小分子药物LS-1-2F促进肿瘤细胞内吞大分子

doi:10.5246/jcps.2019.08.052

中国药学(英文版) ›› 2019, Vol. 28 ›› Issue (8): 547-555.DOI: 10.5246/jcps.2019.08.052

小分子药物LS-1-2F促进肿瘤细胞内吞大分子

杨燕燕¹, 吉登波², 杨思敏¹, 余四旺¹, 李中军¹, 孟祥豹^1*

1. 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
2. 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

收稿日期:2019-04-26 修回日期:2019-05-18 出版日期:2019-09-02 发布日期:2019-05-29
通讯作者: Tel.: +86-10-82801714, E-mail: xbmeng@bjmu.edu.cn
基金资助:
National Natural Science Foundation of China (Grant No. 81573272).

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 Meng^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).

摘要/Abstract

摘要：

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: 巨泡化, 巨胞饮, 大分子内吞, 赫赛汀生物类似物

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

中图分类号:

R962

Supporting:

杨燕燕, 吉登波, 杨思敏, 余四旺, 李中军, 孟祥豹. 小分子药物LS-1-2F促进肿瘤细胞内吞大分子[J]. 中国药学(英文版), 2019, 28(8): 547-555.

Yanyan Yang, Dengbo Ji, Simin Yang, Siwang Yu, Zhongjun Li, Xiangbao Meng. A small molecule LS-1-2F promotes the endocytosis of macromolecules into tumor cells[J]. Journal of Chinese Pharmaceutical Sciences, 2019, 28(8): 547-555.

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小分子药物LS-1-2F促进肿瘤细胞内吞大分子

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

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