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表皮生长因子受体靶向脂质体联合人参皂苷 Rh2 抑制三阴性乳腺癌生长和转移。

EGFR-Targeted Liposomes Combined with Ginsenoside Rh2 Inhibit Triple-Negative Breast Cancer Growth and Metastasis.

机构信息

Laboratory for Forest Resources Conservation and Utilization in the Southwest Mountains of China, Ministry of Education, International Ecological Forestry Research Center of Kunming, Southwest Forestry University, Kunming 650224, China.

Cixi Institute of Biomedical Engineering, Ningbo Key Laboratory of Biomedical Imaging Probe Materials and Technology, International Cooperation Base of Biomedical Materials Technology and Application, Chinese Academy of Sciences (CAS) Key Laboratory of Magnetic Materials and Devices, Zhejiang Engineering Research Center for Biomedical Materials, Ningbo Institute of Materials Technology and Engineering, CAS, Ningbo 315201, China.

出版信息

Bioconjug Chem. 2023 Jun 21;34(6):1157-1165. doi: 10.1021/acs.bioconjchem.3c00207. Epub 2023 May 26.

Abstract

Triple-negative breast cancer (TNBC) remains the most challenging breast cancer subtype due to its lack of targeted therapies and poor prognosis. In order to treat patients with these tumors, efforts have been made to explore feasible targets. Epidermal growth factor receptor (EGFR)-targeted therapy is currently in clinical trials and regarded to be a promising treatment strategy. In this study, an EGFR-targeting nanoliposome (LTL@Rh2@Lipo-GE11) using ginsenoside Rh2 as a wall material was developed, in which GE11 was used as the EGFR-binding peptide to deliver more ginsenoside Rh2 and luteolin into TNBC. In comparison to non-targeted liposomes (Rh2@Lipo and LTL@Rh2@Lipo), the nanoliposomes LTL@Rh2@Lipo-GE11 demonstrated a high specificity to MDA-MB-231 cells that expressed a high level of EGFR both in vitro and in vivo, contributing to the strong inhibitory effects on the growth and migration of TNBC. These results suggest that LTL@Rh2@Lipo-GE11 is a prospective candidate for targeted therapy of TNBC, with a remarkable capability to inhibit tumor development and metastasis.

摘要

三阴性乳腺癌(TNBC)由于缺乏靶向治疗和预后不良,仍然是最具挑战性的乳腺癌亚型。为了治疗这些肿瘤的患者,人们一直在努力探索可行的靶点。表皮生长因子受体(EGFR)靶向治疗目前正在临床试验中,被认为是一种有前途的治疗策略。在这项研究中,开发了一种 EGFR 靶向纳米脂质体(LTL@Rh2@Lipo-GE11),使用人参皂苷 Rh2 作为壁材,其中 GE11 被用作 EGFR 结合肽,将更多的人参皂苷 Rh2 和木犀草素递送至 TNBC 中。与非靶向脂质体(Rh2@Lipo 和 LTL@Rh2@Lipo)相比,纳米脂质体 LTL@Rh2@Lipo-GE11 在体外和体内均对表达高水平 EGFR 的 MDA-MB-231 细胞表现出高特异性,有助于对 TNBC 的生长和迁移产生强烈的抑制作用。这些结果表明,LTL@Rh2@Lipo-GE11 是 TNBC 靶向治疗的有前途的候选药物,具有显著抑制肿瘤发展和转移的能力。

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