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1. Quantitative Determination of Acetylcholine and Choline with Graphene Oxide-Based MALDI-TOF-MS | |||
LI Yan,ZHOU Ning,DUAN Gengli,YU Yingjia | |||
Pharmacy 30 August 2011 | |||
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Abstract:Purpose: The aim of this work is to establish a novel method for quick quantitative determination of acetylcholine (ACh) and choline (Ch) with mass spectrometry. Method and Results: The determination of ACh and Ch has been established by matrix-assisted laser desorption/ionization time-of-flight mass spectrometry (MALDI-TOF MS) with grapheme oxide instead of conventional organic acid as matrix. The obtained results indicated a low limit of detection (LOD) for ACh (0.25 fmol/μL), and excellent linearity (R2=0.9998) maintained over the range of 0.5 and 250 fmol/μL. Choline was quantified over the range of 0.05 and 15 pmol/μL, also with excellent linearity (R2=0.9994) and low LOD (15 fmol/μL). Good accuracy and precision were obtained for all concentrations within the range of the standard curves. Conclusion: The developed method was quick and reliable for quantitative determination of ACh and Ch, and may have great potential in high throughput screening of acetylcholinesterase inhibitor (AChEI). | |||
TO cite this article:LI Yan,ZHOU Ning,DUAN Gengli, et al. Quantitative Determination of Acetylcholine and Choline with Graphene Oxide-Based MALDI-TOF-MS[OL].[30 August 2011] http://en.paper.edu.cn/en_releasepaper/content/4441258 |
2. Antidepressant effect of Cynanchum wallichii in Mice | |||
YANG Qiong-xiong,HUANG Xiao-yan | |||
Pharmacy 28 July 2011 | |||
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Abstract:In this paper, the antidepressant activity of the total glycosides from C. wallichii (TGCW) is investigated for the first time. The tail suspension test (TST), forced swimming test (FST) and open field test (OPT) in mice were used to evaluated the antidepressant effect of TGCW, and experiment of antagonism of reserpine-induced ptosis and hypothermia in mice was conducted to evaluate whether the central monoaminergic neurotransmitter system was involved in the mechanism of the antidepressant activity. The results showed that reduction of the immobility duration in TST and FST in mice showed the obvious dose-response relation for TGCW. With a dose of 80 mg/kg, reduction degree was 47.4% (p<0.01) in TST and 48.2% (p<0.01) in FST, corresponding to 64.1% (p<0.01) and 62.3% (p<0.01) for the positive control chlorimipramine (20 mg/kg, i.g.). The number of crossing and rearing mice in treating groups was not significantly different from that in the vehicle control group, and only at dose of 80mg/kg significantly antagonized reserpine-induced ptosis and hypothermia in mice. These findings demonstrate that TGCW have apparent antidepressant activity, and the mechanism via central monoaminergic neurotransmitter system for the antidepressant activity of TGCW may be involved. | |||
TO cite this article:YANG Qiong-xiong,HUANG Xiao-yan. Antidepressant effect of Cynanchum wallichii in Mice[OL].[28 July 2011] http://en.paper.edu.cn/en_releasepaper/content/4436987 |
3. Pharmacokinetic study of isoimperatorin in rats using UPLC-MS/MS and a drug dissolution/absorption simulating system | |||
LI Chao,Feng Shan,HE Xin | |||
Pharmacy 04 June 2011 | |||
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Abstract:A pharmacokinetic study of isoimperatorin (IO), one of the major bioactive ingredients in the herb, Angelicae dahuricae, was performed in rats (n = 10) using a newly developed ultra-performance liquid chromatography-tandem mass spectrometry method. Tandem mass spectrometry was performed and the protonated parent→daughter ion pairs at m/z 271.02→202.9 for IO and m/z 216.9→173.7 for the internal standard, bergapten, were monitored. The analysis was validated with respect to linearity, recovery, specificity, accuracy, and precision. The pharmacokinetic parameters were obtained by non-compartmental analysis. After administration, IO was extensively distributed and rapidly eliminated from the plasma. The parameters also indicate a lower IO plasma concentration and poor absorption. Factors that led to this result were the instability of IO in acidic and basic conditions, poor solubility, and low dissolution rate. The stability of IO was observed at different pH levels using high-performance liquid chromatography, and the solubility at physiological conditions was determined using a novel drug dissolution/absorption simulating system. | |||
