Novel phototherapeutic agents:Investigation and progress of hypocrellin derivatives  

作　　者：XUShancgjie ZHANGXiaoxing CHENShen ZHANGManhua SHENTao WANGZhengping 

机构地区：[1]CenterforPhotochemistry,InstituteofChemistry,ChineseAcademyofSciences,Beijing100080,China [2]DepartmentofChemicalEngineer,HarbinEngineeringUniversity,Harbin150001,China

出　　处：《Chinese Science Bulletin》2003年第17期1775-1785,共11页

基　　金：supported by the National Natural Science Foundation of China(Grant No.20172058).

摘　　要：Hypocrellins, as a kind of novel phototherapeu-tic agents, have several advantages over the clinically used hematoporphyrin derivatives, including high-excited triplet state yield, high phototoxicity, low dark toxicity, and rapid metabolism. However, they exhibit little absorption in the photodynamic window (600—900 nm) and are not water soluble, which limits their application in photodynamic therapy. Sulfonated and metal-ioned hypocrellins have been designed and synthesized to improve their water solubility. Unfortunately, the water-soluble derivatives obtained exhibit lower photodynamic activity than the parent hypocrellins. Thiolated and aminated hypocrellins have also been designed and synthesized to enlarge their photoresponse. Among them, the aminated hypocrellins possess the highest photodynamic activity. We recently have further designed and synthesized some amphiphilic aminated hypocrellin derivatives. Thus, not only the photoresponse but also the water solubility is enhanced. The experiments in vitro and in vivo on the deriva-tives are under way at present.Hypocrellins, as a kind of novel phototherapeu-tic agents, have several advantages over the clinically used hematoporphyrin derivatives, including high-excited triplet state yield, high phototoxicity, low dark toxicity, and rapid metabolism. However, they exhibit little absorption in the photodynamic window (600—900 nm) and are not water soluble, which limits their application in photodynamic therapy. Sulfonated and metal-ioned hypocrellins have been designed and synthesized to improve their water solubility. Unfortunately, the water-soluble derivatives obtained exhibit lower photodynamic activity than the parent hypocrellins. Thiolated and aminated hypocrellins have also been designed and synthesized to enlarge their photoresponse. Among them, the aminated hypocrellins possess the highest photodynamic activity. We recently have further designed and synthesized some amphiphilic aminated hypocrellin derivatives. Thus, not only the photoresponse but also the water solubility is enhanced. The experiments in vitro and in vivo on the deriva-tives are under way at present.

关 键 词：光动力性疗法 光敏剂 纯态氧 过氧离子团 电子顺磁共振 

分 类 号：R454.2[医药卫生—治疗学]