The Effects of Serum on Cellular Uptake and Phototoxicity of Mono‐L‐Aspartyl Chlorin e6 (NPe6) In Vitro
The Effects of Serum on Cellular Uptake and Phototoxicity of Mono‐L‐Aspartyl Chlorin e6 (NPe6) In Vitro
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体外血清对单左旋天冬氨酰二氯 e6 (NPe6) 细胞摄取和光毒性的影响
DOI：
10.1111/j.1751-1097.1998.tb03260.x
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发表时间：
1998
影响因子：
3.3
通讯作者：
H. Kato
中科院分区：
文献类型：
--
作者：
Llyar Sheyhedin;K. Aizawa;M. Araake;H. Kumasaka;T. Okunaka;H. Kato
摘要-已有报道表明，光敏剂L天冬氨酸单酯e6(NPe6)可与血清蛋白结合。然而，这种结合对NPe6细胞摄取和光动力疗法(PDT)光毒性的影响仍不明确。本文研究了血清对体外培养的P388细胞对NPe6的摄取和PDT光毒性的影响。(1)检测蛋白结合NPe6引起的红移(654 nm Q带吸收峰)；(2)用高效液相色谱法检测NPe6的细胞内浓度；(3)用四甲基偶氮唑盐比色法测定PDT后细胞存活率。NPe6与血清蛋白结合后，其654 nm Q带峰移至665 nm。蛋白质结合的NPe6不能被细胞摄取，因此没有PDT的光毒性。当NPe6浓度超过血清蛋白结合能力或培养液中有游离血清蛋白时，光毒性恢复。这些数据表明，细胞对NPe6的摄取受到培养液中血清成分的抑制，即使在相对较长的培养时间内，P388细胞也只积累了游离的NPe6。PDT的细胞毒性主要依赖于培养液中的游离NPe6水平。
Abstract— Previous reports showed that the photosensitizer mono‐l‐aspartyl chlorin e6 (NPe6) binds to serum proteins. However, the influence of this binding on the cellular uptake and photodynamic therapy (PDT) phototoxicity of NPe6 is still undefined. In this paper, we studied how serum in medium affected the P388 cellular uptake and PDT phototoxicity of NPe6 in vitro. This was assessed by (1) detection of the red shift (654 nm Q band peak of absorption) induced by protein binding NPe6; (2) detection of intracellular concentration of NPe6 by HPLC and (3) measurements of the cell survival ratio after PDT by MTT assay. The 654 nm Q band peak of NPe6 shifted to 665 nm after binding of NPe6 and serum proteins. The protein‐bound NPe6 cannot be uptaken by cells, thus there was no PDT phototoxicity. Nevertheless, phototoxicity recovered when the concentration of NPe6 excessed the serum protein binding ability or there was free serum protein in the medium. These data suggested that the cellular uptake of NPe6 is inhibited by serum components in the medium, and that only free NPe6 is accumulated by P388 cells even during relatively long incubations. The cytotoxicity of PDT mainly depends on the free NPe6 level in the medium.
影响因子：
11.2
作者：
C. Gomer;A. Ferrario
通讯作者：
C. Gomer;A. Ferrario