Synthesis and biological evaluation of novel peptides based on antimicrobial peptides as potential agents with anti-tumor and multidrug resistance-reversing activities

Abstract

Tumor chemotherapy, which plays an important role in the clinical treatment of metastatic cancer, is limited by low selectivity and drug resistance in clinical application. In our study, we selected antimicrobial peptide BP100 as a lead peptide, designed and synthesized a series of novel antineoplastic peptides through solid-phase synthesis. Amongst them, B4 and B8 showed excellent anti-cancer activity. As revealed by further investigations, these peptides could disrupt the cell membrane, trigger the cytochrome C release into cytoplasm and ultimately lead to apoptosis. In addition, they also showed multidrug resistance-reversing effects by performing effective anti-tumor activity against multidrug resistant cells. As a result, these peptides may possibly be regarded as a promising candidate for cancer treatment.

This article is protected by copyright. All rights reserved.

In our study, we selected antimicrobial peptide BP100 as a lead peptide, designed and synthesized a series of novel antineoplastic peptides through solid-phase synthesis.

http://ift.tt/2qZArVH