2004-A-Anti-windup synthesis via sampled-data piecewise affine optimal control
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FAPα靶向标记化合物131I-FAPI-03的合成及初步体内外实验研究马 欢1,2, 廖家莉2, 杨远友2, 刘 宁2, 李飞泽2(1. 四川省医学科学院 四川省人民医院(电子科技大学附属医院) 核医学科,成都 610072;2. 四川大学 原子核科学技术研究所,辐射物理及技术教育部重点实验室,成都 610064)摘要:本研究以4-喹啉基-甘氨基-2-氰基吡咯烷为骨架,对连接基团进行碳链延长及羟基修饰成功合成FAPI 衍生物ATE-FAPI-03;通过亲电取代反应实现其131I 标记,并对标记化合物131I-FAPI-03的脂水分配比、体外稳定性等进行分析;开展细胞结合、内吞、流出等实验以评价131I-FAPI-03的体外动力学特征;并考察了131I-FAPI-03在荷胶质瘤小鼠体内的分布情况。
结果表明:131I-FAPI-03为亲脂性小分子,并具有良好的体外稳定性;与FAPα阳性细胞U87MG 孵育10 min 时的结合率为(22.00 ± 0.35)%,且随着孵育时间的延长结合率有明显的上升趋势,而与FAPα阴性细胞MCF-7的结合率始终处于较低水平;通过竞争结合实验测得131I-FAPI-03的IC 50值为45.5 nM ,表明其对FAPα具有较高的亲和力;大部分与U87MG 细胞结合的131I-FAPI-03可被细胞内吞,但其在细胞中的滞留能力偏低。
131I-FAPI-03在荷胶质瘤小鼠体内具有快速的肿瘤靶向能力:经尾静脉注射5 min 后,肿瘤组织对131I-FAPI-03的放射性摄取值为(14.90 ±3.21)% ID/g ,注射2 h 后,肿瘤/肌肉的放射性摄取比值达到(43.7 ± 16.7)。
上述结果为新型FAPα靶向药物的研发提供了重要的参考。
关键词:FAPα;131I ;FAPI ;胶质瘤中图分类号:TL92+3 文献标志码:A 文章编号:1000-7512(2024)02-0097-09doi :10.7538/tws.2024.37.02.0097Synthesis and Preliminary Evaluation of FAPα Targeted Tracer 131I-FAPI-03MA Huan 1,2, LIAO Jiali 2, YANG Yuanyou 2, LIU Ning 2, LI Feize2(1. Department of Nuclear Medicine , Sichuan Provincial People’s Hospital ,University of Electronic Science and Technology of China , Chengdu 610072, China ;2. Key Laboratory of Radiation Physics and Technology of the Ministry of Education ,Institute of Nuclear Science and Technology , Sichuan University , Chengdu 610064, China )Abstract: Using N-(4-quinolinoyl)-Gly-(2-cyanopyrrolidine) as scaffold ,we prolonged the linker with serine to obtain a FAPI derivative ATE-FAPI-03,which was subsequently labeled with131I byelectrophilic substitution. Then the in vitro stability ,Log P value ,binding affinity ,targeting properties and biodistribution behavior of 131I-FAPI-03 was evaluated. Results show that 131I-FAPI-03 was lipophilic and stable in vitro ,capable of specifically binding to FAPα-positive U87MG cells收稿日期:2023-12-04;修回日期:2024-01-18基金项目:中央高校基本科研业务费专项资金资助(2023SCU12132);四川省医学科学院.四川省人民医院青年人才基金(2022QN32)通信作者:李飞泽第37卷 第2期同 位 素Vol. 37 No. 22024年 4 月Journal of IsotopesApr. 2024fast with a major proportion trapped intracellularly. After 10 min of incubation,131I-FAPI-03 showed a specific binding rate of (22.00 ± 0.35)%,and the binding rate increased with the incubation time,to a peak of (37.5 ± 0.83)% at 180 min. However,the FAPα-negative MCF-7 cells exhibited very low uptake of 131I-FAPI-03 at any time point. The IC50 measured by the competition assay indicated significant binding property of 131I-FAPI-03. Biodistribution studies revealed that 131I-FAPI-03 could rapidly accumulate in tumor sites with an uptake of (14.90 ± 3.21)% ID/g at 5 min post injection. At 2 h post injection,131I-FAPI-03 displayed the highest tumor-to-muscle ratio of 43.7 ± 16.7. All above results provided important reference for the development of novel FAPα-targeting tracers.Key words: FAPα; 131I; FAPI; glioma肿瘤相关成纤维细胞(CAF)作为肿瘤微环境的主要组成部分,积极参与细胞外基质结构的重塑、肿瘤侵袭与转移、免疫抑制和耐药生成过程[1-3]。
