Synthesis and antidepressant activity of novel 1-(1-benzoylpiperidin-4-yl) methanamine derivatives selectively targeting SSRI/5-HT1A.

A series of novel 1-(1-benzoylpiperidin-4-yl) methanamine derivatives were synthesized and evaluated for the serotonin reuptake inhibitory abilities and binding affinities to the 5-HT1A receptor. The metabolic stabilities of these compounds were measured in vitro using human or mouse liver microsomes and the antidepressant activities were explored In vivo using the forced swimming test (FST) and tail suspension test (TST) in mice. The results indicated that the compound 12a exhibited strongest serotonin reuptake inhibition (IC50 = 8.2 nM) and marked 5-HT1A receptor affinity (Ki = 0.069 nM), which were significantly superior to lead compounds Ⅰ and Ⅱ. Meanwhile, compound 12a showed good metabolic stability in vitro and exhibited potential antidepressant-like effects in the FST and TST in mice.

Synthesis and biological evaluation of novel antipsychotic trans-4-(2-(1,2,4,5-tetrahydro-3H-benzo[d]azepin-3-yl)ethyl)cyclohexan-1-amine derivatives targeting dopamine/serotonin receptor subtypes.

In this study, a series of trans-4-(2-(1,2,4,5-tetrahydro-3H-benzo[d]azepin-3-yl)ethyl)cyclohexan-1-amine derivatives as potential antipsychotics were synthesized and biologically evaluated to discover potential antipsychotics with good drug target selectivity. The preliminary structure-activity relationship was discussed, and optimal compound 12a showed both nanomolar affinity for D2/D3/5-HT1A/5-HT2A receptors and weak α1 and H1 receptor binding affinity. In addition, 12a was metabolically stable in vitro, displayed micromolar affinity for the hERG channel, and exhibited antipsychotic efficacy in the animal model of locomotor-stimulating effects of phencyclidine.

Synthesis and antidepressant-like activity of novel alkoxy-piperidine derivatives targeting SSRI/5-HT1A/5-HT7.

A series of novel alkoxy-piperidine derivatives were synthesized and evaluated for their serotonin reuptake inhibitory and binding affinities for 5-HT1A/5-HT7 receptors. In vivo antidepressant activities of the selective compounds were explored using the forced swimming test (FST) and tail suspension test (TST) in mice. The results showed that compounds 7a (reuptake inhibition (RUI), IC50 = 177 nM; 5-HT1A, Ki = 12 nM; 5-HT7, Ki = 25 nM) and 15g (RUI, IC50 = 85 nM; 5-HT1A, Ki = 17 nM; 5-HT7, Ki = 35 nM) were potential antidepressant agents in animal behavioral models with high 5-HT1A/5-HT7 receptor affinities and moderate serotonin reuptake inhibition, and good metabolic stability in vitro.

Optically tunable microwave, millimeter-wave and submillimeter-wave utilizing single-mode Fabry-Pérot laser diode subject to optical feedback.

In this paper, we use optical feedback injection technique to generate tunable microwave, millimeter-wave and submillimeter-wave signals using single-mode Fabry-Pérot laser diode. The beat frequency of the proposed generator ranges from 30.4 GHz to 3.40 THz. The peak power ratio between two resonating modes at the output spectrum of can be less than 0.5 dB by judiciously selecting feedback wavelength. In the stabilization test, the peak fluctuation of photonic signal is as low as 0.19 dB within half hour. Aside from locking regions, where the laser is easily locked by the injection beam, the side-mode suppression ratio is well over 25 dB with the maximum value of 36.6 dB at 30.4 GHz beat frequency. In addition, the minimum beat frequency interval between two adjacent photonic signals is as low as 10 GHz.

Proteomic Analysis of the Peritrophic Matrix from the Midgut of Third Instar Larvae, Musca domestica.