TO cite this article:LI Chao,Feng Shan,HE Xin. Pharmacokinetic study of isoimperatorin in rats using UPLC-MS/MS and a drug dissolution/absorption simulating system[OL].[ 4 June 2011] http://en.paper.edu.cn/en_releasepaper/content/4431337 |
4. Spectral, Mathematical and Electrophoretic Models for Anti-tumor Activity Evaluation and Intercalation Mechanism Investigation of Small Molecules | |||
XU Yanxia,ZHAO Ming,ZHANG Xiaoyi,WANG Yuji,WU Jianhui,HU Fei,ZHANG Jianwei,PENG Shiqi | |||
Pharmacy 24 February 2011 | |||
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Abstract:For improving the cancer chemotherapy the discovery of new DNA intercalators is one of the effective approaches. The investigations have demonstrated the utility of the models in both anti-tumor activity evaluation and the intercalation mechanism identification. This paper described the DOCK score, ultraviolet (UV), fluorescence, circular dichroism (CD), relative viscosity, melting curve, kinetics in CT DNA sta- cking of small molecule intercalator, kinetics in CT DNA intercalation of small mole- cule intercalator, interaction stabilizing the stacking complex of small molecule inter- calator and CT DNA and the gel electrophoresis based models as well as their use in the identification of small molecule intercalating towards DNA. | |||
TO cite this article:XU Yanxia,ZHAO Ming,ZHANG Xiaoyi, et al. Spectral, Mathematical and Electrophoretic Models for Anti-tumor Activity Evaluation and Intercalation Mechanism Investigation of Small Molecules[OL].[24 February 2011] http://en.paper.edu.cn/en_releasepaper/content/4412178 |
5. Fluroscence-based assay to calculate dissociation rate constant of β-secretase (BACE1) inhibitors | |||
ZHAO Ying | |||
Pharmacy 17 February 2011 | |||
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Abstract:β-secretase (BACE1) is one of the potential drug target for Alzheimer's Disease (AD). The ideal clinically available BACE1 inhibitors should have some features, such as good effect, low dose and high selectivity. The dissociation rate constant (Koff) is useful to predict the selectivity of a BACE1 inhibitor. Based on the common used fluorescent inhibitory activity measurement, we developed the assay to measure Ki and Kon of BACE1 inhibitor, and calculated Koff using the relationship of Ki = Koff / Kon. In our assay, a tight-binding inhibitor of BACE1, OM99-2, was measured to have the Koff of 9.54×10-4 S-1, which is in good accordance with previous literature. This assay is economic and simple to use, providing a rapid way for Koff measurement of BACE1 inhibitors, which may further contribute to SAR studies. | |||
TO cite this article:ZHAO Ying. Fluroscence-based assay to calculate dissociation rate constant of β-secretase (BACE1) inhibitors[OL].[17 February 2011] http://en.paper.edu.cn/en_releasepaper/content/4411026 |
6. A Pharmacophore Model and Database Searching for Serotonin 2A Receptor Antagonists | |||
FU Wei,LIU Huifang,LI Bian | |||
Pharmacy 06 January 2011 | |||