当代化工研究Modem Chemical Research35 2021・05基础研究氮掺杂花状黑色二氧化钛(TQ)的制备及光催化性能研究*秦莲郭紫露刘娜马海燕王强段志英(西北民族大学化工学院甘肃730000)摘耍:本论文以金属钛粉和尿素为原料,利用水热法制备出氮掺杂黑色二氧化钛(Ti()2)光催化剂,并对其光催化性能进行了红外光谱、紫外光谱和SEM等表征实验,探讨了氮掺杂花状黑色二氧化钛(Tit)2)光催化剂的光催化性能.将甲基橙溶液作为目标降解染料,在模拟太阳光条件下照射含有不同氮掺杂含量的光催化剂的甲基橙溶液,紫外一可见分光光度计测试不同光催化剂的光催化性能.通过对不同形貌,不同掺杂量的催化剂比较研究,探讨结构与光催化性能之间丝关系.实验结果表明:以尿素:黑色花状二氧化钛=2:1餉比例制备的氮掺杂花状黑色二氧化钛催化剂对甲基橙溶液的催化降解效果最好,提高了对染料的降解作用°关键词:水热法;氮掺杂;花状黑色二氧化钛;可见光催化中图55•类号:0文献标识码:AStudy on Preparation of Nitrogen Doped Flower Black Titanium Dioxide(TiO2)and ItsPhotocatalytic PerformanceQin Lian,Guo Zilu,Liu Na,Ma Haiyan,Wang Qiang,Duan Zhiying(School of Chemical Engineering,Northwest University for Nationalities,Gansu,730000) Abstract:In this paper,the nitrogen-doped black titanium dioxide(RO)photocatalyst was prepared by hydrothermal method using titanium powder and urea as raw materials.The photocatalytic performance of the nitrogen-doped f lower black titanium dioxide(TiO^photocatalyst was studied by infrared spectroscopy,ultraviolet spectroscopy and SEM.Methyl orange solution was used as the target dye for degradation.Methyl orange solution containing different nitrogen doping content was irradiated under simulated sunlight conditions.The photocatalytic performance of different p hotocatalysts was tested by UV-Vis spectrophotometer.The relationship between the structure and p hotocatalytic p erformance was studied by comparing the catalysts with different morphologies and doping amounts.The experimental results showed that the nitrogen-doped f lowery black titanium dioxide catalyst prepared yvith the ratio of u rea to black f lowery titanium dioxide=2:l had the best catalytic degradation effect on methyl orange solution,which improved the degradation effect of d ye.Key words:hydrothermal method^N-doped\floral black titanium dioxide^visible light catalysis随着人类生活方式的改变和工业化的持续发展,如危险响口甸。
第39卷第1期 2018年2月1青岛科技大学学报(自然科学版"1Journal of Qingdao University of Science and TechnologyCNatural Science Edition)Vol. 39 No. 1Feb. 2018文章编号:1672-6987(2018)01-0018-04#!O I: 10.16351%.1672-6987.2018.01.0033-(4-甲氧基苯基)-4-甲基-5-异噻唑胺的合成及表征冯柏成,郭超(青岛科技大学化工学院,山东青岛266042)摘要:以对甲氧基苯甲醛为起始原料,经过肟化-脱水、交叉偶联、亲核加成和氧化闭环4步反应合成了目标产物3-(4-甲氧基苯基)-4-甲基-5-异噻唑胺,并且总收率可达47. 15%。
通过工艺条件优化,得到了盐酸羟胺和硫代乙酰胺的最佳用量。
目标化合物的结构通过GC-MS和1H N M R进行了鉴定。
实验结果表明:该反应条件温和,产品收率高,后处理简单,三废较少,具有良好的工业应用前景。
