Co-reporter:Qi Xu;Jia-Li Wang;Ya-Li Luo;Juan-Juan Li;Ke-Rang Wang;Xiao-Liu Li
Chemical Communications 2017 vol. 53(Issue 14) pp:2241-2244
Publication Date(Web):2017/02/14
DOI:10.1039/C6CC08811B
A system of controllable capture and release of protein was constructed by multiple, interconnected supramolecular binding modules based on lactose modified mono-cationic perylene bisimide derivatives, cucurbit[8]uril (CB[8]), 1-adamantanamine (ADA) and peanut agglutinin (PNA) lectins.
Co-reporter:Haiying Wei;Mengjiao Lv;Xiaoxu Duan;Shuai Li;Yuchao Yao
Medicinal Chemistry Research 2014 Volume 23( Issue 5) pp:2277-2286
Publication Date(Web):2014 May
DOI:10.1007/s00044-013-0823-x
A series of novel water-soluble tri-substituted naphthalene diimide (NDI) derivatives bearing 2-oligoethoxy ethanamine side chain end-labeled with tertiary amino groups have been designed and synthesized. The cytotoxicity of the novel naphthalene diimides against cancer cell lines (K562, A549 and HeLa) showed that these compounds had excellent anti-cancer activity and the short length of the side chain (having one oxyethylene) was found to be beneficial to the observed anti-proliferative activity. Their DNA-binding properties were also studied using UV–Vis spectroscopy, fluorescence spectroscopy, and circular dichroism. The results showed that such tri-substituted NDI as DNA intercalators exhibited strong π–π stack binding capability and high binding affinities towards calf thymus (Ct) DNA and G-quadruplex (G4) DNA. The order of the binding constants is Ct-DNA > G4 DNA, which suggested that these compounds are more effective ligands to the duplex DNA.
Co-reporter:Hua Chen;Fang Gao;Chunxiao Li;Xiaoliu Li;Na Li
Medicinal Chemistry Research 2013 Volume 22( Issue 12) pp:5723-5729
Publication Date(Web):2013 December
DOI:10.1007/s00044-013-0560-1
Several novel C-pseudonucleosides containing N-phenyl thiazolidin-4-one were synthesized at room temperature using the unprotected sugar aldehyde as the starting material. The effects of the compounds on Con A-induced T cell proliferation were evaluated at five concentrations of 5, 10, 25, 50, and 100 μM. Some compounds, such as 5d, 5e, 5f, and 4g could significantly increase the proliferation by 62, 63, 70, and 53 % at low concentration of 5 μM, respectively. The structure–activity relationship indicated that the lipophilicity substituents like chloro atom, methyl, and methoxyl on the para position of N-3 phenyl at the thiazolidin-4-one ring had a detrimental impact on the T cell proliferation. The C-2 configuration and the electronic property of the lipophilicity substituents likely had slight effects on the immunostimulatory activities of such C-pseudonucleosides.
Co-reporter:Zhenghao Liu;Yunkai Lv;Jungang Gao;Xiaoliu Li;Xuefei Zhai;Jianhua Zhao;Xiangjie Xu
Journal of Applied Polymer Science 2012 Volume 126( Issue 4) pp:1247-1256
Publication Date(Web):
DOI:10.1002/app.36938
Abstract
Molecularly imprinted membranes with different ratio of acrylamide (AM) versus methacrylic acid (MAA) were prepared by photocopolymerization on commercial filter paper using nicosulfuron as the template. The structures, the thermal stability, and the morphology of membranes were characterized by infrared spectroscopy (IR), thermogravimetric analysis (TGA), and scanning electron microscopy (SEM), respectively. Static equilibrium binding and competitive recognition properties of the membranes to nicosulfuron and its analogs (pyrazosulfuron ethyl and bensulfuron methyl) were tested. The results showed that nicosulfuron-imprinted membranes had the best recognition capacity to nicosulfuron compared with its analogs. The biggest selectivity factors of and were 1.28 and 1.83 and the imprinted factor reached to 2.34. The results of this study implied that the molecularly imprinted composite membranes could be used as separation membranes for nicosulfuron enrichment. The Scatchard plot revealed that one class of binding sites was mainly produced in the imprinted composite membrane in the studied concentration range of nicosulfuron. © 2012 Wiley Periodicals, Inc. J Appl Polym Sci, 2012
Co-reporter:Fengjuan Shen, Xiaoliu Li, Xiaoyuan Zhang, Qingmei Yin, Zhanbin Qin, Hua Chen, Jinchao Zhang and Zhaipu Ma
Organic & Biomolecular Chemistry 2011 vol. 9(Issue 16) pp:5766-5772
Publication Date(Web):17 May 2011
DOI:10.1039/C1OB05675A
Dinucleosides containing a thiazolidin-4-one linkage were prepared by one-pot tandem Staudinger/aza-Wittig/intermolecular cyclization under microwave irradiation and their structures were confirmed. Preliminary examination of HIV-RT inhibition showed that the dinucleosides containing (R)-thiazolidin-4-one linkage are significantly more active than those containing (S)-thiazolidin-4-one linkage.
