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| 1 | Discovery of a series of dimethoxybenzene FGFR inhibitors with 5H-pyrrolo[2,3-b]pyrazine scaffold: structure–activity relationship, crystal structural characterization and in vivo study显示文摘Genomic alterations are commonly found in the signaling pathways of fibroblast growth factor receptors(FGFRs). Although there is no selective FGFR inhibitors in market, several promising inhibitors have been investigated in clinical trials, and showed encouraging efficacies in patients. By designing a hybrid between the FGFR-selectivity-enhancing motif dimethoxybenzene group and our previously identified novel scaffold, we discovered a new series of potent FGFR inhibitors, with the best one showing sub-nanomolar enzymatic activity. After several round of optimization and with the solved crystal structure, detailed structure–activity relationship was elaborated. Together with in vitro metabolic stability tests and in vivo pharmacokinetic profiling, a representative compound(35) was selected and tested in xenograft mouse model, and the result demonstrated that inhibitor 35 was effective against tumors with FGFR genetic alterations, exhibiting potential for further development. | Peng Wei Bo Liu Ruifeng Wang Yinglei Gao Lanlan Li Yuchi Ma Zhiwei Qian Yuelei Chen Maosheng Cheng Meiyu Geng Jingkang Shen Dongmei Zhao Jing Ai Bing Xiong | 2019 | Acta Pharmaceutica Sinica B2019，9，2： | 2 |
| 2 | Engineering cobalt sulfide/oxide heterostructure with atomically mixed interfaces for synergistic electrocatalytic water splitting显示文摘It remains challenging to develop economical and bifunctional electrocatalysts toward oxygen/hydrogen evolution reactions(OER/HER).Herein,we construct Co_(9)S_(8) nanoflakes decorated Co_(3)O_(4) nanoarrays with enriched heterogeneous interface zones on Ni foam(Co_(9)S_(8)@CO_(3)O_(4)/NF)via a novel step-wise approach.The Co_(9)S_(8)@Co_(3)O_(4)/NF hybrid manifests excellent performance with low overpotentials of 130 mV for HER(10 mA·cm^(-2))and 331 mV for OER(100 mA·cm^(-2)),delivering a small voltage of 1.52 V for water splitting at 10 mA·cm^(-2) as well as outstanding catalytic durability,which surpasses precious metals and previously reported earth-abundant nanocatalysts.Further experimental and theoretical investigations demonstrate that the excellent performance is attributed to the followings:(i)Highly conductive Ni facilitates the efficient charge transfer;(ii)porous core-shell nanoarchitecture benefits the infiltration and transportation of gases/ions;(iii)heterogeneous interface zones synergistically lower the chemisorption energy of hydrogen/oxygen intermediates.This work will shed light on the controllable synthesis and engineering of heterostructure nanomaterials for clean energy storage and conversion technologies. | Xiaoyang Wang Yu He Xiaopeng Han Jun Zhao Lanlan Li Jinfeng Zhang Cheng Zhong Yida Deng Wenbin Hu | 2022 | Nano Research2022，15，2： | 2 |
| 3 | Highly stable aqueous rechargeable Zn-ion battery:The synergistic effect between NaV_(6)O_(15) and V_(2)O_(5) in skin-core heterostructured nanowires cathode显示文摘The aqueous rechargeable Zn-ion batteries based on the safe,low cost and environmental benignity aqueous electrolytes are one of the most compelling candidates for large scale energy storage applications.However,pursuing suitable insertion materials may be a great challenge due to the strong electrostatic interaction between Zn^(^(2+))and cathode materials.Hence,a novel NaV_(6)O_(15)/V_(2)O_(5) skin-core heterostructure nanowire is reported via a one-step hydrothermal method and subsequent calcination for high-stable aqueous Zn-ion batteries(ZIBs).The NaV_(6)O_(15)/V_(2)O_(5) cathode delivers high specific capacity of 390 m Ah/g at 0.3 A/g and outstanding cycling stability of 267 m Ah/g at 5 A/g with high capacity retention over 92.3%after 3000 cycles.The superior electrochemical performances are attributed to the synergistic effect of skin-core heterostructured NaV_(6)O_(15)/V_(2)O_(5),in which the sheath of NaV_(6)O_(15) possesses high stability and conductivity,and the V_(2)O_(5) endows high specific capacity.Besides,the heterojunction structure not only accelerates intercalation kinetics of Zn^(2+)transport but also further consolidates the stability of the layers of V_(2)O_(5) during the cyclic process.This work provides a new perspective in developing feasible insertion materials for rechargeable aqueous ZIBs. | Lanlan Fan Zhenhuan Li Weimin Kang Bowen Cheng | 2021 | Journal of Energy Chemistry2021，30，4： | 0 |
