원문정보
초록
영어
Overexpression of human epidermal growth factor receptor 2 (HER2) in cancer cells results in increased resistance to antitumor drugs, such as paclitaxel. Epothilone B is a promising anti-tumor agent has potential to overcome the well-known paclitaxel resistance. For effective delivery and targeting to cancer cells, epothilone B was assembled with apolipoprotein A-I (apoA-I), resulting in high density lipoprotein-like epothilone B nanoparticle (Ept B-NP). It is known that apoA-I in HDL is recognized by scavenger receptor class B1 (SR-BI), which is expressed by most cancer cells. Here, we report a strategy to prepare of Ept B-NP with high yield. The Ept B-NP lacking lipid adjurvants exhibited pH-responsive unloading of epothilone B, which is a required characteristic of anti-tumor chemotherapy. We tested the antitumoral efficacy of Ept B-NP in various cancer cell lines and show that Ept B-NP is relative to SR-BI receptor, kills well HER2-overexpressing cells and is safe to unrelated cells.