过氧化氢激活型近红外氟硼二吡咯光敏剂的设计、合成及光动力治疗研究

基于传统的氟硼二吡咯(BODIPY)荧光染料,设计合成了一种过氧化氢(H₂O₂)激活型近红外光敏剂中位-N-(4-硼酸苄基)吡啶鎓盐取代的碘化双苯乙烯基氟硼二吡咯(FP-IBDP). FP-IBDP在乙腈中的吸收和发射波长均达到近红外区,最大吸收和发射波长分别为681 nm和740 nm,对应的荧光量子效率和单线态氧效率分别为0.01和0.09.在被H₂O₂激活后, FP-IBDP转变为IBDP,其在乙腈中的最大吸收和发射波长分别为661 nm和701 nm.与FP-IBDP相比, IBDP的荧光量子效率和单线态氧效率大幅提升,分别达到0.11和0.48.细胞水平的荧光影像实验表明FP-IBDP对癌细胞内的H₂O₂具有灵敏的响应,并能通过明显的荧光增强变化实现癌细胞与正常细胞的有效区分.活性氧检测实验证明FP-IBDP能够被癌细胞内过表达的H₂O₂激活,并能在660nm光照射下在癌细胞内产生单线态氧.噻唑蓝(MT...     

肿瘤光动力治疗临床应用的光敏剂及其研究概况

光动力治疗是一种非侵蚀性并具有一定靶向性的肿瘤治疗新方法。 光动力治疗需要光敏剂、光和氧结合产生光动力反应。 光敏剂是光动力治疗的关键和物质基础。 本文概括介绍了已上市的和已被批准进入临床试验中的光敏剂,并根据其分子的骨架结构,将其分为分卟啉类、二氢卟吩（叶绿素）类和菌绿素/酞菁三类。 同时从理想光敏剂应具备特点出发,探讨了研究中的光敏剂和光动力治疗的发展前景。     

卟啉类光敏剂在光动力治疗中的应用研究

作为光动力疗法中至关重要的决定性因素,光敏剂的研究受到越来越多的重视.重点综述了多种新型卟啉类化合物、酞菁类化合物和二氢卟吩类化合物的合成及其在光动力治疗中的应用研究.     

可双光子激发的聚集诱导发光光敏剂及其生物医学应用

综合评述了双光子激发的聚集诱导发光(AIE)光敏剂的研究进展,重点讨论了双光子激发的AIE光敏剂的设计思路及在生物医学中的应用,并对其发展前景进行了展望。     

取代酞菁光敏剂的光动力疗法研究进展

酞菁类化合物作为新一代光敏剂用于光动力学治疗癌症,因表现出良好的光动力活性、靶组织选择性和低毒等优点而备受关注。本文对近几年取代酞菁光敏剂的光动力疗法研究进展作一简单介绍。     

光动力疗法用糖基光敏剂的研究进展

作为光动力疗法中至关重要的决定性因素,光敏剂的研究受到越来越多的重视.而糖基的引入,可以大大提高光敏剂母体的膜透过性和特异吸收性.从糖基光敏剂的母体结构、糖基光敏剂分子的构效关系、糖基的作用机理以及糖基光敏剂的药物动力学和代谢产物这四个方面对近年来糖基光敏剂的研究现状进行了综述,对其发展趋势进行了展望.     

有机光敏剂结构与性能调控及其光诊疗应用

光动力治疗(Photodynamic Therapy,PDT)作为一种新兴的高效治疗方式,具有毒性低、非侵入性和可控等优点,已被广泛用于增生性皮肤疾病和肿瘤等疾病治疗.然而,已开发的PDT光敏剂在实际生物应用中仍面临诸多挑战,如:肿瘤乏氧环境降低治疗效果,光敏剂靶向性差易造成对正常组织的损伤.为了解决上述问题,研究者们开发了许多有效改善有机光敏剂治疗效果的方法.在此,主要综述了有机光敏剂的结构与性能调控策略.此外,对有机光敏剂在抗肿瘤、抗菌治疗以及余辉成像中的应用进行了介绍.最后,对有机小分子光敏剂的设计策略进行了总结与展望,以期促进该领域的发展.     

