论文部分内容阅读
首先将对氰基溴化苄与3,5-二羟基苯甲醇通过Frétchet反应合成芳基苄醚树枝分子3,5-[二-(4’-氰基苯甲氧基)]苯甲醇(1),1与4-硝基邻苯二甲腈合成前驱物4-{3’,5’-[二-(4’’-氰基苯甲氧基)]}苯甲氧基邻苯二甲腈(3),然后3在乙酸锌,1,8-二氮杂二环(5,4,0)-7-十一烯(DBU)和正戊醇存在下合成以氰基为端基的芳基苄醚树形酞菁锌配合物四-{3,5-[二-(4’-氰基苯甲氧基)-苯甲氧基]}锌酞菁(4),最后4在氢氧化钠中水解制备以羧基为端基的芳基苄醚树形酞菁锌四-{3,5-[二-(4’-羧基苯甲氧基)-苯甲氧基]}锌酞菁(5).采用元素分析、ⅠR,1H NMR,ESⅠ-MS和MALDⅠ-TOF-MS对上述化合物的结构进行了表征.带有负电荷的5与两嵌段共聚物聚乙二醇单甲醚-聚L-赖氨酸(PEG-b-PLL)(6)通过静电作用自组装成负载5的聚合物纳米粒子(5/m).AFM和TEM表明5/m为直径约为100 nm的核壳结构纳米粒子.通过紫外光谱和荧光光谱法研究了5和5/m的光物理性质:5包裹入聚合物胶束后,5/m的Q带最大吸收峰强度增加,位置红移,荧光强度增加,荧光寿命减少.不同孵育时间HUVEC细胞(人体静脉内皮细胞)的5和5/m的药代动力学和MTT法研究表明:与自由酞菁5相比,5/m摄取率增加,提前1 h达到最大浓度而且细胞抑制率也大大增加.
First, the aryl benzyl ether dendrimer 3,5- [di- (4’-cyanobenzyloxy)] benzyl alcohol (1 ), 1 Synthesis of 4- {3 ’, 5’ - [di- (4 "-cyanobenzyloxy)]} benzyloxyphthalide precursor with 4-nitrophthalonitrile Nitrile (3) and then 3 to synthesize a cyano-terminated aromatic group in the presence of zinc acetate, 1,8-diazabicyclo (5,4,0) -7- undecene (DBU) Zinc phthalocyanine tetrakis- {3,5- [di- (4’-cyanobenzyloxy) -benzyloxy] zinc phthalocyanine (4) Preparation of Zinc Phthalocyanine Tetrakis {3,5- [Di- (4’-Carboxybenzyloxy) -benzyloxy]} Phthalocyanine Carboxyl Group- 5) The structures of these compounds were characterized by elemental analysis, IR, 1H NMR, ESⅠ-MS and MALDⅠ-TOF-MS. Poly (L-Lysine) (PEG-b-PLL) (6) self-assembled into 5 nanoparticles (5 / m) by electrostatic interaction.AFM and TEM showed that 5 / m was a core with a diameter of about 100 nm Shell structure of nanoparticles.Ultraviolet spectroscopy and fluorescence spectroscopy of 5 and 5 / The optical properties of m: 5 encapsulated into polymer micelles, 5 / m Q band maximum absorption intensity increased, the location of redshift, fluorescence intensity increased, fluorescence life reduced.Different incubation time HUVEC cells (human vein endothelial cells) The 5 and 5 / m pharmacokinetic and MTT studies showed that 5 / m uptake rate increased compared with free phthalocyanine 5, reached the maximum concentration 1 h before, and the cell inhibition rate also increased greatly.