OBJECTIVE: To better comprehend the molecular structure and physiological function of the housefly larval peritrophic matrix (PM), a mass spectrometry approach was used to investigate the PM protein composition. METHODS: The PM was dissected from the midgut of the third instar larvae, and protein extracted from the PM was evaluated using SDS-PAGE. A 1D-PAGE lane containing all protein bands was cut from top to bottom, the proteins in-gel trypsinised and analysed via shotgun liquid chromatography- tandem mass spectrometry (LC-MS/MS). RESULTS: In total, 374 proteins, with molecular weights varying from 8.225 kD to 996.065 kD and isoelectric points ranging from 3.83 to 11.24 were successfully identified, most identified proteins were mainly related to immunity, digestion, nutrient metabolism and PM structure. Furthermore, many of these proteins were functionally associated with pattern binding, polysaccharide binding, structural constituent of peritrophic membrane and chitin binding, according to Gene Ontology annotation. CONCLUSION: The PM protein composition, which provides a basis for further functional investigations of the identified proteins, will be useful for understanding the housefly larval gut immune system and may help to identify potential targets and exploit new bioinsecticides.

In vivo study of pedicle screw augmentation using bioactive glass in osteoporosis sheep.

STUDY DESIGN: Augmentation of pedicle screws with bioactive glass (BG) was performed in osteoporotic ovine spine in vivo. Biomechanical tests, micro-computed tomography (CT) analysis, and histologic observation were performed. OBJECTIVE: To investigate the biomechanical stability of pedicle screws augmented by BG in osteoporotic sheep and observe the bone-screw interface histologically. SUMMARY OF BACKGROUND DATA: There is little information on the long-term biomechanical performance and screw-bone interfacial bonding of pedicle screws augmented with BG in osteoporotic spine in vivo. METHODS: Twelve months after ovariectomy combined with methylprednisolone injection, 8 adult female sheep were randomly divided into 2 groups (3- and 6-mo time point groups). In each time point group, pedicles were randomly selected from the lumbar spine (L1-L6) and implanted with (1) pedicle screw alone; (2) pedicle screw augmented by polymethylmethacrylate; or (3) pedicle screw augmented by BG. Three and 6 months after implantation, animals were labeled with tetracycline and calcein before being killed. Then vertebrae with pedicle screws were obtained, and a micro-CT scan, histologic analysis, and biomechanical tests were performed. RESULTS: Three months after implantation, micro-CT reconstruction showed that microstructural parameters of the BG group were significantly better compared with those in the other 2 groups (P<0.05). Histologic observation revealed that bone trabeculae around the screws in the BG group were more in number and denser than those in the control group. The average mineral apposition rate of the bone in the BG group was also higher than that in the other 2 groups (P<0.05). The mechanical properties in the BG group were also significantly higher than that in the control group. Six months after implantation, similar results except mineral apposition rate can be obtained among different groups. CONCLUSIONS: BG can significantly improve bone microstructure of the interface in osteoporosis condition and increase the hold strength of the pedicle screw.

[Tissue localization and expression difference of endogenous beta-glucosidase in digestive system of Musca domestica third instar larvae].