用于光动力治疗酞菁类光敏剂的合成研究进展

简单介绍了光动力疗法的作用原理和机制,重点对多氟取代酞菁的几种主要合成方法进行了介绍。     

光动力抗菌光敏剂的研究进展

光动力抗菌化学疗法是一种结合光敏剂分子和可见光产生的活性氧物种杀灭病原微生物的抗感染治疗方法.活性氧物种能够与致病菌中的多种生物活性分子反应,这一特性使得微生物不易对该方法产生耐药性,这也是该方法近年来备受关注的主要原因.本文重点介绍了近年来光动力抗菌化学疗法领域新型光敏剂药物的研究进展,包括卟啉类衍生物、BODIPY化合物、共轭聚合物和钌多吡啶配合物.     

光动力疗法所用叶绿素类光敏剂的研究进展

以叶绿素-a及其衍生物的化学修饰为基点,综述叶绿素类二氢卟吩光敏剂合成的研究进展。     

酞菁在光动力治疗中的应用

光动力治疗因具有低毒、副作用小、抗癌广谱、高选择性等优势,正吸引着人们越来越多的关注。提高光敏剂的选择性和光毒性已经成为研究的热点。本文简单介绍了光敏剂的发展历程,并对酞菁类第三代光动力治疗光敏剂的最新研究进展进行了论述。     

酞菁在光动力治疗中的应用

光动力治疗因具有低毒、副作用小、抗癌广谱、高选择性等优势, 正吸引着人们越来越多的关注。提高光敏剂的选择性和光毒性已经成为研究的热点。本文简单介绍了光敏剂的发展历程, 并对酞菁类第三代光动力治疗光敏剂的最新研究进展进行了论述。     

Unraveling the Photodynamic Activity of Cationic Benzoporphyrin-Based Photosensitizers against Bladder Cancer Cells

In this study, we report the preparation of new mono-charged benzoporphyrin complexes by reaction of the appropriate neutral benzoporphyrin with (2,2′-bipyridine)dichloroplatinum(II) and of the analogs’ derivatives synthesized through alkylation of the neutral scaffold with iodomethane. All derivatives were incorporated into polyvinylpyrrolidone (PVP) micelles. The ability of the resultant formulations to generate reactive oxygen species was evaluated, mainly the singlet oxygen formation. Then, the capability of the PVP formulations to act as photosensitizers against bladder cancer cells was assessed. Some of the studied formulations were the most active photosensitizers causing a decrease in HT-1376 cells’ viability. This creates an avenue to further studies related to bladder cancer cells.     

GSH and H2O2 Co‐Activatable Mitochondria‐Targeted Photodynamic Therapy under Normoxia and Hypoxia

Currently, photosensitizers (PSs) that are microenvironment responsive and hypoxia active are scarcely available and urgently desired for antitumor photodynamic therapy (PDT). Presented herein is the design of a redox stimuli activatable metal‐free photosensitizer (aPS), also functioning as a pre‐photosensitizer as it is converted to a PS by the mutual presence of glutathione (GSH) and hydrogen peroxide (H₂O₂) with high specificity on a basis of domino reactions on the benzothiadiazole ring. Superior to traditional PSs, the activated aPS contributed to efficient generation of reactive oxygen species including singlet oxygen and superoxide ion through both type 1 and type 2 pathways, alleviating the aerobic requirement for PDT. Equipped with a triphenylphosphine ligand for mitochondria targeting, ^mito aPS showed excellent phototoxicity to tumor cells with low light fluence under both normoxic and hypoxic conditions, after activation by intracellular GSH and H₂O₂. The ^mito aPS was also compatible to near infrared PDT with two photon excitation (800 nm) for extensive bioapplications.     

