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1. Synthesis, Crystal Structure and Theoretical Study of Novel Bromoquinoline | |||
REN Yu,CUI Sheng-Feng,GENG Rong-Xia,ZHOU Cheng-He | |||
Pharmacy 26 February 2014 | |||
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Abstract:A new 4-bromo-6,8-difluoro substituted quinoline derivative 3 was synthesized and characterized by IR, 1H NMR, MS and X-ray single-crystal diffraction. The target compound crystallized in a orthorhombic system, space group Pbca with a = 13.6139(3), b = 13.6440(3), c = 17.4199(4) ?, α = 90.000(2), β = 90.000(2), γ = 90.000(2) , V = 3235.71(13) ?3, Z = 8, C14H11N2OF2Br3, Mr = 500.96, F(000) = 1920, Dc = 2.057 g/cm3, μ = 9.47 mm?1, R = 0.040 and wR = 0.103 for 2888 independent (Rint = 0.026) and 2463 observed (I > 2σ(I)) reflections. In this crystal, one of the Br atoms on the alkyl chain was disordered over two positions with refined occupancies of 0.8698(1) and 0.1301(9). The calculated geometrical parameters of this compound were consistent with the experimental values. This compound possessed moderate antimicrobial activity. | |||
TO cite this article:REN Yu,CUI Sheng-Feng,GENG Rong-Xia, et al. Synthesis, Crystal Structure and Theoretical Study of Novel Bromoquinoline[OL].[26 February 2014] http://en.paper.edu.cn/en_releasepaper/content/4587493 |
2. Synthesis, Characterization, and Crystal Structures of Propargyl Naphthalimides | |||
PENG Li-Ping,LV Jing-Song,ZHOU Cheng-He | |||
Pharmacy 26 February 2014 | |||
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Abstract:Two title molecules, 6-bromo-2-(prop-2-ynylamino)-1H-benzo[de]isoquinoline -1,3(2H)-dione (4) and 6-bromo-2-(diprop-2-ynylamino)-1H-benzo[de]isoquinoline-1,3(2H)-dione (5), were synthesized and characterized by single-crystal X-ray diffraction, IR, 1H NMR, MS, fluorescence spectra, and powder X-ray diffraction (PXRD). The structure of crystal 4 (CCDC 981232) belongs to the triclinic system, space group P-1 with a = 7.5827(5), b = 7.8886(6), c = 10.5217(7) ?, α = 96.368(6), β = 90.223(5), γ = 92.353(6)o, V = 624.95(7) ?3, Dc = 1.749 g/cm3, μ = 4.52 mm-1, F(000) = 328, Rint = 0.0260, R (I > 2σ(I)) = 0.0622, wR (I > 2σ(I)) = 0.1454, R (all data) = 0.0683 and wR (all data) = 0.1484. In this crystal, a 2D layer supramolecular network structure was formed through hydrogen bonds of N(2)?H(2)oooO(1) and C(15)?H(15)oooO(1), and the Br atom was disordered over two positions with refined occupancies of 0.8589(3) and 0.1410(7). The calculated bond lengths and bond angles of compound 4 were consistent with the result of crystallography. Fluorescence properties of compounds 4 and 5 in different solvents were also studied. Moreover, the two synthesized compounds 4 and 5 were screened for their antimicrobial activities against seven bacteria and four fungi. Bioactive assay manifested that the two compounds exhibited moderate antibacterial and antifungal activities against the tested strains in comparison with the reference drugs norfloxacin, chloromycin and fluconazole. | |||
TO cite this article:PENG Li-Ping,LV Jing-Song,ZHOU Cheng-He. Synthesis, Characterization, and Crystal Structures of Propargyl Naphthalimides[OL].[26 February 2014] http://en.paper.edu.cn/en_releasepaper/content/4587490 |
3. The Peraration of Self-Microemulsifying Drug Delivery System for Elemene and Its In vitro Evaluation | |||
GU Mancang,QIAN Yafang,CHEN Jing | |||
Pharmacy 02 February 2014 | |||
