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1. 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 |
2. Design,synthesis and biological evaluation of novel asymmetric monocarbonyl analogues of curcumin (MACs ) as anti-inflammatory agents | |||
ZHANG Yali,ZOU Peng,ZHAO Chengguang,LIANG Guang,YANG Shulin | |||
Pharmacy 09 March 2013 | |||
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Abstract:In the past several years, a lot of symmetric mono-carbonyl analogues of curcumin (MACs) have been designed and synthesized in our laboratory. In the recent study, Eleven asymmetric MACs were designed and synthesized. Their bioactivities were evaluated by inhibit LPS-stimulated macrophages release proinflammation cytokines TNF-α and IL-6. The compound 1d exhibit the most inhibit activity among the test compounds. These data show that asymmetric MACs might serve as potential agents for the treatment of inflammatory diseases. | |||
TO cite this article:ZHANG Yali,ZOU Peng,ZHAO Chengguang, et al. Design,synthesis and biological evaluation of novel asymmetric monocarbonyl analogues of curcumin (MACs ) as anti-inflammatory agents[OL].[ 9 March 2013] http://en.paper.edu.cn/en_releasepaper/content/4528456 |
3. Screening an anti-angiogenesis component from Tupistra Cinensis Bak. using cell membrane chromatography combined with chicken chorioallantoic membrane assay | |||
Langchong He,Cuiqin Li,,Sicen Wang | |||
Pharmacy 13 January 2009 | |||
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Abstract:We tried to find an anti-angiogenesis component from Tupistra Cinensis Bak., a natural medicinal herb in China, using the ECV304 cell membrane chromatography (CMC) combined with chicken chorioallantoic membrane (CAM) assay. Samples were obtained using ethanol extraction, a resin column and a normal-phase column separation from Tupistra Cinensis Bak. Samples were screened by an ECV304 CMC model with the anti-flt-1 antibody as the control molecule. An active component that acted on the ECV304 cell membrane receptor (e.g., VEGFR) was found. The structure of this component was determined by UV, IR, MS and NMR and named as (5?-oleandrigenin-3-(?L-rhamnopyranoside) or ODGR. The pharmacological effect of ODGR was tested by a chicken CAM neovascularization model in vivo. ODGR significantly inhibited CAM angiogenesis within 0.94?5 礸/egg. CAM histomorphological results indicated that ODGR could inhibit sprouting of blood vessels and proliferation of vascular endothelial cells. These findings suggest that ODGR is a promising inhibitor of angiogenesis. The method of ECV304 CMC combined with chicken CAM assay can be used for discovering compounds with anti-angiogenesis actions from natural medicinal herbs. | |||
TO cite this article:Langchong He,Cuiqin Li,,Sicen Wang. Screening an anti-angiogenesis component from Tupistra Cinensis Bak. using cell membrane chromatography combined with chicken chorioallantoic membrane assay[OL].[13 January 2009] http://en.paper.edu.cn/en_releasepaper/content/27719 |
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