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Biotransformation of naringin by human intestinal flora

Journal of Chinese Pharmaceutical Sciences 2013年第4期22卷 329-333页

作者：冉丽吴帅徐嵬张友波杨秀伟北京大学医学部天然药物及仿生药物国家重点实验室药学院天然药物学系北京100191

Naringin （1）, the highest-content flavanone glycoside in sour oranges, was incubated with human intestinal flora, and four biotransforrnation products （2-5） were obtained from the incubated mixture by chromatographic methods. The chemical structures of the four products were elucidated as naringin-6＂acetate （2）, naringenin （3）, phloretic acid （4）, and phloroglucinol （5） on the basis of their spectroscopic data. Naringin-6＂-acetate was specifically formed by acetylation at C6-OH of glucosyl group of 1. The result obtained in the present research could account for the lower bioavailability of 1 after oral administration, suggesting that some biological properties of 1 in vivo may be mediated by its intestinal flora converted product 3. The biotransforrnation of 1 by intestinal flora leading to their systemic absorption deserves further attention and may provide valuable insights into pre-systemic drug metabolism, delivery or toxicity.

关键词： Naringin Naringenin Naringin-6-acetate Biotransformation Human intestinal flora

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A mechanism study on the tamoxifen-mediated cellular internalization of liposomes

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Journal of Chinese Pharmaceutical Sciences 2014年第9期23卷 595-600页

作者：汪小又陈显慧杨秀聪何冰代文兵王学清王坚成张烜张强北京大学医学部天然药物及仿生药物国家重点实验室药学院药剂学系北京100191

It was reported previously that tamoxifen （TAM） could increase the intracellular accumulation of drug-loaded liposomes, but the exact mechanism is unknown although it was supposed that TAM might enhance the cell uptake by inhibiting the drug efflux caused by P-glycoprotein （P-gp）. To identify the mechanism of increased cellular uptake of liposomes induced by tamoxifen, PEGgylated liposomes （SSL） ofP-gp-substrate doxorubicin （DOX） or non-P-gp-substrate coumarin （Cou） were prepared with or without TAM. The cell uptake of these liposome systems was investigated in cell lines with different P-gp-expressing levels and the interaction of TAM with lipid membrane was also studied. As the results, the co-encapsulation of TAM with DOX-SSL increased the intracellular uptake in all three tumor cell lines. In P-gp-highly-expressing MCF-7/Adr cells, the effect of TAM was the strongest and in negative control Hela cells, the impact weakened but still significant. The improvement was also observed in the cellular uptake of Cou-SSL. Surface plasmon resonance （SPR） studies demonstrated that TAM-SSL exhibited a much stronger atYmity with model biomembrane compared with empty SSL, and ft^her test with isothermal titration calorimetry （ITC） showed that free TAM had an obvious interaction with lipid membrane. In conclusion, TAM could increase the affinity of liposomes with biomembrane and enhance the intracellular accumulation of liposomes via both TAM-mediated P-gp inhibition and the increased interaction between hydrophobic TAM molecules and lipid membrane.

关键词： Liposomes Tamoxifen Doxorubicin Biomembrane Affinity

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Targeting glioblastoma cancer stem cell marker CD133 by heptapeptidemodified DSPE-PEG micelles

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Journal of Chinese Pharmaceutical Sciences 2015年第1期24卷 34-39页

作者：王景达何冰代文兵王学清王坚成张烜张强北京大学医学部天然药物及仿生药物国家重点实验室药学院药剂学系北京100191

Cancer stem cells have become the new target of chemotherapy with specific cell marker. CD133 is shown to be highly expressed in glioma cancer stem cells. In this study, a drug delivery system is designed to target CD133 by a seven amino acid peptide （TR peptide）, which is capable to specifically bind to CD 133. First, TR was conjugated to DSPE-PEG and coumarin-6 was loaded into the DSPE-PEG micelles. Then fluorescence-activated cell sorting （FACS） and tumorsphere culture were conducted to isolate cancer stern cells in C6 cells. The enhanced uptake of micelles was observed by confocal microscopy and flow cytometry, suggesting that TR peptide-modified micelles may exhibit better anti-cancer efficacy by targeting CD133^＋ glioma stem *** conclusion, TR peptide-modified micelles may provide new strategy to achieve enhanced specificity to CD 133^＋ glioma stem cells.

