共查询到19条相似文献,搜索用时 78 毫秒
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利用侧链带有羧基的官能化两亲性聚己内酯基共聚物Pluronic-b-poly(ε-caprolactone-co-6-carboxylic-ε- caprolactone) [Pluronic-b-P(CL-co-CCL), FC]为底物, 与紫杉醇(PTX)反应得到了一系列PTX的聚合物前药FCPTX. 通过核磁共振(1H NMR)和高效液相色谱(HPLC)表征了聚合物前药结构并分析了前药中的PTX接枝率. 通过聚合物前药胶束进一步物理包载PTX, 得到载有PTX的聚合物前药胶束PTX/FCPTX, 其载药量和包封率随着前药FCPTX中的PTX接枝率的增加而提高. 利用荧光光谱(FS)、透射电镜(TEM)和粒径分析仪(DLS)表征了胶束的临界胶束浓度(CMC), 形态和粒径. 体外细胞评价表明, 聚合物前药FCPTX具有较高的胞内累积量和良好的血液相容性、能有效降低紫杉醇的药物毒性. 作为一种优秀的药物载体, 聚合物前药FCPTX在联合化疗领域有着较大的应用潜力. 相似文献
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聚乙二醇接枝聚乳酸的自组装纳米微球的制备及性能 总被引:1,自引:0,他引:1
对制备的新型聚乙二醇(PEG)接枝聚乳酸(PLA)在水中的自组装性能进行研究, 探讨其作为纳米药物载体的可行性和稳定性. 目测法得到其溶解度为(2.16~4.32)×10-2 mg•mL-1; 荧光法得到聚合物的临界胶束浓度为1.12×10-3 mg•mL-1; 透射电子显微镜观察显示该聚合物在水中的自组装聚集体为纳米级球形; 动态激光光散射测试微球的粒径和Zeta电位发现, 在微球的制备过程中, 聚合物的亲/疏水性比例、水相介质及水溶液的pH值对它影响显著; 而制备后, 稀释和冷冻对它无显著影响, 改变微球的环境pH值至酸性, 出现聚集, 至碱性无影响. 研究结果显示, 该聚合物在水和磷酸钠盐缓冲液中可形成稳定的纳米微球, 通过微球的制备条件和存在环境可控制其粒径和Zeta电位, 因此根据应用需要, 通过控制其粒径和Zeta电位, 可能提高微球的在体血液循环时间并实现靶向缓释. 相似文献
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手性和螺旋是生命体系中对生物功能起着重要作用的两大元素。近年来,由于螺旋状配合物特别是手性螺旋配合物被陆续发现在不对称催化、分子识别、手性拆分、非线性光学材料等方面存在较大的应用价值而备受化学家的关注。该文主要针对国内外已报道的手性螺旋配合物的组装方式进行分类总结,概括了手性螺旋配合物的主要构筑途径,包括:氢键作用、配位作用、π-π堆积以及亲银作用。 相似文献
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金-硫键自组装生物分子膜 总被引:5,自引:0,他引:5
应用硫原子与金表面的强烈相互作用,可获得具有特定功能的生物分子自组装膜,在生物学、药理学及仿生学方面有重要的研究意义。本文着重介绍了一些相关的生物分子自组装体系,包括葡萄糖氧化酶、类脂、核酸传感器等在金基底表面的自组装。 相似文献
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利用光气法,以三光气和苯丙氨酸为原料,合成了苯丙氨酸酸酐(b-Phe-NCA).用端氨基聚乙二醇单甲醚(MPEG-NH2)作大分子引发剂,引发b-Phe-NCA开环聚合,合成了不同分子量的聚乙二醇单甲醚-聚(L-苯丙氨酸)(MPEG44-b-Phe)AB型二嵌段共聚多肽.利用IR1、H-NMR、GPC对共聚物结构进行了表征.利用TEM研究了二嵌段共聚多肽MPEG44-b-Phe50及MPEG44-b-Phe7在水溶液中的自组装形态,结果表明合成出的两亲性二嵌段共聚物在水溶液中自组装形成胶束,随着嵌段共聚物中亲水嵌段含量的增高,共聚物溶水性增强,其在水溶液中的自组装形态更加均一. 相似文献
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Lys(z)-NCA was synthesized in the presence of triphosgene, amphiphilic triblock copolymers poly(N^c-CBZ-Lysine)-PEG-poly(N^c-CBZ-Lysine) were synthesized in DMF using amino-end ended PEG as initiator with the mechanism of anion ring opening polymerization. The structures of block copolymers were characterized by IR, ^1H-NMR,GPC and DSC. The results showed triblock copolymers with expected structure and low polydispersity in molecular weight could be synthesized by this method. At the same time, the self-assembling behaviors of block copolymer were investigated by TEM. A novel helical aggregates were found to be formed in DMF. Because of biocompatibility of two components of block copolymers, these block copolymers have potential applications in the field of biomaterials. 相似文献
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采用金属离子为模板合成了-类由无金属或金属卟啉修饰的冠醚大分子环,并通过1HNMR、MS、紫外、荧光等方法对其进行了结构表征和性能测试.采用具有4,4,-联吡啶的客体分子与冠醚环进行组装,以荧光滴定法测定了主客体分子问的结合常数.结果表明,这种冠醚环不仅具有卟啉优异的光电性质而且能与客体分子形成了1:1的类轮烷体系. 相似文献
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In this study, a coarse-grained lattice Monte Carlo model was used to investigate the formation of Sierpiński triangle (ST) fractals through self-assembly on a triangular lattice surface. In the simulations, both symmetric and asymmetric molecular building blocks can spontaneously form ST fractal patterns, although the mixture of enantiomers of asymmetric molecule is more difficult to self-organize into ST of a high order owing to the presence of a large variety of competing three-membered nodes. The formation of ST fractals is favored at low surface coverage and is sensitive to temperature. Furthermore, to test whether the assembly pathway and outcome could be controlled by molecular design, we guided the self-assembly process forming ST fractal into the otherwise disfavored self-assembled structures using templates different from the assembling molecules. The templates are designed to act as"catassemblers"that initiate the self-assembling but are excluded from the final assembled structure. 相似文献
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Dr. Shiyu Zhou Prof. Xiuli Hu Dr. Rui Xia Shi Liu Qing Pei Prof. Guang Chen Prof. Zhigang Xie Prof. Xiabin Jing 《Angewandte Chemie (Weinheim an der Bergstrasse, Germany)》2020,132(51):23398-23405
