Synthesis and antimicrobial activity of polyhalobenzonitrile quinazolin-4(3H)-one derivatives

A novel series of polyhalobenzonitrile quinazolin-4(3H)-one derivatives were synthesized and characterized by NMR, IR, MS, and HRMS spectra. All of the newly prepared compounds were screened for antimicrobial activities against four strains of bacteria (Gram-positive bacterial: Staphylococcus aureus and Bacillus cereus; Gram-negative bacterial: Escherichia coli and Pseudomonas aeruginosa) and one strain of fungi (Candida albicans). Among the synthesized compounds, 5-(dimethylamino)-8-(2,4,5-trichloro-isophthalonitrile) quinazolin-4(3H)-one (7k) exhibited significant activity towards Gram-positive bacterial, Gram-negative bacterial, and the fungi strains. The MIC (0.8–3.3 μg/mL) and MBC (2.6–7.8 μg/mL) for this compound were close to those of nofloxacin, chlorothalonil, and fluconazole, making it the most potent antimicrobial agents in the series.     

Anatomical and Chemical Alterations but not Photosynthetic Dynamics and Apoplastic Transport Changes are Involved in the Brittleness Culm Mutation of Rice

Brittleness culm is an important agronomic trait that has a potential usefulness in agricultural activity as animal forage although the developmental mechanism is not clear yet. In the present study, the anatomical and chemical characteristics as well as some ecophysiological features in the brittleness culm mutation of rice (Oryza sativa L.) were investigated. Compared with the wild type (WT), the brittleness culm mutant (bcm) exhibited higher culm vascular bundle distance and lower culm wall thickness, leaf interveinal distance and leaf thickness. Ratio of bundle sheath cell/whole bundle and areas of whole vascular bundles and bundle sheath of leaves were reduced while ratios of xylem and phloem to whole bundles were elevated in bcm. The Fourier transform infrared (FTIR) microspectroscopy analysis and further histochemical and physiological measurements revealed that the different contents and depositions of cell wall components such as pectins, lignin, suberin and cellulose all participated in the mutation of brittleness. However, the mutant presented no significant changes in leaf photosynthetic dynamics and apoplastic transport ability. These results strongly indicate that the alterations in anatomical and chemical characteristics, rather than changes in major ecophysiological features such as photosynthesis and apoplastic transport were involved in the brittleness mutation of rice.     

Drought-Stimulated Activity of Plasma Membrane Nicotinamide Adenine Dinucleotide Phosphate Oxidase and Its Catalytic Properties in Rice

The activity of plasma membrane (PM) nicoUnamide adenine dinucleotide phosphate (NADPH) oxidase and Its catalytic properties in rice was investigated under drought stress conditions. Drought stress led to decreased leaf relative water content (RWC) and, as a result of drought-induced oxidative stress, the activities of antioxidant enzymes increased significantly. More interestingly, the intensity of applied water stress was correlated with increased production of H_2O_2and O_2~- and elevated activity of PM NADPH oxidase, a key enzyme of reactive oxygen species generation in plants.Histochemlcal analyses also revealed increased H_2O_2 and O_2~- production in drought-stressed leaves. Application of dlphenylene iodonium (DPI), an Inhibitor of PM NADPH oxidasa, did not alleviate drought-induced production of H_2O_2 and O_2~-. Catalysis experiments indicated that the dce PM NADPH oxidass was partially fiavin-dependent. The pH and temperature optima for this enzyme were 9.8 and 40 ℃, respectively. In addition, drought stress enhanced the activity under alkaline pH and high temperature conditions. These results suggest that a complex regulatory mechanism, associated with the NADPH oxidase-H_2O_2 system, is involved in the response of rice to drought stress.     

Drought-Stimulated Activity of Plasma Membrane Nicotinamide Adenine Dinucleotide Phosphate Oxidase and Its Catalytic Properties in Rice

The activity of plasma membrane （PM） nicotinamide adenine dinucleotide phosphate （NADPH） oxidase and its catalytic properties in rice was investigated under drought stress conditions. Drought stress led to decreased leaf relative water content （RWC） and, as a result of drought-induced oxidative stress, the activities of antioxidant enzymes increased significantly. More interestingly, the intensity of applied water stress was correlated with increased production of H2O2 and O2^- and elevated activity of PM NADPH oxidase, a key enzyme of reactive oxygen species generation in plants. Histochemical analyses also revealed increased H2O2 and O2^- production in drought-stressed leaves. Application of diphenylene iodonium （DPI）, an inhibitor of PM NADPH oxidase, did not alleviate drought-induced production of H2O2 and O2^-. Catalysis experiments indicated that the rice PM NADPH oxidase was partially fiavin-dependent. The pH and temperature optima for this enzyme were 9.8 and 40 ℃, respectively. In addition, drought stress enhanced the activity under alkaline pH and high temperature conditions. These results suggest that a complex regulatory mechanism, associated with the NADPH oxidase-H2O2 system, is involved in the response of rice to drought stress.     