关键词： Cancer stem cell CD 133 TR peptide Micelle Tumorsphere FACS

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Efficacy and mechanism of a compound epirubicin plus quinine injection for the treatment of drug--resistant breast cancer

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Journal of Chinese Pharmaceutical Sciences 2015年第9期24卷 563-571页

作者：刘磊居瑞军谢红军曾凡张诚翔赵炜煜吕万良北京大学医学部天然药物及仿生药物国家重点实验室?药学院药剂学系北京100191

A single drug chemotherapy fails to eliminate residual cancer cells due to the existence of the multidrug resistance （MDR）. In the present study, we aimed to develop a compound epirubicin plus quinine injection, to characterize the efficacy in treatment of the drug-resistant breast cancer, and to reveal the involved mechanisms. The HPLC-UV methods were developed for quantifications, and the evaluations were performed on the drug-resistant human breast cancer MCF-7/adr cells using a high content screening system. Results demonstrated that the compound epirubicin plus quinine injection was able to effectively block the drug efflux, exhibiting an evidently overall efficacy in treatment of the resistant breast cancer cells by direct killing effect and by apoptosis-inducing effect. In the formulation, quinine played multiple roles in blocking drug efflux and in inducing the apoptosis of the resistant breast cancer cells. The apoptosis signaling pathways were associated with a cascade of reactions by activating Caspase family and by inhibiting Bcl-2 family. In conclusion, the present study preliminarily revealed the efficacy and mechanism of the compound epirubicin plus quinine formulation in treatment of the drug-resistant breast cancer, and offered a potential strategy to overcome drug resistance in cancer treatments.

关键词： Compound epirubicin plus quinine injection Blocking drug effiux Apoptosis Resistant breast cancer Efficacy

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A study of liposomal doxorubicin modified by tumor metastasis targeting peptide for its specificity to highly metastatic breast cancer cells

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Journal of Chinese Pharmaceutical Sciences 2014年第2期23卷 83-88页

作者：杨芳何冰代文兵王学清王坚成北京大学医学部天然药物及仿生药物国家重点实验室药学院药剂学系北京100191

Tumor metastasis emerges as a crucial target for tumor therapy. In this study, a tumor metastasis targeting peptide（TMT） was conjugated to a lipid material（PEG-DSPE） to obtain the targeting compound（TMT-PEG-DSPE）, which was used to construct the targeted liposomal doxorubicin（TMT-LS-DOX）. We showed that TMT-LS-DOX presented satisfactory pharmaceutical characteristics. This metastasis-specific delivery system was tested in two highly metastatic breast cancer cell lines（MDA-MB-435S and MDA-MB-231） with a non-metastatic breast cancer cell line（MCF-7） as the control. The free TMT peptide itself showed no cytotoxicity even at the concentration of 100 μg/mL. Importantly, the enhanced cellular uptake of TMT-LS-DOX to both MDA-MB-435S and MDA-MB-231 cell lines was demonstrated as compared to MCF-7 cells, via a TMT-mediated mechanism demonstrated by a receptor competition study. In conclusion, the TMT modified nanocarriers might provide a strategy to enhance the specificity of chemotherapeutic agents to highly metastatic breast cancer.

关键词： Highly metastatic breastcancer Tumor metastasis targeting peptide Liposomes Doxorubicin

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The impact of Rho GTPases on the cell uptake of single-walled carbon nanohorns

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Journal of Chinese Pharmaceutical Sciences 2017年第6期26卷 395-403页

作者：傅洪哲宋佳芳宋歌宋思洋樊志璞杨岸蒲何冰代文兵张华王学清张强北京大学医学部药学院天然药物及仿生药物国家重点实验室药学院药剂学系北京100191

Rho GTPases play an important role on the regulation of cytoskeleton, which can affect the cell morphogenesis, cell migration, endocytosis and vesicle transport by controlling the growth and maintenance of microfilaments and microtubules. It has been known that regulation of cell cytoskeleton is inseparable from the cell uptake of nano-medicine or nano-drug delivery systems. However, only few studies have focused on the impacts of Rho GTPases on cell uptake of nano-medicine or nano-drug delivery systems. This study selected single-walled carbon nanohoms （SWCNHs）, which have emerged as promising drug delivery systems, to explore the impacts of Rho GTPases on cell uptake of nano-drug delivery systems. SWCNHs were oxidized with concentrated nitric acid and prepared into nano dispersion by ultrasonic dispersion. Confocal laser scanning microscope （CLSM） and transmission electron microscopy （TEM） were used to observe the cell uptake and intracellular distribution of nanoparticles after incubated A549 cells with the dispersion mentioned above. Mechanism of cell uptake was assessed using various inhibitors. The results showed that the cell uptake of oxSWCNHs was significantly reduced when RhoA was inhibited. The oxSWCNHs were internalized through clathrin-mediated endocytosis and mainly positioned in lysosomes ofA549 cells.