Co-reporter:Hua Chen, Qingmei Yin, Chunxiao Li, Enkai Wang, Fang Gao, Xiaobo Zhang, Zhi Yin, Sinan Wei, Xiaoliu Li, Ming Meng, Pingzhu Zhang, Na Li, and Jinchao Zhang
ACS Medicinal Chemistry Letters 2011 Volume 2(Issue 11) pp:845
Publication Date(Web):September 7, 2011
DOI:10.1021/ml200155k
Several novel C-pseudonucleosides bearing thiazolidin-4-one were synthesized by one-pot three-component condensation using unprotected sugar aldehyde at room temperature, and their effects on T cells, B cells, the cytokine secretion of IL-2, IL-4, and IFN-γ, T cell-associated molecules (CD3, CD4, CD8), and B cell-associated molecules (CD19) were first evaluated. The experimental data demonstrated that such thiazolidin-4-one C-pseudonucleosides hold potential as immunostimulating agents.Keywords: C-pseudonucleosides; Immunostimulating agents; thiazolidin-4-one
Co-reporter:Fengjuan Shen;Xiaoliu Li;Xiaojuan Zhang;Zhanbin Qin;Qingmei Yin;Hua Chen;Jinchao Zhang
Chinese Journal of Chemistry 2011 Volume 29( Issue 6) pp:1205-1210
Publication Date(Web):
DOI:10.1002/cjoc.201190224
Abstract
A general synthesis of 1-aryl-1-H-indazoles from o-halogenated aryl aldehydes or ketones and aryl hydrazines was described. This protocol included an intermolecular condensation and a ligand-free copper-catalyzed intramolecular Ullmann-type coupling reaction. This method was applied to a wide range of substrates to produce the indazole products in good yields.
Co-reporter:Kerang Wang, Ling Wu, Zhanbin Qin, Xinhao Yan, Xiaoliu Li, Hua Chen, Pingzhu Zhang, Jinchao Zhang
Bioorganic & Medicinal Chemistry Letters 2011 Volume 21(Issue 3) pp:916-919
Publication Date(Web):1 February 2011
DOI:10.1016/j.bmcl.2010.12.069
A series of novel ribonucleosides with C-5 OH replaced by a diaminopyrimidinyl group were synthesized by successively nucleophilic substitutions of 5′-deoxy-5′-amino-ribonucleosides with 2,4-dichloropyrimidine and then with various fatty amines under microwave irradiation. Their anticancer activities in vitro were preliminarily evaluated. Compounds 7a and 8a only exhibited anticancer activity against A549 cell line with the IC50 values of 10.73 and 10.99 μM, respectively. In addition, 7h and 8h showed potent activities against both A549 and Hela cell lines with the IC50 values of 12.71, 8.55 and 8.44, 5.55 μM, respectively.
Co-reporter:Xiao-liu Li;Xiao-li Zhen;Jian-rong Han
Journal of Chemical Crystallography 2009 Volume 39( Issue 12) pp:
Publication Date(Web):2009 December
DOI:10.1007/s10870-009-9581-5
As precursors of α-amino acids, methyl 2-hydroxyimino-3-phenyl-propionate (F.W. 193.20) was synthesized, characterized by 1H NMR, IR, element analysis and confirmed by X-ray crystal structure analysis. This compound crystallizes in monoclinic class under the space group P21/c with cell parameters, a = 8.6435(17) Å, b = 5.4957(11) Å, c = 21.146(4) Å; β = 97.12(3)°, and Z = 4. The structure exhibits inter-molecular hydrogen bonds of the type O–H···N, O–H···O, C–H···O.