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Abstract:Our study developed a noval self-microemulsifying drug delivery system (SMEDDS) to enhance oral absorption of elemene and evaluated its oral bioavailability in rats. Pseudo-ternary phase diagrams were constructed to identify the efficient self-microemulsification region. SMEDDS formulations were further optimized by measurement of mean droplet size and emulsification time. The in vitro release profile of SMEDDS was determined in different aqueous media. The optimal formulation consisted of 10%Miglyol? 812, 41.7%Cremophor? EL, 8.3%Labrasol? ,20%Transcutol? P as well as 200 mg/g elemene, and demonstrated a higher release rate in simulated gastric fluid than emulsion and pure drug. Our results indicate that SMEDDS is a potential and promising drug delivery system for lipophilic Chinese herbal medicines, such as elemene. | |||
TO cite this article:GU Mancang,QIAN Yafang,CHEN Jing. The Peraration of Self-Microemulsifying Drug Delivery System for Elemene and Its In vitro Evaluation[OL].[ 2 February 2014] http://en.paper.edu.cn/en_releasepaper/content/4584449 |
4. The influence of C-terminal residue N-methylation on opioid activities of endomorphin-2 | |||
DIAO Yuxiang,WANG Changlin | |||
Pharmacy 21 January 2014 | |||
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Abstract:In the present study, the endomorphin-2 (EM-2) analogs with N-methylated modifications at C-terminal residue were investigated. Evaluating the opioid affinity, guinea pig ileum (GPI) / mouse vas deferens (MVD) potency and in vitro colonic contraction of these analogs, our results demonstrated that all analogs exerted lower μ-opioid receptor affinities and GPI/MVD potencies. The μ-opioid affinity of analog 3 was qualitatively similar to that of analog 1, but lower than that of EM-2. However, this analog showed a δ-opioid receptor affinity approximately 2-fold higher than that of EM-2. Moreover, the EC50 values on contractions of the longitudinal muscle of distal colon induced by analogs 1 and 3 were about 1.5 and 4-fold higher than that of EM-2, respectively, and the contractile effects induced by analogs 2 and 4 were deeply attenuated. Our recent results gave the evidence that N-methylated modifications of the C-terminal residue was crucial for opioid pharmacological activities of EM-2 analogs. | |||
TO cite this article:DIAO Yuxiang,WANG Changlin. The influence of C-terminal residue N-methylation on opioid activities of endomorphin-2[OL].[21 January 2014] http://en.paper.edu.cn/en_releasepaper/content/4583402 |
5. Preparation and evaluation of Angiopep-2 peptide grafted micelle for brain targeting delivery | |||
QUAN Yi,JIN Mingji,LI Yunfei,WANG Qiming,SHAO Rongguang,GAO Zhonggao | |||
Pharmacy 20 January 2014 | |||
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Abstract:In this paper, a novel drug-loaded micelle for brain targeting delivery was developed by conjugating the targetable moiety Angiopep-2 peptide on the surface of micelle. In order to monitoring the size of the tumor inside of the brain after treatment, the technique of bioluminescence imaging in living rats was developed. The luciferase-labelled glioma cell line C6-Luc was firstly constructed through cell transfection and monoclone screening, and then evaluated by luciferase reporter assay. The anti-glioma effect of Doxorubicin-loaded targetable micelle was assessed through cell MTT assay and determining the survival time of glioma bearing rats. The results demonstrated that such Doxorubicin-loaded targetable micelle showed a strong anti-glioma effect, and it could significantly prolong the life span of glioma bearing rats, which suggested that Angiopep-2 modified micelles is a promising carrier for drug brain targeting delivery. | |||
TO cite this article:QUAN Yi,JIN Mingji,LI Yunfei, et al. Preparation and evaluation of Angiopep-2 peptide grafted micelle for brain targeting delivery[OL].[20 January 2014] http://en.paper.edu.cn/en_releasepaper/content/4583312 |
6. Synthesis and biological evaluation of cytotoxic activity of 14-(β-D-2-deoxy-ribopyranosyl)-naphtho [2,1-a]pyrrolo[3,4-c]carbazole-5,7(6H,12H)-dione | |||
