小分子药物LS-1-2F促进肿瘤细胞内吞大分子（英文）

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。

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

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.