一种新型制剂显著提高了亚麻籽环肽（linusorbs）LOB3和LOB2对人乳腺癌MDA-MB-231细胞的细胞毒性。

A novel formulation significantly increases the cytotoxicity of flaxseed orbitides (linusorbs) LOB3 and LOB2 towards human breast cancer MDA-MB-231 cells.

作者信息

Yang Jina, Jadhav P D, Reaney M J T, Sammynaiken R, Yang Jian

出版信息

Pharmazie. 2019 Sep 1;74(9):520-522. doi: 10.1691/ph.2019.9055.

DOI:10.1691/ph.2019.9055

Abstract

Flaxseed orbitides (linusorbs) are a family of N to C linked bioactive cyclic octa-, nona-, and decapeptides present in flaxseed oil. They are highly hydrophobic and thermally stable. Our previous studies showed that [1-9-NC]-linusorb B3 (LOB3) and [1-9-NC]-linusorb B2 (LOB2) exhibited cytotoxic effects towards human breast cancer HER2-subtype Sk-Br-3 cells at a concentration of ~400 μM. However, this high concentration significantly limits their potential clinical applications. In the current study, we developed a novel polyethylene glycol-based formulation for linusorbs and showed that both LOB3 and LOB2, especially LOB3, exhibited strong cytotoxicity towards human breast cancer triple-negative-subtype MDA-MB-231 cells at low nanomolar concentrations.

摘要

亚麻籽环肽（亚麻环肽）是一类存在于亚麻籽油中的N端至C端相连的生物活性环状八肽、九肽和十肽。它们具有高度疏水性且热稳定性良好。我们之前的研究表明，[1-9-NC]-亚麻环肽B3（LOB3）和[1-9-NC]-亚麻环肽B2（LOB2）在浓度约为400μM时对人乳腺癌HER2亚型的Sk-Br-3细胞表现出细胞毒性作用。然而，如此高的浓度严重限制了它们潜在的临床应用。在当前研究中，我们开发了一种基于聚乙二醇的新型亚麻环肽制剂，并表明LOB3和LOB2，尤其是LOB3，在低纳摩尔浓度下对人乳腺癌三阴性亚型的MDA-MB-231细胞表现出强大的细胞毒性。