OBJECTIVE: To study the tissue localization and expression difference of endogenous beta-glucosidase in digestive system of Musca domestica third instar larvae. METHODS: The digestive system of the 3rd instar larvae of Musca domestic was taken for the below tests. Tissue localization of endogenous beta-glucosidase mRNA was identified by in situ hybridization. Cellulase was localized by immunohistochemistry. The enzymatic activity of beta-glucosidase was measured by 3, 5-dinitrosalicylic acid(DNS) assay. The relative mRNA expression levels of M. domestica beta-glucosidase gene in these organs were determined by RT-PCR. RESULTS: Beta-glucosidase mRNA, with in situ hybridization, was shown in the epithelial cells of midgut, salivary glands and foregut of the larvae. The immunohistochemical analysis on larvae tissues revealed that cellulase was produced and secreted by the epithelial cells of the midgut, salivary glands and foregut. beta-glucosidase activity in salivary glands, foregut, midgut, and hindgut was (0.80 +/- 0.06), (0.38 +/- 0.02), (1.20 +/- 0.05) and (0.26 +/- 0.02) IU/mg, respectively. There was significant difference in beta-glucosidase activity among these digestive organs (P < 0.05). The activity level of beta-glucosidase was highest in midgut [(45.45 +/- 1.27)%], and lowest in hindgut [(9.85 +/- 0.88)%]. However, beta-glucosidase gene were only expressed in the salivary gland, foregut and midgut. Significant differences in gene expression level of beta-glucosidase was found among these organs (P < 0.05). The relative expression quantity of beta-glucosidase gene in midgut and salivary glands were 5 and 3 times higher than that in foregut. CONCLUSION: The endogenous beta-glucosidase gene is expressed in the foregut, midgut and salivary glands. The midgut and salivary glands of Musca domestica 3rd instar larvae are the primary organs of this enzyme secretion.

Using dashboards to verify coronavirus (COVID-19) vaccinations can reduce fatality rates in countries/regions: Development and usability study.

BACKGROUND: The new coronavirus disease 2019 (COVID-19) pandemic is raging worldwide. The administered vaccination has become a significant vehicle against the virus. Three hypotheses were made and required for validation: the number of vaccines administered is related to the country gross domestic product (GDP), vaccines can reduce the fatality rate (FR), and dashboards can present more meaningful information than traditionally static visualizations. Research data were downloaded from the GitHub website. The aims of this study are to verify that the number of vaccination uptakes is related to the country GDP, that vaccines can reduce FR, and that dashboards can provide more meaningful information than traditionally static visualizations. METHODS: The COVID-19 cumulative number of confirmed cases (CNCCs) and deaths were downloaded from the GitHub website for countries/regions on November 6, 2021. Four variables between January 1, 2021, and November 6, 2021, were collected, including CNCCs and deaths, GDP per capita, and vaccine doses administered per 100 people (VD100) in countries/regions. We applied the Kano model, forest plot, and choropleth map to demonstrate and verify the 3 hypotheses using correlation coefficients (CC) between vaccination and FRs. Dashboards used to display the vaccination effects were on Google Maps. RESULTS: We observed that the higher the GDP, the more vaccines are administered (Association = 0.68, t = 13.14, P < .001) in countries, the FR can be reduced by administering vaccinations that are proven except for the 4 groups of Asia, Low income, Lower middle income, and South America, as well as the application (app) with dashboard-type choropleth map can be used to show the comparison of vaccination rates for countries/regions using line charts. CONCLUSION: This research uses the Kano map, forest plot, and choropleth map to verify the 3 hypotheses and provides insights into the vaccination effect against the FR for relevant epidemic studies in the future.

Trend and prediction of citations on the topic of neuromuscular junctions in 100 top-cited articles since 2001 using a temporal bar graph: A bibliometric analysis.

BACKGROUND: A neuromuscular junction (NMJ) (or myoneural junction) is a chemical synapse between a motor neuron (MN) and a muscle fiber. Although numerous articles have been published, no such analyses on trend or prediction of citations in NMJ were characterized using the temporal bar graph (TBG). This study is to identify the most dominant entities in the 100 top-cited articles in NMJ (T100MNJ for short) since 2001; to verify the improved TBG that is viable for trend analysis; and to investigate whether medical subject headings (MeSH terms) can be used to predict article citations. METHODS: We downloaded T100MNJ from the PubMed database by searching the string ("NMJ" [MeSH Major Topic] AND ("2001" [Date - Modification]: "2021" [Date - Modification])) and matching citations to each article. Cluster analysis of citations was performed to select the most cited entities (e.g., authors, research institutes, affiliated countries, journals, and MeSH terms) in T100MNJ using social network analysis. The trend analysis was displayed using TBG with two major features of burst spot and trend development. Next, we examined the MeSH prediction effect on article citations using its correlation coefficients (CC) when the mean citations in MeSH terms were collected in 100 top-cited articles related to NMJ (T100NMJs). RESULTS: The most dominant entities (i.e., country, journal, MesH term, and article in T100NMJ) in citations were the US (with impact factor [IF] = 142.2 = 10237/72), neuron (with IF = 151.3 = 3630/24), metabolism (with IF = 133.02), and article authored by Wagh et al from Germany in 2006 (with 342 citing articles). The improved TBG was demonstrated to highlight the citation evolution using burst spots, trend development, and line-chart plots. MeSH terms were evident in the prediction power on the number of article citations (CC = 0.40, t = 4.34). CONCLUSION: Two major breakthroughs were made by developing the improved TBG applied to bibliographical studies and the prediction of article citations using the impact factor of MeSH terms in T100NMJ. These visualizations of improved TBG and scatter plots in trend, and prediction analyses are recommended for future academic pursuits and applications in other disciplines.

Using the alluvial plot to visualize the network characteristics of 100 top-cited articles on attention-deficit/hyperactivity disorder (ADHD) since 2011: Bibliometric analysis.

BACKGROUND: Attention-deficit/hyperactivity disorder (ADHD) is a common neuro developmental disorder that affects children and adolescents. It is estimated that the prevalence of ADHD is 7.2% throughout the world. There have been a number of articles published in the literature related to ADHD. However, it remains unclear which countries, journals, subject categories, and articles have the greatest influence. The purpose of this study was to display influential entities in 100 top-cited ADHD-related articles (T100ADHD) on an alluvial plot and apply alluvial to better understand the network characteristics of T100ADHD across entities. METHODS: Using the PubMed and Web of Science (WoS) databases, T100ADHD data since 2011 were downloaded. The dominant entities were compared using alluvial plots based on citation analysis. Based on medical subject headings (MeSH terms) and research areas extracted from PubMed and WoS, social network analysis (SNA) was performed to classify subject categories. To examine the difference in article citations among subject categories and the predictive power of MeSH terms on article citations in T100ADHD, one-way analysis of variance and regression analysis were used. RESULTS: The top 3 countries (the United States, the United Kingdom, and the Netherlands) accounted for 75% of T100ADHD. The most citations per article were earned by Brazil (=415.33). The overall impact factor (IF = citations per 100) of the T100ADHD series is 188.24. The most cited article was written by Polanczyk et al from Brazil, with 772 citations since 2014. The majority of the articles were published and cited in Biol Psychiatry (13%; IF = 174.15). The SNA was used to categorize 6 subject areas. On the alluvial plots, T100ADHD's network characteristics were successfully displayed. There was no difference in article citations among subject categories (F = 1.19, P = .320). The most frequently occurring MeSH terms were physiopathology, diagnosis, and epidemiology. A significant correlation was observed between MeSH terms and the number of article citations (F = 25.36; P < .001). CONCLUSION: Drawing the alluvial plot to display network characteristics in T100ADHD was a breakthrough. Article subject categories can be classified using MeSH terms to predict T100ADHD citations. Bibliometric analyses of 100 top-cited articles can be conducted in the future.

Using the forest plot to compare citation achievements in bibliographic and meta-analysis studies since 2011 using data on PubMed Central: A retrospective study.

BACKGROUND: We saw a steady increase in the number of bibliographic studies published over the years. The reason for this rise is attributed to the better accessibility of bibliographic data and software packages that specialize in bibliographic analyses. Any difference in citation achievements between bibliographic and meta-analysis studies observed so far need to be verified. In this study, we aimed to identify the frequently observed MeSH terms in these 2 types of study and investigate whether the highlighted MeSH terms are strongly associated with one of the study types. METHODS: By searching the PubMed Central database, 5121 articles relevant to bibliometric and meta-analysis studies were downloaded since 2011. Social network analysis was applied to highlight the major MeSH terms of quantitative and statistical methods in these 2 types of studies. MeSH terms were then individually tested for any differences in event counts over the years between study types using odds of 95% confidence intervals for comparison. RESULTS: In these 2 studies, we found that the most productive countries were the United States (19.9%), followed by the United Kingdom (8.8%) and China (8.7%); the most number of articles were published in PLoS One (2.9%), Stat Med (2.5%), and Res Synth (2.4%); and the most frequently observed MeSH terms were statistics and numerical data in bibliographic studies and methods in meta-analysis. Differences were found when compared to the event counts and the citation achievements in these 2 study types. CONCLUSION: The breakthrough was made by developing a dashboard using forest plots to display the difference in event counts. The visualization of the observed MeSH terms could be replicated for future academic pursuits and applications in other disciplines using the odds of 95% confidence intervals.

Comprehensive Assessment of Eutrophication in Xiamen Bay and Its Implications for Management Strategy in Southeast China.

The eutrophication of coastal water has been a critical environmental problem in China's offshore areas. How to effectively assess the status of coastal waters is key for pollution treatment and environmental protection. In recent years, eutrophication-symptom-based and multi-indicator methods, termed "phase II" methods, have been gradually adopted to assess the eutrophication status in some coastal waters in China and have achieved success. The cumulative quantile is typically selected to determine the characteristic value of an indicator in "phase II" methods. The influence of small-scale damaged water bodies on eutrophication assessment may be exaggerated, which often leads to the overassessment of the eutrophication status. In this study, the area ratio method was integrated into the assessment of the estuarine trophic status (ASSETS) method in order to assess the eutrophication status of Xiamen Bay in 2016. The results indicated that, in 2016, the eutrophication status of Xiamen Bay coastal waters was moderate and exhibited spatiotemporal variation. The area ratio method can effectively reduce the effect of small-scale coastal waters with extremely high eutrophication on the overassessment of eutrophication at the broader scale, allowing the eutrophication status to be better reflected, even with limited observation data. The centralized distribution of pollution sources and poor hydrodynamic conditions are the main reasons for the aforementioned phenomenon. Controlling the pollution discharge from the Jiulong River in flood seasons is key to reducing eutrophication in Xiamen coastal waters.

Functional and expression characteristics identification of Phormicins, novel AMPs from Musca domestica with anti-MRSA biofilm activity, in response to different stimuli.

Antibiotic-resistant bacteria (including MRSA) in the clinic pose a growing threat to public health, and antimicrobial peptides (AMPs) have great potential as efficient treatment alternatives. Houseflies have evolved over long periods in complex, dirty environments, developing a special immune system to overcome challenges in harmful environments. AMPs are key innate immune molecules. Herein, two differentially expressed AMPs, Phormicins A and B, were identified by screening transcriptomic changes in response to microbial stimulation. Structural mimic assays indicated that these AMPs exhibited functional divergence due to their C-terminal features. Expression analysis showed that they had different expression patterns. Phormicin B had higher constitutive expression than Phormicin A. However, Phormicin B was sharply downregulated, whereas Phormicin A was highly upregulated, after microbial stimulation. The MIC, MBC and time-growth curves showed the antibacterial spectrum of these peptides. Crystal violet staining and SEM showed that Phormicin D inhibited MRSA biofilm formation. TEM suggested that Phormicin D disrupted the MRSA cell membrane. Furthermore, Phormicin D inhibited biofilm formation by downregulating the expression of biofilm-related genes, including altE and embp. Therefore, housefly Phormicins were functionally characterized as having differential expression patterns and antibacterial & antibiofilm activities. This study provides a new potential peptide for clinical MRSA therapy.

An Immune Risk Score Predicts Survival of Patients with Acute Myeloid Leukemia Receiving Chemotherapy.

PURPOSE: Prediction models for acute myeloid leukemia (AML) are useful, but have considerable inaccuracy and imprecision. No current model includes covariates related to immune cells in the AML microenvironment. Here, an immune risk score was explored to predict the survival of patients with AML. EXPERIMENTAL DESIGN: We evaluated the predictive accuracy of several in silico algorithms for immune composition in AML based on a reference of multi-parameter flow cytometry. CIBERSORTx was chosen to enumerate immune cells from public datasets and develop an immune risk score for survival in a training cohort using least absolute shrinkage and selection operator Cox regression model. RESULTS: Six flow cytometry-validated immune cell features were informative. The model had high predictive accuracy in the training and four external validation cohorts. Subjects in the training cohort with low scores had prolonged survival compared with subjects with high scores, with 5-year survival rates of 46% versus 19% (P < 0.001). Parallel survival rates in validation cohorts-1, -2, -3, and -4 were 46% versus 6% (P < 0.001), 44% versus 18% (P = 0.041), 44% versus 24% (P = 0.004), and 62% versus 32% (P < 0.001). Gene set enrichment analysis indicated significant enrichment of immune relation pathways in the low-score cohort. In multivariable analyses, high-risk score independently predicted shorter survival with HRs of 1.45 (P = 0.005), 2.12 (P = 0.004), 2.02 (P = 0.034), 1.66 (P = 0.019), and 1.59 (P = 0.001) in the training and validation cohorts, respectively. CONCLUSIONS: Our immune risk score complements current AML prediction models.

[Effects of limb ischemia preconditioning on pulmonary free radicals and cytokine levels in a rabbit model of lung ischemia-reperfusion injury].

OBJECTIVE: To study the effects of limb ischemia preconditioning on pulmonary free radicals and cytokine levels during lung ischemia-reperfusion injury in rabbits. METHODS: Eighteen healthy rabbits were randomly divided into three groups: control group (group C, n = 6), ischemia/reperfusion group (group I/R, n = 6), limb ischemia preconditioning group (group L, n = 6). At the end of experiments, the wet to dry-weight ratio (W/D), activities of superoxide dismutase (SOD) and myeloperoxidase (MPO), levels of malondialdehyde (MDA) and the contents of cytokines (TNF-α, IL-6, IL-8 and IL-10) were determined in lung tissues. Protein levels of bronchoalveolar lavage fluid and serum were measured to calculate the lung permeability index. Pathologic changes of lung tissues were also observed. RESULTS: Compared to the group I/R, the lung tissue W/D ratio, MPO activity, lung permeability index, MDA and the cytokines (TNF-α, IL-6 and IL-8) levels were significantly decreased in group L (P < 0.05), while the SOD activity (P < 0.05) and IL-10 contents were significantly increased (P < 0.01). There was no statistical difference in the changes of the above parameters between group L and group C (P > 0.05). The morphologic damages were significantly reduced in group L than that in group I/R. CONCLUSION: Limb ischemia preconditioning has protective effect against lung ischemia-reperfusion injury, which may at least in part through inhibiting the release of oxygen-derived free radicals and pro-inflammatory cytokines (TNF-α, IL-6, IL-8) and increasing the production of anti-inflammatory cytokine IL-10.

Optimization of hepatobiliary phase delay time of Gd-EOB-DTPA-enhanced magnetic resonance imaging for identification of hepatocellular carcinoma in patients with cirrhosis of different degrees of severity.

