Design, synthesis, X-ray crystal structure, and antimicrobial evaluation of novel quinazolinone derivatives containing the 1,2,4-triazole Schiff base moiety and an isopropanol linker.

A series of novel quinazolinone derivatives (E1-E31) containing the 1,2,4-triazole Schiff base moiety and an isopropanol linker were designed, synthesized and assessed as antimicrobial agents in agriculture. All the target compounds were fully characterized by 1 H NMR, 13 C NMR, and high-resolution mass spectrometry (HRMS). Among them, the structure of compound E12 was further confirmed via single crystal X-ray diffraction method. The experimental results indicated that many compounds displayed good in vitro antibacterial efficacies against the tested phytopathogenic bacteria including Xanthomonas oryzae pv. oryzae (Xoo), Xanthomonas axonopodis pv. citri (Xac), and Ralstonia solanacearum (Rs). For example, compounds E3, E4, E10, E13, and E22 had EC50 (half-maximal effective concentration) values of 55.4, 39.5, 49.5, 53.5, and 57.4 µg/mL against Xoo, respectively, superior to the commercialized bactericide Bismerthiazol (94.5 µg/mL). In addition, the antibacterial efficacies of compounds E10 and E13 against Xac were about two times more effective than control Bismerthiazol, in terms of their EC50 values. Last, the antifungal assays showed that compounds E22 and E30 had the inhibition rates of 52.7% and 54.6% at 50 µg/mL against Gibberella zeae, respectively, higher than the commercialized fungicide Hymexazol (48.4%).

Associations between serum ferritin, iron, and liver transaminases in adolescents: a large cross-sectional study.

Introduction: Introduction: few previous studies suggest that serum iron status may be associated with liver function, but the relevant evidence remains limited, especially in adolescents. Objective: we aimed to investigate the association between serum ferritin, iron, and liver transaminases in adolescents. Methods: a cross-sectional study including 3,404 adolescents aged 10-19 was performed based on the National Health and Nutrition Examination Survey. Weighted multivariate regression, subgroup analysis, and sensitivity analysis were used. Results: a total of 3,404 adolescents were eventually included. Serum ferritin and iron were positively correlated to alanine aminotransferase (ALT) and aspartate aminotransferase (AST). The association between serum ferritin and ALT remained positive in all genders and races, but only remained positive in girls and several races between serum ferritin and AST. The positive correlations kept present among girls between serum iron and ALT, and also kept present among girls and non-Hispanic whites between serum iron and AST. Additionally, serum ferritin and iron were also positively correlated to elevated ALT and elevated AST using binary logistic regression analysis. After excluding the subjects with serum ferritin levels above the upper limit of normal, the main results remained the same basically. Conclusion: the present results add novel evidences about the associations between serum ferritin, iron, and liver transaminases, which requires more confirmatory studies.

Introducción: Introducción: pocos estudios previos sugieren que el estado del hierro sérico pueda estar asociado con la función hepática, pero la evidencia relevante sigue siendo limitada, especialmente en adolescentes. Objetivo: nuestro objetivo fue investigar la asociación entre la ferritina sérica, el hierro y las transaminasas hepáticas en adolescentes. Métodos: se realizó un estudio transversal que incluyó a 3,404 adolescentes de diez a 19 años de edad, basado en la Encuesta Nacional de Examen de Salud y Nutrición. Se utilizaron la regresión multivariada ponderada, el análisis de subgrupos y el análisis de sensibilidad. Resultados: finalmente, se incluyó un total de 3.404 adolescentes. La ferritina sérica y el hierro se correlacionaron positivamente con la alanina aminotransferasa (ALT) y la aspartato aminotransferasa (AST). La asociación entre ferritina sérica y ALT se mantuvo positiva en todos los géneros y razas, pero solo se mantuvo positiva en niñas y en varias razas entre ferritina sérica y AST. Las correlaciones positivas siguieron presentes en las niñas entre el hierro sérico y la ALT, y también en las niñas y personas blancas no hispanas entre el hierro sérico y la AST. Además, la ferritina sérica y el hierro también se correlacionaron positivamente con ALT elevada y AST elevada mediante análisis de regresión logística binaria. Después de excluir a los sujetos con niveles de ferritina sérica por encima del límite superior de la normalidad, los resultados principales se mantuvieron básicamente iguales. Conclusión: los presentes resultados agregan evidencias novedosas sobre las asociaciones entre la ferritina sérica, el hierro y las transaminasas hepáticas, lo que requiere más estudios confirmatorios.

A two-stage method for automated detection of ring-like endosomes in fluorescent microscopy images.

Endosomes are subcellular organelles which serve as important transport compartments in eukaryotic cells. Fluorescence microscopy is a widely applied technology to study endosomes at the subcellular level. In general, a microscopy image can contain a large number of organelles and endosomes in particular. Detecting and annotating endosomes in fluorescence microscopy images is a critical part in the study of subcellular trafficking processes. Such annotation is usually performed by human inspection, which is time-consuming and prone to inaccuracy if carried out by inexperienced analysts. This paper proposes a two-stage method for automated detection of ring-like endosomes. The method consists of a localization stage cascaded by an identification stage. Given a test microscopy image, the localization stage generates a voting-map by locally comparing the query endosome patches and the test image based on a bag-of-words model. Using the voting-map, a number of candidate patches of endosomes are determined. Subsequently, in the identification stage, a support vector machine (SVM) is trained using the endosome patches and the background pattern patches. Each of the candidate patches is classified by the SVM to rule out those patches of endosome-like background patterns. The performance of the proposed method is evaluated with real microscopy images of human myeloid endothelial cells. It is shown that the proposed method significantly outperforms several state-of-the-art competing methods using multiple performance metrics.

