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Synthesis and biological evaluation of novel peptides based on antimicrobial peptides as potential agents with antitumor and multidrug resistance‐reversing activities
Author(s) -
Zhang Bo,
Shi Wei,
Li Jieming,
Liao Chen,
Yang Limei,
Huang Wenlong,
Qian Hai
Publication year - 2017
Publication title -
chemical biology and drug design
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.59
H-Index - 77
eISSN - 1747-0285
pISSN - 1747-0277
DOI - 10.1111/cbdd.13023
Subject(s) - multiple drug resistance , antimicrobial , antimicrobial peptides , reversing , pharmacology , antibiotic resistance , biology , computational biology , microbiology and biotechnology , chemistry , drug resistance , antibiotics , materials science , composite material
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 BP 100 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.