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

小分子药物LS-1-2F促进肿瘤细胞内吞大分子（英文）

作　　者：Yanyan Yang Dengbo Ji Simin Yang Siwang Yu Zhongjun Li Xiangbao Meng 杨燕燕;吉登波;杨思敏;余四旺;李中军;孟祥豹(北京大学医学部药学院天然药物及仿生药物国家重点实验室,北京100191;北京大学肿瘤医院恶性肿瘤发病机制及转化研究教育部重点实验室,北京100142)

机构地区：[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

出　　处：《Journal of Chinese Pharmaceutical Sciences》2019年第8期547-555,共9页中国药学（英文版）

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

摘　　要：In the previous research, we found that anticancer agent LS-1-2 F could cause the vacuolation of tumor cells. Herein we investigated the effect of compound LS-1-2 F 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-1-2 F could accelerate the endocytosis of these large molecules by laser confocal microscope and flow cytometry. The effect of LS-1-2 F 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.在之前的研究中,我们发现抗肿瘤药物LS-1-2F可以引起肿瘤细胞的空泡化现象。本文中研究了化合物LS-1-2F对大分子(包括荧光量子点、人血清白蛋白、单链RNA和单克隆抗体)内吞进入肿瘤细胞内的作用。通过激光共聚焦显微镜和流式细胞仪,研究发现LS-1-2F能促进这些大分子的内吞作用,对提高赫赛汀生物类似物内化效率的作用尤为显著。促进内吞将有助于提高耐药肿瘤细胞对液相药物的吸收效率,还有望促进纳米颗粒递送载体中药物的利用。

关 键 词：Methuosis Macropinosomes Endocytosis of macromolecule Herceptin biosimilar 

分 类 号：R962[医药卫生—药理学]