Kessel D
Photochem Photobiol. 1989 Apr;49(4):447-52. doi: 10.1111/j.1751-1097.1989.tb09193.x.
The mono-N-aspartyl derivative of chlorin e6 (MACE) is a new photosensitizer being examined for use in anti-neoplastic photodynamic therapy. Studies were carried out to identify unique aspects of MACE localization by murine leukemia L1210 cells in vitro. Octanol/water partitioning studies were used to quantitate the hydrophobicity of MACE and two analogs, chlorin e6 and mesochlorin. Sites of cellular localization of these dyes were probed by fluorescence studies, and by examining loci of photodamage. These studies indicate that MACE, a hydrophilic dye, partitions to cytoplasmic loci. Data obtained with chlorin e6, a more hydrophobic dye, are consistent with binding at both membrane and cytoplasmic sites. A substantially more hydrophobic product, meso-chlorin, binds primarily to the cell membrane. While the tumor-localizing porphyrin product HPD binds to plasma LDL less than HDL, MACE and CE are predominantly bound to plasma protein and HDL. Patterns of distribution and localization of MACE differ substantially from those observed with HPD and other hydrophobic sensitizers. Phototoxic effects of MACE could not be specifically attributed to membrane or mitochondrial damage.
二氢卟吩e6单-N-天冬氨酸衍生物（MACE）是一种正在研究用于抗肿瘤光动力疗法的新型光敏剂。开展了相关研究以确定小鼠白血病L1210细胞在体外对MACE的独特摄取特性。采用正辛醇/水分配研究来定量MACE以及两种类似物二氢卟吩e6和中位二氢卟吩的疏水性。通过荧光研究以及检测光损伤位点来探究这些染料在细胞内的定位位点。这些研究表明，亲水性染料MACE分配至细胞质位点。用疏水性更强的染料二氢卟吩e6获得的数据与在膜和细胞质位点的结合情况一致。疏水性更强的产物中位二氢卟吩主要结合至细胞膜。虽然肿瘤定位卟啉产物血卟啉衍生物与血浆低密度脂蛋白的结合少于高密度脂蛋白，但MACE和二氢卟吩e6主要结合至血浆蛋白和高密度脂蛋白。MACE的分布和定位模式与血卟啉衍生物及其他疏水性光敏剂的显著不同。MACE的光毒性作用不能特异性归因于膜或线粒体损伤。