Co-reporter:Chunxiao Li, Ming Meng, Dongzhi Chen, Zerui Wang, Hua Han, Hua Chen, Jinchao Zhang, Xiaoliu Li
International Immunopharmacology (November 2013) Volume 17(Issue 3) pp:698-703
Publication Date(Web):1 November 2013
DOI:10.1016/j.intimp.2013.08.011
•CH2b could increase the production of NO by the LPS-activated RAW 264.7 cells.•CH2b could significantly elevate the phagocytosis of LPS-activated RAW 264.7 cells.•CH2b could markedly increase the secretion of IL-6, IL-8 and TNF-α.•CH2b could increase the LPS-induced activation of NF-κB and p38 MAPK in RAW 264.7 cells.This study was designed to confirm the effect of the novel immunostimulators CH1b and CH2b with a thiazolidin-4-one ring on the function of macrophages. We used these two molecules to stimulate LPS-activated RAW 264.7 macrophages in vitro. After a series of essential assays, we found that CH1b and CH2b could significantly increase the production of nitric oxide (NO) by the LPS-activated RAW 264.7 macrophages, and also found that CH2b could more significantly increase the proliferation, phagocytic activity, and secretion of IL-6, IL-8 and TNF-α by LPS-activated RAW 264.7 cells more than CH1b. Furthermore, CH2b could increase the degradation of IκB-α and could promote the nuclear translocation of nuclear factor (NF)-κB p65 in LPS-activated RAW 264.7 cells. However, CH2b could also increase the phosphorylation of p38 mitogen-activated protein kinase (p38 MAPK). Taken together, we got that CH2b could further increase the LPS-induced activation of NF-κB and p38 MAPK in RAW 264.7 macrophages to elevate the function of macrophages, including iNOS expression, NO production, cytokines secretion, and phagocytosis.
Co-reporter:Ming Meng, Chunxiao Li, Dongzhi Chen, Zerui Wang, Yang Hong, Hua Chen, Xiaoliu Li, Jinchao Zhang, Fu-Sheng Wang
International Immunopharmacology (April 2013) Volume 15(Issue 4) pp:655-660
Publication Date(Web):1 April 2013
DOI:10.1016/j.intimp.2013.02.019
•CH1b and CH2b induce the production of IFN-γ and TNF-α by NK cells.•CH1b and CH2b elevate the cytotoxicity of human NK cells.•ERK 1/2 was significantly phosphorylated after treatment with CH1b and CH2b in NK cells.To investigate how the novel synthetic immunostimulators (CH1a, CH2a, CH1b and CH2b) with a core substructure of thiazolidin-4-one ring influence the function of human natural killer (NK) cells in vitro, first, we obtained highly purified and viable NK cells from peripheral blood mononuclear cells (PBMCs) by a magnetic cell sorter (MACS). Then, the cytotoxicity and proliferative capacity of NK cells were explored after treatment with CH1a, CH2a, CH1b and CH2b. Moreover, the production of IFN-γ and TNF-α was also analyzed. We found that CH1b and CH2b could induce a significant enhancement of cytotoxicity and cytokine production including IFN-γ and TNF-α by NK cells. However, CH1b and CH2b could hardly promote the proliferation of NK cells. In immunoblotting analysis assay, we found that ERK 1/2 could be significantly phosphorylated after treatment with CH1b and CH2b, while the same phenomenon did not emerge after blockade with PD098059, the specific inhibitor of ERK1/2 signaling pathways. Taken together, we can conclude that CH1b and CH2b can elevate the cytotoxicity probably via ERK 1/2 activation.
Co-reporter:Qi Xu, Jia-Li Wang, Ya-Li Luo, Juan-Juan Li, Ke-Rang Wang and Xiao-Liu Li
Chemical Communications 2017 - vol. 53(Issue 14) pp:NaN2244-2244
Publication Date(Web):2017/01/25
DOI:10.1039/C6CC08811B
A system of controllable capture and release of protein was constructed by multiple, interconnected supramolecular binding modules based on lactose modified mono-cationic perylene bisimide derivatives, cucurbit[8]uril (CB[8]), 1-adamantanamine (ADA) and peanut agglutinin (PNA) lectins.
Co-reporter:Fengjuan Shen, Xiaoliu Li, Xiaoyuan Zhang, Qingmei Yin, Zhanbin Qin, Hua Chen, Jinchao Zhang and Zhaipu Ma
Organic & Biomolecular Chemistry 2011 - vol. 9(Issue 16) pp:NaN5772-5772
Publication Date(Web):2011/05/17
DOI:10.1039/C1OB05675A
Dinucleosides containing a thiazolidin-4-one linkage were prepared by one-pot tandem Staudinger/aza-Wittig/intermolecular cyclization under microwave irradiation and their structures were confirmed. Preliminary examination of HIV-RT inhibition showed that the dinucleosides containing (R)-thiazolidin-4-one linkage are significantly more active than those containing (S)-thiazolidin-4-one linkage.