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. Among them, B4 and B8 showed excellent anticancer 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 antitumor activity against multidrug-resistant cells. As a result, these peptides may possibly be regarded as a promising candidate for cancer treatment.
Keywords: anticancer; antimicrobial peptides; helix; membrane disruption; multidrug resistance-reversing effects.
© 2017 John Wiley & Sons A/S.