AIM: To optimize the hepatobiliary phase delay time (HBP-DT) of Gd-EOB-DTPA-enhanced magnetic resonance imaging (GED-MRI) for more efficient identification of hepatocellular carcinoma (HCC) occurring in different degrees of cirrhosis assessed by Child-Pugh (CP) score. METHODS: The liver parenchyma signal intensity (LPSI), the liver parenchyma (LP)/HCC signal ratios, and the visibility of HCC at HBP-DT of 5, 10, 15, 20, and 25 min (i.e., DT-5, DT-10, DT-15, DT-20, and DT-25 ) after injection of Gd-EOB-DTPA were collected and analyzed in 73 patients with cirrhosis of different degrees of severity (including 42 patients suffering from HCC) and 18 healthy adult controls. RESULTS: The LPSI increased with HBP-DT more significantly in the healthy group than in the cirrhosis group (F = 17.361, P < 0.001). The LP/HCC signal ratios had a significant difference (F = 12.453, P < 0.001) among various HBP-DT points, as well as between CP-A and CP-B/C subgroups (F = 9.761, P < 0.001). The constituent ratios of HCC foci identified as obvious hypointensity (+++), moderate hypointensity (++), and mild hypointensity or isointensity (+/-) kept stable from DT-10 to DT-25: 90.6%, 9.4%, and 0.0% in the CP-A subgroup; 50.0%, 50.0%, and 0.0% in the CP-B subgroup; and 0.0%, 0.0%, and 100.0% in the CP-C subgroup, respectively. CONCLUSION: The severity of liver cirrhosis has significant negative influence on the HCC visualization by GED-MRI. DT-10 is more efficient and practical than other HBP-DT points to identify most of HCC foci emerging in CP-A cirrhosis, as well as in CP-B cirrhosis; but an HBP-DT of 15 min or longer seems more appropriate than DT-10 for visualization of HCC in patients with CP-C cirrhosis.

[Study on immunological effect of housefly protein in mice].

OBJECTIVE: To study the immunological effect of the housefly protein in mice. METHODS: The housefly protein was given orally in normal and Cyclophosphamide (CY) immunosuppressive mice, and then the indexes of the clearance rate of carbon particles and the serum hemolysin against SRBC were detected. RESULTS: The housefly protein could increase HC50 significantly in the normal mice, but could not in the CY immunosppressive mice. It could increase phagocytic index significantly in the normal mice, but could not in the CY immunosuppressive mice. CONCLUSION: The results suggest that the housefly protein can promote humoral immunity functions of normal mice. It has distinct preventive and cure effect on the CY immunosuppressive.

[Isolation and purification of antibacterial peptides from the larvae secretion of housefly and the characteristics].

OBJECTIVE: To isolate and purify the antibacterial peptides from larvae secretion of housefly (Musca domestica) and study their partial characteristics. METHODS: Protein isolation and purification were performed by routine process, namely, ultrafiltration, solid phase extraction (SPE) and reversed-phase high-performance liquid chromatography (RP-HPLC). The minimal inhibitory concentration (MIC) and minimal bactericidal concentration (MBC) of the antibacterial peptides were examined. The antibacterial effect of peptides was studied in nutritive medium with different pH value(pH 5.0-10.0), divalent cations (Mg2+: (0.5 x 10(-3) - 10.0 x 10(-3))mol/L, Na+, K+: (10 x 10(-3) - 100 x 10(-3))mol/L), and serum content (12.5%-75%). RESULTS: Molecular weight of the peptides was about Mr 3 000-30 000 after ultrafiltration. The fractions eluted with 20%, 30%, 70%, and 80% of acetonitrile (ACN) all showed antibacterial activity by solid phase extraction. The fractions eluted with 70% ACN showed strongest and stable st antibacterial activity which was further purified by RP-HPLC. Two sub-fractions appeared at around RT 15.5 min and 18.5 min were obtained with antibacterial activity. The MIC to those standard Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus, and Bacillus subtilis was 32.7380, 16.3688, 65.4750 and 32.7380 microg/ml respectively. In the nutritive medium of pH 6.0-9.0, different divalent cations and serum content, the increment of A570 in experiment groups was less than 0.05, while that of the control group was greater than 0.3 (P<0.01). CONCLUSION: SPE and RP-HPLC have been effective in purifying the antibacterial peptides which show strong activity in different conditions.

