Arylazolyl(azinyl)thioacetanilide. Part 9#: Synthesis and Biological Investigation of Thiazolylthioacetamides Derivatives as a Novel Class of Potential Antiviral Agents

Peng Zhan,Xinyong Liu,Liu Wang,Hong Liu,Xuwang Chen,Xiao Li,Xin Jiang,Qiangqiang Zhang,Christophe Pannecouque,Lieve Naesens,Erik De Clercq,Ailin Liu,Guanhua Du 대한약학회 2012 Archives of Pharmacal Research Vol.35 No.6

In continuation of our endeavor to develop new, potent, selective and less toxic antiviral agents, a novel series of 2-(2-amino/chloro-4-(2,4-dibromophenyl) thiazol-5-ylthio)acetamide derivatives was synthesized via an expeditious route and evaluated for their anti-HIV activities against wild-type virus and clinically relevant mutant strains, and for their anti-influenza virus activities against influenza A (H1N1 and H3N2) and influenza B in cellular assays. The selected active compounds were also assayed for their enzymic inhibitory activities. The results showed that some 2-chloro substituted thiazolylthioacetamide derivatives possessed potent activity against wild type HIV-1 and several key mutant strains (E138K, K103N, L100I) of HIV-1 in MT-4 cells with EC50 values in micromolar range. Two 2-amino substituted thiazole derivatives 8a7 and 8a8 displayed significant potency against influenza A/H1N1 in MDCK cells with EC50 values much lower than that of oseltamivir carboxylate, ribavirin, amantadine and rimantadine. Though the mechanism of actions is still unclear, these novel thiazolylthioacetamides might serve as original leads for further pharmacological investigations as potential therapeutic agents against HIV-1 or influenza virus.

Shortest Path Analyses in the Protein-Protein Interaction Network of NGAL (Neutrophil Gelatinase-associated Lipocalin) Overexpression in Esophageal Squamous Cell Carcinoma

Du, Ze-Peng,Wu, Bing-Li,Wang, Shao-Hong,Shen, Jin-Hui,Lin, Xuan-Hao,Zheng, Chun-Peng,Wu, Zhi-Yong,Qiu, Xiao-Yang,Zhan, Xiao-Fen,Xu, Li-Yan,Li, En-Min Asian Pacific Journal of Cancer Prevention 2014 Asian Pacific journal of cancer prevention Vol.15 No.16

NGAL (neutrophil gelatinase-associated lipocalin) is a novel cancer-related protein involves multiple functions in many cancers and other diseases. We previously overexpressed NGAL to analyze its role in esophageal squamous cell carcinoma (ESCC). In this study, a protein-protein interaction (PPI) was constructed and the shortest paths from NGAL to transcription factors in the network were analyzed. We found 28 shortest paths from NGAL to RELA, most of them obeying the principle of extracellular to cytoplasm, then nucleus. These shortest paths were also prioritized according to their normalized intensity from the microarray by the order of interaction cascades. A systems approach was developed in this study by linking differentially expressed genes with publicly available PPI data, Gene Ontology and subcellular localizaton for the integrated analyses. These shortest paths from NGAL to DEG transcription factors or other transcription factors in the PPI network provide important clues for future experimental identification of new pathways.

β-Elemene Induces Apoptosis in Human Renal-cell Carcinoma 786-0 Cells through Inhibition of MAPK/ERK and PI3K/Akt/mTOR Signalling Pathways

Zhan, Yun-Hong,Liu, Jing,Qu, Xiu-Juan,Hou, Ke-Zuo,Wang, Ke-Feng,Liu, Yun-Peng,Wu, Bin Asian Pacific Journal of Cancer Prevention 2012 Asian Pacific journal of cancer prevention Vol.13 No.6

Background: Renal-cell carcinoma (RCC) is resistant to almost all chemotherapeutics and radiation therapy. ${\beta}$-Elemene, a promising anticancer drug extracted from a traditional Chinese medicine, has been shown to be effective against various tumors. In the present study, anti-tumor effects on RCC cells and the involved mechanisms were investigated. Methods: Human RCC 786-0 cells were treated with different concentrations of ${\beta}$-elemene, and cell viability and apoptosis were measured by 3-(4, 5-dimethylthiazol-2-yl)-2, 5-diphenyl tetrazolium bromide (MTT) assay and flow cytometry, respectively. Protein expression was assayed by western blotting. Autophagy was evaluated by transmission electron microscopy. Results: ${\beta}$-Elemene inhibited the viability of 786-0 cells in a dose- and time-dependent manner. The anti-tumor effect was associated with induction of apoptosis. Further study showed that ${\beta}$-elemene inhibited the MAPK/ERK as well as PI3K/Akt/mTOR signalling pathways. Moreover, robust autophagy was observed in cells treated with ${\beta}$-elemene. Combined treatment of ${\beta}$-elemene with autophagy inhibitors 3-methyladenine or chlorochine significantly enhanced the anti-tumor effects. Conclusions: Our data provide first evidence that ${\beta}$-elemene can inhibit the proliferation of RCC 786-0 cells by inducing apoptosis as well as protective autophagy. The anti-tumor effect was associated with the inhibition of MAPK/ERK and PI3K/Akt/mTOR signalling pathway. Inhibition of autophagy might be a useful way to enhance the anti-tumor effect of ${\beta}$-elemene on 786-0 cells.