缓慢干旱下春小麦叶片质膜脂肪酸组成、H+-ATPase及5′-AMPase活力的变化

 研究了田间缓慢干旱胁迫下,抗旱性不同的两个小麦(Triticum aestivum)品种的生长状况、质膜极性脂脂肪酸组成以及质膜关键酶活力的变化。在小麦生长发育的早期,干旱胁迫使其叶片质膜极性脂脂肪酸不饱和度下降、质膜微囊消耗O2的速率升高、膜蛋白含量降低、H+-ATPase (EC 3.6.1.35)活力下降、5'-AMPase (EC 3.1.3.5)活力大幅度升高;在小麦发育的后期,随着干旱的持续,小麦叶片质膜的极性脂脂肪酸不饱和度不变或升高、质膜微囊消耗O2的速率降低、膜蛋白含量与H+-ATPase活力升高、5'-AMPase活力下降。以上结果表明,小麦在发育的早期阶段对干旱较敏感,其细胞质膜流动性降低、细胞中能荷贮备降低;而在后期,则又表现出对干旱的适应。这些结果将有助于阐明自然干旱条件下植物的抗旱机制。     

Gradual Drought Under Field Conditions Influences the Glutathione Metabolism,Redox Balance and Energy Supply in Spring Wheat

Glutathione (GSH) metabolism, redox balance and energy supply in spring wheat (Triticum aestivum L.) during gradual drought stress under field conditions were investigated. Although levels of total and reduced GSH were decreased, the ratio of GSH/GSSG (glutathione disulfide) was markedly increased by drought. Levels of GSH biosynthetic precursors, cysteine (Cys) and -glutamylcysteine (-GC), and the activities of their biosynthetic enzymes, -glutamylcysteine synthetase (-GCS) and glutathione synthetase (GSHS) were also significantly increased in stressed plants. Glutathione reductase (GR) activity, which is responsible for the conversion of GSSG to GSH, was also increased under this field stress. However, two other important enzymes in GSH metabolism, glutathione peroxidase (GP) and glutathione S-transferase (GST), showed decreased activity in the droughted plants. These results suggest that the higher ratio of GSH/GSSG, the rate of GSH biosynthesis and the capacity of its redox cycling rather than GSH accumulation might be essential for drought resistance of plants. Activities of the two key Calvin-cycle enzymes possessing exposed sulfhydryl groups, NADP⁺-dependent glyceraldehydes-3-phosphate dehydrogenase (G3PD) and fructose-1,6-bisphosphatase (FBPase) were not affected by drought stress, whereas, activity of the key enzyme in the pentose-phosphate pathway (PPP), 6-phosphogluconate dehydrogenase (6-PGD), increased in the droughted plants. The ratios of NADPH/NADP⁺, NADH/NAD⁺ and ATP/ADP increased in the droughted plants, indicating that an up-regulation of the reduced redox state and the energy supply in the plant cells might be an important physiological strategy for plants responding to drought stress. A simple correlation between the high ratio of GSH/GSSG, the rate of GSH biosynthesis and the redox cycle and the high reduction states of redox status in the plant cells was also observed under field drought.     

Analysis of the recurrence risk factors for the patients with hepatocellular carcinoma meeting University of California San Francisco criteria after curative hepatectomy

We report a rare male case of an undifferentiated carcinoma with osteoclast-like giant cells originating in an indeterminate mucin-producing cystic neoplasm of the pancreas. A 59-year-old Japanese man with diabetes visited our hospital, complaining of fullness in the upper abdomen. A laboratory analysis revealed anemia (Hemoglobin; 9.7 g/dl) and elevated C-reactive protein (3.01 mg/dl). Carbohydrate antigen 19-9 was 274 U/ml and Carcinoembryonic antigen was 29.6 ng/ml. A computed tomography scan of the abdomen revealed a 14-cm cystic mass in the upper left quadrant of the abdomen that appeared to originate from the pancreatic tail. The patient underwent distal pancreatectomy/splenectomy/total gastrectomy/cholecystectomy. The mass consisted of a multilocular cystic lesion. Microscopically, the cyst was lined by cuboidal or columnar epithelium, including mucinous epithelium. Sarcomatous mononuclear cells and multinucleated osteoclast-like giant cells were found in the stroma. Ovarian-type stroma was not seen. We made a diagnosis of osteoclast-like giant cell tumor originating in an indeterminate mucin-producing cystic neoplasm of the pancreas. All surgical margins were negative, however, two peripancreatic lymph nodes were positive. The patient recovered uneventfully. Two months after the operation, multiple metastases occurred in the liver. He died 4 months after the operation.