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FG020326-loaded nanoparticle with PEG and PDLLA improved pharmacodynamics of reversing multidrug resistance in vitro and in vivo

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Acta Pharmacologica Sinica 2007年第6期28卷 913-920页

作者： Wen-jing DENG~2,Xiao-qiang YANG~2,Yong-ju LIANG~2,Li-ming CHEN~2,Yan-yan YAN~2,Xin-tao SHUAI~3,Li-wu FU~(2,4)~2 State Key Laboratory of Oncology in Southern China Cancer Center,Sun Yat-Sen University,Guangzhou 510060,China ~3 School ofChemistry and Chemical Engineering of Sun Yat-Sen University,Guangzhou 510275,China StateKeyLaboratoryofOncologyinSouthernChinaCancerCenter SunYat-SenUniversityGuangzhou510060China schoolofchemistryandchemicalengineeringofsunyat-senuniversity Guangzhou510275China

Aim:FG020326,a novel imidazole derivative,is a potent multidrug-resistance(MDR) modulator in vitro and in ***,FG020326 is ***-FG020326 is a FG020326-1oaded nanoparticle formed with diblock copolymers ofpoly (ethylene glycol)-block-poly (D,L-lactic acid) (PEG:PDLLA,PEDLLA) thatcan solubilize *** work was intended to evaluate the pharmacody-namics of PEDLLA-FG020326 on reversing MDR in vitro and in ***:Cytotoxicity was determined by tetrazolium *** intracellular accumulationand efflux of doxorubicin (Dox) were detected by fluorescence *** function of P-glycoprotein was examined by Rhodamine 123 (Rh123) accumu-lation detected by flow *** KBv200 cell xenograft model was estab-lished to investigate the effect of PEDLLA-FG020326 on reversing MDR in ***:PEDLLA-FG020326 and FG020326 exhibited 56.4-and 35.9-fold activityin reversing KBv200 cells to vincristine (VCR) resistance,respectively and 14.98-and 7.64-fold to Dox resistance,***-FG020326 was much stron-ger than FG020326,resulting in the increase of Dox and Rh 123 accumulation andthe decrease of intracellular Dox extrusion in KBv200 ***,PEDLLA-FG020326 exhibited more powerful activity than FG020326 in enhancing the effectof VCR against KBv200 cell xenografts in nude mice,but did not appear more ***:The pharmacodynamics of FG020326 was improved by incorporatingit into a micellar nanoparticle formed with PEG-block-PDLLA copolymers.

关键词： FG020326 micellar nanoparticle multidrug resistance xenografts

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Analysis of Glutamic Acid in Cerebrospinal Fluid by Capillary Electrophoresis with High Frequency Conductivity Detection

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Chinese Chemical Letters 2005年第2期16卷 225-228页

作者： HalYunZHAI JunMeiWANG XiaoLiYAO XueCaiTAN PeiXiangCAI ZuanGuangCHEN CollegeofChemistryandChemicalEngineering SunYat-senUniversityGuangzhou510275 DepartmentofChemistry MedicalCollegeSunYat-senUniversityGuangzhou510089 TheFirstAffiliatedHospital SunYat-senUniversityGuangzhou510080

A rapid method to determine glutamic acid (Glu) in cerebrospinal fluid (CSF) by capillaryelectrophoresis with high frequency conductivity detection (contactless conductivity detection) wasdescribed. The CSF sample was pretreated with silver cation resin to remove high concentration ofCl- ions in CSF. The separation was achieved in the buffer solution of 10 mmol/L Tris and 8mmol/L boric acid at the separation voltage of 20.0 kV. Glu showed linear response in the range of5.0×10-6 to 6.0×10-3 mol/L, the limit of detection was 1.0×10-6 mol/L. The method was used foranalysis Glu in CSF satisfactorily with a recovery of 97.8-98.8%.

关键词： Capillary electrophoresis high frequency conductivity detection contactless conducti-vity detection glutamic acid cerebrospinal fluid.

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Synthesis and Characterization of Novel Multifunctional Acylthiourea Polymers

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Chinese Chemical Letters 2005年第5期16卷 609-612页

作者： XuePuMAO JinFengHUANG ZhiFangDUAN ZhiYunDU ZhiShuHUANG LinMA LianQuanGU SchoolofChemistryandChemicalEngineering SunYat-senUniversityGuangzhou510275 SchoolofChemistryandChemicalEngineering SunYat-senUniversityGuangzhou510275／／SchoolofPharmaceuticalSciencesSunYat-senUniversityGuangzhou510080 SchoolofPharmaceuticalSciences SunYat-senUniversityGuangzhou510080

Several thiourea polymers have been synthesized through the reaction of diamine with 1, 4- or 1, 3- benzenedicarbonyl chloride and ammonium thiocyanate by solid-liquid phase transfer catalysis of polyethylene glycol-400 (PEG-400). The polymers were characterized and identified by elemental analysis, IR, 1HNMR and GPC. The multifunctional polymers have potential value as an ideal support for immobilized enzymes.

关键词： Synthesis acylthiourea polymers solid-liquid phase transfer catalysis.

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Synthesis of New Benzoimidazole Derivatives

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Chinese Chemical Letters 2005年第1期16卷 7-10页

作者： LinKunAN XianZhangBU ZhiShuHUANG LinMA LianQuanGU AlbertS.C.CHAN YueMingLI SchoolofPharmaceuticalSciences SunYat-SenUniversityGuangzhou510080 SchoolofChemistryandChemicalEngineering SunYat-SenUniversityGuangzhou510275 SchoolofPharmaceuticalSciences SunYat-SenUniversityGuangzhou510080／／SchoolofChemistryandChemicalEngineeringSunYat-SenUniversityGuangzhou510275 DepartmentofABCT TheHongKongPolytechnicUniversityKowloonHongKong

The reactions of cryptotanshinone and tanshinone IIA with cadaverine and putrescine were investigated. Six new compounds, four with imidazole functional groups and two with oxazole groups, were obtained. The possibl... 详细信息

关键词： Cryptotanshinone tanshinone IIA putrescine cadaverine biogenic bisamines.