Immune and Anti-oxidant Functions of Ethanol Extracts of Scutellaria baicalensis Georgi in Mice Bearing U14 Cervical Cancers

Peng, Yong,Guo, Cong-Shan,Li, Pan-Xia,Fu, Zhan-Zhao,Gao, Li-Ming,Di, Ya,Ju, Ya-Kun,Tian, Ru,Xue, Jia-Jia Asian Pacific Journal of Cancer Prevention 2014 Asian Pacific journal of cancer prevention Vol.15 No.10

Background: The objective was to study the effect of Scutellaria baicalensis Georgi ethanol extracts (SBGE) on immune and anti-oxidant function in U14 tumor-bearing mice. Materials and Methods: U14 tumor-bearing mice were randomly divided into eight groups: a control group, a cyclophosphamide (CTX) group, three dose groups of SBGEI (high, medium, low), and three dose groups of SBGEII (high, medium, low). After two weeks, the thymus and spleen weight indices of mice bearing U14 cervical cancer were calculated. Enzyme linked immunosorbent assays (ELISA) was used to determine the levels of serum IL-2, TNF-${\alpha}$, IL-8, and PCNA. MDA activity and SOD activity in plasma were measured with detection kits. Results: In the SBGE groups, thymus weight and spleen weight indices of U14 tumor-bearing mice were significantly higher than in the control group or CTX group (p<0.05). Compared to control group, the levels of serum IL-2 and TNF-${\alpha}$ in U14 tumor-bearing mice increased significantly, whereas the contents of serum IL-8 and PCNA decreased (p<0.05). The activity of SOD increased with the growing dose of SBGE, while the activity of MDA decreased significantly in the highe-rdose groups of SBGE. Conclusions: These findings suggested that SBGE, especially at high dose, 1000 mg/kg, showed significant immune and anti-oxidant effects infU14 tumor-bearing mice, which might be the mechanisms of SBGE inhibition of tumor growth.

Experimental and analytical behavior of stiffened angle joints

Peng Wang,Jianrong Pan,Zhan Wang,Shizhe Chen 국제구조공학회 2018 Steel and Composite Structures, An International J Vol.26 No.1

The application of rib stiffeners is common on steel connections, with regard to the stiffened angle connection, experimental results about the influence of stiffeners under monotonic and cyclic loading are very limited. Consequently, this paper presents the experimental investigation on four types angle connections with or without stiffener under static loading and another four type stiffened angle connections subjected to cyclic loading. The static experimental result showed that the rib stiffener weld in tension zone of the connection greatly enhanced its initial rotational stiffness and flexural strength. While a stiffener was applied to the compression zone of the connection, it had not obvious influences on the initial rotational stiffness, but increased its flexural strength. The moment-rotation curves, skeleton curves, ductility, energy dissipation and rigidity were evaluated under cyclic loading. Stiffened top-and-seat angle connections behaved as semi-rigid and partial strength, and rotation of all stiffened angle connections exceeded 0.04rad. The failure modes between monotonic and cyclic loading test were completely different and indicated certain robustness.

The Changes of Absorption and Catalytic Capacity on Reduced Graphene Oxide After Electron Beam Irradiation

Peng Liu,Wei Qi,Wenzhen An,Longlong Tian,Zhan Li,Xiaolei Chen,Wang-Suo Wu 성균관대학교(자연과학캠퍼스) 성균나노과학기술원 2015 NANO Vol.10 No.3

As is well-known, porous nanomaterials have attracted increasing attention recently, and graphene-related materials (such as porous graphene) have been studied both experimentally and theoretically. Almost all researches are focused on nanoelectronics, supercapacitors, multifunctional membrances, bio-applications or others. Consequently, in order to understand the differences between porous graphene and normal graphene at adsorption and catalytic property, in this experiment, with the removal of metal ion (152Eu(III)) and organic matter (gallic acid) and reduction of 4-nitrophenol (4-NP) by NaBH4 as model reactions, a systematic investigation into the adsorptive performance as well as catalytic activity of graphene with or without electron beam irradiation exposure had been carried out. As the results showed, compared with the reduction of pristine graphene oxidized (R-GO), the reduction of graphene oxidized with electron beam irradiation exposure (100 MGy, about 2 h, radiation graphene oxide (R-RGO)) had many irregular defects caused by lack of atoms; the adsorptive performance of the R-RGO increased for metals but decreased for organic matter. However, the adsorption rate of the R-RGO was lower for metals, but higher for organic matter than that of the R-GO. In addition, the results also showed that the R-RGO had a better catalytic capacity than the R-GO.

