http://chineseinput.net/에서 pinyin(병음)방식으로 중국어를 변환할 수 있습니다.
변환된 중국어를 복사하여 사용하시면 됩니다.
Design and Synthesis of Pyrazolyl Thiosemicarbazones as New Anticonvulsants
Deng, Xian Qing,Song, Ming Xia Korean Chemical Society 2014 Bulletin of the Korean Chemical Society Vol.35 No.9
A series of pyrazolyl thiosemicarbazone derivatives were synthesized and evaluated for their anticonvulsant activity using the maximal electroshock (MES) method. Interestingly, all compounds prepared showed long duration of protection effect in the MES screens. Among them, compound 5b was considered as the most promising one with an $ED_{50}$ value of 47.3 mg/kg, and a PI value of 4.8, which was superior to phenobarbital and valproate in the aspect of safety. Furthermore, compound 5b showed protection against seizures induced by pentylenetetrazole suggesting that compound 5b may exert anticonvulsant activity through GABA-mediated mechanisms.
Deng, Xian-Qing,Wei, Cheng-Xi,Song, Ming-Xia,Chai, Kyu-Yun,Sun, Zhi-Gang,Quan, Zhe-Shan Korean Chemical Society 2010 Bulletin of the Korean Chemical Society Vol.31 No.2
A series of 5-alkoxy-tetrazolo[1,5-a]quinolines were synthesized to evaluate their anticonvulsant and antidepressant effects. Anticonvulsant effects and neurotoxicity of the compounds when injected intraperitoneally to mice were determined by a maximal electroshock (MES) test and a rotarod test, respectively. Only three of the synthesized compounds (4a, 4b, 4c) displayed anticonvulsant activity at a dose of 300 mg/kg. Most of the compounds significantly reduced immobility times during the forced swimming test (FST) at a dose of 100 mg/kg, indicative of antidepressant activity. Among the compounds, 5-(2-fluorobenzyloxy)tetrazolo[1,5-a]quinoline (4k) reduced immobility time by 66.85% at 30 mg/kg compared with the same dose of Fluoxetine, which reduced immobility time by 52.30%. According to the results of the 5-Hydroxytryptophan induced head-twitch test and yohimbine toxicity potentiation test, the noradrenergic system seems not to be involved in the antidepressant-like effect of compound 4k while the serotonergic system seems a little to be involved.
Design and Synthesis of Pyrazolyl Thiosemicarbazones as New Anticonvulsants
Xian Qing Deng,Ming-Xia Song 대한화학회 2014 Bulletin of the Korean Chemical Society Vol.35 No.9
A series of pyrazolyl thiosemicarbazone derivatives were synthesized and evaluated for their anticonvulsant activity using the maximal electroshock (MES) method. Interestingly, all compounds prepared showed long duration of protection effect in the MES screens. Among them, compound 5b was considered as the most promising one with an ED50 value of 47.3 mg/kg, and a PI value of 4.8, which was superior to phenobarbital and valproate in the aspect of safety. Furthermore, compound 5b showed protection against seizures induced by pentylenetetrazole suggesting that compound 5b may exert anticonvulsant activity through GABAmediated mechanisms.
Xian-Qing Deng,Cheng-Xi Wei,Ming-Xia Song,채규윤,Zhi-Gang Sun,Zhe-Shan Quan 대한화학회 2010 Bulletin of the Korean Chemical Society Vol.31 No.2
A series of 5-alkoxy-tetrazolo[1,5-a]quinolines were synthesized to evaluate their anticonvulsant and antidepressant effects. Anticonvulsant effects and neurotoxicity of the compounds when injected intraperitoneally to mice were determined by a maximal electroshock (MES) test and a rotarod test, respectively. Only three of the synthesized compounds (4a, 4b, 4c) displayed anticonvulsant activity at a dose of 300 mg/kg. Most of the compounds significantly reduced immobility times during the forced swimming test (FST) at a dose of 100 mg/kg, indicative of antidepressant activity. Among the compounds, 5-(2-fluorobenzyloxy)tetrazolo[1,5-a]quinoline (4k) reduced immobility time by 66.85% at 30 mg/kg compared with the same dose of Fluoxetine, which reduced immobility time by 52.30%. According to the results of the 5-Hydroxytryptophan induced head-twitch test and yohimbine toxicity potentiation test, the noradrenergic system seems not to be involved in the antidepressant-like effect of compound 4k while the serotonergic system seems a little to be involved.