| 4 | Inhibitory effect of resveratrol on the proliferation of GH3 pituitary-adenoma cells and voltage-dependent potassium current显示文摘BACKGROUND: Recent researches indicate that activation of potassium channel is likely to cause many kinds of cells to proliferate and differentiate; using chemical to block the potassium channel can restrain the proliferation of small lung-cancer cells, breast cancer, prostate cancer and human lymphocyte, etc. Previous researches proved that resveratrol (RE), a selective estrogen receptor modulator (SERM), could inhibit growth of GH3 cells, induce apoptosis, and resist tumor through interfering K+ channel. OBJECTIVE: To investigate the effects of RE on voltage-dependent K+ current [IK(V)] and cell proliferation in GH3 pituitary-tumor cells. DESIGN: Observational contrast study. SETTING: Department of Neurosurgery, the First Clinical Hospital of Harbin Medical University; Department of Microbiology, Harbin Medical University; Department of Pharmacology, Harbin Medical University. MATERIALS: GH3 pituitary-tumor cell line of rats was purchased from the American Type Culture Collection (ATCC). RE and [3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-tetrazolium bromide] (MTT) were obtained from Sigma Chemical Co, St Louis, USA; Ham’s F-10 medium from Gibco BRL; Equine serum and fetal bovine serum from Hyclone Laboratories, Logan, UT; FACSCalibur flow cytometer from BD Company, USA. RE was dissolved in ethanol and stored at -20 ℃. It was diluted to different concentrations (10, 50, 100 μmol/L) with medium and extra cellular solution when needed. The final concentration of ethanol was less than 0.01%. METHODS: The experiment was carried out in the Department of Microbiology and Pharmacology of Harbin Medical University from March 2005 to January 2006. ① Cell preparation: Proliferating indexes affected by 10, 50 and 100 μmol/L RE were measured with MTT, respectively. 0.000 1 volume fraction of ethanol was added into control group. Inhibitory rate of cellular growth was calculated as the following formula: Inhibitory rate (%) = (1 - A value in experimental group/ A value in control group)×100%. The experiments mentioned above were done for 3 times. ② Cell cycle with flow cytometry: Cell cycle and apoptosis rate were measured in RE groups (affected by RE in various concentrations) and control group (affected by 0.000 1 volume fraction of ethanol) with flow cytometry. ③ Whole-cell patch clamp electrophysiological recording: The GH3 cells were used for experiment when adhesion was well to the bottom with continuously flush of Ca2+-free Tyrode’s solution at 3 mL/min after 48 hours incubation in 3.5 cm diameter plate. The potassium current and resting potential of the same cell without RE and with different concentrations of RE were recorded with the whole cell voltage-clamp method and current-clamp method. Cells before adding medicines were regarded as in control group; otherwise in experimental group. ④ Statistical analysis: The differences between different treatment groups were determined by the analysis of variance and t test. MAIN OUTCOME MEASURES: Effect of RE in different concentrations on cell proliferation, distribution of cell cycle, and IK (V) in GH3 cell. RESULTS: ① Influence of RE in different concentrations on the proliferation of GH3 cell: MTT assay showed the cell growth suppression rate was 44.6%, 52.3%, 61.9% respectively at the dose of 10 μmol/L, 50 μmol/L and 100 μmol/L and had a dose-effect relationship after 3 days incubation with RE. They were statistically significant in comparison with the cells without treatment of RE (P < 0.05-0.01). ② Influence of RE on GH3 cell proliferating cycle: Flow cytometry results revealed all cells with treatment of RE were blocked in the G0/G1 stage of cell cycle. The cell proportion in the S and G2/M stage