karst tunnel is derived based on the inversion of complex function and groundwater hydraulics theory. The solution considers the distance between the tunnel and the cavern, the size of the cavern, and the properties of the lining structure, such as the permeability coefficient as well as the radius of the grouting ring. This paper also performed numerical simulations for two cases: the application of gravity and the absence of gravity. The numerical solution was obtained to verify the analytical solution, and a good agreement was found. Then, the effect of parameters is discussed in detail, including the distance between the tunnel and the cavern, the radius of the cavern, the grouting ring, and the initial support. The results show that when the radius of the cavern is constant, the pressure head and seepage flow decrease as the distance between the tunnel and the cavern increases. When the distance is constant, the pressure head and seepage flow increase with the increase of the radius of the cavern. In addition, the pressure head and the seepage flow decrease with the increase of the thickness of the grouting ring and decrease with the decrease of the permeability coefficient. As the thickness of the initial support increases, the pressure head gradually increases and the percolation decreases. Furthermore, due to the great influence of the grouting ring and initial support on the pressure head and seepage flow, the thickness and permeability coefficient of the grouting ring and initial support should be taken into account carefully during construction.

The present study aimed to investigate the mechanisms underlying the antidepressant-like effects of puerarin via the chronic unpredictable stress (CUS) procedure in rats. Similar to Sertraline (Ser), Chronic treatment of puerarin (60 and 120 mg/kg, i.g) elicited the antidepressant-like effects by reversing the decreased sucrose preference in sucrose preference test (SPT), by blocking the increased latency to feed in novelty-suppressed feeding test (NSFT) and the increased immobility time in forced swimming test (FST) without affecting locomotor activity. However, acute puerarin treatment did not ameliorate the antidepressant- and anxiolytic- like effects in FST and NSFT, respectively. In addition, enzyme linked immunosorbent assay (ELISA) and high performance liquid chromatography-electrochemical detection (HPLC-ECD) showed that chronic treatment of puerarin (60 and 120 mg/kg, i.g) reversed the decreased levels of progesterone, allopregnanolone, serotonin (5-HT) and 5-Hydroxyindoleacetic acid (5-HIAA) in prefrontal cortex and hippocampus of post-CUS rats. Furthermore, puerarin (60 and 120 mg/kg, i.g) blocked the increased corticotropin releasing hormone (CRH), corticosterone (Cort) and adrenocorticotropic hormone (ACTH). Collectively, repeated administration of puerarin alleviated the behavioral deficits induced by chronic stress which was associated with the biosynthesis of neurosteroids, normalization of serotonergic system and preventing HPA axis dysfunction.

Post-traumatic stress disorder (PTSD) has become a major psychiatric and neurological issue. Resveratrol is shown to be effective on depression and anxiety. However, the mechanism of anti-PTSD-like effects of resveratrol remains unknown. The present study aimed to explore the possible molecular and cellular mechanisms underlying the anti-PTSD-like effects of resveratrol. Following a 2-day exposure to inescapable electric foot shocks, animals were administered resveratrol (10, 20, and 40mg/kg, i.g.) during the behavioral tests, which included contextual freezing measurement, elevated plus maze test, staircase test, and open field test. Similar to the positive control drug sertraline (15mg/kg, i.g.), the behavioral deficits of stressed mice were blocked by resveratrol (20 and 40mg/kg, i.g.), which reversed the increased freezing time in contextual freezing measurement and the number of rears in the staircase test and blocked the decrease in time and number of entries in open arms in the elevated plus maze test without affecting the locomotor activity in the open field test. In addition, resveratrol (20 and 40mg/kg, i.g.) antagonized the decrease in the levels of progesterone and allopregnanolone in the prefrontal cortex and hippocampus. Furthermore, long-term resveratrol attenuated the dysfunctions of hypothalamic-pituitary-adrenal axis simultaneously. Collectively, the evidence indicated that the anti-PTSD-like effects of resveratrol were associated with the normalization of biosynthesis of neurosteroids in the brain and prevention of the hypothalamic-pituitary-adrenal axis dysfunction.

In this paper, the response of a rigid pile under a combined load on a cohesionless soil slope is investigated. The ultimate soil resistance in front of piles varies nonlinearly with depth, while both the ultimate soil resistance behind piles and the subgrade reaction modulus vary linearly with depth. The expressions of ultimate soil resistance behind and in front of the pile and the subgrade reaction modulus are determined. In addition, the variation law of the modulus of the subgrade reaction with relative density is also considered. Based on the balance between force and moment, the balance equation of a soil-pile system is derived, and a nonlinear analysis method of a rigid pile under a combined load on a cohesionless soil slope is proposed. The feasibility of this method is verified by the experimental results.