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Incoherently Coupled Grey Photovoltaic Spatial Soliton Families

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Chinese Physics Letters 2005年第1期22卷 128-131页

作者：王红成佘卫龙 StateKeyLaboratoryofOptoelectronicMaterialsandTechnologies SunYat-senUniversityGuangzhou510275

A theory is developed for incoherently coupled grey photovoltaic soliton families in unbiased photovoltaic crystals. Both the properties and the forming conditions of these soliton families are discussed in detail. The theory can also be used to investigate the dark photovoltaic soliton families. Some relevant examples are presented, in which the photovoltaic-photorefractive crystal is of lithium niobate type.

关键词：光电空间孤波族不一致偶合光折射

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Fabrication of Compound Lattice by Holographic Lithography

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Chinese Physics Letters 2005年第2期22卷 369-372页

作者：钟永春朱少安汪河洲 StateKeyLaboratoryofOptoelectronicMaterialsandTechnologies SunYat-SenUniversityGuangzhou510275

Some compound lattices in photonic crystals with large complete photonic band gaps, such as the diamond structure and the two-dimensional hexagonal compound structure, is desired for fabrication. A novel method for fabrication of compound lattices by holographic lithography is reported. The key point is phase modulation by photoelectrical control and multiple-exposure techniques. This technique introduces many advances: for instance, using the same coherent beams and without changing the position of the sample during multiple-exposure.

关键词：全息平版印刷复点阵光子晶体微观结构光电控制

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Generalized Theory of One-Dimensional Steady-State Optical Spatial Solitons

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Chinese Physics Letters 2004年第12期21卷 2441-2444页

作者：王红成王晓生佘卫龙 StateKeyLaboratoryofOptoelectronicMaterialsandTechnologies SunYat-senUniversityGuangzhou510275

We present a generalized soliton theory based on the one-dimensional generalized nonlinear Schrodinger equation, from which one can easily obtain the bright, dark, and grey soliton waveforms, and their existence curves. We show that the forming conditions of spatial solitons are directly dependent on the relationship between the index perturbation and the intensity, no matter whether the index perturbation is positive or negative. Some relevant examples are presented when the solitons are supported by the photoisomerization nonlinearity.

关键词： Solitons

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Adaptive Control on a Class of Uncertain Chaotic Systems

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Chinese Physics Letters 2005年第5期22卷 1069-1071页

作者：刘国刚赵怡 DepartmentofMathematics SunYat-SenUniversityGuangzhou510275

By using a simple combination of feedback entrainment control (with an updating feedback strength) and adaptive scheme, for a large class of chaotic systems, it is proven rigorously by using the invariance principle of differential equations that all unknown model parameters can be estimated dynamically and the uncertain system can be controlled to an arbitrary desired smooth orbit. The illustration of the Lorenz system and the corresponding numerical results on the effect of noise are given.

关键词： Chaotic systems

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Ultrafast Relaxation of Coherent Control Photocurrent in AlGaAs／GaAs Multi Quantum Wells

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Chinese Physics Letters 2005年第1期22卷 188-190页

作者：林位株寿倩刘鲁宁吴羽文锦辉赖天树 StateKeyLaboratoryofOptoelectronicMaterialsandTechnologies SunYat-SenUniversityGuangzhou510275

We theoretically and experimentally study the ultrafast dynamics of coherent control photocurrent in As-GaAs/GaAs multi quantum wells at room temperature. A ballistic photocurrent relaxation time of similar to200fs is deduced based on the theory of density matrix and is evidenced with the three-colour femtosecond pump-probe measurements.

关键词： GAAS SEMICONDUCTORS CURRENTS Quantum wells Relaxation time Photocurrent gallium arsenides currents Density matrix Semiconductor materials

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Synthesis and Crystal Structure of a New Hexadentate Ligand N,N'-Bis(di(2-pyridyl)methyl)ethylenediamine

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Chinese Journal of Structural Chemistry 2004年第3期23卷 242-246页

作者： YEBao-Hui CHENXiao-Ming SchoolofChemistryandChemicalEngineering SunYat-SenUniversityGuangzhou510275China

The reaction of di(2-pyridyl)ketone with ethylenediamine produced hexadentate Schiff base 1 which can be reduced to form a new ligand N,N-bis(di(2-pyridyl)-methyl)ethylene- diamine (BDPM) in ethanol solution. The two compounds were characterized by elemental analyses and spectroscopic methods. Their structures were determined by X-ray diffraction study. Crystal data for 1: C24H20N6, Mr = 392.5, monoclinic, P21/c, a = 13.871(3), b = 13.510(2), c = 12.153(2) ? b = 112.97(2)? Z = 4, V = 2094.1(6) ?, Dc = 1.245 g/cm3, m(MoKa) = 0.078 mm-1, F(000) = 824, the final R = 0.0545 and wR = 0.0557 for 2048 observed reflections (I > 2s(I)); for BDPM: C24H24N6, Mr = 396.49, monoclinic, C2/c, a = 21.411(3), b = 8.053(1), c = 11.868(1) ? b = 92.63(1)? Z = 4, V = 2044.2(4) 3, Dc = 1.288 g/cm3, m(MoKa) = 0.080 mm-1, F(000) = 840, the final R = 0.0401 and wR = 0.0939 for 1673 observed reflections (I > 2s(I)).

关键词： synthesis crystal structure hexadentate ligand di-2-pyridyl ketone

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