[Pattern of electrogastrogram in healthy neonates].

OBJECTIVE: To investigate the electrogastrogram (EGG) characteristics of healthy neonates. METHODS: Twenty healthy neonates born at 37-39 weeks of gestation (11 males and 9 females, Apagar's score 9.3 +/- 0.4) were enrolled in this study. EGG recordings were performed for half an hour pre- and postprandially at an interval of a week from birth until age 4 weeks. The EEG variables measured included the percentage of normal gastric rhythm, the percentage of tachygastria and bradygastria, the fed-to-fasting ratio of the EEG dominant power, as well as the EEG dominant frequency and its instability coefficient. The paired sample t test (95% CI) was used to compare the recordings. RESULTS: Between birth and age 28 days, the percentage of normal gastric rhythm ranged from 38.2 +/- 4.9% to 39.7 +/- 3.5% of recorded time, tachygastria was observed in the range of 23.7 +/- 5.4% to 23.5 +/- 4.3% of recorded time, and bradygastria was shown to be in the range of 38.1 +/- 5.5% to 36.8 +/- 3.9% of recorded time in the 20 neonates before meal. Statistically significant differences were not seen in neonates with different ages as well as during pre- and postprandial periods. The EEG dominant frequency of neonates before meal was 2.38 +/- 0.5, 2.43 +/- 0.2, 2.54 +/- 0.3, 2.57 +/- 0.2 and 2.59 +/- 0.1 cpm at birth and at postnatal age of 7, 14, 21 and 28 days respectively. There were no significant differences in the dominant frequency and the coefficient of instability of the dominant frequency during pre- and postprandial periods. The EEG dominant frequency at postnatal age of 14, 21 and 28 days during pre- and postprandial periods was significantly higher than that at birth and at postnatal age of 7 days (P < 0.05). The coefficient of instability of the dominant frequency at postnatal age of 21 and 28 days was significantly lower than that at birth and at postnatal age of 7 and 14 days (P < 0.05). There were no statistically significant differences in the fed-to-fasting ratio of EGG dominant power in neonates with different ages. CONCLUSIONS: The pattern of electrical activity in the normal neonatal stomach appears to be different from that demonstrated in adults and children. The percentage of normal gastric rhythm is lower, and tachygastria and bradygastria are more frequently seen. The EEG dominant frequency increases with postnatal age in neonates.

[Synergistic Killing Effects of Arsenic Trioxide Combined with Itraconazole on KG1a Cells].

OBJECTIVE: To explore the effect of arsenic trioxide combined with itraconazole on proliferation and apoptosis of KG1a cells and its potential mechanism. METHODS: The cell morphology was observed with Wrighe-Giemsa staining; cell survival rate was examined by CCK-8; and colony formation capacity was measured by methylcellulose colony formation test; the flow cytometry was used to analyse the cell apoptosis rate and cell cycle; the protein expressions of BCL-2,caspase-3,BAX,SMO,Gli1 and Gli2 were detected by Western-blot. RESULTS: The arsenic trioxide and itraconazole alone both could inhibit the KG1a cell proliferation in dose-and time-dependent manner. In comparison between single and combined drug-treatment group, both the cell survival rate and the colony number of the single drug-treatment group were significantly lower(P<0.05), and the apoptosis rate was higher in the combined drug-treatment group. In the combined-treatment group, the protein expression of Caspase-3 and BAX was upregulated, while the protein expression of BCL-2,SMO,Gli1 and Gli2 was downregulated. CONCLUSION: Arsenic trioxide combined with itraconazole can inhibit the KG1a cell proliferation and induce apoptosis, which may be related with the inhibition of Hh signaling pathway and upregulation of both Caspase-3 and BAX protein expression, and provided experimental data of arsenic trioxide combined with itraconazole for the treatment of refractory AML.