The innate hypoxic microenvironment of most solid tumors has a major influence on tumor growth, invasiveness, and distant metastasis. Here, a hypoxia-activated self-immolative prodrug of paclitaxel (PTX2-Azo) was synthesized and encapsulated by a peptide copolymer decorated with the photosensitizer chlorin e6 (Ce6) to prepare light-boosted PTX nanoparticle (Ce6/PTX2-Azo NP). In this nanoparticle, PTX2-Azo prevents premature drug leakage and realizes specific release in hypoxic tumor microenvironment and the photosensitizer Ce6 not only efficiently generates singlet oxygen under light irradiation but also acts as a positive amplifier to promote the release of PTX. The combination of photodynamic therapy (PDT) and chemotherapy results in excellent antitumor efficacy, demonstrating the great potential for synergistic cancer therapy. 相似文献
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保护的预酯化紫杉醇侧链的合成 总被引:1,自引:1,他引:0
以市场可购得的(2R,3S)-苯基异丝氨酸盐酸盐为起始原料,通过在甲醇的氯化亚砜溶液中进行酯化反应,及随后对氨基进行苯甲酰化,氨基羟基的环化保护,最后对其酯进行水解,合成得到保护的预酯化的紫杉醇侧链.整个过程无需柱层析操作,适于工业化生产.为制备保护的预酯化紫杉醇侧链提供了一种有效而又实用的合成方法. 相似文献
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Federico Zappaterra Stefania Costa Daniela Summa Bruno Semeraro Virginia Cristofori Claudio Trapella Elena Tamburini 《Molecules (Basel, Switzerland)》2021,26(19)
Bile acids (BAs) are a family of steroids synthesized from cholesterol in the liver. Among bile acids, ursodeoxycholic acid (UDCA) is the drug of choice for treating primary biliary cirrhosis and dissolving cholesterol gallstones. The clinical effectiveness of UDCA includes its choleretic activity, the capability to inhibit hydrophobic bile acid absorption by the intestine under cholestatic conditions, reducing cholangiocyte injury, stimulation of impaired biliary output, and inhibition of hepatocyte apoptosis. Despite its clinical effectiveness, UDCA is poorly soluble in the gastro-duodeno-jejunal contents, and pharmacological doses of UDCA are not readily soluble in the stomach and intestine, resulting in incomplete absorption. Indeed, the solubility of 20 mg/L greatly limits the bioavailability of UDCA. Since the bioavailability of drug products plays a critical role in the design of oral administration dosages, we investigated the enzymatic esterification of UDCA as a strategy of hydrophilization. Therefore, we decided to enzymatically synthesize a glyceric ester of UDCA bile acid to produce a more water-soluble molecule. The esterification reactions between UDCA and glycerol were performed with an immobilized lipase B from Candida antarctica (Novozym 435) in solvent-free and solvent-assisted systems. The characterization of the UDCA-monoglyceride, enzymatically synthesized, has been performed by 1H-NMR, 13C-NMR, COSY, HSQC, HMBC, IR, and MS spectroscopy. 相似文献
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Qing Song ZHOU Xue Hua JIANG Jia Rui YU Ke Jia LI West China School of Pharmacy Sichuan University Chengdu 《中国化学快报》2006,17(1)
Scutellarin is the active ingredient extracted from Erigeron breviscapus, a traditional Chinese herbal medicine. Pharmacological study showed that scutellarin could significantly reduce the blood viscosity, improve the blood flow, decrease the vascular re… 相似文献
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M. Hess B.-W. Jo B. Wermeckes S. Dehne J.-S. Sohn S. Wunderlich M. Zähres 《Macromolecular Symposia》2005,231(1):28-46
A summary of the most recent investigations of conformation and solution properties of a polymer conjugate of the anti-cancer drug paclitaxel is given. First results of spectroscopic studies of interaction with model proteins in the solid state and in solution are discussed. 相似文献
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Qing Song ZHOU Xue Hua JIANG Jia Rui YU Ke Jia LI 《中国化学快报》2006,17(1):85-88
Highly water soluble esters of scutellarin with variable molecular weight polyethylene glycol (PEG) were prepared via PEGylation. The physicochemical properties and the stabilities under different conditions were investigated. By PEG modification, the greatly increased water solubility and desirable partition coefficient of scuteUarin were obtained, and the results showed that these conjugates were potential prodrugs for the oral delivery of scuteUarin. 相似文献
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A novel method was developed to prepare the branch of paclitaxel using 2,4-dichlorophenylaldehyde as the starting material.The branch was synthesized through condensation, cydoaddltion and catalyzing hydrogenation of dichlorophenyl intermediate. Tripolycyanamide formaldehyde resin-Pd complex as hydrogenation catalyst has been studied. The influence of temperature and N/Pd atomic ratio of the catalyst on the effect of catalytic hydrogenation was investigated and the optimum conditious were found. Because of the mild cyclization reaction condition, convenient asymmetric resolution operation and high yield, the synthetic route was practical. 相似文献