Synthesis and Anticonvulsant Activity of 1-Formamide-triazolo[4,3- a]quinoline Derivatives

Cheng-Xi Wei,Xian-Qing Deng,채규윤,Zhi-Gang Sun,Zhe-Shan Quan 대한약학회 2010 Archives of Pharmacal Research Vol.33 No.5

Using 6-hydroxy-3,4-dihydro-2(1H)-quinolone as the starting material, a series of 1-formamide-triazolo[4, 3-a]quinoline derivatives (6a-6n) was synthesized, the anticonvulsant effect and neurotoxicity of the compounds was calculated with maximal electroshock test and rotarod tests with intraperitoneally injected in KunMing mice. The results demonstrated that compound 7-(hexyloxy)-4,5-dihydro-[1,2,4] triazolo[4,3-a]quinoline-1-carboxamide (6d) was the most active one and also had the lowest toxicity. In the anti-maximal electroshock potency test, it showed median effective dose (ED50) of 30.1 mg/kg, median toxicity dose (TD50) of 286 mg/kg, and the protective index of 9.5 which is greater than the reference drug carbamazepine with the protective index value of 6.0.

Synthesis of 2-Substituted-6-(4H-1,2,4-triazol-4-yl)benzo[d]oxazoles as Potential Anticonvulsant Agents

Cheng-Xi Wei,Li-Ping Guan,Jing-Hao Jia,채규윤,Zhe-Shan Quan 대한약학회 2009 Archives of Pharmacal Research Vol.32 No.1

A series of 2-substituted-6-(4H-1,2,4-triazol-4-yl)benzo[d]oxazoles were synthesized. The anticonvulsant effect and neurotoxicity of the compounds (intraperitoneally) were evaluated with the maximal electroshock (MES) test, subcutaneous pentylenetetrazole (sc-PTZ), and rotarod tests in mice. 2-Phenyl- 6- (4H-1,2,4-triazol-4-yl)benzo[d]oxazole (3g) was the most active and also had the lowest toxicity. In the anti-MES potency test, it showed median effective dose (ED50) of 29.5 mg/kg, a median toxicity dose (TD50) of 285 mg/kg, and a protective index (PI) of 9.7, which is greater than the reference drug, carbamazepine, which has a PI of 6.4.

Metagenomics analysis of the gut microbiome in healthy and bacterial pneumonia forest musk deer

Wei Zhao,Ziwei Ren,Yan Luo,Jianguo Cheng,Jie Wang,Yin Wang,Zexiao Yang,Xueping Yao,Zhijun Zhong,Wei Yang,Xi Wu 한국유전학회 2021 Genes & Genomics Vol.43 No.1

Background The forest musk deer (FMD, Moschus berezovskii) is an threatened species in China. Bacterial pneumonia was found to seriously restrict the development of FMD captive breeding. Historical evidence has demonstrated the relationship between immune system and intestinal Lactobacillus in FMD. Objective We sought to elucidate the diferences in the gut microbiota of healthy and bacterial pneumonia FMD. Methods The bacterial pneumonia FMD was demonstrated by bacterial and pathological diagnosis, and the gut microbiome of healthy and bacterial pneumonia FMD was sequenced and analysed. Results There are three pathogens (Pseudomonas aeruginosa, Streptococcus equinus and Trueperella pyogenes) isolated from the bacterial pneumonia FMD individuals. Compared with the healthy group, the abundance of Firmicutes and Proteobacteria in the pneumonia group was changed, and a high level of Proteobacteria was found in the pneumonia group. In addition, a higher abundance of Acinetobacter (p=0.01) was observed in the population of the pneumonia group compared with the healthy group. Several potentially harmful bacteria and disease-related KEGG subsystems were only found in the gut of the bacterial pneumonia group. Analysis of KEGG revealed that many genes related to type IV secretion system, type IV pilus, lipopolysaccharide export system, HTH-type transcriptional regulator/antitoxin MqsA, and ArsR family transcriptional regulator were signifcantly enriched in the metagenome of the bacterial pneumonia FMD. Conclusion Our results demonstrated that the gut microbiome was signifcantly altered in the bacterial pneumonia group. Overall, our research improves the understanding of the potential role of the gut microbiota in the FMD bacterial pneumonia.

