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| 1 | Pharmacokinetics and tissue distribution of 5-fluorouracil encapsulated by galactosylceramide liposomes in mice显示文摘Aim: To study the pharmacokinetics and tissue distribution of 5-fluorouracil encapsulated by galactosylceramide liposomes (5-Fu-GCL) in mice. Methods: The concentration of 5-fluorouracil (5-Fu) in serum was detected by high performance liquid chromatography after 5-Fu-GCL (80, 40, 20 mg/kg) and free 5-Fu (40 mg/kg) were injected intravenously into mice. The tissue distribution of 5-Fu-GCL (40 mg/kg) and free 5-Fu (40 mg/kg) was investigated, and concentration-time profile of the two preparations in the liver were studied. Data were analyzed by 3p97 program. Results: Serum concentration-time curves of 5-Fu-GCL and free 5-Fu conformed to one compartment model of first order absorption. 5-Fu-GCL at 80, 40, and 20 mg/kg had T1/2Ke of 25.8±4.2, 27.3±4.4, and 28.2±5.6 min; C0 of 24.9±4.9, 17.7±3.6, and 11.5±2.7 mg/L; and AUC of 990.0±45.2, 622.5±38.3, and 340.4±25.6 mg.min-L^-4, respectively. In contrast free 5-Fu at 40 kg/mg had T1/2ke of 15.8±2.2 min, C0 of 35.8±6.2 mg/L, AUC of 639.0±35.9 mg-min.L^-1. The tissue distribution of 5-Fu-GCL in the liver and immune organs was significantly increased, while in heart and kidney it was remarkably decreased. The AUC of 5-Fu-GCL in the liver was 3 times higher than that of free 5-Fu. Conclusion: The pharmacokinetics and tissue distribution of 5-Fu-GCL appears to be linear-related and dose-dependent, and exhibits sustained-release and hepatic target characteristics. | YongJIN JunLI Long-fuRONG Xiong-wenLü YanHUANG Shu-yunXU | 2005 | Acta Pharmacologica Sinica2005,26,2: | 10 |
| 2 | Gastroprotective effect and mechanism of amtolmetin guacyl in mice显示文摘AIM: To investigate the gastroprotective effect and mechanism of amtolmetin guacyl (AMG, MED15) in mice.METHODS: Male and female Kunming strain mice,weighing 18-22 g, were utilized in the experiment. Normal or ethanol-induced gastric mucosal damage models in mice were successfully established to investigate the gastroprotective effect and mechanism of AMG. In the experiment of gastric mucosal damage after repeated treatment with AMG, the mice were randomly divided into 5 groups: normal group, 3 AMG groups receiving (75, 150 and 300 mg/kg), and tolmetin group receiving 90 mg/kg.The mice were randomly divided into 6 groups as follows:normal group, model group, AMG groups with doses of 75, 150 and 300 mg/kg, respectively, and tolmetin group with a dose of 90 mg/kg in ethanol-induced gastric mucosal damage experiment. The severity of gastric mucosal lesions was scored from 0 to 5. Gastric tissue sections were stained with hematoxylin and eosin (HE) and examined under light microscopy. Also gastric tissue sections were stained with uranyl acetate and lead citrate, and examined under electron microscopy. In addition, nitric oxide (NO) and malondialdehyde (MDA) contents, and nitric oxide synthase (NOS) and superoxide dismutase (SOD) activities in the stomach tissue homogenates were measured by biochemical methods.RESULTS: Repeated treatment with AMG (75, 150 and3 00 mg/kg) for 7 d did not induce any appreciable mucosal damage, and the average score was not significantly different from that of normal mice. In contrast, tolmetin (90 mg/kg) produced significant gastric mucosal lesions compared with the normal group (P<0.01). AMG (75, 150 and 300 mg/kg) significantly reduced the severity of gastric lesions induced by ethanol in a dose-dependent manner as compared with the model group (P<0.05, AMG 75 and 150 mg/kg vs model; P<0.01, AMG 300 mg/kg vs model).Light and electron microscopy revealed that AMG (150 and 300 mg/kg) induced minimal changes in the surface epithelium layer, without vascular congestion or leucocyte adherence. AMG (75,150 and 300 mg/kg) demonstrated dose-dependent gastroprotective effects on mice in ourstudy. AMG (75, 150 and 300 mg/kg) could significantly increase NO content and NOS