靶标性酞菁类光敏剂的光动力疗法研究进展

光动力治疗（Photodynamic therapy,PDT）作为一种有别于传统癌症治疗方式的新型疗法,近些年来受到了科学家们越来越多的关注.它凭借着自身创伤性小,毒性低微,适用性好,可协同手术治疗以及可重复治疗等独特优势,在许多肿瘤的治疗方面有着广泛的应用.本文简要概述了光动力疗法的原理以及光敏剂的发展历程,并对理想光敏剂的特点作了总结.目前,以酞菁类化合物为主的第三代光敏剂已经成为光动力疗法的研究热点,然而如何提高光敏剂分子的靶向性达到精准的光动力治疗仍然是亟待解决的问题.因此,主要综述了近年来靶向性酞菁类光敏剂的研究进展,并对未来光敏剂的重点研究方向做出了展望.从目前来看,如何克服癌症低氧微环境的限制,发展Type I型不依赖氧的体系以及光穿透力强的靶向光敏剂在光动力治疗方面存在着巨大的潜质,有望成为新一代十分优良的光动力疗法用光敏剂.     

聚集诱导发光型光敏剂用于线粒体靶向光动力治疗

光动力治疗是一种基于光敏剂和光照的安全无创性治疗方法,在癌症治疗和杀菌等方面具有广阔的应用前景。光敏剂在光照激发下与氧气作用会生成高反应活性的活性氧。在细胞中过量的活性氧会氧化损伤蛋白质、核酸和脂质等细胞组分,诱导细胞凋亡或坏死。新兴的聚集诱导发光型光敏剂在分子聚集状态下光照激发能发射强的荧光,同时高效地产生活性氧,解决了传统光敏剂在分子聚集时荧光猝灭的问题,易实现成像指导的光动力治疗,近年来备受关注。线粒体作为细胞能量工厂富含氧气,是理想的光动力治疗靶点。本文总结了靶向癌细胞线粒体的聚集诱导发光型光敏剂的分子类型和设计策略,以及其在光动力治疗肿瘤方面的应用。     

Covalently Assembled Dipeptide Nanospheres as Intrinsic Photosensitizers for Efficient Photodynamic Therapy in Vitro

Monodispersed diphenylalanine‐based nanospheres with excellent biocompatibility are fabricated through a facile covalent reaction‐induced assembly. Interestingly, the nanospheres exhibit red autofluorescence. Most importantly, such assembled dipeptide nanospheres can serve as intrinsic photosensitizer to convert O₂ to singlet oxygen (¹O₂). Thus, photodynamic therapy in vitro can be achieved effectively. The versatile strategy could be extended to other biomolecules containing a primary amine group for the fabrication of potential intrinsic photosensitizers.     

Enzyme-Triggered Disassembly of Perylene Monoimide-based Nanoclusters for Activatable and Deep Photodynamic Therapy

Photodynamic therapy (PDT) exhibits great potential for cancer therapy, but still suffers from nonspecific photosensitivity and poor penetration of photosensitizer. Herein, a smart perylene monoimide-based nanocluster capable of enzyme-triggered disassembly is reported as an activatable and deeply penetrable photosensitizer. A novel carboxylesterase (CE)-responsive tetrachloroperylene monoimide (P1) was synthesized and assembled with folate-decorated albumins into a nanocluster ( FHP ) with a diameter of circa 100 nm. Once P1 is hydrolyzed by the tumor-specific CE, FHP disassembles into ultrasmall nanoparticles (ca. 10 nm), facilitating the deep tumor penetration of FHP . Furthermore, such enzyme-triggered disassembly of FHP leads to enhanced fluorescence intensity (ca. 8-fold) and elevated singlet oxygen generation ability (ca. 4-fold), enabling in situ near-infrared fluorescence imaging and promoted PDT. FHP permits remarkable tumor inhibition in vivo with minimal side effects through imaging-guided, activatable, and deep PDT. This work confirms that this cascaded multifunctional control through enzyme-triggered molecular disassembly is an effective strategy for precise cancer theranostics.