Experimental study on seismic behavior of exterior composite beam-to-column joints with large size stiffened angles

Peng Wang,Zhan Wang,Jianrong Pan,Bin Li,Bo Wang 국제구조공학회 2020 Steel and Composite Structures, An International J Vol.37 No.1

The top-and-seat angles with double web angles are commonly used in the design of beam-to-column joints in Asian and North American countries. The seismic behavior analysis of these joints with large cross-section size of beam and column (often connected by four or more bolts) is a challenge due to the effects from the relatively larger size of stiffened angles and the composite action from the adjacent concrete slab. This paper presents an experimental investigation on the seismic performance of exterior composite beam-to-column joints with stiffened angles under cyclic loading. Four full-scale composite joints with different configuration (only one specimen contain top angle in concrete slab) were designed and tested. The joint specimens were designed by considering the effects of top angles, longitudinal reinforcement bars and arrangement of bolts. The behavior of the joints was carefully investigated, in terms of the failure modes, slippage, backbone curves, strength degradation, and energy dissipation abilities. It was found that the slippage between top-and-seat angles and beam flange, web angle and beam web led to a notable pinching effect, in addition, the ability of the energy dissipation was significantly reduced. The effect of anchored beams on the behavior of the joints was limited due to premature failure in concrete, the concrete slab that closes to the column flange and upper flange of beam plays an significant role when the joint subjected to the sagging moment. It is demonstrated that the ductility of the joints was significantly improved by the staggered bolts and welded longitudinal reinforcement bars.

Antibacterial Constituents from Fruit Bodies of Ascomyce Bulgaria inquinans

Peng Zhang,Xian Li,Ning Li,Jing Xu,Zhan-Lin Li,Yi Wang,Jin-Hui Wang 대한약학회 2005 Archives of Pharmacal Research Vol.28 No.8

Two ergosterins and two triterpenoids were isolated from the dried fruit bodies of Ascomyce Bulgaria inquinans. By means of chemical (hydrolysis) and spectroscopic methods (NMR, EIMS), their structures were established as betuinic acid (1), cerevisterol (2), (24R)ergosta-7, 22Ediene- 3β, 5α, 6β-triol-3-O-palmitate (3) and ursolic acid (4). Compound 3 is a new compound.

Glulam Beam-to-Column Connection with Coupled Steel Rods with Screwheads: Concept and Experimental Verifications

Zhan Shu,Bo Ning,Hanlin Dong,Zheng Li,Zengxin Peng,Yiyu Yang 대한토목학회 2023 KSCE Journal of Civil Engineering Vol.27 No.6

The bolted connections with slotted-in steel plates are basic beam-to-column connections of modern post-and-beam timber building structures. However, due to significantly pinched rotational behaviors, the moment resistance of such connections are usually ignored in design. In this study, the connection-level moment resistance is enabled for modern glulam frame structures with an innovative connection design. A pair of long steel rods with screwheads is designed to generate a force couple at the sides of the connection. The proposed connection could be considered as the key lateral force resisting component, indicating a significant reduction of lateral braces and shear walls. Specimens of the target connection were carefully designed and tested in the lab to obtain their mechanical properties and failure modes. Finite element models were established and calibrated according to the tested data. The moment-rotation curves of the new connection could be easily estimated through a fitted formula. Moreover, the suggestions to improve the proposed connection is also discussed based on the observed damage modes. Results show that the new connection could be treated as rigid moment-resisting connections while the ductility could be further improved.

<Retraction> INVESTIGATION OF HIGH-COERCIVITY FePt-C NANOGRANULAR FILMS FOR PERPENDICULAR MAGNETIC RECORDING (PMR) MEDIA

JIEGANG PENG,S. XUE,Z. YAN,X. WU,L. ZHAN 성균관대학교(자연과학캠퍼스) 성균나노과학기술원 2011 NANO Vol.6 No.6

In this work, we studied FePt-C nanogranular films were fabricated for ultrahigh density perpendicular recording media towards 1 Tbits/in^2. For the optimized growth conditions, we achieved a Fe_(52)Pt_(48)-C50% granular film with uniform grain size of 6.4 ± 1.5 nm, shown in the TEM image. It also has an excellent MH loop shape with a perpendicular coercivity of 20 kOe, and squareness of 1.We studied the thermal stability of the optimized film and obtained the energy barrier Eb of 340 k_BT at room temperature, meaning that excellent thermal stability as magnetic recording media.