Effect of Joint Stiffness on the Stability of Cable-braced Grid Shells

Xi Wang,Ruo-qiang Feng,Gui-rong Yan,Feng-cheng Liu,Wei-jia Xu 한국강구조학회 2016 International Journal of Steel Structures Vol.16 No.4

Bolted joints used in cable-braced grid shells are typically semi-rigid joints, and the joint stiffness has a significant effect on the stability of cable-braced grid shells. The effect of joint stiffness on the stability of cable-braced grid shells is studied in this paper. Based on the experimental results of improved bolted joints, finite element models of elliptic paraboloid cable-braced grid shells with bolted joints are established, and spring elements are used to simulate the joint stiffness. The effect of the joint stiffness on the nonlinear buckling load is studied by changing the joint stiffness. The main conclusions are as follows. First, the joint rotational stiffness has a significant effect on the failure mode. When the joint rotational stiffness is small to a certain extent, the failure mode of cable-braced grid shells changes from overall buckling to local buckling. Second, the nonlinear failure mode is similar to the first-order eigenvalue buckling mode and the maximal compression stress distribution. The structural integrity is weakened, and the maximal steel tube compression stress decreases with the decrease of the joint rotational stiffness. The smaller the joint rotational stiffness, the lower the utilization rate of steel strength. The results suggest that the joint stiffness of elliptic paraboloid cable-braced grid shells should not be less than 20% of the rigid joint stiffness.

Optimal Tracking Performance of NCSs with Time-delay and Encoding-decoding Constraints

Jun-Wei Hu,Xi-Sheng Zhan,Jie Wu,Huai-Cheng Yan 제어·로봇·시스템학회 2020 International Journal of Control, Automation, and Vol.18 No.4

In this paper, the tracking performance of networked control systems (NCSs) under energy constraints with time-delay and encoding-decoding is studied. Through spectral factorization and partial decomposition techniques, we can obtain the explicit representation of the optimal performance. It is shown that the optimal performance is affected by non minimum phase (NMP) zeros, unstable poles and other multiple communication constraints such as time-delay, encoding-decoding and additive white Gaussian noise (AWGN). At the same time, the obtained result shows that a two-parameter compensator is superior to a one-parameter compensator. In addition, it is found that time-delay, encoding-decoding and AWGN affected the tracking capability of NCSs. Finally, an example is given for verifying the correctness of the conclusions.

NOX4/Src regulates ANP secretion through activating ERK1/2 and Akt/GATA4 signaling in beating rat hypoxic atria

Wu, Cheng-zhe,Li, Xiang,Hong, Lan,Han, Zhuo-na,Liu, Ying,Wei, Cheng-xi,Cui, Xun The Korean Society of Pharmacology 2021 The Korean Journal of Physiology & Pharmacology Vol.25 No.2

Nicotinamide adenine dinucleotide phosphate oxidases (NOXs) are the major enzymatic source of reactive oxygen species (ROS). NOX2 and NOX4 are expressed in the heart but its role in hypoxia-induced atrial natriuretic peptide (ANP) secretion is unclear. This study investigated the effect of NOX on ANP secretion induced by hypoxia in isolated beating rat atria. The results showed that hypoxia significantly upregulated NOX4 but not NOX2 expression, which was completely abolished by endothelin-1 (ET-1) type A and B receptor antagonists BQ123 (0.3 μM) and BQ788 (0.3 μM). ET-1-upregulated NOX4 expression was also blocked by antagonists of secreted phospholipase A2 (sPLA2; varespladib, 5.0 μM) and cytosolic PLA2 (cPLA2; CAY10650, 120.0 nM), and ET-1-induced cPLA2 expression was inhibited by varespladib under normoxia. Moreover, hypoxia-increased ANP secretion was evidently attenuated by the NOX4 antagonist GLX351322 (35.0 μM) and inhibitor of ROS N-Acetyl-D-cysteine (NAC, 15.0 mM), and hypoxia-increased production of ROS was blocked by GLX351322. In addition, hypoxia markedly upregulated Src expression, which was blocked by ET receptors, NOX4, and ROS antagonists. ET-1-increased Src expression was also inhibited by NAC under normoxia. Furthermore, hypoxia-activated extracellular signal-regulated kinase 1/2 (ERK1/2) and protein kinase B (Akt) were completely abolished by Src inhibitor 1 (1.0 μM), and hypoxia-increased GATA4 was inhibited by the ERK1/2 and Akt antagonists PD98059 (10.0 μM) and LY294002 (10.0 μM), respectively. However, hypoxia-induced ANP secretion was substantially inhibited by Src inhibitor. These results indicate that NOX4/Src modulated by ET-1 regulates ANP secretion by activating ERK1/2 and Akt/GATA4 signaling in isolated beating rat hypoxic atria.