DING Ning | |||
Pharmacy 20 January 2014 | |||
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Abstract:Naphtho[2,1-a]pyrrolo[3,4-c]carbazole-5,7(6H,12H)-dione (NPCD) is known to be a very potent and selective cyclin D1-CDK4 inhibitors and could induce strong G1 phase arrest in breast tumor cell lines. In this work, the synthesis and biological evaluation of cytotoxic activity of a novel NPCD glycoside, 14-(α-L-rhamnopyranosyl)-naphtho[2,1-a]pyrrolo[3,4-c] carbazole-5,7 (6H,12H)- dione (1) were reported. The results showed the NPCD glycoside 1 displayed strong tumor cell growth inhibitory activities in the range of micromolar IC50 towards a broad spectrum of tumor cell lines. Analysis of cell cycle profiles revealed that NPCD glycoside 1 arrested the cells at different phases depending on the cell lines.) | |||
TO cite this article:DING Ning. Synthesis and biological evaluation of cytotoxic activity of 14-(β-D-2-deoxy-ribopyranosyl)-naphtho [2,1-a]pyrrolo[3,4-c]carbazole-5,7(6H,12H)-dione[OL].[20 January 2014] http://en.paper.edu.cn/en_releasepaper/content/4583216 |
7. The antinociceptive effects of endomorphin-2 analogs with N-methylated modifications at C-terminus | |||
WANG Changlin,DIAO Yuxiang | |||
Pharmacy 14 January 2014 | |||
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Abstract:In endomorphins (EMs), the C-terminal amide is an important element that can interact with opioid receptor directly. Presently, the antinociceptive effects of endomorphin-2 (EM-2) and its analogs with N-methylated modifications at C-terminus were determined using tail-flick test. The results indicated that both analogs 1 and 2 produced potent antinociceptive effects by a central opioid mechanism. At the dose of 20 nmol/kg, the maximal %MPE values of analogs 1 and 2 were 65.4 ± 4.0 and 57.8 ± 3.1, respectively, similar to that of EM-2 (60.1 ± 5.8). It was noteworthy that analog 1 showed a higher antinociceptive effect compared to EM-2, which would be helpful in the development of suitable μ-opioid therapeutics. Overall, the present results indicated that the N-methylated modifications of EM-2 C-terminus produced significant central antinociception, and N-methylation of C-terminus of EM-2 may play an important role in the regulation of antinociceptive effects. | |||
TO cite this article:WANG Changlin,DIAO Yuxiang. The antinociceptive effects of endomorphin-2 analogs with N-methylated modifications at C-terminus[OL].[14 January 2014] http://en.paper.edu.cn/en_releasepaper/content/4582354 |
8. Influence of Liquid Lipid Content on the Properties of Puerarin-loaded Lipid Nanoparticles | |||
HU Xiaofen | |||
Pharmacy 08 January 2014 | |||
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Abstract:The present study described the fabrication and characterization of puerarin-loaded lipid nanoparticles with blends of glyceryl monostearate (solid lipid phase) and DELIOS? MCT (liquid lipid phase) as the lipid matrices. Solid lipid nanoparticles (SLN) and nanostructured lipid carriers (NLC) were prepared via controlling the ratio of liquid lipid to solid lipid. The drug-lipid compatibility was evaluated via theoretical calculation of solubility parameters and X-ray diffraction analysis. The influence of liquid lipid content on the particle size, morphology, stability, drug loading properties of the lipid nanoparticles and in vitro release behavior of puerarin was investigated. Both SLN and NLC exhibited well stability and spherical shapes, and no significant difference in particle size occurred for the NLC series. The drug loading capacity (LC) and entrapment efficiency (EE) of the lipid nanoparticles were affected as increasing the liquid lipid content, and the presence of liquid lipid had a positive effect on improved drug payload. The in vitro release behavior of puerarin was intimately associated with the constituent of the lipid matrix. A sustained release of puerarin from NLC was observed in the selected experimental time window. The results of the current study displayed the application potential of NLC as nano-sized delivery carriers for puerarin. | |||
