Amino Acids

, Volume 49, Issue 8, pp 1355–1364 | Cite as

Design, synthesis and biological evaluation of novel peptides as potential agents with anti-tumor and multidrug resistance-reversing activities

Original Article


Tumor chemotherapy is an important mean in the clinical treatment of metastatic cancer,but low selectivity and drug resistance restrict its clinical application. BP100 is a multifunctional membrane-active peptide with high antimicrobial activity. We selected BP100 as a lead peptide, designed and synthesized a series of BP100 analogs through solid-phase synthesis. Amongst them, peptides with the Tyr10 residue substituted by leucine and histidine showed the highest anti-cancer activity. Further experiments revealed that BP100 and its analogs could disrupt the cell membrane and trigger the cytochrome C release into cytoplasm, which ultimately resulted in apoptosis. Meanwhile, BP100 and its analogs also exhibited effective anti-tumor activity against multidrug-resistant cells, showing multidrug resistance-reversing effects. In conclusion, these peptides might be promising candidates for cancer therapy.


Anti-cancer Multidrug resistance-reversing effects Membrane-disruption Antimicrobial peptides 



This study was supported by Grants from the National Natural Science Foundation of China (Grants 81673299 and 81273376).

Compliance with ethical standards

Conflict of interest

The authors have no conflicts of interest to declare.

Supplementary material

726_2017_2434_MOESM1_ESM.docx (1.2 mb)
Supplementary material 1 (DOCX 1253 kb)


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Copyright information

© Springer-Verlag Wien 2017

Authors and Affiliations

  1. 1.Center of Drug Discovery, State Key Laboratory of Natural MedicinesChina Pharmaceutical UniversityNanjingPeople’s Republic of China
  2. 2.Jiangsu Key Laboratory of Drug Discovery for Metabolic DiseaseChina Pharmaceutical UniversityNanjingPeople’s Republic of China

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