新型靶向光敏剂Ⅰ对Hep-2细胞的光动力抑瘤活性  

Photodynamic activity of novel targeting photosensitizerⅠfor Hep-2 cells

作　　者：李东红[1] 李鹏熙[1] 蒋宗林[2] 郭林峰[2] 

机构地区：[1]创伤、烧伤、复合伤国家重点实验室第三军医大学大坪医院野战外科研究所二室,重庆400042 [2]华西师范大学化学系

出　　处：《肿瘤研究与临床》2013年第1期1-4,共4页Cancer Research and Clinic

基　　金：国家自然科学基金（21072227）

摘　　要：目的 评价新型靶向性光敏剂Ⅰ（PSⅠ）对喉癌Hep-2细胞的靶向性和光动力活性。方法 采用bleaching实验评价PSⅠ的稳定性； 荧光测定法观察Hep-2细胞对PSⅠ的摄取能力； 四甲基偶氮唑蓝（MTT）比色法检测PSⅠ浓度、光照剂量及光照时间点对Hep-2细胞存活率的影响。结果 在光照50 min后，PSⅠ的吸光度（A）值仅降低了11 %，表明其稳定性可满足光动力治疗的需要；Hep-2细胞对PSⅠ的摄取随PSⅠ浓度的增加而增加，但过量叶酸的存在可明显抑制Hep-2细胞对PSⅠ的摄取（t值分别为5.96，4.89，均P＜0.01）；MTT实验结果表明Hep-2细胞的存活率与PSⅠ浓度和光照剂量呈负相关（r＝-0.763，P＝0.017； r＝-0.946，P＝0.001）。当PSⅠ浓度为14 μmol／L、光照剂量为18 J／cm2时，Hep-2细胞的存活率仅为34 %，而在无光照时即使光敏剂浓度升至110 μmol／L，Hep-2细胞的存活率仍为100 %；给予PSⅠ 24 h后再进行光动力治疗（PDT）可有效地抑制Hep-2细胞的生长，其存活率只有32 %。结论 PSⅠ拥有满意的光稳定性和低的暗毒性，对Hep-2细胞有很好的靶向性和光动力活性。Objective To evaluate the targeting and photodynamic activity of photosensitizer Ⅰ（PSⅠ） for laryngocarcinoma Hep-2 cells. Methods The photostability of PSⅠ was measured by bleaching assay. The cellular uptake of PSⅠ by Hep-2 cells were evaluated by fluorescence spectroscopy, the effects of PSⅠ concentration, irradiation dose and etc on the viability of Hep-2 cells were investigated by MTT assay. Results After irradiation of 50 min, the OD value of PSⅠ decreased 11 %, which indicated that the stability of PSⅠ can meet the requirement of PDT. The cellular uptake of PSⅠ by Hep-2 cells increased with the concentration of PSⅠ and can be obviously inhibited by the presence of excessive free folic acid （P 〈 0.01）. The results of MTT assays demonstrated that the viability of Hep-2 showed negative correlation with the PSⅠ concentration and irradiation dose. The viability of Hep-2 was only 34 % after PDT with 14 μmol/L of the PSⅠ and 18 J/cm2 of irradiation. However, the viability of Hep-2 was still 100 % without irradiation, even though the concentration of PSⅠ was up to 110 μmol/L. The PDT carried out after 24 h of PSⅠ administration can efficiently inhibited the growth of Hep-2 with the survival rate of 32 %. Conclusion The PSⅠ posses satisfactory photostability and lower dark cytotoxicity, and displays significant targeting and photocytotoxicity for Hep-2 cells.

关 键 词：光敏剂Ⅰ HEP-2细胞 肿瘤靶向性 光动力活性 

分 类 号：R739.65[医药卫生—肿瘤]