关键词： Rho GTPases Single-walled carbon nanohoms A549 cells Cell uptake

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Synthesis of tetrahydrofuro[3,2-b]quinolin-2(3H)-one derivatives from 2-aminobenzaldehydes and α-angelica lactone via a tandem Aldol/Michael addition

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Journal of Chinese Pharmaceutical Sciences 2017年第3期26卷 163-172页

作者：季泠尹大伟王欣李润涛北京大学医学部药学院天然药物及仿生国家重点实验室北京100191

An efficient synthesis of tetrahydrofuro[3,2-b]quinolin-2（3H）-ones from α-angelica lactone and 2-aminobenzaldehydes via a tandem Aldol-Michael addition is described. The reactions were carried out using DBU as the ... 详细信息

关键词： Aldol/Michael tandem cyclization Tetrahydroquinoline Furanone

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In vitro and in vivo antitumor efficacy of CLA-PTX on B16-F10 melanoma cells

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Journal of Chinese Pharmaceutical Sciences 2014年第1期23卷 46-53页

作者：李捷思杨科柯曦宇杜若张烜张强北京大学医学部药学院药剂学系北京100191 北京大学医学部天然药物及仿生药物国家重点实验室北京100191

The purpose of this study was to investigate the potential antitumor efficacy of conjugated linoleic acid-paclitaxel （CLA-PTX） on B16-F10 melanoma cell line in vitro and in vivo. The in vitro cytotoxicity, apoptosis and cell cycle of CLA-PTX were investigated. The in vitro cellular uptake of CLA-PTX in B16-F10 cells was also analyzed. The antitumor activity of CLA-PTX was also evaluated in B16-F10 tumor-bearing C57BL6/N mice in vivo. The in vitro cytotoxicity results showed that the IC50 of the CLA-PTX is （4.25±0.43） μM, compared with that of （6.70±0.80） μM in PTX treatment group （P〈0.01）. CLA-PTX increased the percentage of total apoptotic cells compared with that of control and PTX treatment groups （P〈0.01）. Compared with untreated cells, CLA-PTX arrested cell cycle progression at the S phase, whereas PTX caused accumulation of cell at GE-M phase both along with the reduction of the cellular fraction arrested at the G1 phase. The amount of cellular uptake of CLA-PTX was significantly higher than that of PTX （P〈0.01）. The in vivo antitumor activity of CLA-PTX was significantly higher than that of control and PTX treatment groups （P〈0.01 or P〈0.05）. In conclusion, our study demonstrated that CLA-PTX has significant antitumor activity in B 16-F 10 cell line.

关键词： CLA-PTX Apoptosis Cell cycle Cellular uptake Antitumor efficacy

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新型叶酸拮抗剂吡啶并嘌呤衍生物的环合反应研究

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化学通报 2018年第7期81卷 653-656页

作者：薛良敏王锰刘俊义张志丽北京大学医学部药学院天然药物及仿生药物国家重点实验室北京100191

将6-取代-2,4-二氨基哌啶并[3,2-d]嘧啶衍生物与N,N-二甲基甲酰胺、三氯乙酰氯在25℃反应2h,"一锅法"环合反应生成7-取代-2-氨基-7,8-二氢-6H-吡啶并[1,2,3-gh]嘌呤衍生物,利用NMR、HRMS确定目标化合物的结构。考察了不同底... 详细信息

将6-取代-2,4-二氨基哌啶并[3,2-d]嘧啶衍生物与N,N-二甲基甲酰胺、三氯乙酰氯在25℃反应2h,"一锅法"环合反应生成7-取代-2-氨基-7,8-二氢-6H-吡啶并[1,2,3-gh]嘌呤衍生物,利用NMR、HRMS确定目标化合物的结构。考察了不同底物、反应底物比例、反应时间、温度对反应产率的影响,并提出可能的反应机理。该反应条件温和、效率高、操作简单。

关键词： N,N二甲基甲酰胺三氯乙酰氯环合反应

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Simultaneous determination of sunitinib and its active metabolites N-desethylsunitinib(SU12662) in nude mice plasma by liquid chromatography tandem mass spectrometry and its application to a pharmacokinetic study

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Journal of Chinese Pharmaceutical Sciences 2015年第4期24卷 217-224页

作者：李静云李健王思媛袁茵苏青虹卢炜周田彦北京大学医学部药学院药剂学系北京100191 北京大学医学部天然药物及仿生药物国家重点实验室北京100191

A sensitive, rapid, and simple liquid chromatography tandem mass spectrometry（LC-MS/MS） method for simultaneous determination of sunitinib and its active metabolites in plasma of BABL/c nude mice was developed and validated. Plasma samples were pre-treated by protein precipitation with pazopanib and used as an internal standard. Separation was performed on a reversed phase C18 column with a mobile phase composing of 10 m M ammonium formate p H 3.25（adjusted with formic acid） and acetonitrile（65：35, v/v） at a flow rate of 0.5 mL /min. Triple quadrupole tandem mass in multiple reaction monitoring（MRM） mode with electrospray positive ionization was used to monitor all the compounds. The current LC-MS/MS method was highly selective and sensitive with lowest limit of quantitation（LLOQ） of 0.5 ng/mL for both analytes and reliable intra- and inter-day precision and accuracy validated by relative error（RE%） and relative standard deviation（RSD%）. Linearity of calibration curve was excellent（r0.99） within a concentration range of 0.5–1000 ng/mL. This method was successfully applied to a pharmacokinetics study on BABL/c nude mice given with single dose of oral administration of sunitinib at 20 mg/kg.

关键词： LC-MS/MS Sunitinib SU12662 Nude mice Pharmacokinetics

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