Meta-analysis of the CYP1A2 -163C>A Polymorphism and Lung Cancer Risk
Deng, Sheng-Qiong,Zeng, Xian-Tao,Wang, Yun,Ke, Qing,Xu, Qiong-Li Asian Pacific Journal of Cancer Prevention 2013 Asian Pacific journal of cancer prevention Vol.14 No.5
Many published studies have concerned associations between the CYP1A2 -163 C>A polymorphism and risk of lung cancer, but the results have been inconsistent. Therefore, we performed a meta-analysis to obtain a more precise estimate. We searched the PubMed database up to March 1, 2013 for relevant cohort and case-control studies. Supplementary search was conducted manually by searching the references of the included studies and relevant meta-analyses. A meta-analysis was performed using RevMan 5.2 software for calculation of pooled odds ratios (ORs) and relevant 95% confidence intervals (CIs) after data extraction. Finally, seven case-control studies and one nested case-control study involving 1,675 lung cancer patients and 2,393 controls were included. The meta-analysis showed that there was no association of CYP1A2 -163 C>A polymorphism with risk of lung cancer overall [(OR=0.89, 95%CI= 0.74-1.07) for C vs. A; (OR=0.73, 95%CI= 0.50-1.07) for AA vs. CC ; (OR=0.82, 95%CI= 0.62-1.09) for AC vs. CC; (OR=0.79, 95%CI= 0.58-1.07) for (AC+AA) vs. CC; and (OR=0.87, 95%CI= 0.67-1.13) for AA vs. (CC+AC)]. Subgroup analysis indicated that there was an associationbetween CYP1A2 -163C>A polymorphism and lung cancer risk for population-based controls, a trend risk for SCCL (squamous cell carcinoma of lung) and Caucasians. These results suggested that -163 C>A polymorphism is likely to be associated with risk of lung cancer compared with population-based controls.
Deng, Bao-Guo,Yao, Jin-Hua,Liu, Qing-Yin,Feng, Xian-Jun,Liu, Dong,Zhao, Li,Tu, Bin,Yang, Fan Asian Pacific Journal of Cancer Prevention 2013 Asian Pacific journal of cancer prevention Vol.14 No.10
Background: At present, the diagnosis of colorectal cancer (CRC) requires a colorectal biopsy which is an invasive procedure. We undertook this pilot study to develop an alternative method and potential new biomarkers for diagnosis, and validated a set of well-integrated tools called ClinProt to investigate the serum peptidome in CRC patients. Methods: Fasting blood samples from 67 patients diagnosed with CRC by histological diagnosis, 55 patients diagnosed with colorectal adenoma by biopsy, and 65 healthy volunteers were collected. Division was into a model construction group and an external validation group randomly. The present work focused on serum proteomic analysis of model construction group by ClinProt Kit combined with mass spectrometry. This approach allowed construction of a peptide pattern able to differentiate the studied populations. An external validation group was used to verify the diagnostic capability of the peptidome pattern blindly. An immunoassay method was used to determine serum CEA of CRC and controls. Results: The results showed 59 differential peptide peaks in CRC, colorectal adenoma and health volunteers. A genetic algorithm was used to set up the classification models. Four of the identified peaks at m/z 797, 810, 4078 and 5343 were used to construct peptidome patterns, achieving an accuracy of 100% (> CEA, P<0.05). Furthermore, the peptidome patterns could differentiate the validation group with high accuracy close to 100%. Conclusions: Our results showed that proteomic analysis of serum with MALDI-TOF MS is a fast and reproducible approach, which may provide a novel approach to screening for CRC.