关键词:对甲氧基苯甲醛;苯甲腈;异噻唑;mGluR1拮抗剂中图分类号:0 626.29 文献标志码:A引用格式:冯柏成,郭超.3-(4-甲氧基苯基)-4-甲基-5-异噻唑胺的合成及表征青岛科技大学学报(自然科学版& 2018, 39(1): 18-21.FENG Baicheng,GU0Chao.Synthesis and characterization of3-( 4-methoxyphenyl)-4-methyl-5-isothiazolamine[J],Journal of Qingdao University of Science and TechnologyCNatural Science Edition),2018,39(1):18-21.Synthesis and Characterization of 3-(4-Methoxyphenyl)-4-methyl-5-isothiazolamineFENG Baicheng,GUO Chao(College of Chemical Engineerings Qingdao University of Science and Techn.ology» Qingdao 266042 &China)Abstract:Utilize p-methoxybenzaldehyde as a starting material,after oximation-dehydra-tion,cross-coupling,nucleophilic addition and oxidation closed-loop four-step reactions synthesized target product3-(4-methoxy-phenyl)-4-methyl-5-isothiazoleamine&and the totalyield is up to47. 15%. By optimizing the process conditions obtained the optimum dosage ofhydroxylamine hydrochloride and thioacetamide.The structure of the target product was confirmed by GC-MS and1H NMR.The experimental results show that the reaction condition ismild,product yield is high,simple workup,less three wastes,and with good industrial applications.Keywords: /i-methoxybenzaldehyde;menzonitrile;isothiazole;GluR1antagonistL-谷氨酸是中枢神经系统中主要的兴奋性神经 递质,其受体由两种主要的亚型组成:离子型受体和 代谢型受体(mGlU R)[12]。
SHANDONGCHEMDCALDNDUSTRY ・12・2020年第49卷3-四氢咲喃甲酸的生化与手性拆分吕宜春(山东化工职业学院化学工程系,山东潍坊261108)摘要:手性3- 咲喃 泛应用于新药研发,开发对其实用、 的手性分析方法尤为重要° 分子极性大,直接拆分困难,且在常规 灵敏度低,主 采用衍生化的方法对其进行间接拆分’但现 的衍生化方法存在着衍生化反应 长,反应不彻问题,不能满足快速、准确的 求’设计以硝基苯基重氮甲烷为衍生化 $ 考衍生化 结构、手性 、流对衍生化 识别拆分效果的 以及衍生化方法学的评价,建 了一套可靠的3- 咲喃 的快速手性法’方法基Chiralpak ID 手性柱为色谱柱$4-硝基苯基重氮甲烷为衍生化 ,衍 化反应在15 min 内完成,色谱分 8 min ° 解决了 3-咲喃 的 手性 ,还为它手性 手性酸的 法开发提供了参考’关键词:3- 咲喃 %手性拆分;衍 化%重氮烷T中图分类号:O657.72 文献标识码:A 文章编号:1008-021X ( 2020) 23-0012-04Rapid Derivatization and Chiral Resolution of Tetrahydrofuran-3 -carboxylic AcidLyu Yichun(Chemical Engineering Department ,Shandong Vocational CoLeee of Chemical Engineering , Weifang 261108, China)Abstract : Chiral tetrahydrofuran - 3 - c arboxylic aciO is widel- used in the research and developmeni of new drugs.The developmeniof practical and eeicieni chiral analysis method O particularl- ioportant for io At present , the resolution O mainly achieved byindirect method- of derivatization because of its larae polarity , dOf'iculth in direct resolution and low sensitivity in conventional detectoe. But there are problem- such a- long derivatization tioe and incomplete reaction , which cannot meet the need- of rapiO andaccurate detection.Herein,nitrophenyl diazomethane was first used as a derivative reagent.Then,the influence of the structure ofderivative reagent , chirai stationara phase and mobile phase on the recoLnition effect of resolution substrates was investivated ..heaccuracy and reliabilim of the method are verified. BinHy, a fast chiral detection method for tetrahydrofuran- 3 - carboxylic acid was established based on Chiralpak ID chiral cclumn and 4 -niOophenyl diazomethane as a derivative reagent. The