引用本文:李鹏熙, 刘忠洪, 杨玲玲, 杨兵.多肽修饰的还原敏感型靶向光敏剂的合成及生物活性评价[J].西南师范大学学报(自然科学版),2019,44(7):23~29
【打印本页】   【HTML】   【下载PDF全文】   查看/发表评论  【EndNote】   【RefMan】   【BibTex】
←前一篇|后一篇→ 过刊浏览    高级检索
本文已被:浏览 63次   下载 44 本文二维码信息
码上扫一扫!
分享到: 微信 更多
多肽修饰的还原敏感型靶向光敏剂的合成及生物活性评价
李鹏熙, 刘忠洪, 杨玲玲, 杨兵1,2
1. 重庆化工职业学院 环境与质量检测学院, 重庆 401228;2. 第三军医大学 军事预防医学院, 重庆 400038
摘要:
采用穿膜肽(八聚精氨酸)作为连接基团,双硫键为敏感化学键,叶酸作为靶向基团,修饰光敏剂替莫卟吩(m-THPC),制备了一种多肽修饰的还原敏感型靶向光敏剂1,其结构经核磁共振氢谱(1HNMR)和基质辅助激光离子化飞行时间型质谱仪(MALDI-TOF-MS)进行表征.研究表明,八聚精氨酸的引入,可显著改善m-THPC的溶解度和提高肿瘤细胞的靶向性;在谷光甘肽(GSH)作用下,光敏剂1可释放出m-THPC,6 h时的释放率大于80%.细胞毒性实验表明,光敏剂1在浓度为15 μmol/L时,HeLa细胞的存活率可降至36.1%,细胞毒性大于叶酸-PEG-羧酸卟吩(光敏剂7).
关键词:  八聚精氨酸  还原敏感型  叶酸靶向  光敏剂  生物活性
DOI:10.13718/j.cnki.xsxb.2019.07.004
分类号:O625.6
基金项目:重庆市基础与前沿研究计划项目(cstc2016jcyjA0075).
Design, Synthesis and Biological Activity of R8-Modified Reduction-Sensitive Targeting Photosensitizer
LI Peng-xi, LIU Zhong-hong, YANG Ling-ling, YANG Bing1,2
1. School of Environmental and Quality Detection, Chongqing Chemical Industry Vocational College, Chongqing 401228, China;2. Department of Occupational Health, Third Military Medical University, Chongqing 400038, China
Abstract:
The present study reported the preparation of a novel R8-modified redox-reponsive prodrug containing meso-tetra (m-hydroxy phenyl) chlorin (m-THPC), octaarginine(R8) and folate. The structure of target compound was characterized by UV-Vis, IR, HPLC, 1HNMR, MS spectra. The results show that the introduction of octa-arginine can significantly improve the solubility of m-THPC and increase the targeting property for tumor cells. m-THPC can be released from photosensitizer 1 under the action of GSH, and the release rate was more than 80% at 6 h. The cytotoxicity test showed that the survival rate of HeLa cell can be reduced to 36.1% whenthe concentration of photosensitizer 1 is 15 μmol/L, and the cytotoxicity of photosensitizer 1 is stronger than photosensitizer 7.
Key words:  octa-arginine  reduction-sensitive type  folate-targeted  photosensitizer  biological activity
手机扫一扫看