( Yun Deng ),( Yong Qing Li ),( Xiong Wei Fan ),( Wu Zhou Yuan ),( Hua Ping Xie ),( Xiao Yang Mo ),( Yan Yan ),( Jun Mei Zhou ),( Yue Qun Wang ),( Xian Li Ye ),( Yong Qi Wan ),( Xiu Shan Wu ) 생화학분자생물학회 (구 한국생화학분자생물학회) 2010 BMB Reports Vol.43 No.6
LBH is a transcription factor as a candidate gene for CHD associated with partial trisomy 2p syndrome. To identify potential LBH-interacting partners, a yeast two-hybrid screen using LBH as a bait was performed with a human heart cDNA library. One of the clones identified encodes αB-crystallin. Co-immunoprecipitation and GST pull-down assays showed that LBH interacts with αB-crystallin, which is further confirmed by mammalian two-hybrid assays. Co-localization analysis showed that in COS-7 cells, αB-crystallin that is cytoplasmic alone, accumulates partialy in the nucleus when co-transfected with LBH. Transient transfection assays indicated that overexpression of LBH or αB-crystallin reduced the transcriptional activities of p53 and p21, respectively, Overexpression of both αB-crystallin and LBH together resulted in a stronger repression of the transcriptional activities of p21 and p53. These results showed that the interaction of LBH and αB-crystallin may inhibit synergistically the transcriptional regulation of p53 and p21. [BMB reports 2010; 43(6): 432-437]
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.
Shi-Ben Wang,Xian-Qing Deng,Yan Zheng,Hong-Jian Zhang,Zhe-Shan Quan 대한약학회 2013 Archives of Pharmacal Research Vol.36 No.1
Two series of 8-alkoxy-5-(4H-1,2,4-triazol-4-yl)quinolines and 8-alkoxy-5-(2H-1,2,4-triazol-3-one-4-yl)quinolineswere synthesized.The anticonvulsant activity ofthese compounds was evaluated with maximal electroshockseizure test and rotarod test. Among the synthesized compounds,8-octoxy-5-(4H-1,2,4-triazol-4-yl)quinoline (4g)was the most active compound with ED50 of 8.80 mg/kg,TD50 of 176.03 mg/kg and protective index of 20.0. Itsneurotoxicity was lower than all other synthesized compoundsand also markedly lower than that of the referencedrug carbamazepine. In addition, the potency of compound 4gagainst seizures induced by pentylenetetrazole, 3-mercaptopropionicacid, and bicuculline suggested its broad spectrumactivity, and the mechanisms of action including inhibition ofvoltage-gated ion channels and modulation of GABAergicactivity might involve in its anticonvulsant activity.
Song, Ming-Xia,Deng, Xian-Qing,Wei, Zhi-Yu,Zheng, Chang-Ji,Wu, Yan,An, Chang-Shan,Piao, Hu-Ri Shaheed Beheshti University of Medical Sciences 2015 Iranian journal of pharmaceutical research Vol.14 No.1
<P>The microbial resistance has become a global hazard with the irrational use of antibiotics. Infection of drug-resistant bacteria seriously threatens human health. Currently, there is an urgent need for the development of novel antimicrobial agents with new mechanisms and lower levels of toxicity. In this paper, a series of (<I>S</I><I>,Z</I>)-4-methyl-2-(4-oxo-5-((5-substitutedphenylfuran-2-yl) methylene)-2-thioxothiazolidin-3-yl)pentanoic acids via a Knoevenagel condensation were synthesized and evaluated for their antibacterial activity <I>in</I><I>-</I><I>vitro</I>. The synthesized compounds were characterized by IR, <SUP>1</SUP>H NMR and MS. The antibacterial test<I> in</I><I>-</I><I>vitro</I> showed that all of the synthesized compounds had good antibacterial activity against several Gram-positive bacteria (including multidrug-resistant clinical isolates) with minimum inhibitory concentration (MIC) values in the range of 2–4 µg/mL. Especially compounds 4c, 4d, 4e and 4f were the most potent, with MIC values of 2 µg/mL against four multidrug-resistant Gram-positive bacterial strains.</P>