derivatizationreaction was completed in 15 minutes and the chromatoLraphic analysis time was onty 8 minutes.This study not onty solved thehigh -efficienca chii ■s I detection of tetrahydrofuran - 3 -carboxylic acid, but alse provided a referencc foe the development of detection methods for other chiral or non-chOal aci-s.Key wordt : tetrahydrofuran-3-carboxyliv acid ; chOai resolution ; derivatization reaaents ; diazoalkancs手性3-四氢咲喃甲酸近年来被广泛应用于新药研发[1-4], 它的合成与分析引起了科技工作者的高度重视(5-)。
专利名称:Novel enzyme发明人:スクイレル デイヴィッド ジェームズ,マーフィーメレニー ジェーン,プライス レイチェル ルイーズ,ロウ クリストファー ロビン,ホワイト ピーター ジョン,ティシ ローレンス カーロ,マーレージェームス オウガスタス ヘンリー申请号:JP特願2000-578432(P2000-578432)申请日:19991026公开号:JP特表2003-518912(P2003-518912A)A公开日:20030617专利内容由知识产权出版社提供摘要: (57) and has a [summary] luciferase activity, Rushiora-Raterarisu Fotinasu pyralis, Rushiora-Mingurerika, or Rushiora-Kurushiata, Hotaria-Paroura, Piroforasu Pula formic off trout cod, Ramupirisu-Nokuchiruka, Piroko area Nayako or a protein having at least 60% similarity with the luciferase Fotinasu pen silane Vu~ani mosquito derived, in the sequence of the enzyme, the amino acid residue corresponding to amino acid residues 214 (a) Fotinasu pyralis luciferase derived from, amino acid residue corresponding to amino acid residues 232 (b) Fotinasu pyralis luciferase derived from an amino acid residue corresponding to amino acid residues 295 (c) Fotinasu pyralis luciferase derived from amino acids (d) Fotinasu pyralis luciferase derived from amino acid residue corresponding to amino acid residue corresponding to residue 14, the amino acid residue corresponding to amino acid residues 35 (e) Fotinasu pyralis luciferase derived from, the amino acid residue 105 (f) Fotinasu pyralis luciferase derived from, amino acid residue corresponding to amino acid residues 234 (g) Fotinasu pyralis luciferase derivedfrom an amino acid residue corresponding to amino acid residues 420 (h) Fotinasu pyralis luciferase derived from, (i) amino acids Fotinasu pyralis luciferase derived from at least one among the amino acid residue corresponding to residue 310, but and are those different from the amino acids that appear in the wild-type sequence corresponding the luciferase enzyme, the enzyme having the amino acid of the wild-type luciferase corresponding to the site enzyme characterized by having increased thermal stability as compared to.申请人:イギリス国地址:イギリス国 ウィルシャー エスピー4 0ジェイキュー ソールズベリー ポートンダウンディーエスティーエル国籍:GB代理人:中村 稔 (外9名)更多信息请下载全文后查看。
Vol. 35 No. 5功 能 高 分 子 学 报2022 年 10 月Journal of Functional Polymers417文章编号: 1008-9357(2022)05-0417-08DOI: 10.14133/ki.1008-9357.20220105001磷腈碱催化开环聚合制备含氟聚乙基硅氧烷刘正阳1, 时金凤1, 赵 娜1, 李志波1,2(青岛科技大学 1. 高分子科学与工程学院; 2. 化工学院, 山东 青岛 266042)摘 要: 以有机环三磷腈碱(CTPB)作为催化剂,在温和条件下催化六乙基环三硅氧烷(E3)开环聚合(ROP),以及E3与1,3,5-三甲基-1,3,5-三(3,3,3-三氟丙基)环三硅氧烷(F3)开环共聚合,制备了聚二乙基硅氧烷(PDES)和含有不同三氟丙基甲基硅氧(F)单元摩尔分数(0~46%)的聚(二乙基-ran-三氟丙基甲基)硅氧烷(PDES-ran-PTFPMS)。
