INVITRO CHARACTERIZATION OF MONOASPARTYL CHLORIN E6 AND DIASPARTYL CHLORIN E6 FOR PHOTODYNAMIC THERAPY
INVITRO CHARACTERIZATION OF MONOASPARTYL CHLORIN E6 AND DIASPARTYL CHLORIN E6 FOR PHOTODYNAMIC THERAPY
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DOI：
10.1093/jnci/80.5.330
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发表时间：
1988-05-04
影响因子：
10.3
通讯作者：
BERNS, MW
中科院分区：
文献类型：
--
作者：
ROBERTS, WG;SHIAU, FY;BERNS, MW
通过细胞培养，测定了两种新的二氢卟酚类光敏剂的光毒性、亚细胞定位和光物理性质。二氢卟酚e6（MACE）和二烯丙基二氢卟酚e6（DACE）是新的光敏剂，显示出用于光动力疗法的前景。这些二氢卟酚是纯的单体化合物，通过高压液相色谱法测定。这两种化合物在比二血卟啉醚酯（DHE）更长的波长（664 nm）处吸收显著。由于化合物的纯度和单一的荧光发射峰，使用荧光进行肿瘤诊断应该是容易的。使用标准的克隆形成试验完成敏化剂的光毒性剂量-反应曲线，以确定细胞活力。二氢卟酚类化合物对光有较好的敏化作用。此外，使用荧光显微镜研究了MACE、DACE和DHE的亚细胞定位。而DHE位于整个细胞质，本地化的二氢卟酚的主要网站似乎是在溶酶体。结果表明，MACE和DACE在体外是有效的光敏剂，并优于DHE。
The characteristics of two new chlorin photosensitizers were studied in cell culture by determining phototoxicity, subcellular localization, and photophysical properties. Monoaspartyl chlorin e6 (MACE) and diaspartyl chlorin e6 (DACE) are new photosensitizers that show promise for use in photodynamic therapy. These chlorins are pure, monomeric compounds as determined by high-pressure liquid chromatography. Both compounds absorb substantially at a longer wavelength (664 nm) than does dihematoporphyrin ether-ester (DHE). Tumor diagnosis with the use of fluorescence should be facilitated due to the purity of the compounds and the single fluorescence emission peak. Phototoxicity dose-response curves of the sensitizers were completed using a standard clonogenic assay to determine cell viability. The chlorins showed good sensitizing capabilities with light. In addition, subcellular localization of MACE, DACE, and DHE was studied using fluorescence microscopy. Whereas DHE was located throughout the cytoplasm, the primary site of localization of the chlorins appeared to be in the lysosome. The results demonstrate that MACE and DACE are effective photosensitizing agents in vitro and compare favorably to DHE.