Beijing National Laboratory for Molecular Sciences, Key Laboratory of Analytical Chemistry for Living Biosystems, CAS Research/Education Center for Excellence in Molecular Sciences, Institute of Chemistry, Chinese Academy of Sciences, Beijing 100190, China; Department of Pharmaceutical Chemistry, School of Pharmaceutical Sciences, Guangxi Medical University, No. 22, Shuangyong Road, Nanning 530021, Guangxi, PR China.
Molecular Science and Biomedicine Laboratory, State Key Laboratory of Chemo/Bio-Sensing and Chemometrics, College of Biology and College of Chemistry and Chemical Engineering, Hunan University Changsha, 410082, China.
EBioMedicine. 2017 Sep;23:25-33. doi: 10.1016/j.ebiom.2017.08.010. Epub 2017 Aug 9.
The lack of ideal photosensitizers limits the clinicalapplication of photodynamic therapy (PDT). Here we report the PDT efficiency of dicyanomethylene substituted benzothiazole squaraine derivatives. This class of squaraine derivatives possess strong absorption and long excitation and emission wavelengths (ex/em, 685/720nm). They show negligible dark toxicity, but can generate singlet oxygen under irradiation resulting in the apoptosis and necrosis of cells (phototoxicity). Changing the side chains of these compounds greatly influences their albumin-binding rate, cellular uptake and their phototoxicity. One of the squaraine derivatives with two methyl butyrate side chains shows high PDT efficiency in a mouse subcutaneous xenograft model under the irradiation of a 690nm laser. These results show the great potential of dicyanomethylene substituted benzothiazole squaraines to be the leading compound of near-infrared photosensitizers in PDT.
缺乏理想的光敏剂限制了光动力疗法（PDT）的临床应用。在这里，我们报告了二氰亚甲基取代苯并噻唑方酸菁衍生物的 PDT 效率。这一类方酸菁衍生物具有很强的吸收和长的激发和发射波长（ex/em，685/720nm）。它们表现出可以忽略的暗毒性，但在光照下可以产生单线态氧，导致细胞凋亡和坏死（光毒性）。改变这些化合物的侧链会极大地影响它们与白蛋白的结合率、细胞摄取率和光毒性。其中一个带有两个甲基丁酸侧链的方酸菁衍生物在 690nm 激光照射下的小鼠皮下异种移植模型中表现出很高的 PDT 效率。这些结果表明，二氰亚甲基取代苯并噻唑方酸菁具有成为 PDT 近红外光敏剂主导化合物的巨大潜力。
