摘要
由于光动力疗法在癌症治疗中前景可观,故光敏剂得到了很大发展。因此,光合色素、叶绿素和细菌叶绿素作为优良的天然光敏剂,一直备受关注。实际上,一些以(细菌)叶绿素为基本的光疗药物已(或即将)进入临床应用。本文旨在介绍过去十年中这些化学合成色素的发展概况,其作为光敏剂用于光动力疗法(PDT),并与其衍生物的应用相关。本文研究重点是采用化学合成的方式获得(细菌)叶绿素新的衍生物,并具有增强光敏作用和肿瘤定位性能,同时提高叶绿素的光稳定性和化学稳定性。这些措施包括在C-17酯基团部分、碳环、中央结合口袋,以及糖、肽、和纳米颗粒部分或其他残留物的C-3和C-7位的衍生化,并对色素基本特征的修饰效果进行了讨论,如活性氧族生成的效率,光稳定性,光毒性和生物相互作用。本文分为如下几部分:第一部分,对PDT与光敏剂作用原理进行简要概述。第二部分,总结了(细菌)叶绿素相关的光物理特征和早期修饰方法。第三部分,进一步详细介绍色素合成方法的研究进展,并探讨修饰作用对色素的光物理活性及生物活性的影响。
关键词: 细菌叶绿素,生物活性,叶绿素,修饰,光动力疗法,光敏剂,活性氧族,肿瘤显像,肿瘤靶向。
Current Medicinal Chemistry
Title:Recent Progress in Chemical Modifications of Chlorophylls and Bacteriochlorophylls for the Applications in Photodynamic Therapy
Volume: 22 Issue: 26
Author(s): Jakub Staron, Bożena Boron, Dariusz Karcz, Malgorzata Szczygiel and Leszek Fiedor
Affiliation:
关键词: 细菌叶绿素,生物活性,叶绿素,修饰,光动力疗法,光敏剂,活性氧族,肿瘤显像,肿瘤靶向。
摘要: Since photodynamic therapy emerged as a promising cancer treatment, the development of photosensitizers has gained great interest. In this context, the photosynthetic pigments, chlorophylls and bacteriochlorophylls, as excellent natural photosensitizers, attracted much attention. In effect, several (bacterio) chlorophyll-based phototherapeutic agents have been developed and (or are about to) enter the clinics. The aim of this review article is to give a survey of the advances in the synthetic chemistry of these pigments which have been made over the last decade, and which are pertinent to the application of their derivatives as photosensitizers for photodynamic therapy (PDT). The review focuses on the synthetic strategies undertaken to obtain novel derivatives of (bacterio)chlorophylls with both enhanced photosensitizing and tumorlocalizing properties, and also improved photo- and chemical stability. These include modifications of the C- 17-ester moiety, the isocyclic ring, the central binding pocket, and the derivatization of peripheral functionalities at the C-3 and C-7 positions with carbohydrate-, peptide-, and nanoparticle moieties or other residues. The effects of these modifications on essential features of the pigments are discussed, such as the efficiency of reactive oxygen species generation, photostability, phototoxicity and interactions with living organisms. The review is divided into several sections. In the first part, the principles of PDT and photosensitizer action are briefly described. Then the relevant photophysical features of (bacterio)chlorophylls and earlier approaches to their modification are summarized. Next, a more detailed overview of the progress in synthetic methods is given, followed by a discussion of the effects of these modifications on the photophysics of the pigments and on their biological activity.
Export Options
About this article
Cite this article as:
Staron Jakub, Boron Bożena, Karcz Dariusz, Szczygiel Malgorzata and Fiedor Leszek, Recent Progress in Chemical Modifications of Chlorophylls and Bacteriochlorophylls for the Applications in Photodynamic Therapy, Current Medicinal Chemistry 2015; 22 (26) . https://dx.doi.org/10.2174/0929867322666150818104034
DOI https://dx.doi.org/10.2174/0929867322666150818104034 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
- Announcements