Biomedical image classification based on a cascade of an SVM with a reject option and subspace analysis.

Automated biomedical image classification could confront the challenges of high level noise, image blur, illumination variation and complicated geometric correspondence among various categorical biomedical patterns in practice. To handle these challenges, we propose a cascade method consisting of two stages for biomedical image classification. At stage 1, we propose a confidence score based classification rule with a reject option for a preliminary decision using the support vector machine (SVM). The testing images going through stage 1 are separated into two groups based on their confidence scores. Those testing images with sufficiently high confidence scores are classified at stage 1 while the others with low confidence scores are rejected and fed to stage 2. At stage 2, the rejected images from stage 1 are first processed by a subspace analysis technique called eigenfeature regularization and extraction (ERE), and then classified by another SVM trained in the transformed subspace learned by ERE. At both stages, images are represented based on two types of local features, i.e., SIFT and SURF, respectively. They are encoded using various bag-of-words (BoW) models to handle biomedical patterns with and without geometric correspondence, respectively. Extensive experiments are implemented to evaluate the proposed method on three benchmark real-world biomedical image datasets. The proposed method significantly outperforms several competing state-of-the-art methods in terms of classification accuracy.

Automatic Endosomal Structure Detection And Localization in Fluorescence Microscopic Images.

This paper proposes a modified spatially-constrained similarity measure (mSCSM) method for endosomal structure detection and localization under the bag-of-words (BoW) framework. To our best knowledge, the proposed mSCSM is the first method for fully automatic detection and localization of complex subcellular compartments like endosomes. Essentially, a new similarity score and a novel two-stage output control scheme are proposed for localization by extracting discriminative information within a group of query images. Compared with the original SCSM which is formulated for instance localization, the proposed mSCSM can address category based localization problems. The preliminary experimental results show the proposed mSCSM can correctly detect and localize 79.17% of the existing endosomal structures in the microscopic images of human myeloid endothelial cells.

[Comparison of protein composition and activities of pilose antler processed by different methods].

To elucidate the influence of processing conditions on pilose antlers therapic effects, the protein composition and activities were compared on three kinds of pilose antler processed by lyophilization, freezing and traditional short-time heating, respectively. The concentration of the water soluble protein in freeze-dried pilose antler was 126.54 mg/g (Folin-Phenol assay), which was 13.1 times higher than that of heating processed antler. These proteins distributed widely in SDS-PAGE electrophoresis and the protein band between 50.0 kDa approximately 60.0 kDa achieved the highest concentration. The water extract of freeze-dried antler promoted the proliferation and IGF-I secretion of rat osteogenic-like cell UMR-106 by 245.25% ( MTT assay) and 66.36 ng/ml, which was respectively 2.2 times and 1.2 times of those of heating processed antler. The same candidate inhibited the growth of human hepatic carcinoma cell BEL-7402 by the highest rate of 47.64% , which was 1.4 times of heating processed antler. The activities of frozen fresh pilose antler were lower than those of its freeze-dried counterpart, but were much higher than those of heating processed antler. The results indicated that lyophilization help to remain the activity of pilose antlers proteins as much as possible and improve its efficacy.

[Purification and characterization of the proliferation of rat osteoblast-like cells UMR-106 from pilose antler].

OBJECTIVE: The activity of deer serum albumin on proliferation of rat osteogenic-like cells UMR-106 and the IGF-I secretion were investigated in order to elucidate pilose antler's bone-strengthening mechanism. METHOD: Deer serum albumin was isolated from freeze-dry pilose antler powder extract. The methods were Sephacryl S-200HR gel filtration, POROS 20QE ion-exchange and TSK G3000SW chromatographies. The effect of deer serum albumin on proliferatio of UMR-106 cells was assaied by MTT, and the secretion of IGF-I of UMR-106 cells was assaied by RIA. RESULT: Deer serum albumin, with the molecular weight of 56.3 kDa, significantly increased the proliferation rate of the osteoblast-like UMR-106 cell and IGF-I secretion. When concentration of deer serum albumin reached 0.149 microg x mL(-1), UMR-106 cell proliferation rate was 241.03% and IGF-I secretion was 66.89 ng x mL(-1). CONCLUSION: The concentration of deer serum albumin, from 14.9 ng x mL(-1) to 14.90 microg x mL(-1), significantly increased the proliferation rate of the osteoblast-like UMR-106 cell and IGF- I secretion.

First report of a novel plant lysozyme with both antifungal and antibacterial activities.

A novel lysozyme exhibiting antifungal activity and with a molecular mass of 14.4kDa in SDS-polyacrylamide gel electrophoresis was isolated from mung bean (Phaseolus mungo) seeds using a procedure that involved aqueous extraction, ammonium sulfate precipitation, ion exchange chromatography on CM-Sephadex, and high-performance liquid chromatography on POROS HS-20. Its N-terminal sequence was very different from that of hen egg white lysozyme. Its pI was estimated to be above 9.7. The specific activity of the lysozyme was 355U/mg at pH 5.5 and 30 degrees C. The lysozyme exhibited a pH optimum at pH 5.5 and a temperature optimum at 55 degrees C. It is reported herein, for the first time, that a novel plant lysozyme exerted an antifungal action toward Fusarium oxysporum, Fusarium solani, Pythium aphanidermatum, Sclerotium rolfsii, and Botrytis cinerea, in addition to an antibacterial action against Staphylococcus aureus.