Department of Pharmacy and Pharmacology, University of Bath, Bath BA2 7AY, UK.
Photochem Photobiol Sci. 2018 Nov 1;17(11):1553-1572. doi: 10.1039/c8pp00362a. Epub 2018 Oct 17.
The administration of 5-aminolevulinic acid (ALA) to generate enhanced intracellular levels of endogenous porphyrins is currently one of the most important approaches for photodynamic therapy (PDT) and photodiagnosis (PDD). Despite the great promise of ALA-based PDT, the physicochemical behaviour and chemical reactivity of ALA are problematic, and a variety of chemical approaches have been brought to bear to improve cellular delivery, enhance porphyrin production, and generate ALA prodrugs that have appropriate stability for convenient clinical use, as well as selectivity for cancerous tissues. While there has been considerable success, there are still a number of challenges to be addressed and opportunities to be exploited through application of chemical insight in this area.
5-氨基酮戊酸（ALA）的给药会增强内源性卟啉的细胞内水平，这是光动力疗法（PDT）和光诊断（PDD）的最重要方法之一。尽管基于 ALA 的 PDT 有很大的前景，但 ALA 的物理化学行为和化学反应性存在问题，已经提出了各种化学方法来改善细胞递药、增强卟啉生成，并生成适合临床使用的方便性和对癌组织的选择性的 ALA 前药。虽然已经取得了相当大的成功，但通过在该领域应用化学洞察力，仍然有许多挑战需要解决，也有许多机会可以利用。