Diabetes mellitus is a chronic disease that is associated with depression. Also, depression is common in adults with type 2 diabetes mellitus (T2DM). Translocator protein (18kDa) (TSPO) and allopregnanolone play an important role in the depression treatment. However, few studies have evaluated TSPO and allopregnanolone in the treatment of depression in T2DM. AC-5216, a ligand for TSPO, produces anxiolytic- and antidepressant-like effects in animal models. The present study aimed to explore antidepressant-like effects of AC-5216 on diabetic rats. Following the development of diabetic model induced by high fat diet (HFD) feeding and streptozotocin (STZ), AC-5216 (0.3 and 1 mg/kg, i.g.) elicited the antidepressant-like effects in behavioral tests while these activities were blocked by TSPO antagonist PK11195 (3 mg/kg, i.p.). The levels of allopregnanolone in the prefrontal cortex and hippocampus were increased by AC-5216 (0.3 and 1 mg/kg, i.g.), which was antagonized by PK11195 (3 mg/kg, i.p.). The increased plasma glucose (PG) and decreased insulin (INS) in HFD-STZ rats were reversed by AC-5216 (0.3 and 1 mg/kg, i.g.). This study indicates that the antidepressant-like effects of AC-5216 on HFD-STZ rats, suggesting that TSPO may represent a novel therapeutic target for depression in T2DM.

Ethnopharmacology relevance Post-traumatic stress disorder (PTSD) is a severe psychiatric disorder that is characterized by symptoms of re-experiencing, avoidance and hyperarousal, as well as social and professional dysfunction at least one month after the exposure to a traumatic event. Biosynthesis of allopregnanolone has been suggested as one of the important contributors to PTSD. Albiflorin (AF) extracted from Radix paeoniae Alba had been shown to be effective in the therapy of depression. However, few studies were concerned about the anti-PTSD-like effects of AF. Aim of the study The current study aimed to evaluate the anti-PTSD-like effects of AF in an animal model and its possible mechanism. Materials and methods To evaluate this, the single prolonged stress (SPS) model was used in the present study. The SPS rats were administered by AF (at doses of 3.5, 7 and 14.0 mg/kg, i.g.) after induction of SPS from days 2–13. After the exposure to SPS, behavioral assessments were conducted, including contextual fear paradigm (CFP), elevated plus-maze test (EPMT), open-field test (OFT). The rats were decapitated at the end of the behavioral tests and levels of allopregnanolone in prefrontal cortex, hippocampus and amygdala were measured by enzyme linked immunosorbent assay (ELISA). Results It had been shown that behavioral deficits of SPS rats were reversed by AF (7.0 and 14.0 mg/kg, i.g.), which attenuated the PTSD-like associated contextual freezing behavior in CFP and improved PTSD-like associated anxiogenic behavior in EPMT without affecting locomotor activity in OFT. Moreover, decreased levels of allopregnanolone in prefrontal cortex, hippocampus, and amygdala were reversed by AF (7.0 and 14.0 mg/kg, i.g.), respectively. Conclusion In summary, the present study indicated that AF exerted the anti-PTSD-like effects, which maybe associated with allopregnanolone biosynthesis in the brain.

The translocator protein (18 kDa) (TSPO) plays an important role in stress-related disorders, such as anxiety, depression and post-traumatic stress disorder (PTSD), caused by neurosteroids (e.g. allopregnanolone). The present study sought to evaluate the significance of TSPO in anxiolytic and antidepressant effects induced by midazolam. The animals were administrated midazolam (0.25, 0.5 and 1 mg/kg, i.p.) and subjected to behavioral tests, including Vogel-type conflict test, elevated plus-maze test, forced swimming test. Midazolam produced anxiolytic- and antidepressant-like effects Vogel-type conflict test (1 mg/kg, i.p.), elevated plus-maze test (0.5 and 1 mg/kg, i.p.), and forced swimming test (0.5 and 1 mg/kg, i.p.). These effects of Midazolam were totally blocked by the TSPO antagonist PK11195 (3 mg/kg, i.p.). To evaluate the role of allopregnanolone in the anxiolytic- and antidepressant-like effects of midazolam, the animals were decapitated at the end of the behavioral tests. The allopregnanolone levels of the prefrontal cortex and hippocampus were measured by enzyme-linked immunosorbent assay (ELISA). The allopregnanolone level of the prefrontal cortex and hippocampus was increased by midazolam (0.5, 1 mg/kg, i.p.) and the increase was reversed by PK11195 (3 mg/kg, i.p.). Overall, the results indicated that the anxiolytic- and antidepressant-like effects of midazolam were mediated by TSPO, via stimulation of allopregnanolone biosynthesis.