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Abstract:The serotonin 2A receptor has been implicated in several neurological conditions and potent 5-HT2A antagonists have therapeutic effects in the treatment of Schizophrenia and depression. In this paper, we reported computational homology modeling of the 5-HT2A receptor based on the high-resolution X-ray structure of β2-adrenergic receptor. The accuracy of the model was validated through Procheck 3.5.4 and AutoDock 4.0 program. The antagonistic conformation of 5-HT2A was obtained by the investigation of the interaction mode of 5-HT2A with well-known potent antagonist ketanserin. The active site of the 5-HT2A receptor was mapped by five types of chemical probes by means of grid calculation. The Cluster analysis in combination with the available experimental pharmacological data was applied to guide the selection of the pharmacophore feature. Pharmacophore model was built by means of the Catalyst 4.10 and database searching was carried out on Asinex Gold Collection database, which contains ca. 200,000 molecules. As a result, 463 hits were obtained. The Lipinski's Rule of Five was used to filter out the non-drug like redundancies, the scoring function was used to rank the hits and docking study was used for the final selection. Finally, 14 molecules were selected and purchased for further biological test. | |||
TO cite this article:FU Wei,LIU Huifang,LI Bian. A Pharmacophore Model and Database Searching for Serotonin 2A Receptor Antagonists[OL].[ 6 January 2011] http://en.paper.edu.cn/en_releasepaper/content/4404495 |
7. Preparation and characterization of novel dendrimer-based gene delivery systems | |||
Huang Rongqin,Liu Shuhuan,Han Liang,Jiang Chen | |||
Pharmacy 04 January 2011 | |||
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Abstract:Purpose: Dendrimers have attracted great interests in the field of gene delivery due to their synthetic controllability and excellent gene transfection efficiency. The aim of this work is to develop a novel dendrimer-based gene delivery system. Methods and Results: Dendrigraft poly-L-lysines (DGLs) were evaluated as a novel gene vector for the first time. Derivatives of DGLs (generation 2 and 3) with different extents of PEGylation were successfully synthesized and used to compact pDNA as complexes. The result of gel retardation assay showed that pDNA could be effectively packed by all the vectors at a DGLs to pDNA weight ratio greater than 2. An increase in the PEGylation extent of vectors resulted in a decrease in the incorporation efficiency and cytotoxicity of complexes in 293 cells, which also decreased the zeta potential a little but did not affect the mean diameter of complexes. Higher generation of DGLs could mediate higher gene transfection in vitro. Confocal microscopy and cellular uptake inhibition studies demonstrated that caveolae-mediated process and macropinocytosis were involved in the cellular uptake of DGLs-based complexes. Conclusion: All the results indicate that proper PEGylated DGLs could mediate efficient gene tranfection, showing their potential as an alternate biodegradable vector in the field of nonviral gene delivery. | |||
TO cite this article:Huang Rongqin,Liu Shuhuan,Han Liang, et al. Preparation and characterization of novel dendrimer-based gene delivery systems[OL].[ 4 January 2011] http://en.paper.edu.cn/en_releasepaper/content/4402823 |
8. A Pharmacophore Model and Database Searching for Dopamine D2 Receptor Antagonists | |||
FU Wei,LI Bian,LIU Huifang | |||
Pharmacy 04 January 2011 | |||
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Abstract:The dopamine D2 receptor (D2R) has been implicated in several neurological conditions and potent D2R antagonists have therapeutic effects in the treatment of schizophrenia and depression. In this paper, we reported computational homology modeling of the D2R based on the high-resolution X-ray structure of β2-adrenergic receptor. The accuracy of the model was validated through Procheck 3.5.4 and AutoDock 4.0 program. The active site of the D2R receptor was mapped by five types of chemical probes by means of grid calculation. The cluster analysis in combination with the available experimental pharmacological data was applied to guide the selection of the pharmacophore feature. Pharmacophore model was built by means of the Catalyst 4.10 and database searching was carried out on Asinex Gold Collection database, which contains ca. 200,000 molecules. As a result, 463 hits were obtained. The Lipinski's Rule of Five was used to filter out the non-drug like molecules, the scoring function was used to rank the hits and docking study was used for the final selection. Finally, 6 molecules were selected and purchased for further biological test. | |||