decreased significantly. There was positive correlation existed between effects of RE and RE concentration. There was significant difference as compared with control group (P < 0.05-0.01). ③ Influence of RE on the voltage-dependent K+ current and membrane resting potential of GH3 cell: The voltage-dependent extroversion K+ current [IK(V)] was recorded in control group; apparently IK(V) decrease in 50 μmol/L and 100 μmol/L RE groups; no changes of IK(V) in 10 μmol/L RE group. The IK(V) value changed from (1 250±62) pA to (93±39) pA (P < 0 05) when 50 μmol/L RE was added. CONCLUSION: The anti-proliferative activity of RE may be partially explained by blockade of voltage-dependent K+ channel present in GH3 cells; meanwhile, the effect is characterized by dosage dependence. | Ming Chu Lanlan Wei Chao Wang Yu Cheng Kongbin Yang Baofeng Yang | 2006 | Neural Regeneration Research2006，1，6： | 0 |
| 5 | Robust Co_(3)O_(4)nanocatalysts supported on biomass-derived porous N-doped carbon toward low-pressure hydrogenation of furfural显示文摘The catalytic conversion of biomass platform chemicals using abundant non-noble metal nanocatalysts is a challenging topic.Here,high-density cobalt oxide nanoparticles loaded on biomass-derived porous N-doped carbon(NC)was fabricated by a tandem hydrothermal pyrolysis and mild nitrate decomposition process,which is a green and cheap preparation method.The Co_(3)O_(4) nanoparticles with the average size of 12 nm were uniformly distributed on the porous NC.The nanocomposites also possessed large surface area,high N content,good dispersibility in isopropanol,and furfural absorbability.Due to these characteristics,the novel cobalt nanocatalyst exhibited high catalytic activity for producing furfuryl alcohol,yielding 98.7%of the conversion and 97.1%of the selectivity at 160℃ for 6 h under 1 bar H2.The control experiments implied that both direct hydrogenation and transfer hydrogenation pathways co-existed in the hydrogenation reaction.The excellent catalytic activity of Co_(3)O_(4)@NC was attributed to the cooperative effects of porous NC and Co_(3)O_(4) nanoparticles.This approach provides a new idea to design effective high-density nonnoble metal oxide nanocatalysts for hydrogenation reactions,which can make full use of sustainable natural biomass. | Lin Zhang Lanlan Cheng Yechen Hu Qingguang Xiao Xiufang Chen Wangyang Lu | 2023 | Frontiers of Materials Science2023，17，2： | 0 |
| 6 | The effect of aluminum of human islet amyioid ion on the aggregation polypeptide (11-28)显示文摘 | Lanlan Su Cheng Lu Peng Yan Nan Zhang Sheng Cai Gongjun Zhang Xingfei Zhou Bin Li | 2017 | Acta Biochimica et Biophysica Sinica2017，49，4： | 0 |
| 7 | On the chronological understanding of the homogeneous dielectric barrier discharge显示文摘Dielectric barrier discharges(DBD)are widely utilised non‐equilibrium atmospheric pressure plasmas with a diverse range of applications,such as material processing,surface treatment,light sources,pollution control,and medicine.Over the course of several decades,extensive research has been dedicated to the generation of homogeneous DBD(H‐DBD),focussing on understanding the transition from H‐DBD to filamentary DBD and exploring strategies to create and sustain H‐DBD.This paper first discusses the in-fluence of various parameters on DBD,including gas flow,dielectric material,surface conductivity,and mesh electrode.Secondly,a chronological literature review is presented,highlighting the development of H‐DBD and the associated understanding of its un-derlying mechanisms.This encompasses the generation of H‐DBD in helium,nitrogen,and air.Lastly,the paper provides a brief overview of multiple‐current‐pulse(MCP)behaviours in H‐DBD.The objective of this article is to provide a chronological un-derstanding of homogeneous dielectric barrier discharge(DBD).This understanding will aid in the design of new experiments aimed at better comprehending the mechanisms behind H‐DBD generation and ultimately assist in achieving large‐volume H‐DBD in an air environment. | Xinpei Lu Zhi Fang Dong Dai Tao Shao Feng Liu Cheng Zhang Dawei Liu Lanlan Nie Chunqi Jiang | 2023 | High Voltage2023，8，6： | 0 |
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