TO cite this article:HU Xiaofen. Influence of Liquid Lipid Content on the Properties of Puerarin-loaded Lipid Nanoparticles[OL].[ 8 January 2014] http://en.paper.edu.cn/en_releasepaper/content/4581343 |
9. Selective bromination of toluidines and cresols with N-bromosuccinimide | |||
Fang Xubin,Fang Lei | |||
Pharmacy 19 December 2013 | |||
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Abstract:Using N-bromosuccinimide (NBS) as a convenientbromine source, bromination of toluidine and cresols was studied systematically to clarify the underlying mechanism and the orientation effect. Based on this methodology, several potential AChE inhibtors i.e. 3-bromo-2-methoxy-5-methyl-9H-carbazole, 3,6-dibromo-2-meth-oxy-5- methyl- 9H-carbazole, and 5-(bromomethyl)- 2-methoxy-9-(phenylsulfonyl)carbazole were synthesized. | |||
TO cite this article:Fang Xubin,Fang Lei. Selective bromination of toluidines and cresols with N-bromosuccinimide[OL].[19 December 2013] http://en.paper.edu.cn/en_releasepaper/content/4576050 |
10. A simple HPLC-UV method for the determination of a novel anticancer candidate compound Z-Gly-Pro-doxorubicin in rat bile and its application to biliary excretion study | |||
HUANG Weixin,WANG Jingjing,MA Li,HAN Hai,XU Jun,CAI Shaohui | |||
Pharmacy 09 July 2013 | |||
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Abstract:Z-Gly-Pro-doxorubicin (Z-GP-DOX), a prodrug of doxorubicin (DOX), has been proved in our previous study to be a good prodrug to achieve targeted delivery of DOX. Also, the pharmacokinetic study of Z-GP-DOX in rat plasma has been completed. In this paper, a simple, sensitive and specific HPLC-UV method for the determination of Z-GP-DOX in rat bile was established and validated. Following liquid-liquid extraction, chromatographic separation was accomplished by the mobile phase acetonitrile-0.1%trifluoroacetic acid (50:50, v/v) with a C18 chromatography column at a flow rate of 1 mL/min, room temperature and detection wavelength of 495 nm. The retention time of Z-GP-DOX was 6.6 min. A linear curve over the concentration range of 1-1200 μg/mL (r2 > 0.999) was established, and the LOD and LOQ for Z-GP-DOX were 0.5 and 1 μg/mL, respectively. Good precision and accuracy at concentrations of 2, 600 and 1000 μg/mL were obtained. The mean extraction recovery of Z-GP-DOX in bile was over 82.92% at the studied concentrations. The intra-day and inter-day relative standard deviations were generally less than 10%. This method was successfully applied to biliary excretion study in rats after intravenous administration of Z-GP-DOX. Bile samples were collected from bile duct cannulated rats after an intravenous bolus dose of 10 mg/kg or 20 mg/kg Z-GP-DOX, and the concentrations were measured by HPLC-UV. The results showed that the concentration of Z-GP-DOX in rat bile was much higher than that in plasma. After dosing, 28.14 ± 2.13% and 20.25 ± 3.59% of the dose were excreted into bile in unchanged form after a 12-h collection. The present study will contribute to supplementing the previous pharmacokinetic study of Z-GP-DOX in rats and will be helpful to improve the druggability study of Z-GP-DOX. | |||
TO cite this article:HUANG Weixin,WANG Jingjing,MA Li, et al. A simple HPLC-UV method for the determination of a novel anticancer candidate compound Z-Gly-Pro-doxorubicin in rat bile and its application to biliary excretion study[OL].[ 9 July 2013] http://en.paper.edu.cn/en_releasepaper/content/4551463 |
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