Simultaneous identification of bearing dynamic coefficients in a water-gas lubricated hydrostatic spindle with a big thrust disc

Feng Cheng,Wei-Xi Ji 대한기계학회 2016 JOURNAL OF MECHANICAL SCIENCE AND TECHNOLOGY Vol.30 No.9

A water-gas lubricated hydrostatic spindle system with big thrust disc, supported by a water-lubricated journal bearing and a gaslubricated thrust bearing, is developed to improve spindle stiffness and to reduce friction power of spindle. A new identification algorithm is derivated to identify simultaneously the eighteen dynamic coefficients of the coupled journal and thrust bearings. A comparison with the available experimental results reveals that the bearing coefficients is well estimated by the present theoretical model. The results also indicate that, the estimated bearing parameters by regularization solution are in good agreement with the assumed values; while it has opposite effect by directed solution for discrete ill-posed problems. It is concluded that, the identification accuracy of bearing parameters is govern by the measured errors; contrast to unbalance mass error and unbalance phase error, the displacement error leads the maximal percentage deviations of estimated coefficients.

Enhanced Salt Stress Tolerance in Transgenic Potato Plants Expressing IbMYB1, a Sweet Potato Transcription Factor

( Yu Jie Cheng ),( Myoung Duck Kim ),( Xi Ping Deng ),( Sang Soo Kwak ),( Wei Chen ) 한국미생물 · 생명공학회 2013 Journal of microbiology and biotechnology Vol.23 No.12

IbMYB1, a transcription factor (TF) for R2R3-type MYB TFs, is a key regulator of anthocyanin biosynthesis during storage of sweet potatoes. Anthocyanins provide important antioxidants of nutritional value to humans, and also protect plants from oxidative stress. This study aimed to increase transgenic potatoes` (Solanum tuberosum cv. LongShu No.3) tolerance to environmental stress and enhance their nutritional value. Transgenic potato plants expressing IbMYB1 genes under the control of an oxidative stress-inducible peroxidase (SWPA2) promoter (referred to as SM plants) were successfully generated through Agrobacterium-mediated transformation. Two representative transgenic SM5 and SM12 lines were evaluated for enhanced tolerance to salinity, UV-B rays, and drought conditions. Following treatment of 100 mM NaCl, seedlings of SM5 and SM12 lines showed less root damage and more shoot growth than control lines expressing only an empty vector. Transgenic potato plants in pots treated with 400 mM NaCl showed high amounts of secondary metabolites, including phenols, anthocyanins, and flavonoids, compared with control plants. After treatment of 400 mM NaCl, transgenic potato plants also showed high DDPH radical scavenging activity and high PS II photochemical efficiency compared with the control line. Furthermore, following treatment of NaCl, UV-B, and drought stress, the expression levels of IbMYB1 and several structural genes in the flavonoid biosynthesis such as CHS, DFR, and ANS in transgenic plants were found to be correlated with plant phenotype. The results suggest that enhanced IbMYB1 expression affects secondary metabolism, which leads to improved tolerance ability in transgenic potatoes.

经管类本科专业公司运营实战实验室建设研究

聂希刚(Nie Xi-Gang),陈荣庚(Cheng Rong-Geng),李强(Li Qiang),高巍(Gao Wei) 동북아시아문화학회 2009 동북아시아문화학회 국제학술대회 발표자료집 Vol.2009 No.5월

Low-dose diethylhexyl phthalate exposure does not impair the expressive patterns of epigenetics-related genes and DNA methylation of breast cancer-related genes in mouse mammary glands

Shun-Feng Cheng,Ling Li,Bo Li,Jing-Cai Liu,Fang-Nong Lai,Yong Zhao,Xi-Feng Zhang,Wei Shen,Lan Li 대한독성 유전단백체 학회 2018 Molecular & cellular toxicology Vol.14 No.2

Backgrounds: Di-(2-ethylhexyl) phthalate (DEHP), as an endocrine-disrupting chemical (EDC), is widely used in plasticizer and other productions. Ubiquitous human exposure to DEHP has been proposed to be a potential risk to public health. Developmental exposure to DEHP could alter epigenetic programming and result in adult-onset disease. Methods: In this study, we investigated whether DEHP exposure to pregnant mice affected epigenetic changes as a result of increase in breast cancer incidence. Results: Our results showed that the expression of total 143 epigenetics-related genes in mammary gland cells, have no significantly altered after short time and low-dose treated with DEHP from 0.5 days post-coitum (dpc) to 3.5 dpc of pregnant mice. DNA methylation status of some neoplastic development genes, such as EGFr, Esr1, Pgr, Fos and Rassf5 also had no obvious change. Conclusion: These finding showed no impact of DEHP on the expressive patterns of epigenetics-related genes and DNA methylation of breast cancer-related genes in pregnant mouse mammary gland cells.