level in the stomach homogenates of mice compared with the model group (P<0.05, AMG 75 mg/kg and 150 mg/kg groups vs model group; P<0.01, AMG 300 mg/kg vs model group) respectively. Moreover, AMG (150 and 300 mg/kg) not only significantly increased SOD activities but also obviously decreased the MDA content in the stomach homogenates of mice.CONCLUSION: AMG exerts significant gastroprotective actions on mice and the involved mechanisms may be its antioxidative effect and induction of NO production. | Yuan-HaiLi JunLi YanHuang Xiong-WenLii YongJin | 2004 | World Journal of Gastroenterology2004,10,24: | 8 |
| 3 | Polymorphisms of death pathway genes FAS and FASL and risk of nasopharyngeal carcinoma显示文摘 | YunCao Xiao‐PingMiao Ma‐YanHuang LingDeng Dong‐XinLin Yi‐XinZeng Jian‐YongShao | 2010 | Mol Carcinog2010,,11: | 1 |
| 4 | Polymorphisms of methylenetetrahydrofolate reductase are associated with a high risk of nasopharyngeal carcinoma in a smoking population from southern China显示文摘 | YunCao Xiao‐PingMiao Ma‐YanHuang LingDeng Xiao‐ManLiang Dong‐XinLin Yi‐XinZeng Jian‐YongShao | 2010 | Mol Carcinog2010,,11: | 1 |
| 5 | Cx31.1 acts as a tumour suppressor in non‐small cell lung cancer (NSCLC) cell lines through inhibition of cell proliferation and metastasis显示文摘 | DeqiangZhang ChengwenChen YuanLi XupingFu YiXie YaoLi YanHuang | 2012 | Journal of Cellular and Molecular Medicine2012,,5: | 1 |
| 6 | Histone methyltransferase G9a and H3K9 dimethylation inhibit the self-renewal of glioma cancer stem cells显示文摘 | Hong Tao Haiying Li Yanhuang Su Danni Feng Xilong Wang Chun Zhang Hui Ma Qikuan Hu | 2014 | Molecular and Cellular Biochemistry . 2014 (1-2)2014,,1: | 1 |
| 7 | Study of Soft Quadrupole Excitation in Nucleus ^(11)Li with Test Particle Method显示文摘The quadrupole excitations in nucleus 11Li have been studied within the nuclear Vlasov equation approach.The classical phase space distribution function is given by the test particle propagation method.A soft mode of quadrupole excitation located around 2MeV is found.The total percentage of E2 energy-weighted sum rule exhausted in this soft resonance region is very sensitive to the extension of neutron halo in nucleus 11Li.The results compared with other recent calculations are analyzed. | CAI Yanhuang ASmerzi MDi Toro | 1994 | Chinese Physics Letters1994,11,6: | 0 |
| 8 | Novel Fluorene-based Conjugated Copolymer Containing Cyclobutenedione Unit for Light Emitting Diodes显示文摘A novel fluorene-based conjugated copolymer containing cyclobutenedione unit was synthesized by Suzuki reaction.Its structure and properties were characterized by FTIR,^1HNMR,elemental analysis,PL spectroscopy,DSC,TGA and cyclic voltammetry.The resulting polymer shows strong yellow PL emission(561nm)and good solubility in polar aprotic solvents,i.e.THF,DMF,DMAC,DMSO,etc.DSC and TGA studies reveal that the novel polymer possesses excellent thermal stability with high glass transition temperature of 127℃ and onset decomposition temperature of 411℃.Cyclic voltammetry measurement demonstrated that the polymer has both hole and electron-transporting property. | QiangPENG YanHUANG ZhiYunLU PingZOU MingGuiXIE | 2004 | Chinese Chemical Letters2004,15,4: | 0 |
| 9 | Isovector Dipole Giant Resonances:a Relativistic Vlasov Equation Approach显示文摘In the framework of relativistic quantum hadron dynamical theory,under semiclassical approximation and taking the vacuum fluctuation into account,a relativistic Vlasov equation(RVE)has been derived.Using RVE and considering other relativistic effects,we have studied the isovector dipole giant resonances built on ground state in spherical nuclei.The main results shown that the resonance energies for each multipole are larger than those obtained from the non-relativistic classical Vlasov approach.But by means of choosing a reasonable symmetry potential as 100MeV,the relativistic results can fit the experimental results very well. | ZHOU Baosen CAI Yanhuang ZHU Zhiyuan | 1995 | Chinese Physics Letters1995,12,3: | 0 |