TO cite this article:FU Wei,LI Bian,LIU Huifang. A Pharmacophore Model and Database Searching for Dopamine D2 Receptor Antagonists[OL].[ 4 January 2011] http://en.paper.edu.cn/en_releasepaper/content/4403687 |
9. Identification of trans-tiliroside as active principle with anti-hyperglycemic,anti-hyperlipedemic and antioxidant effects from Potentilla chinesis | |||
Qiao Wei,Zhao Chuan,Qin Nan,Zhai Huiyuan,Duan Hongquan | |||
Pharmacy 23 December 2010 | |||
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Abstract:Aim of the study: The present study was carried out to isolate and identify trans-tiliroside as principal compound with anti-hyperglycemic, anti-hyperlipidemic and antioxidant effects from Potentilla chinesis. Methods: A bioactive compound, trans-tiliroside has been isolated from the ethanol extract of Potentilla chinesis.The normal, alloxan-induced diabetic mice and streptozotocin-induced diabetic rats were used to evaluate the anti-hyperglycemic, anti-hyperlipidemic and antioxidant effects of trans-tiliroside from Potentilla chinesis. Results: Trans-tiliroside in normal and diabetic mice significantly decrease the level of serum glucose levels, TG and TC in alloxan-induced diabetic mice. In streptozotocin induced diabetic rats, trans-tiliroside showed a significant decrease in blood glucose level. The content of TC, LDL-C and TG levels were decreased and high density lipoprotein HDL-C content was increased, so lipid metabolism was improved. Moreover, trans-tiliroside revealed can increased antioxidant activity in diabetic rats. Histological morphology examination showed that the trans-tiliroside restored the damage of pancreas tissues in rats with diabetes mellitus. Conclusion: Trans-tiliroside revealed significant anti-hyperglycemic, anti-hyperlipidemic and antioxidant activities. | |||
TO cite this article:Qiao Wei,Zhao Chuan,Qin Nan, et al. Identification of trans-tiliroside as active principle with anti-hyperglycemic,anti-hyperlipedemic and antioxidant effects from Potentilla chinesis[OL].[23 December 2010] http://en.paper.edu.cn/en_releasepaper/content/4399296 |
10. Targeted delivery of chlorotoxin-modified DNA-loaded nanoparticles to glioma via intravenous administration | |||
Huang Rongqin ,Ke Weilun ,Jiang Chen | |||
Pharmacy 06 December 2010 | |||
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Abstract:Purpose: Chlorotoxin (CTX) was exploited as the targeting ligand to conjugate the nanoscopic high-branching dendrimer, polyamidoamine (PAMAM), via bifunctional polyethyleneglycol (PEG), yielding PAMAM-PEG-CTX. After complexing with DNA, a novel glioma-targeting gene delivery system was constructed. Methods and Results: The cellular uptake of CTX itself was observed apparently in C6 glioma cells, almost not in 293 cells. The modification of CTX could significantly increase the cellular uptake of vectors and the DNA-loaded nanoparticles (NPs) in C6 cells. The in vivo distribution of PAMAM-PEG-CTX/DNA NPs in the brain was higher than that of PAMAM/DNA NPs and PAMAM-PEG/DNA NPs. Furthermore, the gene expression of PAMAM-PEG-CTX/DNA NPs was higher and boarder in glioma than that of unmodified and PEG-modified counterparts. The TUNEL analysis showed a more wide-extended apoptosis in the CTX-modified group, compared to other groups including commercial temozolomide group. The median survival time of CTX-modified group was 59.5 days, significantly longer than that of other groups. Conclusion: The results suggested that CTX could be exploited as a special glioma-targeting ligand, and PAMAM-PEG-CTX/DNA NPs is a potential non-viral delivery system for gene therapy of glioma via intravenous administration. | |||
TO cite this article:Huang Rongqin ,Ke Weilun ,Jiang Chen . Targeted delivery of chlorotoxin-modified DNA-loaded nanoparticles to glioma via intravenous administration[OL].[ 6 December 2010] http://en.paper.edu.cn/en_releasepaper/content/4394541 |
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