Cell-penetrating riboflavin conjugate for antitumor photodynamic therapy

Wu，Chunlei1; Li，Yanyan1,2; Cheng，Zhehong1; Wang，Pengxin1; Ma，Zhilong1; Liu，Ke1; Cheng，Yulian1; Zhou，Yimin1; Lin，Xian1; Shao，Ximing1; Yang，Yong3; Li，Hongchang1,2; Fang，Lijing1,2

2022

10.1016/j.cclet.2022.01.036

CHINESE CHEMICAL LETTERS   影响因子和分区

1001-8417

Riboflavin (RF, vitamin B2) is an essential vitamin and has been considered as a promising natural photosensitizer for photodynamic therapy (PDT). However, further exploration of RF in antitumor application was limited by its poor cellular uptake. In this study, using cell-penetrating peptides Arg, (Cha-Arg) and small molecule triphenylphosphine (TPP) as delivery compounds, three RF conjugates were prepared to increase the accumulation of RF in cells, termed as Arg-RF, (Cha-Arg)-RF and TPP-RF, respectively. Compared with TPP-RF and Arg-RF, (Cha-Arg)-RF exhibited better cell internalization and stronger cytotoxicity against HeLa cells upon exposure to blue light. Further researches proved that (Cha-Arg)-RF generated reactive oxygen species (ROS) under irradiation, which could indiscriminately destroy endogenous proteins and mitochondria, ultimately inducing cell death. This work provides a new approach to explore RF as a natural photosensitizer for antitumor photodynamic therapy.

Antitumor Cell-penetrating peptides Photodynamic therapy Riboflavin

英语

通讯

Natural Science Foundation of Guangdong Province[2018B030308001];Natural Science Foundation of Guangdong Province[2019A1515012073];National Key Research and Development Program of China[2021YFA0910000];National Natural Science Foundation of China[21977111];National Natural Science Foundation of China[22007096];Science, Technology and Innovation Commission of Shenzhen Municipality[JCYJ20210324120200001];

CHEMISTRY

2-s2.0-85123732625

Scopus

1.Guangdong Key Laboratory of Nanomedicine,Institute of Biomedicine and Biotechnology,Shenzhen Institute of Advanced Technology,Chinese Academy of Sciences,Shenzhen,518055,China
2.University of Chinese Academy of Sciences,Beijing,100049,China
3.Department of Biomedical Engineering,Southern University of Science and Technology (SUSTech),Shenzhen,518055,China

Wu，Chunlei,Li，Yanyan,Cheng，Zhehong,et al. Cell-penetrating riboflavin conjugate for antitumor photodynamic therapy[J]. CHINESE CHEMICAL LETTERS,2022.

Wu，Chunlei.,Li，Yanyan.,Cheng，Zhehong.,Wang，Pengxin.,Ma，Zhilong.,...&Fang，Lijing.(2022).Cell-penetrating riboflavin conjugate for antitumor photodynamic therapy.CHINESE CHEMICAL LETTERS.

Wu，Chunlei,et al."Cell-penetrating riboflavin conjugate for antitumor photodynamic therapy".CHINESE CHEMICAL LETTERS (2022).