采用凝胶渗透色谱仪(GPC)、核磁共振波谱仪(NMR)表征了聚合物的组成和结构,利用差示扫描量热仪(DSC)和微观接触角测量仪对聚合物的性质进行研究。
结果表明:成功制得PDES-ran-PTFPMS。
当F单元摩尔分数高于6%时,可以有效抑制PDES的低温结晶,且PDES-ran-PTFPMS具有极低的玻璃化转变温度(T g =−134 ℃)。
含氟聚乙基硅氧烷薄膜的接触角测试结果表明,F单元的引入有效提高了聚乙基硅氧烷的疏水性及降低了油的浸润性。
关键词: 有机磷腈碱;开环聚合;聚(二乙基- ran-三氟丙基甲基)硅氧烷;低玻璃化转变温度中图分类号: O633.4 文献标志码: APreparation of Fluorine-Containing Polyethylsiloxane by Ring-Opening Polymerization of Cyclic Siloxanes Catalyzed by Phosphazene BaseLIU Zhengyang1, SHI Jinfeng1, ZHAO Na1, LI Zhibo1,2(1. College of Polymer Science and Engineering; 2. College of Chemical Engineering,Qingdao University of Science and Technology, Qingdao 266042, China)Abstract: The ring-opening copolymerization (ROP) of hexaethylcyclotrisiloxane (E3) and 1,3,5-trimethyl-1,3,5-tri(3,3,3-trifluoropropyl) cyclotrisiloxane (F3) was catalyzed by organic cyclotrisiloxane base (CTPB) under mild conditions. CTPB showed high catalytic activity for the polymerization of E3 and F3. Linear polydiethylsiloxanes (PDES) and poly(diethyl-ran-trifluoropropylmethyl) siloxanes (PDES-ran-PTFPMS) with different mole fractions of trifluoropropylmethyl siloxane group (F unit) (mole fraction (f F): 0−46%) were successfully synthesized. The composition and structure of the PDES-ran-PTFPMS copolysiloxanes were characterized in detail by gel permeation chromatography (GPC) and nuclear magnetic resonance (NMR), and the glass transition temperature (T g) and crystallization behavior of the polymers were comprehensively analyzed by differential scanning calorimetry, and the water-oil contact angle of fluorine-containing polyethylsiloxane film was investigated by microscopic contact angle test. The chemical positions of the resonance peaks in the nuclear magnetic收稿日期: 2022-01-05基金项目: 山东省自然科学基金联合基金(No. ZR2020LFG014)作者简介: 刘正阳(1994—),男,山东潍坊人,硕士生,主要研究方向为聚硅氧烷的合成及改性工作。
第24卷 第7期2008年4月甘肃科技Gansu Science and TechnologyV ol.24 N o.7A p r. 2008聚乳酸及其共聚物的应用现状任宗礼(兰州交通大学化学与生物工程学院,甘肃兰州730070)摘 要:聚乳酸(PL A)具有优良的生物相容性和可降解性,在许多领域特别是医用材料方面备受关注,得到了广泛的应用。
文章对聚乳酸及其改性材料在药物控制释放、组织工程和手术缝合线等方面的研究现状做了较为详细的阐述。
关键词:可降解高分子;聚乳酸;应用;进展中图分类号:TQ31 在传统的聚烯烃类高分子材料带来的“白色污染”日趋严重的今天,以可降解的聚酯为代表的可降解高分子材料越来越受到人们的关注和青睐,其中以聚乳酸(PLA)类可降解高分子节尤为重要,每年都有大量相关的研究论文发表在诸如材料、医学、环境等各类学术刊物上。
由于PL A具有良好的降解性和生物相容性,因而在许多领域得到了广泛的应用,具有广阔的市场前景。
如美国阿尔贡国立实验室及Cargill公司已将PL A用于制造一次性食品包装袋、农用品等。
更重要的是其在生物医学工程领域的应用,如用于药物控制释放体系[1,2]、手术缝合线[3]、骨等组织工程材料[4,5]等的研究日益受到广泛关注。
1 药物控制释放体系近年来在医用高分子领域内,高分子药物控制释放体系的研究和开发方兴未艾。
所谓药物控制释放体系就是将药理活性分子与天然或合成高分子载体结合或复合,投施后在不降低原来药效及抑制副作用的情况下,以适当的浓度和持续时间,导向集积到患病的器官、细胞部位以充分发挥原来药物疗效的体系。
包埋有药理活性分子的聚合物微球(胶囊)是最常见的控制释放体系,最常用的制备方法有乳化溶剂挥发法、复乳法、相分离法、喷雾干燥法、熔融法等,实际工作中,要根据药物的理化性质、微球的粒径分布及释药速率等要求选择适当的制备方法,以获取所需的微球。
乳化溶剂挥发法的基本原理是将互不相溶的两相通过机械搅拌或超声乳化等方式制成乳剂,内相溶剂挥发除去后固化成微球。