http://jcps.bjmu.edu.cn

Journal of Chinese Pharmaceutical Sciences ›› 2019, Vol. 28 ›› Issue (8): 547-555.DOI: 10.5246/jcps.2019.08.052

• Original articles • Previous Articles     Next Articles

A small molecule LS-1-2F promotes the endocytosis of macromolecules into tumor cells

Yanyan Yang1, Dengbo Ji2, Simin Yang1, Siwang Yu1, Zhongjun Li1, Xiangbao Meng1*   

  1. 1. State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University Health Science Center, Beijing 100191, China
    2. Key Laboratory of Carcinogenesis and Translational Research, Ministry of Education, Department of Gastrointestinal Surgery III, Peking University Cancer Hospital & Institute, Beijing 100142, China
  • Received:2019-04-26 Revised:2019-05-18 Online:2019-09-02 Published:2019-05-29
  • Contact: Tel.: +86-10-82801714, E-mail: xbmeng@bjmu.edu.cn
  • Supported by:

    National Natural Science Foundation of China (Grant No. 81573272).

Abstract:

In the previous research, we found that anticancer agent LS-1-2F could cause the vacuolation of tumor cells. Herein we investigated the effect of compound LS-1-2F on the endocytosis of macromolecules, including fluorescence quantum dots, human serum albumin, single-stranded RNA, and monoclonal antibody, into tumor cells. We found that LS-1-2F could accelerate the endocytosis of these large molecules by laser confocal microscope and flow cytometry. The effect of LS-1-2F on the improvement of the internalization efficiency of Herceptin biosimilar was particularly significant. Promoting endocytosis will help increase the efficiency of liquid-phase drug uptake in drug-resistant cancer cells and could potentially facilitate the use of drugs in nanoparticle delivery vehicles. 

Key words: Methuosis, Macropinosomes, Endocytosis of macromolecule, Herceptin biosimilar

CLC Number: 

Supporting: